EVALUATION OF THE USE OF PARTITION COEFFICIENTS AND MOLECULAR SURFACE PROPERTIES AS PREDICTORS OF DRUG ABSORPTION: A PROVISIONAL BIOPHARMACEUTICAL CLASSIFICATION OF THE LIST OF NATIONAL ESSENTIAL MEDICINES OF PAKISTAN

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SHAWAHNA R.; RAHMAN N.U.

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Journal Paper

Paper Information

Journal: DARU Journal of Pharmaceutical Sciences Year:2011 | Volume:19 | Issue:2 Page(s): 83-99

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Title

EVALUATION OF THE USE OF PARTITION COEFFICIENTS AND MOLECULAR SURFACE PROPERTIES AS PREDICTORS OF DRUG ABSORPTION: A PROVISIONAL BIOPHARMACEUTICAL CLASSIFICATION OF THE LIST OF NATIONAL ESSENTIAL MEDICINES OF PAKISTAN

Author(s)

SHAWAHNA R. | RAHMAN N.U. | Issue Writer Certificate

Keywords

BIOPHARMACEUTICAL CLASSIFICATION SYSTEM

PERMEABILITY

LOG P

LOG D

PSA

Abstract

Background and the purpose of the study: Partition coefficients (log D and LOG P) and molecular surface area (PSA) are potential predictors of the intestinal PERMEABILITY of drugs. The aim of this investigation was to evaluate and compare these intestinal PERMEABILITY indicators.Methods: Aqueous solubility data were obtained from literature or calculated using ACD/Labs and ALOGPS. PERMEABILITY data were predicted based on LOG P, LOG D at pH 6.0 (log D6.0), and PSA.Results: Metoprolol’s LOG P, LOG D6.0 and a PSA of<65 A correctly predicted 55.9%, 50.8% and 54.2% of PERMEABILITY classes, respectively. Labetalol’s LOG P, LOG D6.0, and PSA correctly predicted 54.2%, 64.4% and 61% of PERMEABILITY classes, respectively. LOG D6.0 correlated well (81%) with Caco-2 PERMEABILITY (Papp). Of the list of national essential medicines, 135 orally administered drugs were classified into BIOPHARMACEUTICAL CLASSIFICATION SYSTEM (BCS). Of these, 57 (42.2%), 28 (20.7%), 44 (32.6%), and 6 (4.4%) were class I, II, III and IV respectively.Conclusion: LOG D6.0 showed better prediction capability than LOG P. Metoprolol as PERMEABILITY internal standard was more conservative than labetalol.

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APA: Copy

SHAWAHNA, R., & RAHMAN, N.U.. (2011). EVALUATION OF THE USE OF PARTITION COEFFICIENTS AND MOLECULAR SURFACE PROPERTIES AS PREDICTORS OF DRUG ABSORPTION: A PROVISIONAL BIOPHARMACEUTICAL CLASSIFICATION OF THE LIST OF NATIONAL ESSENTIAL MEDICINES OF PAKISTAN. DARU JOURNAL OF PHARMACEUTICAL SCIENCE, 19(2), 83-99. SID. https://sid.ir/paper/275607/en

Vancouver: Copy

SHAWAHNA R., RAHMAN N.U.. EVALUATION OF THE USE OF PARTITION COEFFICIENTS AND MOLECULAR SURFACE PROPERTIES AS PREDICTORS OF DRUG ABSORPTION: A PROVISIONAL BIOPHARMACEUTICAL CLASSIFICATION OF THE LIST OF NATIONAL ESSENTIAL MEDICINES OF PAKISTAN. DARU JOURNAL OF PHARMACEUTICAL SCIENCE[Internet]. 2011;19(2):83-99. Available from: https://sid.ir/paper/275607/en

IEEE: Copy

R. SHAWAHNA, and N.U. RAHMAN, “EVALUATION OF THE USE OF PARTITION COEFFICIENTS AND MOLECULAR SURFACE PROPERTIES AS PREDICTORS OF DRUG ABSORPTION: A PROVISIONAL BIOPHARMACEUTICAL CLASSIFICATION OF THE LIST OF NATIONAL ESSENTIAL MEDICINES OF PAKISTAN,” DARU JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 19, no. 2, pp. 83–99, 2011, [Online]. Available: https://sid.ir/paper/275607/en

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