scholarly journals Effect of Common Excipients on the Oral Drug Absorption of Biopharmaceutics Classification System Class 3 Drugs Cimetidine and Acyclovir

2016 ◽  
Vol 105 (2) ◽  
pp. 996-1005 ◽  
Author(s):  
Soundarya Vaithianathan ◽  
Sam H. Haidar ◽  
Xinyuan Zhang ◽  
Wenlei Jiang ◽  
Christopher Avon ◽  
...  
Keyword(s):  
Drug Absorption ◽  
Classification System ◽  
Biopharmaceutics Classification System ◽  
Oral Drug ◽  
Oral Drug Absorption ◽  
Biopharmaceutics Classification System Class ◽  
Biopharmaceutics Classification

scholarly journals Caco-2 Cells, Biopharmaceutics Classification System (BCS) and Biowaiter

2011 ◽  
Vol 54 (1) ◽  
pp. 3-8 ◽  
Author(s):  
Libuše Smetanová ◽  
Věra Štětinová ◽  
Zbyněk Svoboda ◽  
Jaroslav Květina
Keyword(s):  
Drug Absorption ◽  
Classification System ◽  
Drug Transport ◽  
Biopharmaceutics Classification System ◽  
Phenol Red ◽  
Basolateral Side ◽  
Free Transport ◽  
Biopharmaceutics Classification

Almost all orally administered drugs are absorbed across the intestinal mucosa. The Caco-2 monolayers are used as an in vitro model to predict drug absorption in humans and to explore mechanism of drug absorption. The Caco-2 cells are derived from a human colon adenocarcinoma and spontaneously differentiate to form confluent monolayer of polarized cells structurally and functionally resembling the small intestinal epithelium. For studying drug permeability, Caco-2 cells are seeded onto the Transwell inserts with semipermeable membrane and grown to late confluence (21 days). After determination of cell viability, the integrity of monolayer is checked by phenol red permeability and by 14C-mannitol permeability. The transport from apical to basolateral (AP-BL) and basolateral to apical (BL-AP) is studied by adding the diluted drug on the apical or basolateral side and withdrawing the samples from the opposite compartment, respectively, for HPLC analysis or liquid scintillation spectrometry. Ca2+- free transport medium is used to determine paracellular component of the drug transport. On the basis of permeability and solubility, drugs can be categorized into four classes of Biopharmaceutics Classification System (BCS). For certain drugs, the BCS-based biowaiver approach can be used which enables to reduce in vivo bioequivalence studies.

scholarly journals Classification of WHO Essential Oral Medicines for Children Applying a Provisional Pediatric Biopharmaceutics Classification System

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 567 ◽  
Author(s):  
Jose-Manuel delMoral-Sanchez ◽  
Isabel Gonzalez-Alvarez ◽  
Marta Gonzalez-Alvarez ◽  
Andres Navarro ◽  
Marival Bermejo
Keyword(s):  
World Health Organization ◽  
Classification System ◽  
Biopharmaceutics Classification System ◽  
Essential Medicines ◽  
World Health ◽  
Oral Drug ◽  
Essential Medicines List ◽  
The World ◽  
Health Organization ◽  
Biopharmaceutics Classification

The objective was using the Essential Medicines List for children by the World Health Organization (WHO) to create a pediatric biopharmaceutics classification system (pBCS) of the oral drugs included in the Essential Medicines List by the World Health Organization and to compare our results with the BCS for adults (aBCS). Several methods to estimate the oral drug dose in different pediatric groups were used to calculate dose number (Do) and solubility (high/low). The estimation of the gastrointestinal water volume was adapted to each pediatric group. Provisional permeability classification was done by comparison of each drug lipophilicity versus metoprolol as the model drug of high permeability. As a result, 24.5% of the included drugs moved from the favorable to unfavorable class (i.e., from high to low solubility). Observed changes point out potential differences in product performance in pediatrics compared to adults, due to changes in the limiting factors for absorption. BCS Class Changes 1 to 2 or 3 to 4 are indicative of drugs that could be more sensitive to the choice of appropriate excipient in the development process. Validating a pBCS for each age group would provide a valuable tool to apply in specific pediatric formulation design by reducing time and costs and avoiding unnecessary pediatric experiments restricted due to ethical reasons. Additionally, pBCS could minimize the associated risks to the use of adult medicines or pharmaceutical compound formulations.

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