Biopharmaceutics Classification System
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The Biopharmaceutics Classification System (BCS) is a system to differentiate drugs on the basis of their solubility and permeability.[1]
This system restricts the prediction using the parameters solubility and intestinal permeability. The solubility classification is based on a United States Pharmacopoeia (USP) aperture. The intestinal permeability classification is based on a comparison to the intravenous injection. All those factors are highly important because 85% of the most sold drugs in the United States and Europe are orally administered.[citation needed]
Classes
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According to the Biopharmaceutics Classification System (BCS) drug substances are classified to four classes upon their solubility and permeability:[1]
- Class I – high permeability, high solubility
- Example: metoprolol, paracetamol[2]
- Those compounds are well absorbed and their absorption rate is usually higher than excretion.
- Class II – high permeability, low solubility
- Example: glibenclamide, bicalutamide, ezetimibe, aceclofenac
- The bioavailability of those products is limited by their solvation rate. A correlation between the in vivo bioavailability and the in vitro solvation can be found.
- Class III – low permeability, high solubility
- Example: cimetidine
- The absorption is limited by the permeation rate but the drug is solvated very fast. If the formulation does not change the permeability or gastro-intestinal duration time, then class I criteria can be applied.
- Class IV – low permeability, low solubility
- Example: bifonazole
- Those compounds have a poor bioavailability. Usually they are not well absorbed over the intestinal mucosa and a high variability is expected.
Definitions
[edit]The drugs are classified in BCS on the basis of solubility and permeability.
Solubility class boundaries are based on the highest dose strength of an immediate release product. A drug is considered highly soluble when the highest dose strength is soluble in 250 ml or less of aqueous media over the pH range of 1 to 6.8. The volume estimate of 250 ml is derived from typical bioequivalence study protocols that prescribe administration of a drug product to fasting human volunteers with a glass of water.
Permeability class boundaries are based indirectly on the extent of absorption of a drug substance in humans and directly on the measurement of rates of mass transfer across human intestinal membrane. Alternatively non-human systems capable of predicting drug absorption in humans can be used (such as in-vitro culture methods). A drug substance is considered highly permeable when the extent of absorption in humans is determined to be 85% or more of the administered dose based on a mass-balance determination or in comparison to an intravenous dose.
See also
[edit]References
[edit]- ^ a b Mehta M (2016). Biopharmaceutics Classification System (BCS): Development, Implementation, and Growth. Wiley. ISBN 978-1-118-47661-1.
- ^ "Draft agreement" (PDF). www.ema.europa.eu. 22 June 2017. Retrieved 2019-07-03.
Further reading
[edit]- Folkers G, van de Waterbeemd H, Lennernäs H, Artursson P, Mannhold R, Kubinyi H (2003). Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability (Methods and Principles in Medicinal Chemistry). Weinheim: Wiley-VCH. ISBN 3-527-30438-X.
- Amidon GL, Lennernäs H, Shah VP, Crison JR (March 1995). "A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability". Pharm. Res. 12 (3): 413–20. PMID 7617530.