Physicochemical Properties, Form, and Formulation Selection Strategy for a Biopharmaceutical Classification System Class II Preclinical Drug Candidate

2014 ◽  
Vol 103 (10) ◽  
pp. 3007-3021 ◽  
Author(s):  
Sachin Lohani ◽  
Harriet Cooper ◽  
Xiaoling Jin ◽  
Becky P. Nissley ◽  
Kimberly Manser ◽  
...  
INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 47-51
Author(s):  
G Sailesh ◽  
◽  
T. E. G. K. Murthy

Telmisartan is used in the treatment of hypertension. It exhibits poor water solubility. It belongs to class II of Biopharmaceutical Classification system (BCS). It needs enhancement in dissolution and hence bioavailability. The dissolution of drug was improved by coating the drug and carrier over sugar spheres.Size of sugar spheres and concentration of the carrier were two critical variables that were found to affect the dissolution of drug. A 22 factorial design was used to study the effect of concentration of carrier and size of the non-pareil seeds on dissolution. Dissolution of telmisartan was found to increase with increasing concentration of carrier and decreased with respect to size of non-pareil seeds.


CrystEngComm ◽  
2021 ◽  
Author(s):  
Indira S Divya ◽  
Amrutha Surendran ◽  
Sunil SeethaLekshmi ◽  
Sunil Varughese

The anti-malarial drug quinine (QUN) has poor aqueous solubility and belongs to Biopharmaceutical Classification System (BCS) Class-II. We report 12 novel molecular salts of QUN with α,ω-aliphatic dicarboxylic acids, and...


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.


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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