Bakshi A, Bajaj A, Malhotra G, Madan M, Amrutiya N
C. U. Shah College of Pharmacy, SNDT Women's University, Santacruz (W), Mumbai-400 049, India.
Indian J Pharm Sci. 2008 Nov;70(6):733-9. doi: 10.4103/0250-474X.49094.
The objective of the present work was to develop a metered dose spray formulation for transdermal delivery of oxybutynin and to carry out the in vitro characterization of the optimized formulation. Oxybutynin release from a series of ethanol/acetone/methylal based formulations was assessed in vitro and the developed formulation was used for delivery from a metered dose spray. Various qualitative and quantitative parameters like spray pattern, particle size distribution, pH, evaporation time, pump seal efficiency test, average weight per metered dose, content per spray and content uniformity were evaluated. The different film forming agents were assessed and carbopol (0.5%) and lutrol (0.1%) were found to give good clarity of solution, evaporation rate, spray pattern and tackiness of the film. Diffusion studies of the optimized formulations through the semipermeable membrane showed the release of drug to the extent of almost 50% over a period of 24 h. Stability studies were conducted as per ICH guidelines and indicated that formulations were stable. Skin irritation studies were performed using rabbit as an animal model. The results obtained show that the metered dose transdermal spray formulation can be a promising and innovative therapeutic system for the transdermal administration of oxybutynin.
本研究的目的是开发一种用于奥昔布宁透皮给药的定量喷雾制剂，并对优化后的制剂进行体外特性研究。体外评估了一系列基于乙醇/丙酮/甲缩醛的制剂中奥昔布宁的释放情况，并将所开发的制剂用于定量喷雾给药。评估了各种定性和定量参数，如喷雾模式、粒度分布、pH值、蒸发时间、泵密封效率测试、每定量剂量的平均重量、每次喷雾含量和含量均匀度。对不同的成膜剂进行了评估，发现卡波姆（0.5%）和 Lutrol（0.1%）能使溶液具有良好的澄清度、蒸发速率、喷雾模式和膜的粘性。优化制剂通过半透膜的扩散研究表明，在24小时内药物释放量几乎达到50%。按照ICH指南进行了稳定性研究，结果表明制剂是稳定的。以兔子为动物模型进行了皮肤刺激性研究。所得结果表明，定量透皮喷雾制剂可能是一种用于奥昔布宁透皮给药的有前景的创新治疗系统。
