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<title>Biopharmaceutics Classification System</title>

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<span id="openzim-page-title" class="mw-page-title-main"><span class="mw-page-title-main">Biopharmaceutics Classification System</span></span>

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</style><div role="note" class="hatnote navigation-not-searchable">For other uses of "BCS", see <a href="BCS_(disambiguation)" class="mw-redirect mw-disambig" title="BCS (disambiguation)">BCS (disambiguation)</a>.</div>

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<p>The <b>Biopharmaceutics Classification System</b> (<b>BCS</b>) is a system to differentiate drugs on the basis of their solubility and permeability.<sup id="cite_ref-Mehta_2016_1-0" class="reference"><a href="#cite_note-Mehta_2016-1"><span class="cite-bracket">[</span>1<span class="cite-bracket">]</span></a></sup>

</p><p>This system restricts the prediction using the parameters <a href="Solubility" title="Solubility">solubility</a> and <a href="Intestinal_permeability" title="Intestinal permeability">intestinal permeability</a>. The solubility classification is based on a <a href="United_States_Pharmacopoeia" class="mw-redirect" title="United States Pharmacopoeia">United States Pharmacopoeia</a> (USP) aperture. The intestinal permeability classification is based on a comparison to the <a href="Route_of_administration" title="Route of administration">intravenous injection</a>. All those factors are highly important because 85% of the most sold drugs in the <a href="United_States" title="United States">United States</a> and <a href="Europe" title="Europe">Europe</a> are <a href="Route_of_administration" title="Route of administration">orally administered</a>.

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<div class="mw-heading mw-heading2"><h2 id="Classes">Classes</h2></div>

<p>According to the Biopharmaceutics Classification System (BCS) drug substances are classified to four classes upon their solubility and permeability:<sup id="cite_ref-Mehta_2016_1-1" class="reference"><a href="#cite_note-Mehta_2016-1"><span class="cite-bracket">[</span>1<span class="cite-bracket">]</span></a></sup>

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<ul><li><b>Class I – high <a href="Intestinal_permeability" title="Intestinal permeability">permeability</a>, high <a href="Solubility" title="Solubility">solubility</a> </b>

<ul><li>Example: <a href="Metoprolol" title="Metoprolol">metoprolol</a>, <a href="Paracetamol" title="Paracetamol">paracetamol</a><sup id="cite_ref-2" class="reference"><a href="#cite_note-2"><span class="cite-bracket">[</span>2<span class="cite-bracket">]</span></a></sup></li>

<li>Those compounds are well absorbed and their absorption rate is usually higher than excretion.</li></ul></li>

<li><b>Class II – high permeability, low solubility</b>

<ul><li>Example: <a href="Glibenclamide" title="Glibenclamide">glibenclamide</a>, <a href="Bicalutamide" title="Bicalutamide">bicalutamide</a>, <a href="Ezetimibe" title="Ezetimibe">ezetimibe</a>, <a href="Aceclofenac" title="Aceclofenac">aceclofenac</a></li>

<li>The <a href="Bioavailability" title="Bioavailability">bioavailability</a> of those products is limited by their solvation rate. A correlation between the <i><a href="In_vivo" title="In vivo">in vivo</a></i> bioavailability and the <i><a href="In_vitro" title="In vitro">in vitro</a></i> solvation can be found.</li></ul></li>

<li><b>Class III – low permeability, high solubility </b>

<ul><li>Example: <a href="Cimetidine" title="Cimetidine">cimetidine</a></li>

<li>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.</li></ul></li>

<li><b>Class IV – low permeability, low solubility </b>

<ul><li>Example: <a href="Bifonazole" title="Bifonazole">bifonazole</a></li>

<li>Those compounds have a poor bioavailability. Usually they are not well absorbed over the intestinal mucosa and a high variability is expected.</li></ul></li></ul>

<div class="mw-heading mw-heading2"><h2 id="Definitions">Definitions</h2></div>

<p>The drugs are classified in BCS on the basis of solubility and permeability.

</p><p>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 <a href="Bioequivalence" title="Bioequivalence">bioequivalence</a> study protocols that prescribe administration of a drug product to fasting human volunteers with a glass of water.

</p><p>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 <a href="Intravenous" class="mw-redirect" title="Intravenous">intravenous</a> dose.

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<ul><li><a href="Partition_coefficient" title="Partition coefficient">Partition coefficient</a></li>

<li><a href="Bioavailability" title="Bioavailability">Bioavailability</a></li>

<li><a href="Drug_metabolism" title="Drug metabolism">Drug metabolism</a></li>

<li><a href="First_pass_effect" title="First pass effect">First pass effect</a></li></ul></li>

<li><a href="Polar_surface_area" title="Polar surface area">Polar surface area</a></li>

<li><a href="IVIVC" title="IVIVC">IVIVC</a></li></ul>

<div class="mw-heading mw-heading2"><h2 id="References">References</h2></div>

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</style><cite id="CITEREFMehta2016" class="citation book cs1">Mehta M (2016). <i>Biopharmaceutics Classification System (BCS): Development, Implementation, and Growth</i>. Wiley. <a href="ISBN_(identifier)" class="mw-redirect" title="ISBN (identifier)">ISBN</a> <bdi>978-1-118-47661-1</bdi>.</cite></span>

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<li id="cite_note-2"><span class="mw-cite-backlink"><b><a href="#cite_ref-2">^</a></b></span> <span class="reference-text"><cite class="citation web cs1"><a rel="nofollow" class="external text" href="https://www.ema.europa.eu/documents/scientific-guideline/draft-paracetamol-oral-use-immediate-release-formulations-product-specific-bioequivalence-guidance_en.pdf">"Draft agreement"</a> <span class="cs1-format">(PDF)</span>. <i>www.ema.europa.eu</i>. 22 June 2017<span class="reference-accessdate">. Retrieved <span class="nowrap">2019-07-03</span></span>.</cite></span>

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<div class="mw-heading mw-heading2"><h2 id="Further_reading">Further reading</h2></div>

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<ul><li><cite id="CITEREFFolkersvan_de_WaterbeemdLennernäsArtursson2003" class="citation book cs1">Folkers G, van de Waterbeemd H, Lennernäs H, Artursson P, Mannhold R, Kubinyi H (2003). <span class="id-lock-registration" title="Free registration required"><a rel="nofollow" class="external text" href="https://archive.org/details/drugbioavailabil0000unse"><i>Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability (Methods and Principles in Medicinal Chemistry)</i></a></span>. Weinheim: Wiley-VCH. <a href="ISBN_(identifier)" class="mw-redirect" title="ISBN (identifier)">ISBN</a> <bdi>3-527-30438-X</bdi>.</cite></li>

<li><cite id="CITEREFAmidonLennernäsShahCrison1995" class="citation journal cs1">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". <i>Pharm. Res</i>. <b>12</b> (3): <span class="nowrap">413–</span>20. <a href="PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a> <a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/7617530">7617530</a>.</cite></li></ul>

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<div class="mw-heading mw-heading2"><h2 id="External_links">External links</h2></div>

<ul><li><a rel="nofollow" class="external text" href="https://web.archive.org/web/20120912010209/http://www.fda.gov/AboutFDA/CentersOffices/OfficeofMedicalProductsandTobacco/CDER/ucm128219.htm">BCS guidance</a> of the <a href="U.S._Food_and_Drug_Administration" class="mw-redirect" title="U.S. Food and Drug Administration">U.S. Food and Drug Administration</a></li></ul></div><div><div class="zim-footer">

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