ADMET and DMPK最新文献_第10页

Realistic and critical review of the state of systemic antimicrobial peptides 对全身性抗菌肽现状的现实和批判性回顾

IF 2.5

ADMET and DMPK Pub Date : 2022-01-20 DOI: 10.5599/admet.1215

Guangshun Wang, A. Mechesso

引用次数: 2

Therapeutic potential of interferon-gamma in tuberculosis 干扰素- γ在肺结核中的治疗潜力

IF 2.5

ADMET and DMPK Pub Date : 2022-01-14 DOI: 10.5599/admet.1078

S. Berns, J. Isakova, Polina Pekhtereva

引用次数: 2

Synthesis and diverse biological activity profile of triethylammonium isatin-3-hydrazones isatin-3-腙三乙基胺的合成及多种生物活性分析

IF 2.5

ADMET and DMPK Pub Date : 2022-01-12 DOI: 10.5599/admet.1179

A. Bogdanov, O. Tsivileva, A. Voloshina, A. Lyubina, S. Amerhanova, Ekaterina Burtceva, S. Bukharov, Alexander V. Samorodov, V. Pavlov

引用次数: 4

Bioanalysis of aminoglycosides using high-performance liquid chromatography 高效液相色谱法生物分析氨基糖苷

IF 2.5

ADMET and DMPK Pub Date : 2022-01-11 DOI: 10.5599/admet.1183

S. Amponsah, Joseph A. Boadu, Daniel K. Dwamena, K. F. Opuni

{"title":"Bioanalysis of aminoglycosides using high-performance liquid chromatography","authors":"S. Amponsah, Joseph A. Boadu, Daniel K. Dwamena, K. F. Opuni","doi":"10.5599/admet.1183","DOIUrl":"https://doi.org/10.5599/admet.1183","url":null,"abstract":"Aminoglycosides are broad-spectrum antibiotics used in the treatment of gram-negative bacterial infections. Due to their nephrotoxic and ototoxic potential (narrow therapeutic index), the use of aminoglycoside for clinical indications requires monitoring. The objective of this review was to identify relevant literature reporting liquid chromatographic methods for the bioanalysis of aminoglycosides in both preclinical and clinical settings/experiments. Data on liquid chromatographic methods were collected from articles in an online academic database (PubMed, Science Direct, Scopus, and Google Scholar). All 71 articles published from 1977 to 2020 were included in the review. Reversed-phase liquid chromatography was the most used method for the bioanalysis of aminoglycosides. Fluorescence or ultraviolet detection methods were mostly used from 1977 to 2002 (51 articles), while mass spectrometry was predominantly used as a detector from 2003 to 2020 (15 articles). Sixty-seven articles reported calibration ranges, which varied significantly for the various drugs assayed: some in the range of 0.1-0.5 ng/mL and others 1250-200000 ng/mL. Also, 61 articles reported R2 values (0.964-1.0) for almost all analytes under consideration. Sixty-three articles reported percent recoveries mostly between 61.0 % to 114.0 %, with only two articles reporting recoveries of 4.9 % and 36 %. Out of the 71 reviewed articles, 56 reported intermediate precision values ranging between 0.331 % to 19.76 %, which is within the acceptable limit of 20 %. This review will serve as a guide for research and/or routine clinical monitoring of aminoglycosides in biological matrices.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"56 1","pages":"27 - 62"},"PeriodicalIF":2.5,"publicationDate":"2022-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87641306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Impact of host factors on susceptibility to antifungal agents 宿主因素对抗真菌药物敏感性的影响

IF 2.5

ADMET and DMPK Pub Date : 2022-01-07 DOI: 10.5599/admet.1164

B. Plotkin, M. Konaklieva

{"title":"Impact of host factors on susceptibility to antifungal agents","authors":"B. Plotkin, M. Konaklieva","doi":"10.5599/admet.1164","DOIUrl":"https://doi.org/10.5599/admet.1164","url":null,"abstract":"An obstacle to drug development, particularly in this era of multiple drug resistance, is the under-appreciation for the role the host environment plays in microbial response to drugs. With the rise in fungal infection and drug resistance, particularly in individuals with co-morbidities, the influence serum and its components have on antimicrobial susceptibility requires assessment. This study examined the impact of physiologically relevant glucose and insulin levels in the presence and absence of 50 % human plasma on MICs for clinical isolates of Candida lusitaniae, Candida parapsilosis, Candida albicans, Candida tropicalis, Candida glabrata, Candida krusei and Cryptococcus neoformans. The addition of insulin or glucose at physiologic levels in RPMI medium alone altered the MIC in either a positive or negative fashion, depending on the organisms and drug tested, with C. glabrata most significantly altered with a 40, >32- and 46-fold increase in MIC for amphotericin B, itraconazole and miconazole, respectively. The addition of candida-antibody negative plasma also affected MIC, with the addition of glucose and insulin having a tandem effect on MIC. These findings indicate that phenotypic resistance of Candida and Cryptococcus can vary depending on the presence of insulin with glucose and plasma. This modulation of resistance may help explain treatment failures in the diabetic population and facilitate the development of stable drug-resistant strains. Furthermore, these findings indicate the need for a precision approach in the choice of drug treatment and drug development.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"106 1","pages":"153 - 162"},"PeriodicalIF":2.5,"publicationDate":"2022-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74345043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Effect of divalent and trivalent metal ions on artificial membrane permeation of fluoroquinolones. 二价和三价金属离子对氟喹诺酮类药物人工膜渗透的影响。

IF 2.5

ADMET and DMPK Pub Date : 2022-01-01 DOI: 10.5599/admet.1427

Nanami Nakatani, Kiyohiko Sugano

{"title":"Effect of divalent and trivalent metal ions on artificial membrane permeation of fluoroquinolones.","authors":"Nanami Nakatani, Kiyohiko Sugano","doi":"10.5599/admet.1427","DOIUrl":"https://doi.org/10.5599/admet.1427","url":null,"abstract":"The purpose of the present study was to evaluate the predictability of PAMPA for the effect of metal ions on the bioavailability of fluoroquinolones (FQ). Eleven FQs and seven metal ions were employed in this study. The PAMPA membrane consisted of a 10 % soybean lecithin (SL) - decane solution. A drug solution in MES buffer with or without a metal ion (added as a chloride salt) was added to the donor compartment. In the absence of metal ions, FQ showed relatively high permeability (> 5 × 10-6 cm/sec) in SL-PAMPA despite their hydrophilic and zwitterionic properties. As the PAMPA permeability ratio with/without metal ions became smaller, the urinary excretion and AUC ratios tended to be smaller, suggesting that SL-PAMPA is a suitable in vitro model to evaluate the potential effect of metal ions on the bioavailability of FQ. However, the reduction in AUC and urinary excretion was overestimated for low solubility metal ion formulations (dried aluminum hydroxide gel and La2(CO3)3・8H2O). In such cases, the dissolution of the metal ion formulations and the permeation of FQs should be simultaneously evaluated.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 4","pages":"289-297"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9793463/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10800157","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Thickness of the aqueous boundary layer in stirred microtitre plate permeability assays (PAMPA and Caco-2), based on the Levich equation. 基于Levich方程的搅拌微滴板渗透性测定(PAMPA和Caco-2)中水边界层厚度

IF 2.5

ADMET and DMPK Pub Date : 2022-01-01 DOI: 10.5599/admet.1568

Alex Avdeef

引用次数: 0

Impact of gastrointestinal differences in veterinary species on the oral drug solubility, in vivo dissolution, and formulation of veterinary therapeutics 兽药物种胃肠道差异对口服药物溶解度、体内溶出度和兽药制剂的影响

IF 2.5

ADMET and DMPK Pub Date : 2022-01-01 DOI: 10.5599/admet.1140

Marilyn N. Martinez, M. Papich, R. Fahmy

{"title":"Impact of gastrointestinal differences in veterinary species on the oral drug solubility, in vivo dissolution, and formulation of veterinary therapeutics","authors":"Marilyn N. Martinez, M. Papich, R. Fahmy","doi":"10.5599/admet.1140","DOIUrl":"https://doi.org/10.5599/admet.1140","url":null,"abstract":"Many gaps exist in our understanding of species differences in gastrointestinal (GI) fluid composition and the associated impact of food intake and dietary composition on in vivo drug solubilization. This information gap can lead to uncertainties with regard to how best to formulate pharmaceuticals for veterinary use or the in vitro test conditions that will be most predictive of species-specific in vivo oral product performance. To address these challenges, this overview explores species-specific factors that can influence oral drug solubility and the formulation approaches that can be employed to overcome solubility-associated bioavailability difficulties. These discussions are framed around some of the basic principles associated with drug solubilization, reported species differences in GI fluid composition, types of oral dosage forms typically given for the various animal species, and the effect of prandial state in dogs and cats. This basic information is integrated into a question-and-answer section that addresses some of the formulation issues that can arise in the development of veterinary medicinals.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"19 1","pages":"1 - 25"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85821208","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Food effect risk assessment in preformulation stage using material sparing μFLUX methodology. 采用省料μFLUX方法评价制剂预配制阶段的食品效应风险。

IF 2.5

ADMET and DMPK Pub Date : 2022-01-01 DOI: 10.5599/admet.1476

Corinne Jankovsky, Oksana Tsinman, Naveen K Thakral

{"title":"Food effect risk assessment in preformulation stage using material sparing μFLUX methodology.","authors":"Corinne Jankovsky, Oksana Tsinman, Naveen K Thakral","doi":"10.5599/admet.1476","DOIUrl":"https://doi.org/10.5599/admet.1476","url":null,"abstract":"The intake of food and meal type can strongly impact the bioavailability of orally administered drugs and can consequently impact drug efficacy and safety. During the early stages of drug development, only a small amount of drug substance is available, and the solubility difference between fasted state simulated intestinal fluid and fed state simulated intestinal fluid may provide an early indication about the probable food effect. But higher drug solubility in fed state simulated intestinal fluid may not always results in an increased oral absorption. In the present research, we demonstrated using 11 model compounds that in addition to the drug dissolution in biorelevant media, the evaluation of the diffusion flux of a drug in solution, across artificial lipid coated membrane, where only the unbound drug crosses the membrane, is a reliable way to predict the food effect. Although, the combination of dissolution and diffusion flux may not reliably predict the food effect in case of drugs undergoing intestinal metabolism or when transporters are involved in the drug absorption, the technique generally provides good information about the food effect at very early stages of drug development that may help in designing a clinical plan by adjusting the drug dose in the fed state.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 4","pages":"299-314"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9793460/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10800161","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Numerical modeling of the dissolution of drug nanocrystals and its application to industrial product development. 药物纳米晶体溶解的数值模拟及其在工业产品开发中的应用。

IF 2.5

ADMET and DMPK Pub Date : 2022-01-01 DOI: 10.5599/admet.1437

Bastian Bonhoeffer, Andreas Kordikowski, Edgar John, Michael Juhnke

{"title":"Numerical modeling of the dissolution of drug nanocrystals and its application to industrial product development.","authors":"Bastian Bonhoeffer, Andreas Kordikowski, Edgar John, Michael Juhnke","doi":"10.5599/admet.1437","DOIUrl":"https://doi.org/10.5599/admet.1437","url":null,"abstract":"The apparent solubility of drug nanocrystals in equilibrium was experimentally determined for a drug-stabilizer system with different particle size distributions. True supersaturation was identified for ultrafine drug nanocrystals with an almost 2-fold increase compared to the thermodynamic solubility of related coarse drug crystals, highlighting their enabling potential to enhance bioavailability. The experimental results were applied to investigate in silico the associated dissolution behavior in a closed system by numerical modeling according to the Ostwald-Freundlich and Noyes-Whitney / Nernst-Brunner equations. Calculated results were found to be in agreement with the experimental results only when the entire particle size distribution of drug nanocrystals was considered. In silico dissolution, studies were conducted to simulate the complex interplay between drug nanocrystals, dissolution conditions and resulting temporal progression during dissolution up to the equilibrium state. Calculations were performed for selected in vivo and in vitro scenarios considering different drug nanocrystal particle size distributions, drug amount, dissolution media and volume. The achieved results demonstrated the importance of ultrafine drug nanocrystals for potential bioavailability improvement and the functional applicability of the modeling approach to investigate their dissolution behavior for configurable formulation variables in product development in terms of in vivo and in vitro relevant conditions.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"10 4","pages":"253-287"},"PeriodicalIF":2.5,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9793462/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10800155","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0