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Development of USP Apparatus 3 Dissolution Method with IVIVC for Extended Release Tablets of Metformin Hydrochloride and Development of a Generic Formulation.
Chem Pharm Bull (Tokyo). 2019; 67(1):23-31.CP

Abstract

Metformin is a euglycemic drug for the treatment of type 2 diabetes mellitus. To date, there are 13 dissolution methodologies described in the U.S. Pharmacopoeia (USP) to evaluate the release profile of metformin from extended-release tablets utilizing either a USP apparatus 1 (basket) or 2 (paddle). In the absence of a protocol for a USP apparatus 3 (reciprocating cylinder), the goal of this work was to develop an in vitro dissolution method for metformin extended-release tablets based on an in vivo-in vitro correlation (IVIVC). Following a systematic evaluation, a final dissolution method, M4, was defined. It applied 30 dips per minute (dpm) over a total period of 10 h into a series of solutions that included 2 h in HCl media (pH 1.2), 1 h in an acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS) (pH 5.8) and 6 h in PBS (pH 6.8). This method showed a significant IVIVC with a calculated R2 > 0.98 (point-to-point correlation, Level A) and it was successfully used as a tool to assist in the development of generic extended release formulations for metformin consisting of a lipophilic matrix system.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro.

Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro.

Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro.

Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro.

Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro.

Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro.

MeSH

Delayed-Action PreparationsDrug CompoundingDrugs, GenericHumansMetforminPharmacopoeias as TopicTabletsUnited States

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30606948

Citation

Mendes, Thamara de Carvalho, et al. "Development of USP Apparatus 3 Dissolution Method With IVIVC for Extended Release Tablets of Metformin Hydrochloride and Development of a Generic Formulation." Chemical & Pharmaceutical Bulletin, vol. 67, no. 1, 2019, pp. 23-31.

Mendes TC, Simon A, Menezes JCV, et al. Development of USP Apparatus 3 Dissolution Method with IVIVC for Extended Release Tablets of Metformin Hydrochloride and Development of a Generic Formulation. Chem Pharm Bull (Tokyo). 2019;67(1):23-31.

Mendes, T. C., Simon, A., Menezes, J. C. V., Pinto, E. C., Cabral, L. M., & de Sousa, V. P. (2019). Development of USP Apparatus 3 Dissolution Method with IVIVC for Extended Release Tablets of Metformin Hydrochloride and Development of a Generic Formulation. Chemical & Pharmaceutical Bulletin, 67(1), 23-31. https://doi.org/10.1248/cpb.c18-00579

Mendes TC, et al. Development of USP Apparatus 3 Dissolution Method With IVIVC for Extended Release Tablets of Metformin Hydrochloride and Development of a Generic Formulation. Chem Pharm Bull (Tokyo). 2019;67(1):23-31. PubMed PMID: 30606948.

* Article titles in AMA citation format should be in sentence-case

TY - JOUR T1 - Development of USP Apparatus 3 Dissolution Method with IVIVC for Extended Release Tablets of Metformin Hydrochloride and Development of a Generic Formulation. AU - Mendes,Thamara de Carvalho, AU - Simon,Alice, AU - Menezes,Jaqueline Correia Villaça, AU - Pinto,Eduardo Costa, AU - Cabral,Lucio Mendes, AU - de Sousa,Valeria Pereira, PY - 2019/1/5/entrez PY - 2019/1/5/pubmed PY - 2019/2/14/medline KW - United States Pharmacopoeia apparatus 3 KW - dissolution KW - in vivo–in vitro correlation KW - metformin hydrochloride KW - oral extended-release formulation SP - 23 EP - 31 JF - Chemical & pharmaceutical bulletin JO - Chem Pharm Bull (Tokyo) VL - 67 IS - 1 N2 - Metformin is a euglycemic drug for the treatment of type 2 diabetes mellitus. To date, there are 13 dissolution methodologies described in the U.S. Pharmacopoeia (USP) to evaluate the release profile of metformin from extended-release tablets utilizing either a USP apparatus 1 (basket) or 2 (paddle). In the absence of a protocol for a USP apparatus 3 (reciprocating cylinder), the goal of this work was to develop an in vitro dissolution method for metformin extended-release tablets based on an in vivo-in vitro correlation (IVIVC). Following a systematic evaluation, a final dissolution method, M4, was defined. It applied 30 dips per minute (dpm) over a total period of 10 h into a series of solutions that included 2 h in HCl media (pH 1.2), 1 h in an acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS) (pH 5.8) and 6 h in PBS (pH 6.8). This method showed a significant IVIVC with a calculated R2 > 0.98 (point-to-point correlation, Level A) and it was successfully used as a tool to assist in the development of generic extended release formulations for metformin consisting of a lipophilic matrix system. SN - 1347-5223 UR - https://www.unboundmedicine.com/medline/citation/30606948/Development_of_USP_Apparatus_3_Dissolution_Method_with_IVIVC_for_Extended_Release_Tablets_of_Metformin_Hydrochloride_and_Development_of_a_Generic_Formulation_ DB - PRIME DP - Unbound Medicine ER -