Sahajwalla C G, Bhatt A D, Bhatia S C, Bakshi R, Doshi K J, Banavalikar M M, Bharucha E D, Marthak K V, Shah N N, Gupta K C
Research Centre and Medical Department, Hindustan Ciba-Geigy Ltd.
J Assoc Physicians India. 1991 Jul;39(7):546-8.
The objective of the study was to compare the enteric coated diclofenac sodium (Voveran), the slow release formulation developed in India (Voveran SR) and the internationally marketed formulation Voltaren Retard. Ten healthy volunteers were administered 100 mg each of the three formulations in a three-way crossover fashion. Blood samples were collected over 24 hours following administration of the drug; plasma levels of unchanged drug were determined by gas chromatography. Pharmacokinetic parameters for the three formulations were compared. The extent of the drug available from the three formulations was the same as the mean AUC values were not significantly different. Cmax and MRT values for the two slow release formulations were comparable but were significantly different from the values obtained with the enteric coated formulation. Tmax values for the two slow release formulations were similar while the enteric coated tablet had faster time to peak. Voveran SR is comparable to Voltaren Retard and has the distinct advantage of a slow release formulation in that its Cmax is much lower and levels are maintained over 12 hours and detectable upto 24 hours. This slow release formulation will offer clinical advantages of better compliance, relief of early morning symptoms and better tolerability over long term usage.
本研究的目的是比较肠溶性双氯芬酸钠(扶他林)、印度研发的缓释制剂(扶他林SR)以及国际市场上销售的制剂扶他林缓释片。10名健康志愿者以三交叉方式分别服用三种制剂各100毫克。给药后24小时内采集血样;采用气相色谱法测定血浆中未变化药物的水平。比较三种制剂的药代动力学参数。三种制剂的药物可利用程度相同,因为平均曲线下面积值无显著差异。两种缓释制剂的峰浓度和平均滞留时间值相近,但与肠溶性制剂所得的值有显著差异。两种缓释制剂的达峰时间值相似,而肠溶性片剂的达峰时间更快。扶他林SR与扶他林缓释片相当,且具有缓释制剂的显著优势,即其峰浓度低得多,药物水平在12小时内保持稳定,24小时内仍可检测到。这种缓释制剂将带来临床优势,如更好的依从性、缓解清晨症状以及长期使用时更好的耐受性。