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酒石酸托特罗定经皮给药用于膀胱过度活动症治疗的体内外评价

Transdermal delivery of tolterodine tartrate for overactive bladder treatment: In vitro and in vivo evaluation.

作者信息

Rajabalaya Rajan, Mun Chung Yee, Chellian Jestin, Chakravarthi Srikumar, David Sheba R

机构信息

.

出版信息

Acta Pharm. 2017 Sep 1;67(3):325-339. doi: 10.1515/acph-2017-0027.

Abstract

The purpose of the study was to develop a transdermal tolterodine tartrate (TT) patch and to analyse its efficacy for overactive bladder (OAB) treatment. Patches were prepared using various polymers and plasticizers via the solvent casting method. The patches were characterized for tensile strength, thickness, moisture content, modulus of elasticity and water absorption capacity. Differential scanning calorimetry and Fourier transform infrared analyses were also performed. To determine patch effectiveness, in vitro release, permeation and animal studies were performed. The patches showed satisfactory percentage of release, up to 89.9 %, and their mechanical properties included thickness (0.10-0.15 mm), tensile strength (4.62-9.98 MPa) and modulus of elasticity (20-29 MPa). There were no significant interactions between TT and other excipients. Animal studies indicated that the TT patch reduced the incidence of side effects; however, studies of longer duration are required to determine the effectiveness in treating OAB.

摘要

本研究的目的是开发一种酒石酸托特罗定(TT)透皮贴剂,并分析其治疗膀胱过度活动症(OAB)的疗效。通过溶剂浇铸法使用各种聚合物和增塑剂制备贴剂。对贴剂的拉伸强度、厚度、水分含量、弹性模量和吸水能力进行了表征。还进行了差示扫描量热法和傅里叶变换红外分析。为了确定贴剂的有效性,进行了体外释放、渗透和动物研究。贴剂的释放百分比令人满意,高达89.9%,其机械性能包括厚度(0.10 - 0.15毫米)、拉伸强度(4.62 - 9.98兆帕)和弹性模量(20 - 29兆帕)。TT与其他辅料之间没有显著相互作用。动物研究表明,TT贴剂降低了副作用的发生率;然而,需要进行更长时间的研究来确定其治疗OAB的有效性。

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