Preparation and in vivo/in vitro Evaluation of a Tri-layer Tablet Containing Glimepiride/Pioglitazone (IR), Metformin (SR) with an Isolation Layer

被引:0
作者
Zong, Taili [2 ]
Zhang, Tao [2 ]
He, Qin [1 ]
机构
[1] Sichuan Univ, W China Sch Pharm, Minist Educ, Key Lab Drug Targeting, Chengdu 610041, Peoples R China
[2] Chongqing Pharmaceut Res Inst Co Ltd, Chongqing 400061, Peoples R China
来源
PHARMAZEUTISCHE INDUSTRIE | 2011年 / 73卷 / 06期
关键词
Immediate-release layer; In vitro-in vivo correlation; Isolation layer; Sustained-release layer; Tri-layer tablet; GLYCEMIC CONTROL; DIABETES-MELLITUS; PHARMACOKINETICS; PREVALENCE;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The objective of the present study was to develop a tri-layer tablet which was administered once daily to improve diabetes patients compliance and achieve better glycemic control. The tri-layer tablet contained glimepiride (CAS number: 93479-97-1) and pioglitazone hydrochloride (CAS number: 112529-15-4) in the immediate-release layer, metformin hydrochloride (CAS number: 1115-70-4) in the sustained-release layer, and an isolation layer between the immediate-release layer and the sustained-release layer to prevent the interaction of the three active components. Pioglitazone hydrochloride was released from the formulation within 15 minutes (immediately). Glimepiride was released from the formulation within 1 hour (moderately). Metformin hydrochloride was released from the formulation within 12 hours (sustainedly). All these composed a once-daily formulation. No significant difference was observed in metformin in vitro release pattern between the tri-layer tablets and the equivalent dose of marketed formulation (metformin hydrochloride SR tablets) (f2 = 66.5). The two preparations were bioequivalent evaluated by a crossover study in six Beagle dogs. Significant sustained-release character was observed in metformin in vivo release of the tri-layer tablet. Moreover, in vitro-in vivo correlation of metformin from the tri-layer tablet was significant.
引用
收藏
页码:1136 / +
页数:9
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