Studies on drug release from ointments. V. Release of hydrocortisone butyrate propionate from topical dosage forms to silicone rubber

The release of hydrocortisone butyrate propionate (HBP) from oil-in-water (o/w) cream and aqueous gels containing propylene glycol and ethanol to silicone rubber as a model for the skin was investigated. The release of HBP from o/w cream or gels was carried out under open or closed conditions at 35°C and 75% RH. The influence of the evaporation of vehicle components of the cream or gels on the release of HBP was examined. The release of HBP from o/w cream and aqueous gel containing propylene glycol under open conditions was lower than that under closed conditions, while the release of HBP from aqueous gel containing ethanol in open conditions was markedly higher than that under closed conditions. These differences in the release of HBP between open and closed conditions were related to changes in the thermodynamic activity of HBP in the vehicle during the release period. The results of HBP release under open conditions were nearly correlated with those of in vivo vasoconstrictor activity. The release method using silicone rubber under open conditions is considered to be useful for the evaluation of topical dosage forms, particularly those containing volatile components.     

Uncoupling of CA3 pyramidal neurons by propionate

The influence of cytoplasmic acidification on dye-coupling between CA3 pyramidal neurons was examined by Lucifer yellow injections in guinea pig hippocampal brain slices. Neurons were believed to be acidified by exposure to 100 mM propionate. Dye-coupling was reduced significantly to 6% (n = 35) in propionate versus 28% (n = 39) in control solution (P less than 2%). Propionate may be a useful tool for experimental manipulation of coupling in the mammalian CNS.     

HPLC法测定丙酸氯倍他索搽剂的含量

目的建立丙酸氯倍他索搽剂中丙酸氯倍他索含量的HPLC测定法。方法采用ZORBAX SB-C18色谱柱,流动相:乙腈-水(70:30,V／V),检测波长240 nm,流速1．0 mL·min-1。结果丙酸氯倍他索质量浓度为8～160 mg·L-1时有良好的线性关系(r=0．999 9),平均回收率为99．60％,RSD为0．26％(n=5)。结论该法简便、快速、准确,可测定丙酸氯倍他索搽剂中丙酸氯倍他索的含量。     

HPLC法同时测定复方酮康唑凝胶剂中酮康唑和丙酸氯倍他索的含量

目的:建立复方酮康唑凝胶剂中酮康唑和丙酸氯倍他索的含量测定方法.方法:采用高效液相色谱法,色谱柱为Hypersil ODS2 C18柱,甲醇-0.2%三乙胺(醋酸调pH至6.9,V:V=75:25)为流动相,流速1.0mL/min,检测波长239nm.结果:酮康唑在10.08～201.16μg/mL浓度范围内呈良好的线性关系,r=0.999 9;丙酸氯倍他索在0.251～5.02μg/mL浓度范围内呈良好的线性关系,r=0.999 8.酮康唑的平均回收率为99.59%,RSD为0.77%;丙酸氯倍他索的平均回收率为100.76%,RSD为1.18%.结论:本方法分离度好,简便,准确,适用于复方酮康唑凝胶剂中2组分的同时测定,可作为产品的质量控制方法.     

丙酸睾酮致BPH动物模型的评价及针刺作用机理探讨

探讨丙酸睾酮所致BPH动物模型的应用价值及针刺对BPH动物模型性激素水平的影响。采用丙酸睾酮肌注法造模 ,针刺秩边穴进行干预 ,用放免法测定血清T、E2 水平。结果 ,丙酸睾酮可引起大鼠的前列腺发生增生改变 ,针刺可以改善其病理变化 ,降低血清T ,促进E2 的生成。说明丙酸睾酮可以使大鼠的性激素水平发生紊乱 ,引起前列腺增生 ;针刺可以调节大鼠的性激素紊乱过程 ,抑制其病理变化 ,从而起到防治前列腺增生的作用。     

Sexual dimorphic expression of mouse hepatic CYP2B: alterations during development or after hypophysectomy

The constitutive expression of CYP2B mRNA in the livers of mice in the prepubertal stage was sex-independent, with CYP2B9 as the principal isoform. During the maturation stage, CYP2B10 was expressed in both sexes, whereas CYP2B9 was diminished markedly in the males, resulting in a sexually dimorphic expression in adult mice. Hypophysectomy eliminated the sexual dimorphism in the mouse CYP2B subfamily by markedly increasing the expression of both CYP2B9 and CYP2B10 in males to levels similar to those in females.     

喘乐宁与爱喘乐联合辅舒酮吸入治疗毛细支气管炎128例临床分析

目的:探讨喘乐宁与爱喘乐联合辅舒酮吸入治疗毛细支气管炎的临床疗效。方法:毛细支气管炎患儿128例,随机分为观察组(69例)与对照组(59例)。观察组在常规治疗基础上给予喘乐宁与爱喘乐联合辅舒酮吸入,观察2组治愈率及解除主要症状和体征的时间。结果:观察组治愈率、缓解喘憋症状及缩短哮鸣音持续时间均明显优于对照组(P<0.05)。结论:喘乐宁与爱喘乐联合辅舒酮吸入治疗毛细支气管炎显效迅速,疗效显著。     

雌二醇对丙酸睾酮诱导去势大鼠前列腺增生的作用

目的探讨雌二醇对丙酸睾酮诱导去势大鼠前列腺增生的作用。方法建立丙酸睾酮诱导去势大鼠前列腺增生模型,连续皮下注射苯甲酸雌二醇(2.5 mg/kg)4周后处死动物,分离前列腺,测量前列腺体积和湿质量,计算前列腺指数。结果与丙酸睾酮组相比,雌二醇组大鼠前列腺体积、前列腺湿质量和前列腺指数无明显改变(P均>0.05)。结论雌二醇不能抑制丙酸睾酮诱导去势大鼠前列腺增生。     

沙美特罗替卡松粉吸入剂治疗咳嗽变异型哮喘43例临床观察

目的：观察沙美特罗替卡松粉吸入剂治疗咳嗽变异型哮喘（CVA）的临床疗效和安全性。方法：将85例符合诊断的咳嗽变异型哮喘患者,随机分为治疗组43例,对照组42例。治疗组予以沙美特罗替卡松粉吸入剂,每日2次,早晚各吸入1次;对照组予以班布特罗胶囊10 mg晚服,布地耐德干粉吸入剂每日600μg吸入。两组均4周为1疗程,治疗2-3疗程,观察并记录治疗前后临床的症状、体征变化及不良反应。结果：治疗组患者临床症状及疗效明显改善,与对照组比较有显著性差异（P〈0.05）。结论：沙美特罗替卡松粉吸入对咳嗽变异型哮喘病人临床症状缓解及降低气道高反应性疗效肯定,值得临床推广应用。     

米非司酮配伍不同药物用于中期引产临床效果研究分析

目的研究分析米非司酮配伍米索前列醇加注丙酸睾丸酮疗法应用于中期引产的临床效果。方法把病例随机分成实验组A、B及对照组C,实验组A对中期妊娠采用米非司酮配伍米索前列醇加注丙酸睾丸酮引产,实验组B对中期妊娠采用米非司酮配伍米索前列醇加注丙酸睾丸酮和中药方剂引产,对照组C米非司酮配伍米索前列醇引产,每组各160例,观察其引产效果,胎盘胎膜残留情况,胎儿胎盘排出时间及出血量、一个月后随访情况。结果实验组A、B各项指标均显著优于对照组。结论米非司酮配伍米索前列醇加注丙酸睾丸酮应用于中期引产效果显著优于不加注丙酸睾丸酮的引产效果,而与是否再加用中药方剂无差异显著性。