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美洛昔康和氯诺昔康透皮贴剂的设计:制备、物理特性、体外和体内研究。

Design of meloxicam and lornoxicam transdermal patches: Preparation, physical characterization, ex vivo and in vivo studies.

作者信息

Yener Gülgün, Üner Melike, Gönüllü Ümit, Yildirim Sinem, Kiliç Pınar, Aslan Serap Sağlik, Barla Aslı

机构信息

Department of Pharmaceutical Technology, Istanbul University, Turkey.

出版信息

Chem Pharm Bull (Tokyo). 2010 Nov;58(11):1466-73. doi: 10.1248/cpb.58.1466.

Abstract

Transdermal patches of meloxicam (MX) and lornoxicam (LX) were aimed to be prepared in order to overcome their side effects by oral application. The strategy was formulation of optimized films to prepare transdermal patches by determination of physical properties and investigation of drug-excipient compatibility. As the next step, in vitro drug release, assesment of anti-inflammatory effect on Wistar Albino rats, ex vivo skin penetration and investigation of factors on drug release from transdermal patches were studied. Hydroxypropyl methylcellulose (HPMC) was concluded to be suitable polymer for formulation of MX and LX transdermal films indicating pharmaceutical quality required. MX and LX transdermal patches gave satisfactory results regarding to the edema inhibition in the assessment of anti-inflammatory effect. MX was found out to be more effective compared to LX on relieving of edema and swelling. These results were supported by data obtained from ex vivo penetration experiments of drug through rat skin. Indicative parameters like log P, molecular weight and solubility constraint on penetration rate of drugs also indicated good skin penetration. Transdermal patches of MX and LX can be suggested to be used especially for the immediate treatment of inflammated area since it displays anti-inflammatory effect, soon.

摘要

为克服美洛昔康(MX)和氯诺昔康(LX)口服给药的副作用,旨在制备其透皮贴剂。策略是通过测定物理性质和研究药物-辅料相容性来制备优化的薄膜以制备透皮贴剂。作为下一步,研究了体外药物释放、对Wistar白化大鼠的抗炎作用评估、离体皮肤渗透以及透皮贴剂药物释放的影响因素。羟丙基甲基纤维素(HPMC)被认为是制备MX和LX透皮薄膜的合适聚合物,表明其符合所需的药学质量。在抗炎作用评估中,MX和LX透皮贴剂在抑制水肿方面取得了令人满意的结果。发现MX在减轻水肿和肿胀方面比LX更有效。这些结果得到了药物通过大鼠皮肤的离体渗透实验数据的支持。药物渗透速率的指示参数如log P、分子量和溶解度限制也表明其具有良好的皮肤渗透性。MX和LX透皮贴剂因其能迅速发挥抗炎作用,可建议特别用于炎症区域的即时治疗。

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