Comparative Bioavailability of Two Formulations of Biopharmaceutical Classification System (BCS) Class IV Drugs: A Case Study of Lopinavir/Ritonavir

Author(s):  
Ahmed M. Saeed ◽  
Jeffery M. Schmidt ◽  
Wijith P. Munasinghe ◽  
Bhadrish K. Vallabh ◽  
Michael F. Jarvis ◽  
...  
2019 ◽  
Vol 9 (3) ◽  
pp. 300-310
Author(s):  
Manish Kumar ◽  
Nithya Shanthi ◽  
Arun Kumar Mahato

Introduction: Nanocrystals constitutes of 100% drug and considered as a “new drug” by Food and Drug Administration. It is proven to be an effective alternative for topical delivery of drug with increased bioavailability. Recently formulation of the drug as nanocrystals has been accomplished for many drugs exhibiting low aqueous solubility, ineffective permeability or both in order to increase the dermal bioavailability. Conclusion: In this review article, an effort was made to explain the role of nanocrystals in the dermal delivery of the drug which results in increased bioavailability and efficacy through enhancement of solubility, dissolution velocity, permeation and penetration. Recently dermal delivery of the drug as nanocrystals is a challenging method but explained by many researchers through their work. Preparation of drugs as nanocrystals might be a promising method of drug delivery to Class II and Class IV drugs of Biopharmaceutical Classification System. Drug nanocrystals can also be applied in cosmetics for effective results.


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (4) ◽  
pp. 63-73
Author(s):  
Mahesh S. Soni ◽  
◽  
Atmaram P. Pawar ◽  
Chellampillai Bothiraja ◽  
Vinod L. Gaikwad ◽  
...  

The purpose of the present study is to highlight the discriminations if any, between the quality of low and high-cost medicines, which would help to select the right brand of medicine. In the present work, brands of medicines having high, medium, and low prices containing either of biopharmaceutical classification system class-II or class-IV drugs were comparatively evaluated for different pharmacopoeial standards as well as for biopharmaceutical classification system solubility and permeability. An ex vivo permeability test was carried out using a simple and non-invasive everted gut sac technique. Insignificant variation in pharmaceutical quality and permeability of the tested three types of brands was observed; however, the study could not consider the state of quality assurance facilities and parameters used while manufacturing these medicines. The study will help to make aware and assure medical and pharmacy practitioners and consumers for the selection of quality quality generic medicines.


2021 ◽  
Vol 22 (11) ◽  
pp. 5514
Author(s):  
Francesca Truzzi ◽  
Camilla Tibaldi ◽  
Yanxin Zhang ◽  
Giovanni Dinelli ◽  
Eros D′Amen

Polyphenols are natural organic compounds produced by plants, acting as antioxidants by reacting with ROS. These compounds are widely consumed in daily diet and many studies report several benefits to human health thanks to their bioavailability in humans. However, the digestion process of phenolic compounds is still not completely clear. Moreover, bioavailability is dependent on the metabolic phase of these compounds. The LogP value can be managed as a simplified measure of the lipophilicity of a substance ingested within the human body, which affects resultant absorption. The biopharmaceutical classification system (BCS), a method used to classify drugs intended for gastrointestinal absorption, correlates the solubility and permeability of the drug with both the rate and extent of oral absorption. BCS may be helpful to measure the bioactive constituents of foods, such as polyphenols, in order to understand their nutraceutical potential. There are many literature studies that focus on permeability, absorption, and bioavailability of polyphenols and their resultant metabolic byproducts, but there is still confusion about their respective LogP values and BCS classification. This review will provide an overview of the information regarding 10 dietarypolyphenols (ferulic acid, chlorogenic acid, rutin, quercetin, apigenin, cirsimaritin, daidzein, resveratrol, ellagic acid, and curcumin) and their association with the BCS classification.


2020 ◽  
pp. 147592172097970
Author(s):  
Liangliang Cheng ◽  
Vahid Yaghoubi ◽  
Wim Van Paepegem ◽  
Mathias Kersemans

The Mahalanobis–Taguchi system is considered as a promising and powerful tool for handling binary classification cases. Though, the Mahalanobis–Taguchi system has several restrictions in screening useful features and determining the decision boundary in an optimal manner. In this article, an integrated Mahalanobis classification system is proposed which builds on the concept of Mahalanobis distance and its space. The integrated Mahalanobis classification system integrates the decision boundary searching process, based on particle swarm optimizer, directly into the feature selection phase for constructing the Mahalanobis distance space. This integration (a) avoids the need for user-dependent input parameters and (b) improves the classification performance. For the feature selection phase, both the use of binary particle swarm optimizer and binary gravitational search algorithm is investigated. To deal with possible overfitting problems in case of sparse data sets, k-fold cross-validation is considered. The integrated Mahalanobis classification system procedure is benchmarked with the classical Mahalanobis–Taguchi system as well as the recently proposed two-stage Mahalanobis classification system in terms of classification performance. Results are presented on both an experimental case study of complex-shaped metallic turbine blades with various damage types and a synthetic case study of cylindrical dogbone samples with creep and microstructural damage. The results indicate that the proposed integrated Mahalanobis classification system shows good and robust classification performance.


Author(s):  
Ana Jeleapov ◽  

The paper contains the results of classification of rivers and streams of the Republic of Moldova according to classic Strahler method. Mentioned method was applied to estimate the hierarchical rank of the stream segments situated in 50 pilot basins using modern GIS techniques and drainage network of the GIS for Water Resources of Moldova. It was estimated that the maximal order of segments is 7 specific for the Raut and Ialpug rivers. Overall, length of 1st order streams forms 50%, while that of 7th order streams - < 1%. Additionally, stream number and frequency as well as drainage density were calculated for pilot river basins.


ADMET & DMPK ◽  
2016 ◽  
Vol 4 (4) ◽  
pp. 335 ◽  
Author(s):  
Asami Ono ◽  
Takumi Tomono ◽  
Takuo Ogihara ◽  
Katsuhide Terada ◽  
Kiyohiko Sugano

<span style="color: black; font-family: 'Calibri','sans-serif'; font-size: 10pt; mso-fareast-font-family: 'Times New Roman'; mso-bidi-font-family: 'Times New Roman'; mso-ansi-language: EN-GB; mso-fareast-language: DE; mso-bidi-language: AR-SA;" lang="EN-GB">The purpose of this study was to evaluate the biopharmaceutical drug properties suitable for orally disintegrating tablets (ODTs). The net charge at pH 7.4, log D<sub>6.5</sub>, the highest dose strength, solubility in water, dose number, and elimination t<sub>1/2</sub> of 57 ODT drugs and 113 drugs of immediate-release (IR) formulations were compared. These drugs were classified according to the Biopharmaceutical Classification System (BCS). A lower dose strength and a longer elimination t<sub>1/2</sub> have been observed as characteristic properties of ODTs. The proportion of basic drugs was higher in the ODTs than in the IR. A significant difference was not observed between the ODT and the IR formulation for log D<sub>6.5</sub>, solubility in water, and dose number. The distributions of the ODT and IR formulations among each BCS class were similar, suggesting that an ODT can be developed regardless of the BCS class of a drug</span>.


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