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Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and
Prachi B Shekhawat1, Varsha B Pokharkar1
1Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Kothrud, Pune 411038, India.
Acta Pharmaceutica Sinica. B
|May 26, 2017
Abstract:
Oral drug absorption is a process influenced by the physicochemical and biopharmaceutical properties of the drug and its inter-relationship with the gastrointestinal tract. Drug solubility, dissolution and permeability across intestinal barrier are the key parameters controlling absorption. This review provides an overview of the factors that affect drug absorption and the classification of a drug on the basis of solubility and permeability. The biopharmaceutical classification system (BCS) was introduced in early 90׳s and is a regulatory tool used to predict bioavailability problems associated with a new entity, thereby helping in the development of a drug product. Strategies to combat solubility and permeability issues are also discussed.
Keywords:
ABC, ATP-binding cassetteAP, absorption potentialAPI, active pharmaceutical ingredientATP, adenosine triphosphateAZT, azidothymidineBA/BE, bioavailability/bioequivalenceBCRP, breast cancer resistance proteinBCSBCS, biopharmaceutical classification systemBDDS, biopharmaceutical drug disposition systemBSP, bromosulfophthaleinCD, cyclodextrinCDER, Centre for Drug Evaluation and ResearchCNT, Na+-dependent concentrative transporterCNT, concentrative nucleoside transporterCYP, cytochrome P450D:S, dose:solubilityE217G, estradiol 17β-glucuronideEMEA, European Medicines AgencyENT, equilibrative nucleoside transporterFATP, fatty acid transporter proteinFDA, U.S. Food and Drug AdministrationFIP, International Pharmaceutical FederationFaSSIF, fasted state simulated intestinal fluidFactors affecting absorptionFeSSIF, fed state simulated intestinal fluidFormulation strategiesGIS, gastrointestinal simulatorGIT, gastrointestinal tractGITA, gastrointestinal transit and absorptionGLUT, sodium-independent facilitated diffusion transporterGRAS, generally recognized as safeHIV, human immunodeficiency diseaseHPC-SL, LBDDS, lipid based drug delivery systemHUGO, Human Genome OrganizationICH, International Council of HarmonizationIDR, intrinsic dissolution rateIR, immediate releaseISBT, sodium dependent bile salt transporterMCT, monocarboxylate transporterMPP, 1-methyl-4-phenylpyridiniumMRP, multidrug resistance associated proteinNLC, nanostructured lipid carrierNME, new molecular entityNTCP, sodium-dependent taurocholate co-transporting polypeptideOAT, organic anion transporterOATP, organic anion transporting polypeptideOCT, organic cationic transporterOCTN, organic cationic/carnitine transporterOMM, ordered mesoporous materialP-gp, P-glycoproteinPAH, p-aminohippuratePAMPA, parallel artificial membrane permeability assayPEG, polyethylene glycolPEI, polyethyleneiminePEPT, peptide transporterPGA, polyglycolic acidPLA, poly(lactic acid)PLGA, poly-d,l-lactide-co-glycosidePMAT, plasma membrane monoamine transportPSA, polar surface areaPVDF, polyvinylidene difluoridePapp, apparent permeabilityPeff, effective permeabilityPermeabilityPsi, porous siliconRFC, reduced folate transporterSDS, sodium dodecyl sulphateSGLT, sodium dependent secondary active transporterSIF, simulated intestinal fluidSLC, solute carrierSLCO, solute carrier organic anionSLN, solid lipid nanoparticlesSMVT, sodium dependent multivitamin transporterSPIP, single pass intestinal perfusionSUPAC, scale-up and post approval changesSVCT, sodium-dependent vitamin C transporterSolubilityTEOS, tetraethylortho silicateUWL, unstirred water layerVDAD, volume to dissolve applied doseWHO, World Health OrganizationpMMA, polymethyl methacrylatevit. E TPGS, vitamin E tocopherol polyethylene glycol succinate
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