Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class

The main objective of the present study was to develop quantitative-structure property relationship (QSPR) models with predictability for release, transportability and related properties of formulation containing a neutral drug (glimepiride) based on polymeric properties. Such physicochemical proper...

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Main Authors: Vinod L. Gaikwad, Manish S. Bhatia, Indrajeet Singhvi
Format: Article
Language:English
Published: Elsevier 2016-11-01
Series:Arabian Journal of Chemistry
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S187853521500194X
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spelling doaj-bb14714632ae41de91a1483206cca1432020-11-24T22:43:20ZengElsevierArabian Journal of Chemistry1878-53522016-11-019S2S1915S192710.1016/j.arabjc.2015.06.022Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral classVinod L. Gaikwad0Manish S. Bhatia1Indrajeet Singhvi2Department of Pharmaceutics, P.E. Society’s Modern College of Pharmacy, Nigdi, Pune 411044, Maharashtra State, IndiaDepartment of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra State, IndiaDepartment of Pharmaceutical Chemistry, Pacific College of Pharmacy, Udaipur 313024, Rajasthan State, IndiaThe main objective of the present study was to develop quantitative-structure property relationship (QSPR) models with predictability for release, transportability and related properties of formulation containing a neutral drug (glimepiride) based on polymeric properties. Such physicochemical properties are measure of polymers’ behavior in deciding release, transportability and bioavailability of drug. Therefore comprehensive study of properties could help in deciding proper polymer composite for formulation with required characteristics. A total of nine glimepiride (GLMP) tablet batches were prepared using three polymers representing extended, moderate and immediate release categories. Molecular descriptors were calculated from polymeric structures and correlated with formulation characteristics. This leads to generation of predictive models. Compatibility between drug-excipients was confirmed. Weight uniformity, drug content, hardness and friability tests showed acceptable results. In vitro dissolution kinetics exhibited Korsmeyer-peppas model as best fit. Best correlation coefficient and validation of developed QSPRs showed powerful predictability for properties. Transportability was influenced by release rate together with molecular size, pKa, log P and water solubility of GLMP. Generated models were found to significantly predict the release, transportability and related formulation properties. QSPR models were developed with enough prediction potential for the properties of formulation containing any neutral drug and could also help to decide the formulation composition for required characteristics together with pharmacoeconomic impact with respect to time, cost and material.http://www.sciencedirect.com/science/article/pii/S187853521500194XQSPRMathematical modelPolymer systemNeutral drug releaseTransportability profile
collection DOAJ
language English
format Article
sources DOAJ
author Vinod L. Gaikwad
Manish S. Bhatia
Indrajeet Singhvi
spellingShingle Vinod L. Gaikwad
Manish S. Bhatia
Indrajeet Singhvi
Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
Arabian Journal of Chemistry
QSPR
Mathematical model
Polymer system
Neutral drug release
Transportability profile
author_facet Vinod L. Gaikwad
Manish S. Bhatia
Indrajeet Singhvi
author_sort Vinod L. Gaikwad
title Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
title_short Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
title_full Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
title_fullStr Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
title_full_unstemmed Statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
title_sort statistical significance of polymeric physicochemical properties in the development of formulations containing a drug from neutral class
publisher Elsevier
series Arabian Journal of Chemistry
issn 1878-5352
publishDate 2016-11-01
description The main objective of the present study was to develop quantitative-structure property relationship (QSPR) models with predictability for release, transportability and related properties of formulation containing a neutral drug (glimepiride) based on polymeric properties. Such physicochemical properties are measure of polymers’ behavior in deciding release, transportability and bioavailability of drug. Therefore comprehensive study of properties could help in deciding proper polymer composite for formulation with required characteristics. A total of nine glimepiride (GLMP) tablet batches were prepared using three polymers representing extended, moderate and immediate release categories. Molecular descriptors were calculated from polymeric structures and correlated with formulation characteristics. This leads to generation of predictive models. Compatibility between drug-excipients was confirmed. Weight uniformity, drug content, hardness and friability tests showed acceptable results. In vitro dissolution kinetics exhibited Korsmeyer-peppas model as best fit. Best correlation coefficient and validation of developed QSPRs showed powerful predictability for properties. Transportability was influenced by release rate together with molecular size, pKa, log P and water solubility of GLMP. Generated models were found to significantly predict the release, transportability and related formulation properties. QSPR models were developed with enough prediction potential for the properties of formulation containing any neutral drug and could also help to decide the formulation composition for required characteristics together with pharmacoeconomic impact with respect to time, cost and material.
topic QSPR
Mathematical model
Polymer system
Neutral drug release
Transportability profile
url http://www.sciencedirect.com/science/article/pii/S187853521500194X
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