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Shkolnikova, Marina Nikolaevna, and Elena Vladimirovna Voronova. "FLAVONOIDS BIOAVAILABILITY ASSESSMENT USING THE DISSOLUTION TEST." Bulletin of KSAU, no. 6 (2022): 194–203. http://dx.doi.org/10.36718/1819-4036-2022-6-194-203.
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Skogley, Earl O. "The universal bioavailability environment/soil test unibest." Communications in Soil Science and Plant Analysis 23, no. 17-20 (November 1992): 2225–46. http://dx.doi.org/10.1080/00103629209368736.
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Sips, A. J., W. J. van der Vijgh, R. Barto, and J. C. Netelenbos. "Intestinal strontium absorption: from bioavailability to validation of a simple test representative for intestinal calcium absorption." Clinical Chemistry 41, no. 10 (October 1, 1995): 1446–50. http://dx.doi.org/10.1093/clinchem/41.10.1446.
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Abstract Calcium absorption tests have rarely been validated for being representative for absolute bioavailability (true absorption) or for intraindividual variation. Therefore, we investigated the reproducibility of the absolute bioavailability of strontium chloride, a marker for intestinal calcium absorption, in healthy male volunteers (n = 8) by measuring the area under the plasma strontium concentration-time curve after oral and intravenous administration of strontium. Subsequently, we selected a simple test variable as being representative of absolute bioavailability. The mean absolute bioavailability (+/- SD) was 25% +/- 7%. The best test variable appeared to be the fractional absorption at 240 min (Fc240) after oral intake, which demonstrated the highest correlation with absolute bioavailability (r = 0.66). The intraindividual variations of the data for this variable and for the absolute bioavailability are similar to those described for various absorption tests based on the use of calcium isotopes. Thus, the Fc240 of strontium offers the potential of a simple clinical test for use as a measure of intestinal calcium absorption and its modulation.
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Vergin, H., and V. Nitsche. "Oral Bioavailability of Atenolol." Journal of International Medical Research 17, no. 5 (September 1989): 417–25. http://dx.doi.org/10.1177/030006058901700503.
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The bioavailability of two formulations of atenolol was compared in an open, randomized crossover study. Each film-coated tablet contained 100 mg of active drug. The plasma concentrations of atenolol were determined using a newly developed and specific high-performance liquid chromatography procedure. The areas under the concentration – time curves (AUC) were calculated, as were pair differences and ratios for individual AUC values and for maximum plasma levels. The latter were determined (Cmax.(c)) and calculated (Cmax.(c)) at the corresponding time values ( tmax.) for test and reference formulations, and were then tested for statistical significance. The 95% confidence limits for both test and reference preparations, taken according to Westlake or Wilcoxon, were found to be 80.0 − 114.7% for AUC, 80.2 − 119.9% for Cmax. and 74.5 − 132.8% for tmax. In terms of pharmacokinetic target criteria, therefore, it can be seen that there were no substantial differences between the two film-coated tablets. The two atenolol preparations, therefore, may be classified as bioequivalent.
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Nelson, Colin. "Calcium Supplements Differ in Bioavailability, Simple Acid Test Shows." Internal Medicine News 38, no. 15 (August 2005): 15. http://dx.doi.org/10.1016/s1097-8690(05)71237-3.
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Allen, Lindsay Helen. "Bioavailability of Vitamin B12." International Journal for Vitamin and Nutrition Research 80, no. 45 (October 1, 2010): 330–35. http://dx.doi.org/10.1024/0300-9831/a000041.
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Vitamin B12 deficiency is common in people of all ages who consume a low intake of animal-source foods, including populations in developing countries. It is also prevalent among the elderly, even in wealthier countries, due to their malabsorption of B12 from food. Several methods have been applied to diagnose vitamin B12 malabsorption, including Schillings test, which is now used rarely, but these do not quantify percent bioavailability. Most of the information on B12 bioavailability from foods was collected 40 to 50 years ago, using radioactive isotopes of cobalt to label the corrinoid ring. The data are sparse, and the level of radioactivity required for in vivo labeling of animal tissues can be prohibitive. A newer method under development uses a low dose of radioactivity as 14C-labeled B12, with measurement of the isotope excreted in urine and feces by accelerator mass spectrometry. This test has revealed that the unabsorbed vitamin is degraded in the intestine. The percent bioavailability is inversely proportional to the dose consumed due to saturation of the active absorption process, even within the range of usual intake from foods. This has important implications for the assessment and interpretation of bioavailability values, setting dietary requirements, and interpreting relationships between intake and status of the vitamin.
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Bakasta, Deepu, and M. G. Shambhu. "The Development of Models Based on Linear and Nonlinear Multivariate Methods to Predict ADME/PK Properties Using Physicochemical Properties of Kinase, Protease Inhibitors, and GPCR Antagonists." International Journal of Medicinal Chemistry 2013 (March 19, 2013): 1–6. http://dx.doi.org/10.1155/2013/495134.
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Oral bioavailability of a drug compound is the significant property for potential drug candidates. Measuring this property can be costly and time-consuming. Quantitative structure-property relationships (QSPRs) are used to estimate the percentage of oral bioavailability, and they are an attractive alternative to experimental measurements. A data set of 217 drug and drug-like compounds with measured values of the percentage of oral bioavailability taken from the small molecule ChemBioBase database was used to develop and test a QSPR model. Descriptors were calculated for the compounds using Codessa 2.1 tool. Nonlinear general regression neural network model was generated using the DTREG predictive modeling program software. The calculated percentage of oral bioavailability model performs well, with root-mean-square (rms) errors of 4.55% oral bioavailability units for the training set, 14.32% oral bioavailability units for the test set, and 19.12% oral bioavailability units for the external prediction set. Given the structural diversity and bias of the data set, this is a good first attempt at modeling oral bioavailability using QSPR methods. The model can be used as a potential virtual screen or property estimator. With a larger data supply less biased toward the high end values of the percentage of oral bioavailability, a more successful model could likely be developed.
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Yudanti, Gendis Purno, Ilham Kuncahyo, and Endang Diyah Ikasari. "In vitro Naringenin SNEDDS Release Test by Dissolution." Natural Sciences Engineering and Technology Journal 3, no. 2 (June 22, 2022): 179–85. http://dx.doi.org/10.37275/nasetjournal.v3i2.29.
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Naringenin is the main flavanone in grapefruit which has anti-inflammatory, anti-cancer, hepatoprotective and antilipid peroxidation effects. Its low solubility in water causes dissolution and low bioavailability when taken orally. This study aims to increase the solubility and bioavailability of naringenin by using the SNEDDS technique. Initial characterization to determine the optimum formula was carried out using the D-optimal mixture design method, namely by optimizing the composition of SNEDDS which consisted of triacetin as the oil phase, tween 80 as surfactant and transcutol P as cosurfactant as an independent factor and SNEDDS characterization included emulsification time, drug loading, size globules and percent transmittance in response. The optimization results showed that the optimum formula was obtained at the composition of 10% triacetin, 70% tween 80 and 20% transcutol P. The dissolution test showed that the SNEDDS of naringenin was capable of dissolution (Q30) of 87,50% ±1,73 at the 30th minute and the f2 value of 28,93 so it can be concluded that the dissolution profile between the SNEDDS of naringenin and the naringenin capsules is not identical.
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Schweiggert, Ralf M., Rachel E. Kopec, Maria G. Villalobos-Gutierrez, Josef Högel, Silvia Quesada, Patricia Esquivel, Steven J. Schwartz, and Reinhold Carle. "Carotenoids are more bioavailable from papaya than from tomato and carrot in humans: a randomised cross-over study." British Journal of Nutrition 111, no. 3 (August 12, 2013): 490–98. http://dx.doi.org/10.1017/s0007114513002596.
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Carrot, tomato and papaya represent important dietary sources of β-carotene and lycopene. The main objective of the present study was to compare the bioavailability of carotenoids from these food sources in healthy human subjects. A total of sixteen participants were recruited for a randomised cross-over study. Test meals containing raw carrots, tomatoes and papayas were adjusted to deliver an equal amount of β-carotene and lycopene. For the evaluation of bioavailability, TAG-rich lipoprotein (TRL) fractions containing newly absorbed carotenoids were analysed over 9·5 h after test meal consumption. The bioavailability of β-carotene from papayas was approximately three times higher than that from carrots and tomatoes, whereas differences in the bioavailability of β-carotene from carrots and tomatoes were insignificant. Retinyl esters appeared in the TRL fractions at a significantly higher concentration after the consumption of the papaya test meal. Similarly, lycopene was approximately 2·6 times more bioavailable from papayas than from tomatoes. Furthermore, the bioavailability of β-cryptoxanthin from papayas was shown to be 2·9 and 2·3 times higher than that of the other papaya carotenoids β-carotene and lycopene, respectively. The morphology of chromoplasts and the physical deposition form of carotenoids were hypothesised to play a major role in the differences observed in the bioavailability of carotenoids from the foods investigated. Particularly, the liquid-crystalline deposition of β-carotene and the storage of lycopene in very small crystalloids in papayas were found to be associated with their high bioavailability. In conclusion, papaya was shown to provide highly bioavailable β-carotene, β-cryptoxanthin and lycopene and may represent a readily available dietary source of provitamin A for reducing the incidence of vitamin A deficiencies in many subtropical and tropical developing countries.
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Settineri, Robert, Jin Ji, Zenaida P. Shields, and Garth L. Nicolson. "The effects of Membrane Lipid Replacement with NTFactor® Lipids on increasing the bioavailability of three test nutrients." Bioactive Compounds in Health and Disease 5, no. 5 (May 10, 2022): 106. http://dx.doi.org/10.31989/bchd.v5i5.936.
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Introduction: Previous studies indicated that lipids and nanostructured materials may improve the uptake of nutrients with moderate bioabsorption properties. Objectives: This study evaluated the effects of Membrane Lipid Replacement with NTFactor® Lipids (NTFL) on bioabsorption of three poorly to moderately absorbed nutrients (quercetin, curcumin and coenzyme Q10) utilizing the Caco-2 epithelial cell permeability model. Methods: Transfer across a Caco-2 epithelial cell layer has become a reference standard in the pharmaceutical and nutraceutical industries for in vitro prediction of in vivo human intestinal absorption and bioavailability of orally administered substances. The degree of bioabsorption of the test materials was assessed by monitoring the concentrations of the test materials on each side of the Caco-2 monolayers by liquid chromatography and mass spectroscopy (LCMS/MS analysis).Results: When NTFL was added to each of the three test nutrients, there was increased absorption and transfer across a Caco-2 cell layer in a dose-dependent manner for the three nutrients. When compared individually, CoQ10 with NTFL showed the most significant increase in absorption (2.01-times more compared to controls without NTFL, p=0.0011) at a concentration of NTFL of 10 mg/mL. NTFL also increased absorption and transfer across a Caco-2 cell layer of the other test nutrients, but these results did not achieve the same level of significance. Discussion: A variety of Oral membrane lipid replacement supplements with NTFL, such as various vitamins, minerals and nutrients, have been designed to reduce fatigue, improve health conditions, and protect cellular and especially mitochondrial membranes from damage. Here we used NTFL to demonstrate improvements in absorption and bioavailability of three nutrients. Conclusion: Using the Caco-2 bioabsorption and bioavailability in vitro model we found that NTFL could enhance absorption, bioavailability and uptake of nutrients while providing its own clinically demonstrated health benefits. Keywords: Phospholipids, Membrane Lipid Replacement, CoQ10, curcumin, quercetin, bioavailability, absorption, permeability, Caco2, bio-uptake, bioabsorption, glycerolphospholipids, intestinal absorption
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Sakaguchi, Rao, Nakata, Nanbu, and Juneja. "Iron Absorption and Bioavailability in Rats of Micronized Dispersible Ferric Pyrophosphate." International Journal for Vitamin and Nutrition Research 74, no. 1 (January 1, 2004): 3–9. http://dx.doi.org/10.1024/0300-9831.74.1.3.
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Unlike commercial ferric pyrophosphate, micronized dispersible ferric pyrophosphate (MDFP: SunActive FeTM) does not precipitate and is completely dispersible in liquid form. MDFP shows a sharp particle size distribution at a nanometer level, which is several times smaller than that of commercial ferric pyrophosphate. The bioavailability of MDFP was compared to ferric pyrophosphate, sodium ferrous citrate, and ferrous sulfate by three bioavailability tests in rats; namely the serum iron concentration curve, the hemoglobin regeneration efficiency, and Association of Official Analytical Chemists' hemoglobin repletion test. The high area under curve value, a lag in peak time, and continued high serum iron concentration by MDFP over the other iron compounds indicates a sustained release of iron in the serum iron concentration curve method. MDFP showed the highest hemoglobin regeneration efficiency among all the iron compounds tested. The relative biological value of MDFP per unit of ferrous sulfate in each bioavailability test showed a high value as compared to other iron compounds. The above results suggest that MDFP is an ideal compound with high bioavailability for iron fortification in various liquid applications.
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Kamp, Fernanda, Doris Jandel, Imke Hoenicke, Klaus Pietrzk, Rainer Gross, Nadia M. F. Trugo, and Carmen M. Donangelo. "Bioavailability of Iron, Zinc, Folate, and Vitamin C in the Iris Multi-Micronutrient Supplement: Effect of Combination with a Milk-Based Cornstarch Porridge." Food and Nutrition Bulletin 24, no. 3_suppl_1 (January 2003): S20—S26. http://dx.doi.org/10.1177/15648265030243s104.
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The effect of combining a multi-micronutrient supplement with a milk-based cornstarch porridge on the bioavailability of iron, zinc, folate, and vitamin C was evaluated using the plasma curve response over time (8 hours) in healthy women. Three tests were carried out in a crossover design: S (multi-micronutrient supplement), MS (multi-micronutrient supplement plus test meal), and M (test meal). Relative bioavailability was determined as the percent ratio of the area under the curve (AUC) in MS corrected by M, and AUC in S. Compared to S, AUC in MS was smaller for iron (p < .05), for zinc (p < .01), and for folate (p < .05), but not different for vitamin C. Relative bioavailability was lower (p < .05) than 100% for iron (80%), zinc (70%), and folate (85%). The decrease in bioavailability of these nutrients when the multi-micronutrient supplement is combined with a milk-based cornstarch porridge is small. Therefore, the tested meal is a suitable vehicle for the multi-micronutrient supplement.
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Hincal, A. Atilla, Cemre Özseven, Mike van der Meer, Aydin Erenmemişoğlu, Mahmut Bilgiç, and Wolfgang Martin. "Relative bioavailability study of a generic effervescent tablet formulation of dexketoprofen and thiocolchicoside versus the originator 25 mg film coated tablet (dexketoprofen) and 8 mg capsule (thiocolchicoside)." Acta Pharmaceutica Hungarica 92, no. 1 (April 18, 2022): 45–51. http://dx.doi.org/10.33892/aph.2022.92.45-51.
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Aims: The aim of this study was to evaluate the pharmacokinetic profiles and the relative bioavailability of dexketoprofen and thiocolchicoside of the test preparation (dexketoprofen / thiocolchicoside 25 mg / 8 mg effervescent tablet) in comparison with the reference preparations (Keral 25 mg film coated tablet, containing dexketoprofen trometamol equivalent to 25 mg dexketoprofen (Menarini International Operations Luxembourg S.A.) (R1) and Muscoril 8 mg capsule, containing 8 mg thiocolchicoside (Sanofi Aventis İlaçları Ltd. Şti.) (R2) under fasting conditions. Methods: 25 healthy male subjects were enrolled in the study. Volunteers were hospitalised from the evening before drug administration (Day 0) until after the 24-hour blood sampling time on Day 2. Results: 24 subjects completed the study. Relative bioavailability (AUCT/AUCR1) of dexketoprofen from the test preparation was 100.99 %; (AUCT/AUCR2) of 3-O-glucuronide of thiocolchicoside (aglycone) from the test preparation was 100.47 %; (Cmax,T/Cmax,R1) of dexketoprofen from the test preparation was 122.59 %; (Cmax,T/Cmax,R2) of 3-O-glucuronide of thiocolchicoside (aglycone) from the test preparation was 111.43 %. Conclusions: The relative bioavailability AUCT /AUCR of the test preparation compared with both reference preparations is comparable, as shown by the geometric mean ratios of 100.59 % (dexketoprofen) and of 98.20 % (3-O-glucuronide of thiocolchicoside (aglycone).
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Montovani, Patrícia Andréa Bertuol, Ana Maria Pugens Pinto, Mauricio Bedim dos Santos, Daiane Loss Vieira, Anelise Weich do Prado, and Josélia Larger Manfio. "Bioavailability of two oral formulas of secnidazole in healthy volunteers." Brazilian Journal of Pharmaceutical Sciences 45, no. 4 (December 2009): 687–92. http://dx.doi.org/10.1590/s1984-82502009000400011.
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Secnidazole is an antimicrobial agent used primarily in the treatment of amoebiasis. For this bioequivalence study of secnidazole, twenty-eight healthy female volunteers were enrolled in a randomized crossover study. Each volunteer was given a single oral dose of secnidazole test preparation and then the reference preparation, or vice versa, with a wash out interval of two weeks. The plasma concentrations of secnidazole were determined by HPLC, and the samples were extracted with tert-butyl-methyl-ether: dicloromethane (60:40, v/v). Secnidazole and its parent compound metronidazole were separated on a C18 column with water:acetonitrile (85:15, v/v) as the mobile phase, and monitored at 310 nm. The ratio of mean Cmax, AUC0-t and AUC0-∞ values for the test and reference products were within the predetermined range established by ANVISA, demonstrating that the two formulations are bioequivalent in rate and extent of absorption.
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Rai, Deshanie, Abhijeet Morde, Muralidhara Padigaru, Vandita Srivastava, Mohan Lal, Chirag Khatri, and Kotagiri Rao. "Superior Bioavailability of a Patented Lutein & Zeaxanthin Macular Carotenoid (MC) Formulation." Current Developments in Nutrition 5, Supplement_2 (June 2021): 78. http://dx.doi.org/10.1093/cdn/nzab034_012.
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Abstract Objectives Lutein (L) and Zeaxanthin (Z) are the only dietary carotenoids exclusively deposited in the macula and supplementation of these nutrients is associated with visual and cognitive benefits. Ensuring their bioavailability is an important consideration for efficacy. We developed and patented a unique LZ formulation designed for enhanced MC absorption (Test). Our objective was to clinically measure the bioavailability of this Test formulation in comparison to a commercially available formulation (Reference). Methods This randomized, double-blind, parallel study involved ninety healthy, adult human volunteers. All subjects stayed within the study facility three days before administration of the study products and three days post-dose. Volunteers consumed a single-dose of the Test or Reference product, each comprising of 10 mg L and 2 mg Z immediately after breakfast. Blood samples were collected prior to dosing @ −48, −24 & 0 hrs and subsequently at 2, 4, 6, 8, 10, 12, 16, 20, 24, 48 and 72 hrs post-dose. L and Z levels were measured in serum using the validated HPLC method. The primary outcomes of the study included Cmax, AUC0–72, AUC0-T. Secondary outcomes included AUC0-12, AUC0-24, AUC0-48, AUC0-inf, Tmax and t1/2. Results All subjects completed the study with 100% compliance and no drop-outs. Serum L and Z levels were significantly higher in the Test group vs. the Reference group with a 2-fold and 1.5-fold greater absorption of L and Z levels, respectively, at all time points. Cmax, AUC0-72 and AUC0-T for serum L levels were 2.5, 2.9 and 3.2-fold greater, respectively, in the group receiving the Test formula. Similarly, the Cmax, AUC0-72 and AUC0-T for serum Z were also significantly greater with the Test formula. Finally, the Cmax and AUC parameters were significantly higher than the 80–125% criteria established by the FDA for bioequivalence confirming the superior bioavailability of Test product compared to Reference product. Conclusions These clinical findings support the superior bioavailability of this novel and uniquely formulated L Z dietary supplement product. The enhanced bioavailability behavior of this proprietary formulation can be advantageous for individuals looking to quickly improve their L and Z status and enhance their vision protection and performance. Funding Sources OmniActive Health Technologies.
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Santos, Joshua H., Mark Tristan J. Quimque, Allan Patrick G. Macabeo, Mary Jho-Anne T. Corpuz, Yun-Ming Wang, Tsai-Te Lu, Chia-Her Lin, and Oliver B. Villaflores. "Enhanced Oral Bioavailability of the Pharmacologically Active Lignin Magnolol via Zr-Based Metal Organic Framework Impregnation." Pharmaceutics 12, no. 5 (May 9, 2020): 437. http://dx.doi.org/10.3390/pharmaceutics12050437.
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Bioavailability plays an important role in drug activity in the human body, as certain drug amounts should be present to elicit activity. However, low bioavailability of drugs leads to negligible use for human benefit. In this study, the diversely active neolignan, magnolol, was impregnated onto a Zr-based organometallic framework [Uio-66(Zr)] to increase its low bioavailability (4–5%) and to test its potential acute oral toxicity. Synthesis of Uio-66(Zr) was done through the solvothermal method while simple impregnation at different time points was used to incorporate magnolol. The loading capacity of Uio-66(Zr) at 36 h was found to be significantly higher at 72.16 ± 2.15% magnolol than in other incubation time. Based on the OECD 425 (limit test), toxicity was not observed at 2000 mg kg−1 dose of mag@Uio-66(Zr) in female Sprague Dawley rats. The area under the curve (AUC) at 0–720 min of mag@Uio-66(Zr) was significantly higher than the AUC of free magnolol. Moreover, relative bioavailability increased almost two-folds using Uio-66(Zr). Unconjugated magnolol was found in the liver, kidney, and brain of rats in all treatment groups. Collectively, Uio-66(Zr) provided a higher magnolol bioavailability when used as drug carrier. Thus, utilization of Uio-66(Zr) as drug carrier is of importance for maximal use for poorly soluble and lowly bioavailable drugs.
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Bose, R., S. Dan, P. Mandal, P. Sarkar, B. Ghosh, L. K. Ghosh, and T. K. Pal. "BIOANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF MICRONIZED GLICLAZIDE IN HUMAN PLASMA BY LC-MS/MS AND ITS PHARMACOKINETIC STUDIES." INDIAN DRUGS 55, no. 09 (September 28, 2018): 24–33. http://dx.doi.org/10.53879/id.55.09.11405.
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Drugs having poor oral bioavailability, fail to reach the minimum effective concentration required to achieve pharmacological action. Improvement of the oral bioavailability of the drug is the most realistic approach, as it is the most preferred and convenient route of administration. Besides numerous techniques to improve oral bioavailability of the drugs, particle size reduction leads to increase in the effective surface area, resulting in enhancement of solubility and dissolution velocity of the drug. In the present study a sustained release tablet formulation containing 60mg micronized gliclazide was attempted to develop and a randomized, two period, two treatment crossover, single dose, pilot study of test preparation along with a marketed sample of Gliclazide 60mg was carried out on 6 healthy male, adult, human volunteers under fasting condition to establish the bioequivalence of the new formulation with a washout period of one week. The developed method was found to be simple, reproducible, sensitive, and specific for the determination of gliclazide from plasma and was also applied to study the pharmacokinetic parameters of gliclazide. The mean peak plasma levels of gliclazide with the reference preparation on the study day ranged between 2562.27–2823.61ng/mL, while the test preparation ranged between 3091.24–3467.66ng/mL. On the basis of comparison of the AUC0-t for gliclazide after single dose administration, the relative bioavailability of the test preparation was 109.96% of that of the reference preparation.
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Wen, Ting, Boyi Niu, Qiaoli Wu, Yixian Zhou, Xin Pan, Guilan Quan, and Chuanbin Wu. "Fenofibrate Solid Dispersion Processed by Hot-Melt Extrusion: Elevated Bioavailability and Its Cell Transport Mechanism." Current Drug Delivery 16, no. 6 (August 27, 2019): 538–47. http://dx.doi.org/10.2174/1567201816666190122123044.
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Background: Fenofibrate (FNB) is an effective drug for the treatment of hypertriglyceridemia, hypercholesterolemia as well as mixed hyperlipidemia. However, due to its poor aqueous solubility, FNB has the problem of poor oral absorption followed by low bioavailability. Objective: The aim of this research was to construct FNB amorphous solid dispersion employing PVP VA64 as the carrier by hot-melt extrusion method, in order to improve the oral bioavailability. Additionally, the cell transport experiment was conducted to further investigate the mechanism of promoted osmotic absorption. Methods: The physical state of the obtained solid dispersion was characterized using SEM, DSC and XRD. Besides, in vitro Caco-2 cells were used to evaluate the cytotoxicity of the carrier and mimic gastrointestinal drug permeation. At last, in vitro dissolution test and in vivo bioavailability study were also carried out. Results: The prepared FNB solid dispersion was found to be an amorphous state after hot-melt extrusion process. In vitro cytotoxicity test on Caco-2 cells confirmed the excellent biocompatibility of the carrier PVP VA64. Besides, transwell cell transport assay and in vitro dissolution test revealed that FNB released from amorphous solid dispersion was equipped with an improved transmembrane transport and dissolution rate. Moreover, pharmacokinetic study in beagle dogs showed that comparing with commercial micronized product Lipanthyl®, the oral bioavailability of FNB solid dispersion was significantly enhanced (2.45 fold). Conclusion: In conclusion, PVP VA64 can be regarded as a promising polymer to enhance the bioavailability of poorly water-soluble drugs such as FNB processed by hot-melt extrusion. Besides, investigations on the mechanism of the enhanced penetration are expected to lay a foundation on the subsequent development of effective and practical solid dispersion.
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Nakamura, Sadako, Tsuneyuki Oku, and Makoto Ichinose. "Bioavailability of cellobiose by tolerance test and breath hydrogen excretion in humans." Nutrition 20, no. 11-12 (November 2004): 979–83. http://dx.doi.org/10.1016/j.nut.2004.08.005.
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Ruby, Michael V., Andy Davis, Rosalind Schoof, Steve Eberle, and Christopher M. Sellstone. "Estimation of Lead and Arsenic Bioavailability Using a Physiologically Based Extraction Test." Environmental Science & Technology 30, no. 2 (January 1996): 422–30. http://dx.doi.org/10.1021/es950057z.
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Yu, Shengwu, Anika Singh, Huiying Zhang, and David D. Kitts. "An in vitro Method to Determine Intestinal Bioavailability of Glucosamine Salt Mixture." Journal of Nutritional Health & Food Science 9, no. 1 (February 10, 2021): 1–6. http://dx.doi.org/10.15226/jnhfs.2021.001180.
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Glucosamine is an amino sugar commonly used to improve joint health. It is often available for consumers as specialized supplements, the matrixes of which are formulated with components that facilitate enhancing functionality of the bioactive glucosamine. The primary objective of this study was to determine the in vitro bioaccessibility and bioavailability of a commercial glucosamine sulphate supplement, formulated with a mineral clay mixture. We used a modified a 3-step in vitro digestion procedure that included oral, gastric, and gastrointestinal digestions to assess bioaccessibility. Bioavailability followed using a Caco2 cell permeability test. Glucosamine bioaccessibility was not affected by gastric digestion and only marginally affected by gastrointestinal digestion (e.g., > 90% recovery). Bioavailability was dramatically lower, averaging approximately 15%, but similar for both the glucosamine reference standard and clay mineral mix glucosamine formulated product. Our in vitro bioavailability measurement of glucosamine, corrected for bioaccessibility, agree with values from in vitro rodent models. We conclude that the in vitro 3-step digestion of glucosamine, used to mimic gastrointestinal digestion, followed by the Caco2 permeability assay represents an alternative method to assess digestibility and bioavailability of formulated glucosamine products. Keywords: Glucosamine; Clay Mineral Mix; Bioaccessibility; Bioavailability
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Konishi, Hiroki, Takayuki Nakatsuka, Michiaki Yoshida, Shinji Tamaki, Tokuzo Minouchi, Akira Yamaji, and Masahiko Kinoshita. "Pharmacokinetic Analysis of Theophylline to Assess Noncompliance in Therapy." Annals of Pharmacotherapy 36, no. 5 (May 2002): 835–38. http://dx.doi.org/10.1345/aph.1a282.
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OBJECTIVE: To report a case showing patient noncompliance, supported by outcomes of pharmacokinetic analysis of theophylline as a surrogate drug. CASE SUMMARY: A 45-year-old woman with severe hypertension was treated with a variety of oral antihypertensive drugs, but there was no improvement in her elevated blood pressure. Since we suspected that her intestinal drug absorption capacity was impaired, a theophylline absorption test was performed. When oral theophylline was given to the patient in tablet form, the apparent bioavailability was only 20%, which agreed with our hypothesis. However, the bioavailability of theophylline given in liquid form was almost 100%, and theophylline in tablet form was confirmed to be fully bioavailable when the test was performed under supervision by medical staff. DISCUSSION: The almost complete bioavailability of oral theophylline indicated that there was no impairment in intestinal absorption capacity. The low bioavailability of theophylline observed after tablet administration in the first trial was apparently a result of noncompliance, because the staff did not supervise administration to ensure that tablets were swallowed. Thus, the low response to antihypertensive therapy was attributed to patient noncompliance in taking the drugs, despite her insistence to the contrary. CONCLUSIONS: The use of theophylline was a novel approach to evaluating the absorbability of orally administered drugs in a patient suspected of poor compliance with therapy. A great difference in theophylline bioavailability between the supervised and unsupervised trials was strongly indicative of patient noncompliance. The possibility of impaired absorption was virtually ruled out.
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Pardo, Antonio, Mohammed Bouhajib, Eman Rafla, Thomas R. King, and Judith C. Kando. "Comparative Bioavailability of Amphetamine Extended-Release Oral Suspension and Extended-Release Mixed Amphetamine Salts." CNS Spectrums 26, no. 2 (April 2021): 163. http://dx.doi.org/10.1017/s109285292000262x.
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AbstractPurposeThis open-label, single-dose, randomized, two-period, two-treatment, two-sequence, crossover study evaluated the comparative bioavailability between amphetamine extended-release oral suspension (treatment A: AMPH EROS, Dyanavel XR 2.5 mg/mL, 18.8 mg amphetamine base per 7.5 mL) and extended-release mixed amphetamine salts (treatment B: ER MAS, Adderall XR 30 mg capsules, equivalent to 18.8 mg amphetamine base per capsule) after a single dose in healthy adult subjects, under fasted conditions.MethodsThe crossover design allowed for intra-subject PK comparisons. Relative comparable bioavailability was determined by a statistical comparison of the AUC and Cmax parameters for both d- and l-amphetamine, where the geometric mean ratios for AUC and Cmax were within the 90% confidence limits (80.0%–125.0%) to determine comparable bioavailability between test products. Subjects in sequence 1 received treatment A followed by B; subjects in sequence 2 received treatment B followed by treatment A. PK samples were obtained at 0 (pre-dose) through 60 hours post-dose. The safety assessment was based on reported frequency and severity of adverse events.ResultsThirty (30) subjects were enrolled and 28 completed. The mean age of subjects was 35 years, with a mean BMI of 25.9 kg/m2. Most subjects were Male (63.3%) and Black (56.7%). The geometric mean ratios for Cmax and all AUC measurements were within the 80–125% bound indicating comparable bioavailability between both test products. Both test products were generally well-tolerated with no serious AEs reported.ConclusionsThe bioavailability of a single 7.5 mL dose of AMPH EROS 2.5 mg/mL was comparable to a single 30 mg capsule dose of ER MAS. AMPH EROS (both d- and l-amphetamine) showed equivalent peak and overall exposure to ER MAS under fasted conditions.FundingTris Pharma, Inc.
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Barone, Joseph A., Nicholas G. Lordi, Wesley G. Byerly, and John L. Colaizzi. "Comparative Dissolution Performance of Internationally Available Piroxicam Products." Drug Intelligence & Clinical Pharmacy 22, no. 1 (January 1988): 35–40. http://dx.doi.org/10.1177/106002808802200108.
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Piroxicam is a widely used nonsteroidal antiinflammatory drug available worldwide under various trade names by several manufacturers. Only one brand of piroxicam (Feldene) is currently marketed in the U.S., and the United States Pharmacopeial Convention established an official dissolution requirement for piroxicam in 1985. The purpose of this study was to evaluate and compare the dissolution performance of several internationally available piroxicam products using the United States Pharmacopeia (USP) dissolution test for piroxicam capsules. Of 25 brands of piroxicam capsules evaluated, 72 percent of the brands failed to meet the USP requirement, several by a wide margin. Although there is no specific USP dissolution test for tablets, the test for capsules was applied to five different brands of piroxicam tablets, and 80 percent of the tablet brands tested failed to meet the USP requirement. Although comparative bioavailability studies would be required to establish any definitive relationship between dissolution test performance and bioavailability, the failure of most of these products to meet the USP requirement for dissolution indicates formulation differences that could result in altered bioavailability. The substantial differences in dissolution performance observed among the piroxicam oral dosage forms tested have implications concerning the equivalency and standards of multisource products available on the international market, and should be taken into account by health care providers worldwide.
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Sekiya, Mihoko, Shigenori Suzuki, Yusuke Ushida, Ikuo Sato, and Hiroyuki Suganuma. "Neoxanthin is undetectable in human blood after ingestion of fresh young spinach leaf." PLOS ONE 18, no. 7 (July 19, 2023): e0288143. http://dx.doi.org/10.1371/journal.pone.0288143.
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In a previous study, we demonstrated that the carotenoid neoxanthin was contained in young leafy vegetables including spinach and showed a fat accumulation inhibitory effect in vitro. To evaluate the bioavailability of neoxanthin, a raw young spinach leaf (100 g day–1 for 4 weeks) intake test was performed on 14 participants (36.5 ± 8.0 years; male:female ratio = 9:5). Neoxanthin, neochrome, β–carotene, and lutein concentration in the spinach and blood of participants (before and after the test) was measured using high performance liquid chromatography. Neither neoxanthin nor neochrome was detected in the blood samples, whereas β–carotene and lutein concentration significantly increased (1.4– and 1.9–fold, respectively) during testing. Neoxanthin bioavailability in humans is low; thus, it is unlikely to have a fat accumulation inhibitory effect in vivo, contrary to the result in vitro. Ingesting the leafy vegetables raw can help maintain high neoxanthin levels, but it is not beneficial for neoxanthin bioavailability.
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Samran, Samran, and Hari Ronaldo Tanjung. "Metoclopramide-OROS Dispersible Tablets Optimized Formula Bioavailability Study." Open Access Macedonian Journal of Medical Sciences 8, A (July 7, 2020): 338–41. http://dx.doi.org/10.3889/oamjms.2020.3353.
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BACKGROUND: Bioavailability and bioequivalence studies required by regulations to ensure therapeutic equivalence between a pharmaceutically equivalent test product and a reference product.
AIM: This study aimed to evaluate the bioavailability performance between the optimum formula of OROS dispersible tablet-metoclopramide dosage forms (FCL-6) and the Primperan® as the reference product.
METHODS: The FCL-6 formula was design by simplex lattice design model with a three components mixture of excipients: Solid tapai extract, corn starch, and Avicel. The optimum formula of OROS dispersible tablet (ODT)-metoclopramide consists of solid tapai extract (27.038 mg), corn starch (27.407 mg), and Avicel (53.555 mg), metoclopramide hydrochloric acid (HCl) (10.00 mg), LH-11 (22.50 mg), aspartame (5.00 mg), talcum BP (3.00 mg), and Mg stearate (1.50 mg). The in vivo test was done by cross-over design method using six rabbits. The level of metoclopramide concentration from in vivo test was measured by high-performance liquid chromatography instrument.
RESULTS: The study revealed that the tmax, Cmax, and area under curve (AUC) of ODT-metoclopramide FCL-6 were 60 min, 1.95 ± 0.13 μg/mL, and 1118.20 ± 150 μg/mL. min consecutively. The Cmax and the concentration of the drug absorbed in the blood (AUC) of ODT-metoclopramide were larger than Primperan® tablets. Statistical data of the optimized ODT-metoclopramide compared with Primperan® showed that the Cmax and AUC significance values were <0.05 (p < 0.05).
CONCLUSION: The optimized formula of ODT-metoclopramide revealed a better characteristic of Cmax and AUC concentration compared with Primperan®. The optimized ODT-metoclopramide with tapai extract was found to be promising to improved bioavailability of metoclopramide.
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Fan, Wenling, Jiali Wu, Meiqi Gao, Xiaotong Zhang, and Wenjing Zhu. "Preparation of Solid Dispersion of Polygonum Cuspidatum Extract by Hot Melt Extrusion to Enhance Oral Bioavailability of Resveratrol." Molecules 28, no. 2 (January 11, 2023): 737. http://dx.doi.org/10.3390/molecules28020737.
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The aim of this study was to improve the solubility, bioavailability, and stability of resveratrol (RES-SD) Solid Dispersion in Polygonum cuspidatum extract (PCE) by hot melt extrusion (HME). In addition, the role of the auxiliary substances in PCE was also studied. The solid dispersion of Polygonum cuspidatum extract was prepared by hot-melt extrusion. The optimum formula was selected by single factor design and orthogonal test. The optimum formula was barrel temperature 140 °C, screw rotation speed 40 rpm/min, and the ratio of Polygonum cuspidatum extract to HPMCAS was 1:2. The dissolution test showed that PCE-SD increased the dissolution of RES from 46.75 ± 0.47% to 130.06 ± 0.12%. The pharmacokinetics curve of rats showed that PCE-SD increased AUC0-t of RES from 111,471.22 ± 11.4% to 160,458.968 ± 15.7%, indicating an approximately 1.44-fold increase in absorption. In addition, the rotation speed of PCE-SD screw is less than that of RES-SD screw. The bioavailability of PCE-SD was slightly better than that of RES-SD. PCE-SD is more hygroscopic than RES-SD. PCE-SD increased the solubility and oral bioavailability of RES. The auxiliary substances in Polygonum cuspidatum extract have influence on its preparation technology, stability, and bioavailability.
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Borel, Patrick, C. Desmarchelier, U. Dumont, C. Halimi, D. Lairon, D. Page, J. L. Sébédio, C. Buisson, C. Buffière, and D. Rémond. "Dietary calcium impairs tomato lycopene bioavailability in healthy humans." British Journal of Nutrition 116, no. 12 (December 28, 2016): 2091–96. http://dx.doi.org/10.1017/s0007114516004335.
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AbstractLycopene (LYC) bioavailability is relatively low and highly variable, because of the influence of several factors. Recent in vitro data have suggested that dietary Ca can impair LYC micellarisation, but there is no evidence whether this can lead to decreased LYC absorption efficiency in humans. Our objective was to assess whether a nutritional dose of Ca impairs dietary LYC bioavailability and to study the mechanism(s) involved. First, in a randomised, two-way cross-over study, ten healthy adults consumed either a test meal that provided 19-mg (all-E)-LYC from tomato paste or the same meal plus 500-mg calcium carbonate as a supplement. Plasma LYC concentration was measured at regular time intervals over 7 h postprandially. In a second approach, an in vitro digestion model was used to assess the effect of increasing Ca doses on LYC micellarisation and on the size and zeta potential of the mixed micelles produced during digestion of a complex food matrix. LYC bioavailability was diminished by 83 % following the addition of Ca in the test meal. In vitro, Ca affected neither LYC micellarisation nor mixed micelle size but it decreased the absolute value of their charge by 39 %. In conclusion, a nutritional dose of Ca can impair dietary LYC bioavailability in healthy humans. This inhibition could be due to the fact that Ca diminishes the electrical charge of micelles. These results call for a thorough assessment of the effects of Ca, or other divalent minerals, on the bioavailability of other carotenoids and lipophilic micronutrients.
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Kuehr, Sebastian, Boris Meisterjahn, Nicola Schröder, Burkhard Knopf, Doris Völker, Kathrin Schwirn, and Christian Schlechtriem. "Testing the bioaccumulation of manufactured nanomaterials in the freshwater bivalve Corbicula fluminea using a new test method." Environmental Science: Nano 7, no. 2 (2020): 535–53. http://dx.doi.org/10.1039/c9en01112a.
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The elucidation of bioavailability, uptake and elimination as well as accumulation of the test items was possible on the level of total and particle concentrations for the whole soft body as well as the single tissue compartments.
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De Leo, Luigina, Nicola Di Toro, Giuliana Decorti, Noelia Malusà, Alessandro Ventura, and Tarcisio Not. "Fasting Increases Tobramycin Oral Absorption in Mice." Antimicrobial Agents and Chemotherapy 54, no. 4 (January 19, 2010): 1644–46. http://dx.doi.org/10.1128/aac.01172-09.
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ABSTRACT The pharmacokinetics of the aminoglycoside tobramycin was evaluated after oral administration to fed or fasting (15 h) mice. As expected, under normal feeding conditions, oral absorption was negligible; however, fasting induced a dramatic increase in tobramycin bioavailability. The dual-sugar test with lactulose and l-rhamnose confirmed increased small bowel permeability via the paracellular route in fasting animals. When experiments aimed at increasing the oral bioavailability of hydrophilic compounds are performed, timing of fasting should be extremely accurate.
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Yamada, Aya, Yoshiro Ono, Akiko Kida, and Kenji Namiki. "Evaluation of Bioavailability of Heavy Metals in Soil by in vitro Screening Test." Chemistry Letters 32, no. 5 (May 2003): 472–73. http://dx.doi.org/10.1246/cl.2003.472.
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Mbaeyi-Nwaoha, Ifeoma Elizabeth, Ebere Ani, and Ngozi Chioma Okoronkwo. "Toxicity of Soursop Leaf Powder and Its Relevance in Determining The Micronutrient Status in Formulated Complementary Food." Journal of Life and Bio Sciences Research 2, no. 01 (March 19, 2021): 19–25. http://dx.doi.org/10.38094/jlbsr20124.
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Complementary food was produced from blends of hungry rice (A), pigeon pea (P) and soursop leaves (S). The raw materials were washed with portable water, dried at room temperature, milled with hammer mill, fermented for 24 hours at 28 ± 2 °C (28 ± 2 °C), oven-dried at 50 °C for 12 hours, remilled, sieved to 1 mm pore size and packaged in polyethylene bags for further analysis. The samples were in the ratio of 70:30:0 (sample APS), 65:30:5 (sample APS1), 60:30:10 (sample APS2) and 55:30:15 (sample APS3). Toxicity test for lethal dose (LD50) was carried out on the soursop leaves. Bioassay was carried out with male albino rats for 28 days including acclimatization period of 7 days. Feed intake and weight gain of experimental rats were recorded daily and weekly. Blood serum was collected before and after feeding trials for analyzing bioavailability of the selected micronutrients. The data were subjected to one-way analysis of variance. Means were separated using the Duncan’s multiple range test and significance was accepted at probability level of 0.05 %. The toxicity test (LD50) indicated safety of soursop leaf as an infusion (oral administration) at lower doses of 10-1000 mg/kg body weight of rats. The bioassay revealed that food intake was significantly (p < 0.05) different among the samples in the first, second and third week. Rats that ate normal rat chow had the highest food intake while the rats that ate APS3 had the lowest food intake. Weight gain was highest in rats that ate rat chow while it was lowest in the rat that ate APS3. Bioavailability of selected micronutrient revealed that calcium content had the highest bioavailability in rats fed with rat chow and lowest in AP. Sample of APS1 had the highest iron bioavailability (47.83 %) among the fortified samples and the rat chow. Zinc had the highest bioavailability (52.86 %) in APS1. The work revealed that selected vitamins were most available in APS2 and the selected minerals were most available in sample APS1.
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Paoletti, Alyssa, Abrar Fakiha, Zujaja Tul-Noor, Paul B. Pencharz, Crystal L. Levesque, Ronald O. Ball, Dehan Kong, Rajavel Elango, and Glenda Courtney-Martin. "Bioavailable Lysine Assessed Using the Indicator Amino Acid Oxidation Method in Healthy Young Males is High when Sorghum is Cooked by a Moist Cooking Method." Journal of Nutrition 152, no. 3 (December 6, 2021): 770–78. http://dx.doi.org/10.1093/jn/nxab410.
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ABSTRACT Background Sorghum is the fifth most consumed cereal grain but limiting in the indispensable amino acid lysine. Complementing sorghum with lentils can improve the quality of sorghum-based diets. However, knowledge of lysine bioavailability in sorghum is lacking. Objectives The study objectives were to determine the bioavailability of lysine in sorghum and to assess the effect of complementation of sorghum and lentils in a mixed-meal format. Methods We studied 5 healthy young men (≤30 years; BMI <25 kg/m2) in a repeated-measure design using the indicator amino acid oxidation (IAAO) method, with L-[1–13C] phenylalanine as the indicator. Each subject participated in 8 determinations in random order. On the reference diet, subjects received 4 amounts of L-lysine (5, 8, 12, and 15 mg. kg–1 . d–1) from a crystalline amino acid mixture patterned after egg protein. On the test diet, they received 3 levels of lysine (8.2, 12.5, and 15.7 mg. kg–1 . d–1) from sorghum, and on the complementation diet they received 1 level of lysine from a mixed meal of sorghum and lentils. The bioavailability of lysine in sorghum was estimated by comparing the IAAO response to the test diet with the IAAO response to the reference diet using the slope-ratio method. Effectiveness of complementation was assessed by comparing the IAAO response to the mixed meal to the IAAO response to the test protein. Results The bioavailability of lysine from sorghum was 94%. Upon complementation with lentils, there was a decline in the oxidation of L-[1–13C] phenylalanine by 19% (P < 0.0495), reflecting an improvement in available lysine in the mixed meal due to increased lysine intake. Conclusions Although the bioavailability of lysine in sorghum is high, its lysine content is limiting. Complementation with lentils in a 1:1 ratio is recommended to achieve the lysine requirement for adult men consuming a sorghum-based diet. This trial was registered at clinicaltrials.gov as NCT03411005.
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Marković, Ana, Miroslava Spasić, Vesna Savić, Slavica Sunarić, and Marija Tasić-Kostov. "Spectrophotometric method in comparative in vitro dissolution test of branded and generic ibuprofen tablets." Acta Facultatis Medicae Naissensis 38, no. 2 (2021): 147–55. http://dx.doi.org/10.5937/afmnai38-28337.
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The dissolution test is a simple and important in vitro method for assessing the bioequivalence, which aims to compare the bioavailability of generic and branded drugs. It implies the use of a proper apparatus (usually pharmacopoeially defined) in which the dosage form is dissolved, and the dissolution process itself is monitored/quantified using an appropriate analytical method among which high-performance liquid chromatography (HPLC) is widely used. Spectrophotometry could be a significant substitute, through its advantages in terms of simplicity and costs of analysis. In the present study, possible differences in bioavailability between branded and generic ibuprofen coated tablets were predicted using a dissolution test for solid dosage forms. The ibuprofen content and the amount of ibuprofen released in the dissolution test were determined using a simple spectrophotometric method. Based on the obtained results, no significant differences in the dissolution rate of ibuprofen from generic and branded coated tablets were observed. It can be concluded that the spectrophotometric method applied for the dissolution test, among other suitable methods, could be used for bioequivalence screening in conditions where rapid and simple assessment is required or where HPLC method is not available.
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Desager, J. P., and C. Harvengt. "Oral Bioavailability of Nizatidine and Ranitidine Concurrently Administered with Antacid." Journal of International Medical Research 17, no. 1 (January 1989): 62–67. http://dx.doi.org/10.1177/030006058901700109.
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This four-way crossover open-label study on eight healthy subjects was designed to investigate the effect on bioavailability of orally administered nizatidine given concurrently with an antacid (magnesium hydroxide–aluminium hydroxide mixture). Ranitidine was used as a comparison. Subjects were hospitalized overnight for each drug application which was given as a single dose [nizatidine or ranitidine (300 mg) or antacid (20 ml) of a neutralizing capacity of 50 mmol hydrochloric acid]. Plasma nizatidine or ranitidine concentrations were measured by high performance liquid chromatography. No statistically significant difference occurred in the kinetic profile of nizatidine after antacid administration although it took longer to reach maximum concentration in plasma. The area under the concentration–time curve was also reduced (by ≤10%) and there was a longer lag between administration and absorption. Bioequivalence (Westlake test) for ranitidine in the presence or absence of antacid was confirmed (difference ≤12%). For nizatidine, with or without antacid, the value of the Westlake test was just above the limit for bioequivalence (21.4%), whereas the Student's t-test for related means (one-tailed distribution) gave P = 0.045. There was no clinically relevant nizatidine–antacid interaction at the doses used in this study.
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Rees, Chris A., Christina A. Rostad, Grace Mantus, Evan J. Anderson, Ann Chahroudi, Preeti Jaggi, Jens Wrammert, et al. "Altered amino acid profile in patients with SARS-CoV-2 infection." Proceedings of the National Academy of Sciences 118, no. 25 (June 4, 2021): e2101708118. http://dx.doi.org/10.1073/pnas.2101708118.
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Low plasma arginine bioavailability has been implicated in endothelial dysfunction and immune dysregulation. The role of arginine in COVID-19 is unknown, but could contribute to cellular damage if low. Our objective was to determine arginine bioavailability in adults and children with COVID-19 vs. healthy controls. We hypothesized that arginine bioavailability would be low in patients with COVID-19 and multisystem inflammatory syndrome in children (MIS-C). We conducted a prospective observational study of three patient cohorts; arginine bioavailability was determined in asymptomatic healthy controls, adults hospitalized with COVID-19, and hospitalized children/adolescents <21 y old with COVID-19, MIS-C, or asymptomatic severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection identified on admission screen. Mean patient plasma amino acids were compared to controls using the Student’s t test. Arginine-to-ornithine ratio, a biomarker of arginase activity, and global arginine bioavailability ratio (GABR, arginine/[ornithine+citrulline]) were assessed in all three groups. A total of 80 patients were included (28 controls, 32 adults with COVID-19, and 20 pediatric patients with COVID-19/MIS-C). Mean plasma arginine and arginine bioavailability ratios were lower among adult and pediatric patients with COVID-19/MIS-C compared to controls. There was no difference between arginine bioavailability in children with COVID-19 vs. MIS-C. Adults and children with COVID-19 and MIS-C in our cohort had low arginine bioavailability compared to healthy adult controls. This may contribute to immune dysregulation and endothelial dysfunction in COVID-19. Low arginine-to-ornithine ratio in patients with COVID-19 or MIS-C suggests an elevation of arginase activity. Further study is merited to explore the role of arginine dysregulation in COVID-19.
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Lee, Seul-Ji, Myoung-Eun Lee, Jae Woo Chung, Jin Hee Park, Keun Young Huh, and Gee-Ill Jun. "Immobilization of Lead from Pb-Contaminated Soil Amended with Peat Moss." Journal of Chemistry 2013 (2013): 1–6. http://dx.doi.org/10.1155/2013/509520.
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Immobilization of lead (Pb) using soil amendments can reduce Pb toxicity and bioavailability in soil. This study evaluated Pb immobilization in a Pb-contaminated soil by using peat moss through various tests. The Pb-contaminated soil (2000 mg Pb·kg−1) was amended with 1%, 5%, and 10% of peat moss to immobilize Pb in the soil. The immobilization properties of Pb in the contaminated soil were evaluated by a column leaching experiment, a microcosm test, and a batch incubation test. Peat moss significantly reduced the Pb leaching in all of the experiments and more effectively reduced mobility and toxicity of Pb in the column leaching and microcosm tests than bioavailability in the batch incubation test. The immobilized lead from the soils amended with 1%, 5%, and 10% of peat moss was 37.9%, 87.1%, and 95.4% from the column leaching test, 18.5%, 90.9%, and 96.4% from the microcosm test, and 2.0%, 36.9%, and 57.9% from the NH4NO3extraction method, respectively, indicating that peat moss can be effectively used for the remediation of Pb-contaminated soil.
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Valdivia-Tapia, Astrid Carolina, Juliana Nunes Botelho, Cinthia Pereira Machado Tabchoury, Antonio Pedro Ricomini-Filho, Rodrigo Andrés Giacaman, and Jaime Aparecido Cury. "Fluoride bioavailability on demineralized enamel by commercial mouthrinses." Brazilian Dental Journal 32, no. 2 (April 2021): 90–99. http://dx.doi.org/10.1590/0103-6440202104588.
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Abstract The ability of mouthrinses, available in the international market, to form reaction products on demineralized enamel (bioavailability test) was evaluated in vitro. Nine mouthrinses purchased in Chile were evaluated; eight formulated with NaF (one containing 100 µg F/mL and seven containing 226) and one with Na2FPO3 (226 µg F/mL as ion FPO3 ). Demineralized enamel slabs (n=15 per mouthrinse) were sectioned; one half was subjected to the assigned mouthrinse treatment for 10 min and the other half was used to obtain baseline data. Loosely bound and firmly bound fluoride formed on enamel were determined with an ion-specific electrode and the values were expressed in µg F/cm2. The concentration of fluoride and the pH of the mouthrinses were previously determined. Concentrations of loosely bound and firmly bound fluoride formed on enamel were independently analyzed by ANOVA and Tukey’s test (α=5%). The loosely bound and firmly bound fluoride concentrations formed ranged from 3.2 to 36.2 and 0.4 to 1.7, respectively. Loosely bound fluoride formed on enamel was significantly more effective in discriminating the effect of different commercial mouthrinses than firmly bound fluoride. Mouthrinses with 226 ppm F as NaF and low pH presented significantly greater bioavailability of fluoride on enamel than those with higher pH or lower NaF concentration. The mouthrinse with Na2FPO3 showed low reactivity. Although further studies are necessary, the findings showed that commercial fluoride-containing mouthrinses have important variations in enamel fluoride bioavailability, which may result in differences on anticaries efficacy.
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MB, Reddy. "Assessing the Bioavailability and Bioaccessibility of Selenium from Selenium-Rich Algae." Food Science & Nutrition Technology 5, no. 5 (September 30, 2020): 1–9. http://dx.doi.org/10.23880/fsnt-16000228.
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Many new selenium (Se) sources for supplementation use are emerging. The objective of this study was to test the Se bioaccessibility (BAC) and bioavailability (BA) of Se-rich algae. Algal samples were cultivated in media containing selenite or selenate then BAC and BA were compared to Se-salts and Se-amino acids from traditional supplementation. BAC was tested based on the Se solubility post in vitro digestion and BA by induction of cellular glutathione peroxidase activity (GPx) in a Se deficient Caco-2 cell model. Cells treated with algae grown in selenate and selenite had a mean GPx activity that was significantly less than the SeMet treatment (P<0.05). Overall, no algae samples grown in selenite were identified as superior since no significant differences were found among the algae samples. However, the algae grown in the higher concentration of selenate (200 ppm) with no sulfite appeared to have a better BA than all other algae samples. Although Se-rich algae did not increase GPx activity as well as traditional supplementation forms, the results gave an insight for the ways to improve Se BA from this novel source. In addition, evaluation of nutritional profile of the algae will give us a greater understanding of how it can offer other health benefits for future supplementation.
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Blancquaert, Laura, Chris Vervaet, and Wim Derave. "Predicting and Testing Bioavailability of Magnesium Supplements." Nutrients 11, no. 7 (July 20, 2019): 1663. http://dx.doi.org/10.3390/nu11071663.
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Despite the presumption of the beneficial effects of magnesium supplementation, little is known about the pharmacokinetics of different magnesium formulations. We aimed to investigate the value of two in vitro approaches to predict bioavailability of magnesium and to validate this in subsequent in vivo testing. In vitro assessment of 15 commercially available magnesium formulations was performed by means of a Simulator of the Human Intestinal Microbial Ecosystem (SHIME®) and by dissolution tests. Two magnesium formulations with contrasting bioavailability prediction from both in vitro tests (best vs. worst) were selected for in vivo testing in 30 subjects. In vivo bioavailability was compared following one acute ingestion by monitoring blood magnesium concentrations up to 6 h following intake. The in vitro tests showed a very wide variation in absorption and dissolution of the 15 magnesium products. In the in vivo testing, a significant different serum magnesium absorption profile was found up to 4 h following supplement ingestion for the two supplements with opposing in vitro test results. Moreover, maximal serum magnesium increase and total area under the curve were significantly different for both supplements (+6.2% vs. +4.6% and 6.87 vs. 0.31 mM.min, respectively). Collectively, poor bioaccessibility and bioavailability in the SHIME model clearly translated into poor dissolution and poor bioavailability in vivo. This provides a valid methodology for the prediction of in vivo bioavailability and effectiveness of micronutrients by specific in vitro approaches.
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Rodriguez-Mateos, Ana, Maria Jose Oruna-Concha, Catherine Kwik-Uribe, Alberto Vidal, and Jeremy P. E. Spencer. "Influence of sugar type on the bioavailability of cocoa flavanols." British Journal of Nutrition 108, no. 12 (March 7, 2012): 2243–50. http://dx.doi.org/10.1017/s0007114512000475.
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The beneficial effects of cocoa on vascular function are mediated by the absorption of monomeric flavanols into the circulation from the small intestine. As such, an understanding of the impact of the food matrix on the delivery of flavanols to the circulation is critical in assessing the potential vascular impact of a food. In the present study, we investigated the impact of carbohydrate type on flavanol absorption and metabolism from chocolate. A randomised, double-blind, three-arm cross-over study was conducted, where fifteen volunteers were randomly assigned to either a high-flavanol (266 mg) chocolate containing maltitol, a high-flavanol (251 mg) chocolate with sucrose or a low-flavanol (48 mg) chocolate with sucrose. Test chocolates were matched for micro- and macronutrients, including the alkaloids theobromine and caffeine, and were similar in taste and appearance. Total flavanol absorption was lower after consumption of the maltitol-containing test chocolate compared with following consumption of its sucrose-containing equivalent (P = 0·002). Although the O-methylation pattern observed for absorbed flavanols was unaffected by sugar type, individual levels of unmethylated ( − )-epicatechin metabolites, 3′-O-methyl-epicatechin and 4′-O-methyl-epicatechin metabolites were lower for the maltitol-containing test chocolate compared with the sucrose-containing equivalent. Despite a reduction in the total plasma pool of flavanols, the maximum time (Tmax) was unaffected. The present data indicate that full assessment of intervention treatments is vital in future intervention trials with flavanols and that carbohydrate content is an important determinant for the optimal delivery of flavanols to the circulation.
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Teng, Renli, Anna-Carin Hansson, and Inger Börjesson. "Oral Bioavailability of Candesartan Cilexetil Suspension." Journal of Pharmacy Technology 23, no. 5 (September 2007): 270–74. http://dx.doi.org/10.1177/875512250702300503.
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Background: Candesartan cilexetil is a prodrug that is converted to candesartan during absorption from the gastrointestinal tract. Candesartan is a potent, orally active, specific angiotensin II type 1 receptor antagonist that has become a well-accepted treatment for hypertension. Pediatric patients often require alternative dosage forms, as candesartan cilexetil is not yet commercially available as a liquid formulation. Objective: To determine the relative bioavailability of candesartan by comparing a candesartan cilexetil tablet (reference formulation) with an oral candesartan cilexetil suspension (test formulation). Methods: In an open-label, randomized, 2 period, 2 treatment crossover study, 24 healthy volunteers were given a 32 mg candesartan cilexetil tablet and a 32 mg candesartan cilexetil suspension with a 7 day washout period between treatments. Results: Pharmacokinetic analyses showed that the mean relative bioavailability of the candesartan cilexetil commercial 32 mg tablet compared with the suspension of 32 mg candesartan cilexetil was 93%. The 90% CIs of the plasma AUC for the tablet versus suspension (0.861 and 0.998, respectively) were well within the bioequivalence criteria of 80–125%. Administration of candesartan cilexetil suspension was associated with a 17% increase in the maximum plasma concentration (Cmax) relative to the tablet administration (643 vs 523 nM/L, respectively). The 90% CIs on the ratio of mean Cmax for the tablet and suspension were 0.738 and 0.914, respectively. Mean time to peak plasma concentrations (tmax) after suspension administration was 3.1 hours, whereas the tablet resulted in a mean tmax of 3.9 hours. No significant differences in elimination half-life were observed between the 2 formulations. Both formulations were well tolerated, and no serious adverse events were reported. Conclusions: These results demonstrate that administration of candesartan cilexetil suspension achieves an extent of absorption and tolerability that is comparable with those of orally administered candesartan cilexetil tablets.
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Ivanova, N. G., I. A. Nikitin, E. G. Cheremnyh, and G. V. Posnova. "Application of the method of bioastesting on test cultures for the determination of bioavailability and toxicity of flour confectionery products." Khleboproducty 31, no. 6 (2022): 47–51. http://dx.doi.org/10.32462/0235-2508-2022-31-6-47-51.
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The article presents the results of the determination of toxicity and bioavailability on test cultures of Tetrahymena pyriformis samples developed at the Department of Biotechnology of Food from Plant and Animal Raw Materials of the Moscow State University of Technology named after K.G. Razumovsky (PKU) flour confectionery - cake «Zimnii Vitamin» and butter cookies «Isida». Studies have shown that the average cell growth factor of ciliates after 24 hours is higher in prototypes of the developed products compared to traditional ones, which indicates their higher nutritional value and bioavailability (for the «Zimnii Vitamin» cake, 2,48 times higher than the values for capital cupcake prototype, for butter cookies «Isida» 1,1 times higher than the prototype of butter cookies «Glagolici»). Also, the experimental samples had high growth rates of ciliates cells in comparison with the control sample (distilled water), which indicates their biological safety. Positive results of the biological assessment allow for further clinical studies by including the developed products in the diets of the studied consumer groups.
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Gao, Huameng, Fan Yang, Hechao Wang, and Wenxiu Wang. "The Design and Data Analysis of Two Stage Cross-Over Test for Medicament Bioavailability." IOP Conference Series: Materials Science and Engineering 452 (December 12, 2018): 022043. http://dx.doi.org/10.1088/1757-899x/452/2/022043.
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Leclère, V., S. Beaufort, S. Dessoy, P. Dehottay, and P. Jacques. "Development of a biological test to evaluate the bioavailability of iron in culture media." Journal of Applied Microbiology 107, no. 5 (November 2009): 1598–605. http://dx.doi.org/10.1111/j.1365-2672.2009.04345.x.
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Kim, Young Ok, Hye Joo Chung, Hak Soo Kong, Don Woong Choi, and Dae Hyun Cho. "The application of Ion chromatographic method for bioavailability and stability test of iron preparations." Archives of Pharmacal Research 22, no. 3 (June 1999): 288–93. http://dx.doi.org/10.1007/bf02976364.
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Prokop, Zbyněk, and Ivan Holoubek. "The use of a microbial contact toxicity test for evaluating cadmium bioavailability in soil." Journal of Soils and Sediments 1, no. 1 (March 2001): 21–24. http://dx.doi.org/10.1007/bf02986465.
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Sánchez-Marín, Paula. "A review of chemical speciation techniques used for predicting dissolved copper bioavailability in seawater." Environmental Chemistry 17, no. 7 (2020): 469. http://dx.doi.org/10.1071/en19266.
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Environmental contextCopper (Cu) is a metal of ecotoxicological concern in contaminated coastal areas. Cu present as the free ion is considered the most bioavailable fraction of the metal, and there is a need for the correct measurement or estimation of free Cu-ion concentrations in seawater. I review studies that have combined a biological measure of Cu bioavailability with chemical speciation measurements, and critically assess the ability of current methods to predict Cu bioavailability in contaminated coastal ecosystems. AbstractCopper (Cu) is an essential metal, but it is also toxic at concentrations reached in polluted coastal areas. In seawater, the speciation of this metal is largely controlled by the presence of dissolved organic matter (DOM), which binds Cu ions decreasing the concentration of inorganic and free forms of the metal. This is important to aquatic life, given that the bioavailability of dissolved metals is generally expected to be determined by the free ion concentration according to bioavailability models such as the free ion activity model and biotic ligand model (FIAM/BLM). The analytical determination of free metal concentrations in seawater is a challenging task that is needed (in combination with toxicity tests or other means of testing bioavailability) in order to test the applicability of the FIAM/BLM in particular systems and also for its application in monitoring and risk assessment of metals. This review summarises the studies that combine a biological measure of Cu bioavailability with the use of a chemical speciation technique for the measurement of Cu speciation in seawater, and it presents a critical examination of the results of those studies in order to determine which techniques are more suitable for the prediction of Cu bioavailability in seawater and to highlight research needs in the field. The technique showing the highest level of agreement with bioavailability data is anodic stripping voltammetry (ASV). Cathodic stripping voltammetry (CSV), aluminium hydroxide coated exchange resin (ALSA), and diffusion gradients in thin films (DGT) are also promising in this regard, although DGT slightly overestimates bioavailable Cu. More research is needed comparing the performance of different chemical speciation techniques with Cu bioavailability in seawater, especially at environmentally relevant concentrations of Cu.
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Salve, Priyanka M., Shital V. Sonawane, Mayuri B. Patil, and Rajendra K. Surawase. "Dissolution and Dissolution Test Apparatus: A Review." Asian Journal of Research in Pharmaceutical Sciences 11, no. 3 (August 14, 2021): 229–36. http://dx.doi.org/10.52711/2231-5659.2021.00037.
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Dissolution is an official test. These used by pharmacopeias for evaluating drug release of solid and semisolid dosages forms. The application of the dissolution testing ensures consistent product quality and to predict in vivo drug bioavailability. The dissolution test, in its simplest form, placing the formulation in a dissolution apparatus containing suitable dissolution medium, allowing it to dissolved specified period of time and then using appropriate rational method to determine the amount of drug. Dissolution test are probative and analysis like drug degradation profile, shelf-life studies, stability, physical and mechanical testing of dosage forms. The present review outlines findings on various dissolution apparatus, various methods and their modification. Dissolution testing the of various dosage form like Delayed release dosage form, Immediate release dosage form, Extended-release dosage form, Powders, Chewable tablets, Transdermal delivery system, Buccal tablets, Soft gelatin capsule, Chewing gums, Suppositories, Aerosols and others semisolids. This article goal of the description of the all-official dissolution testing apparatus.
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Spogli, Roberto, Maria Bastianini, Francesco Ragonese, Rossana Iannitti, Lorenzo Monarca, Federica Bastioli, Irina Nakashidze, et al. "Solid Dispersion of Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Microparticles Improves Oral Bioavailability." Nutrients 10, no. 12 (December 5, 2018): 1925. http://dx.doi.org/10.3390/nu10121925.
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Resveratrol, because of its low solubility in water and its high membrane permeability, is collocated in the second class of the biopharmaceutical classification system, with limited bioavailability due to its dissolution rate. Solid dispersion of resveratrol supported on Magnesium DiHydroxide (Resv@MDH) was evaluated to improve solubility and increase bioavailability of resveratrol. Fluorimetric microscopy analysis displays three types of microparticles with similar size: Type 1 that emitted preferably fluorescence at 445 nm with bandwidth of 50 nm, type 2 that emitted preferably fluorescence at 605 nm with bandwidth of 70 nm and type 3 that is non-fluorescent. Micronized pure resveratrol displays only microparticles type 1 whereas type 3 are associated to pure magnesium dihydroxide. Dissolution test in simulated gastric environment resveratrol derived from Resv@MDH in comparison to resveratrol alone displayed better solubility. A 3-fold increase of resveratrol bioavailability was observed after oral administration of 50 mg/kg of resveratrol from Resv@MDH in rabbits. We hypothesize that type 2 microparticles represent magnesium dihydroxide microparticles with a resveratrol shell and that they are responsible for the improved resveratrol solubility and bioavailability of Resv@MDH.