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Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: preparation and in vitro/in vivo evaluation.
Int J Pharm. 2014 Dec 10; 476(1-2):223-31.IJ

Abstract

Owing to the complementary mechanisms of action of metformin hydrochloride (MH) and pioglitazone hydrochloride (PG), combination therapy for type 2 diabetes mellitus using the two drugs is highly desired; on the other hand, MH is not well absorbed in lower gastrointestinal tract and has a short half-life, therefore compromising the therapeutic effects. Herein, the present study was to develop gastro-floating bilayer matrix tablets in which the two drugs were incorporated into two separate layers, aiming at sustaining MH release with enhanced absorption and achieving immediate release of PG. The tablets of the optimized formulation floated on the test medium for more than 24 h with 5 min of floating lag time, and sustained MH release for 12 h via a diffusion-dependent manner; and complete release of PG within 5 min were achieved. Moreover, a steady plasma concentration of MH with a 1.5-fold increase in bioavailability, decreased C(max) and reduced T(max) was obtained, and the in vivo behavior of PG was similar to the marked product. Summarily, sustained MH release with improved absorption and immediate release of PG were obtained simultaneously using the gastro-floating bilayer tablet, allowing strengthened combination therapy for diabetes mellitus.

Authors+Show Affiliations

State Key Laboratory of Natural Medicines, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.State Key Laboratory of Natural Medicines, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.State Key Laboratory of Natural Medicines, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.State Key Laboratory of Natural Medicines, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.State Key Laboratory of Natural Medicines, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China. Electronic address: lifangyin@hotmail.com.

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

25283698

Citation

He, Wei, et al. "Gastro-floating Bilayer Tablets for the Sustained Release of Metformin and Immediate Release of Pioglitazone: Preparation and in Vitro/in Vivo Evaluation." International Journal of Pharmaceutics, vol. 476, no. 1-2, 2014, pp. 223-31.
He W, Li Y, Zhang R, et al. Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: preparation and in vitro/in vivo evaluation. Int J Pharm. 2014;476(1-2):223-31.
He, W., Li, Y., Zhang, R., Wu, Z., & Yin, L. (2014). Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: preparation and in vitro/in vivo evaluation. International Journal of Pharmaceutics, 476(1-2), 223-31. https://doi.org/10.1016/j.ijpharm.2014.09.056
He W, et al. Gastro-floating Bilayer Tablets for the Sustained Release of Metformin and Immediate Release of Pioglitazone: Preparation and in Vitro/in Vivo Evaluation. Int J Pharm. 2014 Dec 10;476(1-2):223-31. PubMed PMID: 25283698.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: preparation and in vitro/in vivo evaluation. AU - He,Wei, AU - Li,Yongji, AU - Zhang,Rao, AU - Wu,Zhannan, AU - Yin,Lifang, Y1 - 2014/10/03/ PY - 2014/08/01/received PY - 2014/09/17/revised PY - 2014/09/29/accepted PY - 2014/10/7/entrez PY - 2014/10/7/pubmed PY - 2015/10/21/medline KW - Bilayer tablets KW - Floating drug delivery system KW - In vivo–in vitro correlation KW - Metformin hydrochloride KW - Pharmacokinetics KW - Pioglitazone hydrochloride SP - 223 EP - 31 JF - International journal of pharmaceutics JO - Int J Pharm VL - 476 IS - 1-2 N2 - Owing to the complementary mechanisms of action of metformin hydrochloride (MH) and pioglitazone hydrochloride (PG), combination therapy for type 2 diabetes mellitus using the two drugs is highly desired; on the other hand, MH is not well absorbed in lower gastrointestinal tract and has a short half-life, therefore compromising the therapeutic effects. Herein, the present study was to develop gastro-floating bilayer matrix tablets in which the two drugs were incorporated into two separate layers, aiming at sustaining MH release with enhanced absorption and achieving immediate release of PG. The tablets of the optimized formulation floated on the test medium for more than 24 h with 5 min of floating lag time, and sustained MH release for 12 h via a diffusion-dependent manner; and complete release of PG within 5 min were achieved. Moreover, a steady plasma concentration of MH with a 1.5-fold increase in bioavailability, decreased C(max) and reduced T(max) was obtained, and the in vivo behavior of PG was similar to the marked product. Summarily, sustained MH release with improved absorption and immediate release of PG were obtained simultaneously using the gastro-floating bilayer tablet, allowing strengthened combination therapy for diabetes mellitus. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25283698/Gastro_floating_bilayer_tablets_for_the_sustained_release_of_metformin_and_immediate_release_of_pioglitazone:_preparation_and_in_vitro/in_vivo_evaluation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(14)00711-X DB - PRIME DP - Unbound Medicine ER -