Relevant bibliographies by topics / Drug distribution ratios

Academic literature on the topic 'Drug distribution ratios'

Author: Grafiati
Published: 10 December 2022
Last updated: 28 January 2023

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Journal articles on the topic "Drug distribution ratios"

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Puanglamjeak, Mananya, Siriporn Pranee, and Samitthichai Seeyangnok. "Preparation of Crude Turmeric Extract Loaded Poly(Acrylamide-co-Acrylic Acid) Microspheres for Drug Release System." Materials Science Forum 990 (May 2020): 86–90. http://dx.doi.org/10.4028/www.scientific.net/msf.990.86.

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Crude turmeric extract (CTE), which is a natural substance, is obtained from Curcuma Longa L. This substance is widely used in pharmaceutical application because of its ability to treat various diseases. Dermatitis is one of the many diseases that can be treated by CTE due to their inhibition of gram-negative and gram-positive bacteria. CTE has short half-life and easy to degradation. Therefore, protection has to be applied on CTE to prevent from decomposition before applying to skin. This research mainly focuses on preparation of CTE loaded poly (acrylamide-co-acrylic acid) (PAMAA) hydrogel microspheres (HM) at 9:1, 8:2 and 7:3 mole ratios and investigation of the releasing profile of CTE from microsphere. The particle size distribution of PAMAA microsphere that is analyzed by SEM found that mole ratios of PAMAA with 9:1, 8:2 and 7:3 showed the narrow particle distribution with average particle size at 28.1±7.4, 25.5±6.6 and 23.2±5.5 respectively. Thermal decomposition property of PAMAA is confirmed by TGA and HM swelling ratios are confirmed by weight indicated that the percentage swelling ratios of PAMAA with 9:1, 8:2 and 7:3 mole ratios is 1500, 1230 and 780 respectively. CTE releasing profiles are confirmed by UV-Vis in the media solutions of PBS pH 8.5 and NaOH pH 12.
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Yatscoff, R. W., N. Honcharik, M. Lukowski, J. Thliveris, P. Chackowsky, and C. Faraci. "Distribution of cyclosporin G (NVa2 cyclosporin) in blood and plasma." Clinical Chemistry 39, no. 2 (February 1, 1993): 213–17. http://dx.doi.org/10.1093/clinchem/39.2.213.

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Abstract We report here on the distribution of cyclosporin G (CsG), an analog of cyclosporin A, in whole blood. CsG has a temperature-dependent distribution between erythrocytes (RBCs) and plasma. After 30 min at 37 degrees C, the plasma/whole blood and plasma/RBC ratios were relatively constant (0.7-0.8) up to CsG at 1000 micrograms/L. At 5000 micrograms/L, this ratio increased to 1.0-1.1 for plasma/whole blood and 1.7 for plasma/RBC. The primary CsG metabolites GM1 and GM9 were sequestered within RBCs to a greater extent than was the parent drug. In whole blood, approximately 2% of CsG was bound to granulocytes, 6% to lymphocytes, and 50-55% to RBC, and 35-40% was found in the plasma fraction. The free fraction of the drug as determined by ultracentrifugation was 5-6% and 13-17% of total drug at 37 and 4 degrees C, respectively. In plasma the drug was primarily associated with high-density lipoprotein (50-60%) and to a lesser degree with low-density (20-30%) and very-low-density (10%) lipoproteins.
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Chang, Hsuan Ping, Yuen Kiu Cheung, and Dhaval K. Shah. "Whole-Body Pharmacokinetics and Physiologically Based Pharmacokinetic Model for Monomethyl Auristatin E (MMAE)." Journal of Clinical Medicine 10, no. 6 (March 23, 2021): 1332. http://dx.doi.org/10.3390/jcm10061332.

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Monomethyl auristatin E (MMAE) is one of the most commonly used payloads for developing antibody–drug conjugates (ADC). However, limited studies have comprehensively evaluated the whole-body disposition of MMAE. Consequently, here, we have investigated the whole-body pharmacokinetics (PK) of MMAE in tumor-bearing mice. We show that while MMAE is rapidly eliminated from the plasma, it shows prolonged and extensive distribution in tissues, blood cells, and tumor. Highly perfused tissues (e.g., lung, kidney, heart, liver, and spleen) demonstrated tissue-to-plasma area under the concentration curve (AUC) ratios > 20, and poorly perfused tissues (e.g., fat, pancreas, skin, bone, and muscle) had ratios from 1.3 to 2.4. MMAE distribution was limited in the brain, and tumor had 8-fold higher exposure than plasma. A physiological-based pharmacokinetic (PBPK) model was developed to characterize the whole-body PK of MMAE, which accounted for perfusion/permeability-limited transfer of drug in the tissue, blood cell distribution of the drug, tissue/tumor retention of the drug, and plasma protein binding. The model was able to characterize the PK of MMAE in plasma, tissues, and tumor simultaneously, and model parameters were estimated with good precision. The MMAE PBPK model presented here can facilitate the development of a platform PBPK model for MMAE containing ADCs and help with their preclinical-to-clinical translation and clinical dose optimization.
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Ramesh, Yerikala, Abhilash Kaki Rohan, Balasaradhi Koorapati, and P. Sudarsanam. "Formulation and evaluation of almotriptan controlled release pellets." Journal of Drug Delivery and Therapeutics 9, no. 1-s (February 15, 2019): 312–18. http://dx.doi.org/10.22270/jddt.v9i1-s.2355.

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Abstract: The aim of the present study was to formulate and evaluate Almotriptan pellets. Almotriptan controlled release pellets were prepared by Solution layering technique by using croscarmellose and povidone in former case and three different polymers HPMC K 100, Ethyl cellulose and Eudragit RS 100 as rate controlling polymer in three different ratios like 1:1, 1:1.5 and 1:2 to achieve desired release in later case. Evaluation was performed according to the Pharmacopoeia standards including Drug excipients compatibility, Percentage yield, Particle size distribution, Drug content analysis and in-vitro release study. The best results were found to be using Almotriptan and Eudragit RS 100 in 1:2 ratios. A broad variety of drug release pattern could be achieved by variation of polymers ratios which was optimized to match the target release profile. In comparison of in-vitro release studies for different controlled release formulations, F9 releases 98.54% of drug at the end of 12th hour and was considered as best formulation. Stability study has shown no significant change in the drug content analysis and in-vitro dissolution study of best formulation even after 6 months. Keywords: Almotriptan, Controlled release, Dissolution profile, in-vitro drug release, Stability studies.
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Brunner, Martin, Ursula Hollenstein, Simon Delacher, Dorothea Jäger, Rainer Schmid, Edith Lackner, Apostoulos Georgopoulos, Hans Georg Eichler, and Markus Müller. "Distribution and Antimicrobial Activity of Ciprofloxacin in Human Soft Tissues." Antimicrobial Agents and Chemotherapy 43, no. 5 (May 1, 1999): 1307–9. http://dx.doi.org/10.1128/aac.43.5.1307.

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ABSTRACT Interstitial ciprofloxacin concentrations in soft tissues were measured by microdialysis following intravenous administration of 200 mg to each of eight healthy volunteers. Interstitial ciprofloxacin concentrations were significantly lower than corresponding total serum drug concentrations; the interstitium-to-serum concentration ratios ranged from 0.55 to 0.73. An in vitro simulation based on interstitial pharmacokinetics showed a substantially lower antimicrobial activity than did the simulation based on serum pharmacokinetics. Thus, ciprofloxacin concentrations at the site of effect may be subinhibitory although effective concentrations are attained in serum.
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Odongo, Charles Okot, Lydia Nakiyingi, Clovis Gatete Nkeramihigo, Daniel Seifu, and Kuteesa Ronald Bisaso. "Towards Improved Management of Tuberculous Bloodstream Infections: Pharmacokinetic Considerations with Suggestions for Better Treatment Outcomes." Antibiotics 11, no. 7 (July 5, 2022): 895. http://dx.doi.org/10.3390/antibiotics11070895.

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Mycobacterium tuberculosis is the leading cause of sepsis among HIV-infected adults, yet effective treatment remains a challenge. Efficacy of antituberculous drugs is optimized by high Area Under Curve to Minimum Inhibitory Concentration (AUC/MIC) ratios, suggesting that both the drug concentration at the disease site and time above MIC are critical to treatment outcomes. We elaborate on sepsis pathophysiology and show how it adversely affects antituberculous drug kinetics. Expanding distribution volumes secondary to an increased vascular permeability prevents the attainment of target Cmax concentrations for nearly all drugs. Furthermore, sepsis-induced metabolic acidosis promotes protonation, which increases renal clearance of basic drugs such as isoniazid and ethambutol, and hence AUCs are substantially reduced. Compared with the treatment of non-sepsis TB disease, these distorted kinetics underlie the poor treatment outcomes observed with bloodstream infections. In addition to aggressive hemodynamic management, an increase in both the dose and frequency of drug administration are warranted, at least in the early phase of treatment.
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Robillard, Kevin R., Gary N. Y. Chan, Guijin Zhang, Charles la Porte, William Cameron, and Reina Bendayan. "Role of P-Glycoprotein in the Distribution of the HIV Protease Inhibitor Atazanavir in the Brain and Male Genital Tract." Antimicrobial Agents and Chemotherapy 58, no. 3 (December 30, 2013): 1713–22. http://dx.doi.org/10.1128/aac.02031-13.

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ABSTRACTThe blood-testis barrier and blood-brain barrier are responsible for protecting the male genital tract and central nervous system from xenobiotic exposure. In HIV-infected patients, low concentrations of antiretroviral drugs in cerebrospinal fluid and seminal fluid have been reported. One mechanism that may contribute to reduced concentrations is the expression of ATP-binding cassette drug efflux transporters, such as P-glycoprotein (P-gp). The objective of this study was to investigatein vivothe tissue distribution of the HIV protease inhibitor atazanavir in wild-type (WT) mice, P-gp/breast cancer resistance protein (Bcrp)-knockout (Mdr1a−/−,Mdr1b−/−, andAbcg2−/−triple-knockout [TKO]) mice, and Cyp3a−/−(Cyp) mice. WT mice and Cyp mice were pretreated with a P-gp/Bcrp inhibitor, elacridar (5 mg/kg of body weight), and the HIV protease inhibitor and boosting agent ritonavir (2 mg/kg intravenously [i.v.]), respectively. Atazanavir (10 mg/kg) was administered i.v. Atazanavir concentrations in plasma (Cplasma), brain (Cbrain), and testes (Ctestes) were quantified at various times by liquid chromatography-tandem mass spectrometry. In TKO mice, we demonstrated a significant increase in atazanavirCbrain/Cplasma(5.4-fold) andCtestes/Cplasma(4.6-fold) ratios compared to those in WT mice (P< 0.05). Elacridar-treated WT mice showed a significant increase in atazanavirCbrain/Cplasma(12.3-fold) andCtestes/Cplasma(13.5-fold) ratios compared to those in vehicle-treated WT mice. In Cyp mice pretreated with ritonavir, significant (P< 0.05) increases in atazanavirCbrain/Cplasma(1.8-fold) andCtestes/Cplasma(9.5-fold) ratios compared to those in vehicle-treated WT mice were observed. These data suggest that drug efflux transporters, i.e., P-gp, are involved in limiting the ability of atazanavir to permeate the rodent brain and genital tract. Since these transporters are known to be expressed in humans, they could contribute to the low cerebrospinal and seminal fluid antiretroviral concentrations reported in the clinic.
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Chigumira, Washington, Prosper Maposa, Louis L. Gadaga, Admire Dube, Dexter Tagwireyi, and Charles C. Maponga. "Preparation and Evaluation of Pralidoxime-Loaded PLGA Nanoparticles as Potential Carriers of the Drug across the Blood Brain Barrier." Journal of Nanomaterials 2015 (2015): 1–5. http://dx.doi.org/10.1155/2015/692672.

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Pralidoxime is an organophosphate antidote with poor central nervous system distribution due to a high polarity. In the present study, pralidoxime-loaded poly(lactic-co-glycolic acid) nanoparticles were prepared and evaluated as a potential delivery system of the drug into the central nervous system. The nanoparticles were prepared using double emulsion solvent evaporation method. Poly(lactic-co-glycolic acid) (PLGA) in ethyl acetate made the organic phase and pralidoxime in water made the aqueous phase. The system was stabilized by polyvinyl alcohol. Different drug/polymer ratios were used (1 : 1, 1 : 2, and 1 : 4) and the fabricated particles were characterized for encapsulation efficiency using UV-VIS Spectroscopy; particle size distribution, polydispersity index, and zeta potential using photon correlation spectroscopy; andin vitrodrug release profile using UV-VIS Spectroscopy. Mean particle sizes were 386.6 nm, 304.7 nm, and 322.8 nm, encapsulation efficiency was 28.58%, 51.91%, and 68.78%, and zeta potential was 5.04 mV, 3.31 mV, and 5.98 mV for particles with drug/polymer ratios 1 : 1, 1 : 2, and 1 : 4, respectively.In vitrodrug release profile changed from biphasic to monobasic as the drug/polymer ratio decreased from 1 : 1 to 1 : 4. Stable pralidoxime-loaded PLGA nanoparticles were produced using double emulsion solvent evaporation techniques.
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Nakanishi, Hajime, Nancy F. Cruz, Keiji Adachi, Louis Sokoloff, and Gerald A. Dienel. "Influence of Glucose Supply and Demand on Determination of Brain Glucose Content with Labeled Methylglucose." Journal of Cerebral Blood Flow & Metabolism 16, no. 3 (May 1996): 439–49. http://dx.doi.org/10.1097/00004647-199605000-00010.

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The equilibrium brain/plasma distribution ratio for 3- O-methyl-D-glucose (methylglucose) varies with plasma and tissue glucose contents and can be used to determine local glucose levels in brain. This ratio was previously found to rise as brain glucose concentration fell in response to lowered plasma glucose content. The ratios, however, differed with the same tissue glucose levels in conscious and pentobarbital-sedated rats, suggesting that changes in metabolic demand might alter the quantitative relationship between the methylglucose distribution ratio and brain glucose concentration. To examine this possibility, metabolic rate was varied by focal drug application, and hexose concentrations measured in treated and surrounding tissue. When tissue glucose levels were reduced by raised metabolic demand, methylglucose distribution ratios also fell. When brain glucose levels rose due to reduced consumption, the methylglucose distribution ratio also rose. Thus, in contrast to the inverse relationship between brain/plasma methylglucose ratio and brain glucose concentration when brain glucose content is altered secondarily to changes in plasma glucose level, changes in brain glucose content induced by altered glucose utilization cause the brain glucose level and methylglucose distribution ratio to rise and fall in a direct relationship. Determination of brain glucose content from methylglucose distribution ratios must take into account rates of glucose delivery and consumption.
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Tagger, Aaron Y., Joan Boux, and Jim A. Wright. "Hydroxy[14C]urea uptake by normal and transformed human cells: evidence for a mechanism of passive diffusion." Biochemistry and Cell Biology 65, no. 11 (November 1, 1987): 925–29. http://dx.doi.org/10.1139/o87-120.

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The antitumor agent hydroxyurea is a potent inhibitor of cell division and selectivity toxic for rapidly proliferating cells. This drug has been used in the treatment of human cancer and, since drug transport is an important aspect of drug action, we investigated the mechanism of hydroxy[14C]urea uptake by human diploid fibroblasts and their SV40-virus-transformed counterparts. Kinetic analysis of drug uptake, studies with metabolic inhibitors, and estimates of cell/medium distribution ratios and temperature coefficient (Q10) values indicated that hydroxyurea enters normal and SV40-virus-transformed human cells by a mechanism of diffusion.
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Books on the topic "Drug distribution ratios"

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Wollschlaeger, Bernd. Opioid Overdose Education, Prevention, and Management (DRAFT). Oxford University Press, 2018. http://dx.doi.org/10.1093/med/9780190265366.003.0013.

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In reviewing the elements of opioid overdose education, prevention, and management, this chapter focuses particularly on practical interventions that are available and deserve advocacy; e.g., provision of naloxone to those with opioid use disorder and to possible first responders. It moves from a discussion of the epidemiology of opioid deaths to the more individual topic of patient risk for overdose. Prophylactic interventions in the form of education of the patient’s family and friends, and agreements for treatment with informed consent are described. There follows a discussion of management of the opioid poisoning itself, including use/distribution of naloxone injection. Two figures are included: drug overdose death rates in the United States (2014); a map describing the current states with naloxone or “good Samaritan” laws impacting opioid overdose management. A text box with resources includes directions for initiation of community overdose prevention and intervention schemes.
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Medicaid: Alternatives for improving the distribution of funds to states : fact sheet for Congressional requesters. Washington, DC: The Office, 1993.

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Book chapters on the topic "Drug distribution ratios"

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Basa, Louisette. "Drug-to-Antibody Ratio (DAR) and Drug Load Distribution by LC-ESI-MS." In Methods in Molecular Biology, 285–93. Totowa, NJ: Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-541-5_18.

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Ouyang, Jun. "Drug-to-Antibody Ratio (DAR) and Drug Load Distribution by Hydrophobic Interaction Chromatography and Reversed Phase High-Performance Liquid Chromatography." In Methods in Molecular Biology, 275–83. Totowa, NJ: Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-541-5_17.

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Saltzman, W. Mark. "Pharmacokinetics of Drug Distribution." In Drug Delivery. Oxford University Press, 2001. http://dx.doi.org/10.1093/oso/9780195085891.003.0012.

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Pharmacology, the study of agents and their actions, can be divided into two branches. Pharmacodynamics is concerned with the effects of a drug on the body and, therefore, encompasses dose–response relationships as well as the molecular mechanisms of drug activity. Pharmacokinetics, on the other hand, is concerned with the effect of the body on the drug. Drug metabolism, transport, absorption, and elimination are components of pharmacokinetic analysis. Physiology influences the distribution of drugs within the body; overall distribution depends on rates of drug uptake, rates of distribution between tissue compartments, and rates of drug elimination or biotransformation. Each of these phenomena potentially involves aspects of drug diffusion, permeation through membranes, and fluid movement that were introduced in the previous sections. The goal of pharmacokinetics is synthesis of these isolated basic mechanisms into a functional unit; this goal is most often achieved by development of a mathematical model that incorporates descriptions of the uptake, distribution, and elimination of a drug in humans or animals. This model can then be used to predict the outcome of different dosage regimens on the time course of drug concentrations in tissues. The development of a complete pharmacokinetic model for any given drug is a substantial undertaking, since the fate of any compound introduced into a whole organism is influenced by a variety of factors, and is usually complicated—in ways that are difficult to predict—by the presence of disease. In this section, pharamacokinetics will be introduced by first considering the simplest situation: an agent is introduced into a single body compartment from which it is also eliminated. While quite sophisticated compartmental models can be developed from this basic construct, it is frequently difficult to relate model parameters (such as the volume of specific compartments or the rate of transfer between compartments) to physiological or anatomical parameters. To avoid this difficulty, physiological pharmacokinetic models are frequently employed; in these models, the kinetics of drug uptake, distribution, and elimination from local tissue sites are predicted by constructing anatomically and biochemically accurate models of the tissue environment.
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Burns, Aine, and Caroline Ashley. "Drugs and the kidney." In Oxford Textbook of Medicine, edited by John D. Firth, 5150–66. Oxford University Press, 2020. http://dx.doi.org/10.1093/med/9780198746690.003.0509.

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The kidney plays a critical role in the elimination of many drugs from the body, hence consideration should be given to a patient’s renal function whenever any drug is prescribed. Much kidney disease is unrecognized, but the widespread reporting of estimated glomerular filtration rates (eGFR) has brought greater awareness of the prevalence of chronic kidney disease (CKD), thereby encouraging medical practitioners to take account of reduced renal function when prescribing. CKD is very often one of many coexisting comorbid conditions, especially in elderly patients, when particularly careful thought must be given to appropriate drug dosing and the possibility of drug interactions. A reduced GFR is the primary reason for reduced excretion of drugs in renal failure, but drug absorption, distribution, protein binding, metabolism, and pharmacodynamics may all be affected. Key general points—both filtration and secretion of drugs appear to fall in parallel and in proportion to the GFR. The clinical significance of a reduction in GFR and increased drug half-life depends on the relative importance of renal excretion and metabolism as a mode of elimination, and the therapeutic ratio of the drug. If nonrenal clearance accounts for elimination of more than 50% of a drug, then no adjustment needs be made to dose/frequency of administration. Dosages of drugs which are mainly excreted in active form by the kidney may need to be modified to avoid accumulation. Potentially toxic drugs should only be used in patients with renal failure if there is a specific indication for their use and if therapy can be monitored appropriately. If dose adjustment is required, then dose, dose interval, or both can be adjusted to achieve the desired therapeutic profile.
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Dye, Christopher. "Strains and Drug Resistance." In The Population Biology of Tuberculosis. Princeton University Press, 2015. http://dx.doi.org/10.23943/princeton/9780691154626.003.0005.

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This chapter examines the geographical distribution of resistant forms of Mycobacterium tuberculosis and their time trends. Apart from drug resistance, there are plenty of other main questions about M. tuberculosis population genetics. To combat epidemics of drug-resistant TB, it is vital to understand why some resistant strains have greater reproductive fitness than drug-susceptible strains. The chapter first provides an overview of genetic variation in M. tuberculosis before discussing resistance (new and acquired) to first-and second-line drugs. It then considers the link between drug resistance and HIV coinfection, global distribution of drug-resistant TB, relative reproductive fitness, and absolute reproductive fitness. It shows that drug resistance is preventable and reversible, but this must be corroborated and expanded with longer series of data from a wider range of countries, countries with high rates of HIV infection (for example, Botswana and South Africa), and those reporting cases of extensively drug-resistant TB (XDR-TB).
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Hudson, Irene, Ainura Tursunalieva, and J. Geoffrey Chase. "Copula Modelling of Agitation-Sedation (A-S) in ICU: Threshold Analysis of Nurses’ Scores of A-S and Automated Drug Infusions by Protocol." In Recent Advances in Medical Statistics [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.105753.

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Pain management is increasingly recognised as a formal medical subspecialty worldwide. Empirical distributions of the nurses’ ratings of a patient’s pain and/or agitation levels and the administered dose of sedative are often positively skewed, and if the joint distribution is non-elliptical, then high nurses’ ratings of a patient’s agitation levels may not correspond to the true occurrences of patient’s agitation-sedation (A-S). Copulas are used to capture such nonlinear dependence between skewed distributions and check for the presence of lower (LT) and/or upper tail (UT) dependence between the nurses’ A-S rating and the automated sedation dose, thus finding thresholds and regions of mismatch between the nurse’s scores and automated sedation dose, thereby suggesting a possible way forward for an improved alerting system for over- or under-sedation. We find for LT dependence nurses tend to underestimate the patient’s agitation in the moderate agitation zone. In the mild agitation zone, nurses tend to assign a rating, that is, on average, 0.30 to 0.45 points lower than expected for the patient’s given agitation severity. For UT dependence in the moderate agitation zone, nurses tend to either moderately or strongly underestimate patient’s agitation, but in periods of severe agitation, nurses tend to overestimate a patient’s agitation. Our approach lends credence to augmenting conventional RASS and SAS agitation measures with semi-automated systems and identifying thresholds and regions of deviance for alerting increased risk.
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Beckett, Katherine. "The Limits of Recent Drug Policy Reforms." In Ending Mass Incarceration, 71–90. Oxford University Press, 2022. http://dx.doi.org/10.1093/oso/9780197536575.003.0004.

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Judging by historical standards, it appears that the drug war is alive and well. This chapter identifies several factors that explain why recent drug policy reforms have had such a modest impact on drug arrests and incarceration. First, state lawmakers have focused overwhelmingly on reducing penalties for drug possession, but people who were convicted of this specific offense comprise a very small share (3.5 percent) of the prison population. Second, while reducing the use of confinement in cases involving drug distribution could have a more meaningful impact on the scale of incarceration, policy is moving in the opposite direction. Third, the ongoing commitment to drug war practices in rural and suburban areas is sustaining high drug arrest rates and incarceration. Finally, one of the most pervasive kinds of drug policy reforms—reliance on drug courts—is likely increasing rather than reducing drug arrests and incarceration. There is also evidence that drug courts enhance racial disparities in drug case outcomes.
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A. Badria, Farid. "Perspective Chapter: Repurposing Natural Products to Target COVID-19: Molecular Targets and New Avenues for Drug Discovery." In Antiviral Drugs [Working Title]. IntechOpen, 2022. http://dx.doi.org/10.5772/intechopen.103153.

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World Health Organization (WHO) declared on March 11, 2020, coronavirus disease, which erupted in December 19th, 2019 in Wuhan, China (COVID-19) as worldwide pandemic disease. Researchers worldwide were successful to provide a prophylactic approach via developing several vaccines, which were swiftly approved by WHO under Emergency Use Listing (EUL) status. So far, lopinavir, chloroquine, azithromycin, hydroxychloroquine, favipiravir, umifenovir, ribavirin, remdesivir, and darunavir have been tested clinically. Hydroxychloroquine, favipiravir, and chloroquine exhibited a high ratio of distribution for the lung and were reported to minimize viral tonnage in respiratory system of many COVID-19 cases. However, none of the tested drugs showed a conclusive, safe, and efficient activity against COVID-19. This prompted many experts in drug discovery to fetch in the treasure of many available old drugs of natural origin to repurpose based upon their well-studied pharmacology, pharmacodynamics, virtual screening, and artificial intelligence studies. In this review chapter, we will address the repurposing of natural products and their derivatives to be used in treatment of COVID-19 via targeting host cells machinery and viral proteins either in early stages by blocking virus entry to cells or lately through inhibition of viral replication.
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Chorev, Nitsan. "Kenya in the 1980s." In Give and Take, 55–82. Princeton University Press, 2019. http://dx.doi.org/10.23943/princeton/9780691197845.003.0003.

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This chapter describes the interplay between foreign aid and state policies in Kenya that together contributed to the emergence of a small yet robust locally owned pharmaceutical sector. Most important was a “ration kits” program that helped rationalize the procurement and distribution of drugs in rural areas. As part of that program, a government-funded component was used to specifically purchase locally produced drugs. This proved critical for the emergence and growth of the Kenyan pharmaceutical sector. Other policies in support of the state-owned pharmaceutical firm also indirectly pushed for and later assisted privately owned pharmaceutical firms. With the support of foreign aid, then, the Kenyan government was able to create a market for local producers. Foreign assistance did not come with technology transfer (mentoring), and access to technical know-how was predominantly available to Kenyans of Indian origin, whose social position during colonialism and after independence granted them educational, commercial, and cultural ties abroad. Moreover, there was little attention to quality standards (monitoring).
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Singh, Rahul. "Learning and Prediction of Complex Molecular Structure-Property Relationships." In Machine Learning, 1482–98. IGI Global, 2012. http://dx.doi.org/10.4018/978-1-60960-818-7.ch518.

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The problem of modeling and predicting complex structure-property relationships, such as the absorption, distribution, metabolism, and excretion of putative drug molecules is a fundamental one in contemporary drug discovery. An accurate model can not only be used to predict the behavior of a molecule and understand how structural variations may influence molecular property, but also to identify regions of molecular space that hold promise in context of a specific investigation. However, a variety of factors contribute to the difficulty of constructing robust structure activity models for such complex properties. These include conceptual issues related to how well the true bio-chemical property is accounted for by formulation of the specific learning strategy, algorithmic issues associated with determining the proper molecular descriptors, access to small quantities of data, possibly on tens of molecules only, due to the high cost and complexity of the experimental process, and the complex nature of bio-chemical phenomena underlying the data. This chapter attempts to address this problem from the rudiments: the authors first identify and discuss the salient computational issues that span (and complicate) structure-property modeling formulations and present a brief review of the state-of-the-art. The authors then consider a specific problem: that of modeling intestinal drug absorption, where many of the aforementioned factors play a role. In addressing them, their solution uses a novel characterization of molecular space based on the notion of surface-based molecular similarity. This is followed by identifying a statistically relevant set of molecular descriptors, which along with an appropriate machine learning technique, is used to build the structure-property model. The authors propose simultaneous use of both ratio and ordinal error-measures for model construction and validation. The applicability of the approach is demonstrated in a real world case study.
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Conference papers on the topic "Drug distribution ratios"

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Thomas, Antony, Jifu Tan, Susan Perry, and Yaling Liu. "Characterization of Nanoparticle Distribution in Microcirculation Through a Microfluidics Device." In ASME 2011 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2011. http://dx.doi.org/10.1115/sbc2011-53943.

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Various methods of targeted nano drug delivery have been developed in recent years to reduce side effects, toxicity, and lower drug doses [1]. The use of nanoparticles in drug delivery provides advantages in drug targeting, delivery and release along with serving in diagnosis and therapy [2]. Higher percentage of nanoparticle drug is uptaken by the target cells while larger drug particles are easily cleaned off by the human body. Nanoparticles also have large surface to volume ratio, which aids in attachment of many functional groups and thereby enhances targeting.
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Ma, Tiangang, Yanbing Hu, and Qinghua Zhang. "Composition ration and drug-sensitivity distribution of phlegmy patogenic bacteria from AECOPD inpatients." In ERS International Congress 2020 abstracts. European Respiratory Society, 2020. http://dx.doi.org/10.1183/13993003.congress-2020.2344.

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Bozsak, Franz, Jean-Marc Chomaz, Fulvio Martinelli, and Abdul I. Barakat. "Modeling Arterial Wall Transport for Drug-Eluting Stents." In ASME 2011 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2011. http://dx.doi.org/10.1115/sbc2011-53871.

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Drug-eluting stents (DES) are very commonly used for treating coronary atherosclerotic lesions. Despite the broad effectiveness of DES, ∼5% of treated patients experience complications including in-stent restenosis and late-stent thrombosis. The occurrence of these complications depends on various factors including the concentration of the eluted drug in the arterial wall and the rate of arterial re-endothelialization. Drug concentration in the arterial wall needs to be sufficiently high to be efficacious while remaining sufficiently low to avoid compromising wall stability (leading to stent malapposition). Furthermore, because drugs used in DES modulate proliferation rates of not only smooth muscle cells but also endothelial cells, the drug concentration affects re-endothelialization rates. Drug concentration in the arterial wall is determined by the transport and metabolism of the drug and may also be affected by the flow field in the lumen of the stented vessel. In the present study, we develop a computational model of drug transport in the arterial wall. Previous models have typically treated the arterial wall as a homogeneous porous medium [1] and have often ignored drug reaction with cells in the arterial wall [2]. In the present study, we have developed a model that incorporates the multi-layer structure of the arterial wall and have compared its predictions for the distribution of an eluted drug within the arterial wall with those of the single-layer homogeneous wall model.
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Park, Juyoung, Peter M. Bungay, Robert J. Lutz, James J. Augsburger, Ronald W. Millard, Abhijit S. Roy, and Rupak K. Banerjee. "Comparison of Convective Transport of Drug Between Intravitreal Injection and Controlled Release Implant." In ASME 2004 International Mechanical Engineering Congress and Exposition. ASMEDC, 2004. http://dx.doi.org/10.1115/imece2004-59300.

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It is important to know the drug distribution following administration of drug in order to properly treat with adequate dosage and thus, avoid damage to tissues due to excessive high concentrations. A computer model was developed to determine drug distribution by convective-diffusive transport processes in a rabbit eye. When compared with pure diffusion within vitreous, the ratio of the amount of a model compound, fluorescein, reaching the retina to that cleared by aqueous outflow increased by 93% and 84% for intravitreal injection and implant, respectively, with maximum vitreous outflow (glaucomatous eye). The result shows that the combined “convective” effect due to the vitreous outflow and “wash out” effect by aqueous outflow has significant impact on drug distribution for both intravitreal injection and implant. These two effects should be considered in the design of drug delivery strategies.
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Hu, Y., Y. Guo, and T. Ma. "Analysis for Composition Ration and Drug-Sensitivity Distribution of Phlegmy Patogenic Bacteria from Acute Exacerbation of COPD Inpatients." In American Thoracic Society 2022 International Conference, May 13-18, 2022 - San Francisco, CA. American Thoracic Society, 2022. http://dx.doi.org/10.1164/ajrccm-conference.2022.205.1_meetingabstracts.a1878.

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Vick, B. D., W. Wrigglesworth, L. B. Scott, and K. M. Ragsdell. "Optimal Design of Wind Turbines Using BIAS, A Method of Multipliers Code." In ASME 1988 Design Technology Conferences. American Society of Mechanical Engineers, 1988. http://dx.doi.org/10.1115/detc1988-0026.

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Abstract A method has been developed and is demonstrated which determines the chord and twist distribution for a wind turbine with maximum power coefficient. Only small wind turbines (less than 10 kilowatts) are considered in this study, but the method could be used for larger wind turbines. Glauert determined a method for estimating the chord and twist distribution that will maximize the power coefficient if there is no drag. However, the method proposed here determines the chord and twist distribution which will maximize the power coefficient with the effect of drag included. Including drag in the analysis does not significantly affect the Glauert chord and twist distribution for airfoils with a high lift coefficient at the maximum lift to drag ratio. However, if the airfoil has a fairly low lift coefficient at its maximum lift to drag ratio due to its shape or a rough surface then significant improvement can be obtained in power coefficient by altering the Glauert chord and twist distribution according to the method proposed herein.
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Mejia, Juan, Rosaire Mongrain, Richard Leask, Olivier F. Bertrand, and Josep Cabau-Rodes. "Transient and Non-Newtonian Effects on the Wall Shear Stress Distribution of a Stented Artery." In ASME 2009 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2009. http://dx.doi.org/10.1115/sbc2009-206735.

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For the last few decades stents have played a central role in the treatment of artherosclerosis. Although bare-metal stents (BMS) have significantly reduced levels of restenosis rates by 20 or 30% [1], restenosis rates remain high at around 25% [1]. The introduction of drug-eluting stents have reduced restenosis rates even further [2], but are associated with high risk of late thrombosis [3].
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Huang, Liuyi, Yuyan Li, Jiqiang Xu, Qingchang Xu, Fenfang Zhao, Xinxin Wang, Yanli Tang, Mingxiu Jia, and Zhenlin Liang. "Effects of Aspect Ratio on the Hydrodynamic Performance of Circular Cambered Otter Board." In ASME 2018 37th International Conference on Ocean, Offshore and Arctic Engineering. American Society of Mechanical Engineers, 2018. http://dx.doi.org/10.1115/omae2018-78450.

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An otter board is an important device that provides a desired horizontal opening of a trawl net. A high lift coefficient or lift-to-drag ratio is required for an otter board to maintain fishing efficiency. In the present work, the hydrodynamic performance of a circular cambered otter board was studied by numerical simulation, including the effects of aspect ratios (AR), and flow distribution around the otter board. Model tests were conducted in the flume tank as well as a comparison to the numerical results. It showed that simulation results exhibited very good agreement with experiment results. Results demonstrated that the model otter board had a critical angle of attack (AOA) of 50° (when the stall appeared). The maximum lift coefficient and lift-to-drag ratio of the model otter board were 2.421 and 3.719, respectively. However, the maximum values of the full-scale otter board increased first and then decreased with an increasing AR. And the full-scale otter board had a better performance when AR = 2.489, it can enhance the lift coefficient by 17.4% compared with the initial otter board (AR = 1.25). In addition, the flow distribution around the otter board showed that the flow was smooth at small AOAs, when it attacked at large AOA (exceeded 55°), flow separation and eddies were appeared at the lee-side of the otter board.
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Imao, Shigeki. "Bend Loss Coefficient of Drag-Reducing Surfactant Solution." In ASME/JSME 2003 4th Joint Fluids Summer Engineering Conference. ASMEDC, 2003. http://dx.doi.org/10.1115/fedsm2003-45767.

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In this study, an effect of an additive on a bend loss was examined. Measurements of pressure distributions along pipes connected to pipe bends were performed using a drag-reducing surfactant solution. The additive used is being commercialized as a drag reducer and it has a non-degrading or rapidly repairable nature. Dimensions of the apparatus are pipe diameters d = 5, 10, 15 mm, radius ratios R/r = 20, 40, 60, 100, and a bend angle θ = 180 degree. It has been confirmed that total bend loss coefficients for water can be expressed by the equation deduced by Ito. When the surfactant solution is used, remarkable drag reduction was recognized in the inlet and the exit straight pipes. Pressure recovery length for the surfactant solution after the passage of the bend is longer than that for water. The curve of total bend loss coefficients for the surfactant solution intersects that for water. The former is larger than the latter at low Reynolds number and is smaller at high Reynolds number. The coefficients don’t depend on the pipe diameter but they depend on the radius ratio. It is shown that total bend loss coefficients for the surfactant solution can be expressed by a single curve and the empirical formula is deduced.
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Wen, Yuemin, and Milind A. Jog. "Effect of Temperature Dependent Properties and Particle Shape on Heat Transfer in Plasma Flow." In ASME 2003 International Mechanical Engineering Congress and Exposition. ASMEDC, 2003. http://dx.doi.org/10.1115/imece2003-42015.

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In this paper, plasma flow over non-spherical particles has been investigated numerically. The conservation equations for mass, momentum, and energy are solved simultaneously using finite volume method. To body-fit the non-spherical particle surface, an adaptive orthogonal grid is generated. The flow field and the temperature distribution are calculated for oblate and prolate particle shapes. A number of particle surface temperatures and far field temperatures are considered and thermophysical property variation is fully accounted for in our model. The shapes are represented in terms of variations in the axis ratio which is defined as the ratio of axis along the flow direction to the axis perpendicular to the flow direction. For oblate shape, axis ratios from 0.4 (disk-like) to 1 (sphere) are used whereas for proate shape, axis ratios of 1 (sphere) to 1.6 (cylinder-like) are used. The computational model is first validated by comparison with results and correlations available in literature for constant property flow. Effects of flow Reynolds number, particle shape, surface and far field temperatures, and variable properties, on the flow field, temperature variations, drag coefficient, and Nusselt number are outlined.
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Reports on the topic "Drug distribution ratios"

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Idakwo, Gabriel, Sundar Thangapandian, Joseph Luttrell, Zhaoxian Zhou, Chaoyang Zhang, and Ping Gong. Deep learning-based structure-activity relationship modeling for multi-category toxicity classification : a case study of 10K Tox21 chemicals with high-throughput cell-based androgen receptor bioassay data. Engineer Research and Development Center (U.S.), July 2021. http://dx.doi.org/10.21079/11681/41302.

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Deep learning (DL) has attracted the attention of computational toxicologists as it offers a potentially greater power for in silico predictive toxicology than existing shallow learning algorithms. However, contradicting reports have been documented. To further explore the advantages of DL over shallow learning, we conducted this case study using two cell-based androgen receptor (AR) activity datasets with 10K chemicals generated from the Tox21 program. A nested double-loop cross-validation approach was adopted along with a stratified sampling strategy for partitioning chemicals of multiple AR activity classes (i.e., agonist, antagonist, inactive, and inconclusive) at the same distribution rates amongst the training, validation and test subsets. Deep neural networks (DNN) and random forest (RF), representing deep and shallow learning algorithms, respectively, were chosen to carry out structure-activity relationship-based chemical toxicity prediction. Results suggest that DNN significantly outperformed RF (p < 0.001, ANOVA) by 22–27% for four metrics (precision, recall, F-measure, and AUPRC) and by 11% for another (AUROC). Further in-depth analyses of chemical scaffolding shed insights on structural alerts for AR agonists/antagonists and inactive/inconclusive compounds, which may aid in future drug discovery and improvement of toxicity prediction modeling.
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