The Biopharmaceutics Classification System is a system to differentiate the drugs on the basis of their solubility and permeability.^[1]

We evaluated 263 approved generic drugs of IR products listed on the WHO EML to find out the distribution of BCS Class 1, 2, 3, and 4 drugs in approved ANDA applications during the 2000 to 2011 period. The WHO EML was used as it is a publicly available list of Class 1, 2, 3, and 4 drugs.
BIOPHARMACEUTICS CLASSIFICATION OF THE DRUG SUBSTANCE. BCS-based biowaivers are applicable to drug products where the drug substance(s) exhibit high solubility and, either high permeability (BCS Class I) or low permeability (BCS Class III). A biowaiver is applicable when the drug substance(s) in test and reference products are identical.

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]}.

BCS classes[edit]

BCS classes

According to the Biopharmaceutical 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.

WHO Drug Information Vol. 1, 2016 2 Pre-publication draft - page numbers are not for citation purposes 72 Misoprostol dispersion 76 Misoprostol tablets 79 Carbamazepine 84 Carbamazepine tablets 87 Carbamazepine chewable tablets 90 Carbamazepine oral suspension International Nonproprietary Names (INN) 93 Recommended INN: List 75 Continued.

Definitions[edit]

The drugs are classified in BCS on the basis of solubility, permeability, and dissolution.

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 7.5. 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 90% or more of the administered dose based on a mass-balance determination or in comparison to an intravenous dose.

For dissolution class boundaries, an immediate release product is considered rapidly dissolving when no less than 85% of the labeled amount of the drug substance dissolves within 15 minutes using USP Dissolution Apparatus 1 at 100 RPM or Apparatus 2 at 50 RPM in a volume of 900 ml or less in the following media: 0.1 M HCl or simulated gastric fluid or pH 4.5 buffer and pH 6.8 buffer or simulated intestinal fluid.

References[edit]

^ ^a^bMehta M (2016). Biopharmaceutics Classification System (BCS): Development, Implementation, and Growth. Wiley. ISBN978-1-118-47661-1.
^'Draft agreement'(PDF). www.ema.europa.eu. 22 June 2017. Retrieved 2019-07-03.

External links[edit]

BCS guidance of the U.S. Food and Drug Administration

Retrieved from 'https://en.wikipedia.org/w/index.php?title=Biopharmaceutics_Classification_System&oldid=993894943'

Bcs Classification Bcs Class 2 Drugs List

The BCS classification system is used to categorize drugs and serves to help anticipate whether drugs will have bioavailability/ bioequivalence problems. BCS classifies drugs according to their solubility and permeability. A drug is considered to have high solubility if drug substance at the highest dose strength for an immediate release formulation can be dissolved in < 250 mL of water over a pH range of 1-7.5. A high permeability drug is one that has either complete intestinal absorption (fa > 90%) or exhibits rapid movement through intestinal epithelia cells in vitro. BCS classifies all drugs into four categories as shown in Table 3.3.

Table 3.3. Biopharmaceutics classification system

BCS CLASS I High solubility High permeability

List Of Bcs Class 2 Antidiabetic Drugs

BCS CLASS III High solubility Low permeability

BCS CLASS II Low solubility High permeability

BCS CLASS IV Low solubility Low permeability

BCS class I compounds (high solubility and permeability) are unlikely to show bioavailability/bioequivalence issues. Therefore, for BCS class I drugs, in vitro dissolution studies are thought to provide sufficient information to assure in vivo product performance making full in vivo bioavailability/bioequivalence studies unnecessary. BCS class II and III drugs are not eligible for biowavers due to anticipated formulation differences in oral exposure. BCS class IV compounds, in general, are problematic with both poor solubility and permeability. The following tables (see Tables 3.4-3.7) contain lists of drugs that are categorized as BCS classes I to IV.

Bcs Class 2 Drugs List

Table 3.4. BCS class I compounds (high solubility, high permeability)
Abacavir	Diazepam	Ketorolac	Phenobarbital
Acetaminophen	Diltiazem	Ketoprofen	Phenylalanine
Diphenhydramine	Labetolol	Prednisolone
Crystal reports 2013 keygen. Amiloride	Disopyramide	Primaquine
Amitryptyline	Doxepin	Levofloxacin	Promazine
Antipyrine	Doxycycline	Lidocaine	Propranolol
Atropine	Enalapril	Lomefloxacin	Quinidine
Ephedrine	Meperidine	Rosiglitazone
Caffeine	Ergonovine	Metoprolol	Salicylic acid
Captopril	Ethambut