Approaches of increasing oral bioavailability of class ii active pharmaceutical ingredients in accordance with the biopharmaceutical classification system
Journal Title: Вісник фармації - Year 2019, Vol 98, Issue 2
Abstract
Aim. To compare existing approaches used for enhancing oral bioavailability (BA) of class II active pharmaceutical ingredients (API) and categorize them in the order of most promising. Materials and methods. The material of the article was literary data about approaches used for enhancing oral bioavailability of class II active pharmaceutical ingredients with a high permeability and poor solubility. Methods of information search, methods of comparison and generalization, systematic methods were used to carry out the research tasks. Results and discussion. During last 20 years, the share of class II API in accordance with the biopharmaceutical classification system (i.e. with low solubility and high permeability) is continuously increasing at the world market and different stages of pharmaceutical product development. The approaches to improving oral BA of class II API which can be used to develop generic and modified generic drugs have been discussed in this article. These approaches were considered from the point of view of the principle of increasing the oral BA. It is concluded that promising approaches to increase oral BA should meet the following requirements: rapid achievement of oversaturated API concentration and its subsequent maintenance, keeping the whole API dose dissolved during transit through the intestines. Increased solubility and specific surface area are used as the main levers in all these approaches to improve oral bioavailability. At the same time, the ability to form supersaturated solutions and the retention of high concentrations during transit through the intestine differs depending on the approach. Conclusions. The most promising approaches to increase oral bioavailability, contributing to the formation of supersaturated solutions and maintaining high concentrations during transit are included: solid amorphous dispersions of API; digestible formulations that form micelles/emulsions in the intestine; and digestible inclusion complexes with cyclodextrins.
Authors and Affiliations
V. V. Mohylyuk, L. L. Davtian, D. O. Novykov, M. G. Katynska, Yu. V. Shmyrova, O. O. Dobrovolnyi
Keywords
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- EP ID EP657584
- DOI 10.24959/nphj.19.14
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