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Influence of Drying Procedure and of Low Degree of Substitution on the Structural and Drug Release Properties of Carboxymethyl Starch

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Abstract

The aim of this study was to investigate the influence of drying methods and low range of degrees of substitution (DS) on the structural, physicochemical, and drug-release properties of carboxymethyl high-amylose starch (CMS). CMS with three DS of 0.03, 0.14, and 0.25 was synthesized and dried by either solvent precipitation (SP), spray drying (SD), or lyophilization (Ly). DS had an influence on the crystalline structure of CMS. It was found that a DS of 0.14 or higher induced a modification of polymorphism. The drying method and the DS had both an impact on the physical properties of the CMS powder which can further influence the formulation characteristics and drug-release properties from monolithic tablets. The CMS with DS of 0.14 and 0.25 dried by SP or SD presented good excipient properties in terms of compressibility. With acetaminophen (20%) as tracer, the monolithic CMS tablets showed controlled drug release over 17 h for DS of 0.14 and 10 h for DS of 0.25, almost independent of pH, suggesting interesting properties for sustained release applications.

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Acknowledgements

Natural Sciences and Engineering Research Council of Canada (NSERC) and Canada Foundation for Innovation (CFI) support to M. A. Mateescu is gratefully acknowledged. Ph. D. graduate studentship from NSERC and Corealis Pharma Inc. (Montreal, Canada) awarded to M. Lemieux is also gratefully acknowledged. Special thanks are due to Dr. Roch Thibert for insightful comments on the manuscript and to F. Byette, R. Mineau and M. Preda for providing technical support for this work.

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Authors and Affiliations

  1. Department of Chemistry and Centre Pharmaqam, Université du Québec à Montréal, CP 8888, Succ. A, Montréal, Québec, Canada, H3C 3P8

    Marc Lemieux & Mircea Alexandru Mateescu

  2. Corealis Pharma Inc., 200 boulevard Armand Frappier, Laval, Québec, Canada, H7V 4A6

    Patrick Gosselin

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  1. Marc Lemieux
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  2. Patrick Gosselin
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Correspondence to Mircea Alexandru Mateescu.

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Lemieux, M., Gosselin, P. & Mateescu, M.A. Influence of Drying Procedure and of Low Degree of Substitution on the Structural and Drug Release Properties of Carboxymethyl Starch. AAPS PharmSciTech 11, 775–785 (2010). https://doi.org/10.1208/s12249-010-9437-5

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