Bcs Class 4 Drugs

Drugs

BCS class 4 drugs for enhancement of oral bioavailability. BCS class 4 drugs are the drugs having low solubility and permeability according to classification.

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Abstract Aqueous solubility is one of the most influencing factors when it comes to bioavailability of the. It is the main key for drug effectiveness and enhancing water solubility, which poses one of the greatest challenges in the pharmaceutical industry. Nearly half of newly developed drugs turn out to be insoluble or poorly soluble during initial screening process.

What Are Class 4 Drugs

Poor solubility limits drug delivery and formulation development. Various techniques have been developed to enhance solubility of poorly soluble drugs. Pharmaceuticals falling under the Classification System (BCS) class II and IV are the main emphasis of this review as these drugs are of low solubility. The methods to improve drug solubility; solid dispersions, complexation, dendrimers, nano-suspensions, co-solvency, pH adjustment, self-emulsifying drug delivery system, hydrotrophy, cocrystallization and ionic liquid formation are discussed. Keywords Solubility; Biopharmaceutics Classification System (BCS); Solid dispersions; Complexation; Self-Emulsifying Drug Delivery System (SEDDS); Co crystallization; Ionic liquid formation Introduction Scientists have been trying for decades to find the perfect way to increase the bioavailability of drugs by improving the solubility. A large number (~40%) [] of New Chemical Entities (NCE) synthesized both in academia and industry suffer major setback due to poor water solubility [].

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This is due to the fact that the active pharmaceutical ingredient (API) needs to be in the solution in aqueous intestinal fluid that allows its partitioning across epithelial cell membrane (passive diffusion) []. Drug absorption relies heavily on two factors; solubility and permeability. As the number of poorly soluble drugs has increased, efforts to enhance solubility have evolved. The Biopharmaceutics Classification System [] is used to categorize drugs based on solubility and permeability for formulation development. BCS consists of four classes based on solubility and permeability. Both BCS II and IV compounds are of low solubility ( Table 1), and class IV compounds suffer from additional poor permeability issue.

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