Bcs Class I

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Biopharmaceutics Classification System (BCS) are intended only to investigate. Therefore, both BCS Class I (high solubility and high permeability) and Class.

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  • Whenever a new drug moiety is discovered, one of the 1st questions a pharmaceutical company asks is….whether or not the drug can be effectively administered by the oral route, for its intended use
    Biopharmaceutical Classification System (BCS) is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability
  • Biopharmaceutical Classification System (BCS) is a scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability
  • BCS was originally used to grant biowaivers for scale-up and post-approval changes for drug products, but was later extended to the approval of new generic products.
  • FDA suggests as a potential internal standard
  • (Determination in Caco II cells only applicable to passively absorbed substances)
  • A drug substance is considered “highly soluble” when the highest clinical dose strength is soluble in 250 mL or less of aqueous media over a pH range of 1–7.5 at 37 °C

  • when the dissolution rate is much greater than the gastric emptying, dissolution is not likely to be rate-limiting
  • BCS Can be used to obtain a biowaiver
  • It has been estimated that the application of BCS can result in annual savings of $35 million for
    the pharmaceutical industry
  • Reference: Particle size; Drug development services; Technical Brief 2011 Volume 9
    • Bcs class iii

    The Biopharmaceutics Classification System is a system to differentiate the 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].

    BCS classes[edit]

    According to the Biopharmaceutical Classification System (BCS) drug substances are classified to four classes upon their solubility and permeability:[1]Jab tak hai jaan online.

    • 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.
    Bcs Class I

    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 N HCl or simulated gastric fluid or pH 4.5 buffer and pH 6.8 buffer or simulated intestinal fluid.

    See also[edit]

    Bcs Class Ii Drugs

    • ADME

    References[edit]

    1. ^ abMehta M (2016). Biopharmaceutics Classification System (BCS): Development, Implementation, and Growth. Wiley. ISBN978-1-118-47661-1.
    2. ^https://www.ema.europa.eu/documents/scientific-guideline/draft-paracetamol-oral-use-immediate-release-formulations-product-specific-bioequivalence-guidance_en.pdf

    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. ISBN3-527-30438-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. PMID7617530.

    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=884065387'