模糊物元模型评价几种促透剂的促透效果

目的:探讨模糊物元模型在促透剂促透效果综合评价中的运用.方法:研究氮酮、薄荷醇、樟脑、油酸、丁香油、荆芥油、藿香油促透剂对模型药物扑热息痛在离体兔背部皮肤上的透皮行为,计算渗透系数、稳态流量、滞后时间、增渗倍数,运用基于变异系数权重的模糊物元模型对促透效果进行综合评价.结果:2%丁香和2%樟脑对扑热息痛的促透效果最好,1%氮酮、2%荆芥、2%薄荷醇、2%油酸次之,2%广藿香最差.结论:基于变异系数权重的模糊物元模型可客观地、公正地评价促透剂的促透效果.     

Effects of L-alpha-glycerylphosphorylcholine on the EEG power spectrum in the rat

The effects of L-alpha-glycerylphosphorylcholine (alpha-GPC), a putative acetylcholine precursor, on the EEG power spetrum in rats were investigated. The results show that the oral administration of alpha-GPC (100–300–600 mg/kg) induced a significant decrease in absolute spectral energy in the delta frequency band. A significant increase in absolute spectral energy in the beta frequency band was elicited by alpha-GPC at dose levels of 100 and 300 mg/kg, while the administration of a higher dose (600 mg/kg) of this compound resulted in the loss of response (bell-shaped dose-response curve). No significant changes in the EEG power spectrum were found in rats treated with phosphatidylcholine (PC). The present data, suggesting that the electrocorticographic (ECoG) activation elicited by alpha-GPC may be correlated with its stimulatory effect on brain acetylcholine release, further extend the pharmacological profile of this new cognition enhancer. © 1992 Wiley-Liss, Inc.     

Comparison of the in vivo pharmacological profiles of sabeluzole and its enantiomers

Sabeluzole, a compound with pronounced cognitive enhancing, antihypoxic, and anticonvulsant properties, is the racemic mixture of the enantiomers R 84 439 (R-configuration) and R 84 440 (S-configuration). Sabeluzole and its separate enantiomers were compared in tests evaluating cognitive enhancing, antihypoxic, anticonvulsant, and secondary activity. Only small differences in potency were observed over species (mice, guinea pigs, and rats), routes of administration (i.p., s.c., and p.o.), and time intervals (ranging from 0.5 to 16 hr). R 84 440 was generally slightly more potent (up to 2.6 times) but also slightly shorter acting than R 84 439 (5 vs. 7 hr after s.c. administration in rats). The present data confirm and further extend the pharmacological profile of sabeluzole and indicate that both enantiomers contribute to its biological activity. Selection of one of the enantiomers instead of racemic sabeluzole provides no practical advantage in terms of potency, onset and duration of action, oral absorption, or therapeutic index.     

温经止痛凝胶膏剂的促渗剂优选

目的:优选温经止痛凝胶膏剂中促渗剂的种类及用量。方法:采用改良Franz扩散池,以离体小鼠腹部皮肤为屏障,采用HPLC检测不同促渗剂种类、比例及用量对温经止痛凝胶膏剂中藁本内酯累积透皮量、透皮吸收速率、增渗倍数等参数的影响,流动相甲醇-水(80∶20),检测波长328 nm。结果:氮酮和丙二醇联用的促渗效果明显优于其他几种促渗剂,确定氮酮与丙二醇的用量比(2∶1),总用量4%。藁本内酯24 h的累计透皮量84.16μg·cm-2,透皮速率常数3.28μg·cm-2·h-1,增渗倍数3.33。结论:氮酮和丙二醇组合的透皮促渗效果显著,可作为温经止痛凝胶膏剂的促渗剂。     

主成分分析用于清肺消痤凝胶体外经皮渗透的研究

该文运用主成分分析法建立一种中药复方透皮给药的评价方法,并以此方法优选清肺消痤凝胶的最佳透皮吸收促进剂.实验中以离体小鼠腹部皮肤为透皮屏障,采用改良Franz扩散池装置进行透皮吸收试验,HPLC建立接受液的指纹图谱,确定共有峰,求出各共有峰的面积,应用主成分分析法求得各组不同时间点的总因子得分,并以各因子得分代替药物浓度求得药物累积释放量Q₁₂,算出增渗倍数ER,以此比较各促进剂对药物的透皮促进作用.结果显示,与空白组相比,各促进剂均对药物有促进作用,而以2.5%氮酮+2.5%薄荷醇混合使用时的促进作用最强.主成分分析法可以较全面的反应接受液中药物的信息,以此建立的评价方法可准确的优选出透皮吸收促进剂,并为后续中药复方经皮给药提供了可借鉴的研究思路.     

贴剂研究概况及展望简

该文介绍了透皮贴剂的研究近况,概述了贴剂在药用高分子材料、制备工艺、促进药物渗透的方法和技术等方面的最新进展,突出了这种新剂型的优势和广阔的市场前景,给经皮给药制剂研究提供一定的参考和建议。