Journal of Bioequivalence & Bioavailability最新文献_第3页

Editorial Note for Journal of Bioequivalence & Bioavailability 《生物等效性与生物利用度杂志》编辑说明

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.397

F. Sorgel

引用次数: 0

Editorial Highlights for Journal of Bioequivalence & Bioavailability 《生物等效性与生物利用度杂志》编辑要点

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.394

H. Sahoo

引用次数: 0

Tulsi: The Queen of Medicinal Herbs 图丝:草药女王

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.407

Riddhi Patel

{"title":"Tulsi: The Queen of Medicinal Herbs","authors":"Riddhi Patel","doi":"10.35248/0975-0851.20.12.407","DOIUrl":"https://doi.org/10.35248/0975-0851.20.12.407","url":null,"abstract":"Tulsi has got the great medicinal value. Studies have also shown Tulsi to be effective for diabetes, by reducing blood glucose levels. The same study showed significant reduction in total cholesterol levels with Tulsi. Another study showed that Tulsi's beneficial effect on blood glucose levels is due to its antioxidant properties. The Rama Tulsi is the effective remedy for the severe acute Respiratory Syndrome. Juice of its leaves gives relief in cold, fever, bronchitis and cough. Tulsi oil is also used as the ear drop. Tulsi helps in curing malaria. It is very effective against indigestion, headache, hysteria, insomnia and cholera. The fresh leaves of Tulsi are taken by the millions of people every day. For over the centuries Tulsi (the queen of herbs) has been known for its remarkable healing properties. Modern scientific research offers impressive evidence that Tulsi reduces stress, enhances stamina, relieves inflammation, lowers cholesterol, eliminates toxins, protects against radiation, prevents gastric ulcers, lowers fevers, improves digestion and provides a rich supply of antioxidants and other nutrients. Tulsi is especially effective in supporting the heart, blood vessels, liver and lungs and also regulates blood pressure and blood sugar. Recent studies suggest that Tulsi may be a COX-2 inhibitor, like many modern painkillers, due to its high concentration of eugenol (1-hydroxy-2- methoxy-4- allylbenzene). The anti-flu property of Tulsi has been discovered by medical experts across the world quite recently. Tulsi improves the body's overall defence mechanism including its ability to fight viral diseases.","PeriodicalId":15184,"journal":{"name":"Journal of Bioequivalence & Bioavailability","volume":"428 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77796046","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: 5

Model-Based Elaboration of a Limited Sampling Strategy in the Bioequivalence Assessment of Highly Variable Dabigatran 高变量达比加群生物等效性评价中有限采样策略的基于模型的阐述

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.396

Cass, re Legault, Jun Yu Li

{"title":"Model-Based Elaboration of a Limited Sampling Strategy in the Bioequivalence Assessment of Highly Variable Dabigatran","authors":"Cass, re Legault, Jun Yu Li","doi":"10.35248/0975-0851.20.12.396","DOIUrl":"https://doi.org/10.35248/0975-0851.20.12.396","url":null,"abstract":"Background: The bioequivalence (BE) assessment of generic (Test) and brand name (Reference) formulations of drugs with steep exposure-response relationships exhibiting high pharmacokinetic (PK) variability such as dabigatran represent an expensive challenge for pharmaceutical companies. Supported by the population pharmacokinetics (pop-PK) approach, the present article investigates modelling potential to assess BE using a reduced number of blood samples. Methods: Pop-PK models for the Reference and Test formulations were developed retrospectively using standard modeling techniques for a BE study of dabigatran. Reduced sampling scenarios were selected and the developed pop- PK models were refitted on each dataset for the respective formulations. These models were simulated to generate virtual PK profiles to be tested with the standard BE criteria, in order to identify the scenarios maintaining the original BE conclusions with the least samples required. Results: The BE study original data was best described as a pop-PK model presenting two compartments with first order elimination and absorption, as well as an absorption lag time. Sex was identified as a significant covariate with impact on bioavailability. Using a rational sampling selection procedure under the framework of modeling and simulation, the results proved that the BE verdict could be maintained with only five of the 20 original blood samples using the current regulatory BE standards and criteria. Conclusion: We conclude that the pop-PK model-based BE assessment can be an efficient tool for aiding the BE assessment of dabigatran by significantly reducing the number of samples required, and consequently lower trial costs and increase benefits for enrolled participants.","PeriodicalId":15184,"journal":{"name":"Journal of Bioequivalence & Bioavailability","volume":"256 1","pages":"1-7"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91324581","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

Non-linear Mixed Effects Modeling and Simulation for Exploring VariabilitySources in Dissolution Curves: A BCS Class II Case Example 探索溶解曲线变异性来源的非线性混合效应建模与模拟:一个BCS II类案例示例

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.406

E. Karatza, V. Karalis

{"title":"Non-linear Mixed Effects Modeling and Simulation for Exploring VariabilitySources in Dissolution Curves: A BCS Class II Case Example","authors":"E. Karatza, V. Karalis","doi":"10.35248/0975-0851.20.12.406","DOIUrl":"https://doi.org/10.35248/0975-0851.20.12.406","url":null,"abstract":"Purpose: Irbesartan is a BCS class II compound that exhibits pH– and buffer capacity–dependent dissolution behavior. The aim of this study was to apply non-linear mixed effects modelling on dissolution data of two immediate release products containing Irbesartan in order to characterize and quantify the sources of inter-dissolution profile variability. Methods: Nonlinear mixed effects modelling was applied to describe the dissolution curves obtained for Irbesartan in three different pH-value media (1.2, 4.5, 6.8) with two different products (reference product: Aprovel® and a generic test product). Simulations performed and the impact of inter-dissolution variability was assessed. Results: The % Irbesartan dissolved to time was found to follow a Weibull distribution. Τhe population scale parameter was estimated 0.252 and the shape parameter was estimated 0.706. The pH-value of the dissolution medium was found to significantly affect the scale parameter, while the formulation was found to affect the shape parameter. Simulations showed that probably some discrepancies in the in vivo performance of the two products can be expected. Conclusion: Through this case study the applicability and usefulness of nonlinear mixed effects modelling in oral drug formulation was highlighted and resides in its ability to identify and quantify sources of variability.","PeriodicalId":15184,"journal":{"name":"Journal of Bioequivalence & Bioavailability","volume":"60 1","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81353150","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: 0

COVID-19 Clinical Trials in China COVID-19在中国的临床试验

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.409

F. Sorgel

引用次数: 0

Medicines that are Biologicals, or maybe not: The Strange Case of Teriparatide Forsteo® and its Copy Drugs 生物制剂，或可能不是:特立帕肽Forsteo®及其仿制药的奇怪案例

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.395

D. Pilunni, P. Navarra

引用次数: 1

The Effect of Chemical Modifications of Chitosan on Intestinal Permeability and Oral Bioavailability of Carbamoylphosphonate JS403 壳聚糖化学修饰对氨基膦酸盐JS403肠通透性和口服生物利用度的影响

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.392

Reut Bitton-Dotan, J. Bohrisch, C. Schmidt, Marina Tsuriel, R. P. Tulichala, E. Breuer, R. Reich, A. Hoffman, J. Storsberg

{"title":"The Effect of Chemical Modifications of Chitosan on Intestinal Permeability and Oral Bioavailability of Carbamoylphosphonate JS403","authors":"Reut Bitton-Dotan, J. Bohrisch, C. Schmidt, Marina Tsuriel, R. P. Tulichala, E. Breuer, R. Reich, A. Hoffman, J. Storsberg","doi":"10.35248/0975-0851.20.12.392","DOIUrl":"https://doi.org/10.35248/0975-0851.20.12.392","url":null,"abstract":"JS403, Carbamoylphosphonate molecule, is a promising drug candidate with anti-metastatic activity. The polarity and water solubility of JS403 evolve from the phosphonate moiety that is ionized at physiologic pH. JS403 is regarded as a BCS class III molecule, and exhibit poor absolute oral bioavailability of less than 1%. The aim of this investigation is to identify proper chitosan based absorption enhancer compound(s) that upon oral co-administration with JS403 which would enhance its bioavailability. To determine the optimal properties of the chitosan derivative (CD), 11 relevant compounds were synthesized, each with different attribute, and their impact on the intestinal permeability of JS403 was examined in-vitro using the CaCO2 monolayer model. Then, the oral bioavailability of JS403 coadministered with the selected CD was examined in the freely moving rat model. The in-vitro study identified two leading trimethyl CD, KC13, (85% deacetylation, MW 20,000 g/mol and 66% trimethylation) and a novel derivative of hydroxypropyl chitosan KHC2 (trimethylation 71%) increased JS403 permeability in 2 and 10 folds, respectively. Similar permeability results were obtained when the same chitosan derivatives were coadministered with atenolol, another BSCIII drug. The paracellular absorption mechanism of these BCS III compounds was ascertained using palmitoyl carnitine as positive control. The pharmacokinetic investigation, following gavage coadministration with either KC13 or KHC2, showed a significant increase in JS403 oral AUC of 200%. The in-vitro permeation data correlated with the oral bioavailability outcomes. The relatively modest enhancement (~2 folds) of the chitosan derivatives in-vivo is anticipated as their effect on the enterocytes integrity and tight junction (TJ) need to be moderate. This is required because their noninvasive and reversible impact that is demanded in case of multiple treatment.","PeriodicalId":15184,"journal":{"name":"Journal of Bioequivalence & Bioavailability","volume":"171 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85534931","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

Covid-19 Vaccine Development Covid-19疫苗研制

Journal of Bioequivalence & Bioavailability Pub Date : 2020-01-01 DOI: 10.35248/0975-0851.20.12.408

F. Sorgel

引用次数: 61

Crude Edible Fig (Ficus carica) Leaf Extract Prevents Diethylstilbestrol (DES)-Induced DNA Strand Breaks in Single-Cell Gel Electrophoresis (SCGE)/Comet Assay: Literature Review and Pilot Study 食用无花果(Ficus carica)粗叶提取物在单细胞凝胶电泳(SCGE)/彗星分析中防止己烯雌酚(DES)诱导的DNA链断裂:文献综述和中试研究

Journal of Bioequivalence & Bioavailability Pub Date : 2019-04-01 DOI: 10.35248/0975-0851.19.11.389

Alrena V. Lightbourn, Ronald D. Thomas

{"title":"Crude Edible Fig (Ficus carica) Leaf Extract Prevents Diethylstilbestrol (DES)-Induced DNA Strand Breaks in Single-Cell Gel Electrophoresis (SCGE)/Comet Assay: Literature Review and Pilot Study","authors":"Alrena V. Lightbourn, Ronald D. Thomas","doi":"10.35248/0975-0851.19.11.389","DOIUrl":"https://doi.org/10.35248/0975-0851.19.11.389","url":null,"abstract":"Fig (Ficus carica) trees are among the oldest plants on earth. The chemopreventive properties of constituent polyphenols and fiber that implicate figs in having a functional role in averting cancer have not been fully elucidated. We therefore hypothesized that fig leaf extract would inhibit (or attenuate) DES-induced DNA single-strand breakage in MCF10A human breast epithelial cells. To test this hypothesis, MCF10A cells were treated with DES (1, 10, 100 μM), crude fig leaf extract (5, 10, 15 μL), or concomitant doses of DES (100 μM)/fig leaf extract (5, 10, 15 μL). The cells were analyzed for DNA strand breakage using the SCGE/COMET assay with mean olive tail moment as a marker of DNA damage. DES induced DNA strand breaks at all treatment levels compared to DMSO and non-treatment controls. DES at concentrations of 1, 10, and 100 μM produced mean olive tail moments of 1.2082 (177.6%), 1.2702 (186.7%), and 1.1275 (165.7%), respectively, which were statistically significantly (p<0.05) higher than the DMSO control value (0.6803). Exposure to fig leaf extract produced no DNA damage. Rather, a desirable dose-dependent reduction in DES-induced DNA strand breaks was observed. Composite treatment of MCF10A cells with DES and fig leaf extract attenuated DES-induced DNA strand breaks. Taken together, these results suggest a potential mechanism for cancer chemoprevention. Additional studies are necessary to identify relevant active ingredients, confirm the mechanism of action, and further elucidate the therapeutic potential of fig leaf extract for early-stage breast cancer chemoprevention.","PeriodicalId":15184,"journal":{"name":"Journal of Bioequivalence & Bioavailability","volume":"42 1","pages":"19 - 28"},"PeriodicalIF":0.0,"publicationDate":"2019-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73379703","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: 6