Alam Mohammad Intakhab, Baboota Sanjula, Kohli Kanchan, Ali Javed, Ahuja Alka
Department of Pharmaceutics, Jamia Hamdard, Hamdard Nagar, New Delhi, India.
PDA J Pharm Sci Technol. 2009 Sep-Oct;63(5):429-37.
Low-dose, matrix-type transdermal patches containing celecoxib were developed for the treatment of osteoarthritis. The patches were designed to be used over a period of 24 h. Different ratios of ethyl cellulose/polyvinyl pyrrollidone (EC/PVP) were used for the development of the system. All of the prepared patches were subjected to physicochemical evaluation, in vitro drug release, permeation, and anti-inflammatory studies (in vivo). The release rates and flux increased linearly when an increase in the fraction of PVP was mixed with the formulations. In vitro studies showed enhanced performance in the presence of an enhancer (5% v/v oleic acid). The cumulative amount of drug permeated was found to be proportional to the square root of time (following the Higuchi equation). The anti-inflammatory effect (in vivo) and sustained action were studied by a carrageenan-induced (1% w/v) rat hind paw edema method. The selected formulation (EC/PVP, 2:3) produced 100% inhibition of paw edema in rats up to 6 h after receiving the carrageenan injection. The inhibition was 94.42%, 89.77%, and 86.44% after 8, 12 and 24 h, respectively. From this study it can be concluded that celecoxib can be formulated into a patch for transdermal delivery. Therefore, celecoxib can be recommended for further pharmacokinetic and pharmacodynamic studies in suitable animal models.
开发了含塞来昔布的低剂量基质型透皮贴剂用于骨关节炎的治疗。这些贴剂设计为可使用24小时。采用不同比例的乙基纤维素/聚乙烯吡咯烷酮（EC/PVP）来开发该系统。所有制备的贴剂均进行了理化评价、体外药物释放、渗透及抗炎研究（体内）。当PVP与制剂混合比例增加时，释放速率和通量呈线性增加。体外研究表明，在存在增强剂（5% v/v油酸）的情况下性能增强。发现药物渗透的累积量与时间的平方根成正比（符合Higuchi方程）。通过角叉菜胶诱导（1% w/v）大鼠后爪水肿法研究了抗炎作用（体内）和持续作用。所选制剂（EC/PVP，2:3）在接受角叉菜胶注射后6小时内对大鼠爪水肿产生100%的抑制作用。在8、12和24小时后，抑制率分别为94.42%、89.77%和86.44%。从该研究可以得出结论，塞来昔布可制成透皮给药的贴剂。因此，推荐塞来昔布在合适的动物模型中进行进一步的药代动力学和药效学研究。
