更安颗粒成型工艺研究

目的探讨更安颗粒的成型工艺条件。方法以成型性、流动性、吸湿性和制粒情况为指标,筛选各处方加入辅料的种类、配比及最佳成型工艺。结果最佳制粒工艺为浸膏粉与糊精按1∶1混匀,以75%乙醇为润湿剂制软材,湿粒在60℃下干燥,成品的流动性和抗吸湿性好,临界相对湿度为78%。结论筛选出的工艺简便可行,不失为更安颗粒较好的成型工艺。     

分子吸收光度法测定万寿菊中代森锰锌残留量

目的:采用分子吸收光度法测定万寿菊中代森锰锌残留。方法:通过蒸馏和溶液吸收实验装置,氯化亚锡催化,二乙基二硫代氨基甲酸钠分解定量产生二硫化碳气体,通过浓硫酸脱氧脱水,氢氧化钾的甲醇液吸收,用分光光度法在304 nm波长处测定其标准曲线。代森锰锌以平均相对分子质量333计,可通过平均相对分子质量计算出代谢锰锌的含量。结果:万寿菊中添加浓度为10 mg.kg-1和20 mg.kg-1(以二硫化碳计)的回收率(n=5)分别为95.9%和93.2%,RSD分别为4.8%和3.7%;最低检测限为2 mg.kg-1。结论:该方法操作简单,灵敏度高,适合大批量样品的检测。     

The action of cisapride on gastric emptying and the pharmacodynamics and pharmacokinetics of oral diazepam

Summary The effects of the benzamide cisapride (C) (8 mg) i.v. have been compared to placebo (P) in a double blind randomised study. The effects on gastric emptying, the absorption and effects of oral diazepam, and BP and pulse were observed.Cisapride increased the rate of gastric emptying of 500 ml liquid containing diazepam 10 mg (t_1/2 C: 7.4 min, P: 14.9 min). The initial rate of absorption of diazepam contained in the drink was increased by C (AUC 0–1 h C: 328 µg h 1^–1, P: 253 µg h 1^–1, but there was no change in overall bioavailability. This change in diazepam kinetics was associated with a significantly greater impairment in reaction time in the first 45 min after drinking but not in self rated sedation. Cisapride produced a significant tachycardia (e.g. after 10 min C: 82 beats/min, P: 69 beats/min) which probably reflects a peripheral vasodilator action. Cisapride may therefore alter the pharmacokinetics and dynamics of concurrently administered drugs.     

口疳散穴位贴敷的制备工艺及体外透皮吸收研究

目的：考察不同制备工艺,包括药材粉碎方法、黏合剂以及透皮吸收剂对穴位贴敷有效成分透皮吸收的影响。方法：以裸鼠腹部皮肤为体外透皮实验材料,以吴茱萸碱为指标成分,用改良Franz扩散池法建立透皮吸收试验方法,收集穴位贴敷的透皮接受液,用高效液相色谱法测定其吴茱萸碱的含量,计算其累积透皮量、透皮速率和皮肤滞留量。结果：吴茱萸碱可以透过离体皮肤,药材粉末使用超微粉能显著提升吴茱萸碱的累积透皮量（P<0.01）。醋为黏合剂相较于水,其累积透皮量显著增加（P<0.001）;再加入3%氮酮能显著增加吴茱萸碱的累积透皮量（P<0.05）。结论：药材粉末为超微粉,用醋作为黏合剂并加入3%氮酮,所制得的口疳散穴位贴敷透皮吸收效果最佳。     

新型选择性胆固醇吸收抑制剂依泽麦布

依泽麦布为一种新型口服调血脂药物，它能选择性抑制肠道对胆固醇和相关植物甾醇的吸收。单独应用或与他汀类药物合用，均能降低具有冠心病风险患者的血清胆固醇水平。本文主要对其作用机制、药代动力学、临床疗效和安全性进行综述。     

Percutaneous Absorption of Nicardipine and Ketorolac in Rhesus Monkeys

Vehicle effects on the percutaneous absorption of nicardipine base, nicardipine hydrochloride, ketorolac acid, and ketorolac tromethamine were determined using the rhesus monkey as an in vivo model for human skin penetration. Vehicles investigated included blends of propylene glycol, trimethylene glycol, ethanol, Azone, Tween 20, water, and long-chain fatty acids. Formulations were prepared such that the compound dose, application area, and percentage saturation of the compound in the vehicle were held constant. Variations in absorption of the compounds were therefore attributable to vehicle effects. Each formulation was applied to three monkeys for a period of 24 hr using 10 Hill Top Chambers. Plasma samples were taken at appropriate intervals for 36 to 48 hr. The results indicated that trimethylene glycol and Tween 20 did not enhance absorption of the test compounds despite claims by other investigators. Azone and ethanol provided moderate enhancement of both the rate and the extent of absorption, while long-chain fatty acids in combination with propylene glycol significantly enhanced penetration. In general, higher fluxes were observed with the more lipophilic compounds nicardipine base and ketorolac acid as compared to the hydrochloride and tromethamine salts.     

壳聚糖衍生物——N-三甲基壳聚糖的促吸收作用研究进展

目的:探讨壳聚糖衍生物——N-三甲基壳聚糖促吸收作用的研究进展。方法:查阅国内外有关N-三甲基壳聚糖促吸收作用的机制、影响因素及应用的文献,并进行分析、总结。结果:N-三甲基壳聚糖可增加细胞旁路途径的跨膜转运,具有促进药物吸收的作用。结论:N-三甲基壳聚糖有望作为一种有效促吸收剂应用于药物制剂。     

在裸小鼠皮肤上松节油对双氯芬酸钠的渗透动力学研究

目的以双氯芬酸钠为模型药物,研究松节油对药物的透皮吸收促透作用.方法采用氮酮、松节油对皮肤预处理的方法,通过离体裸小鼠皮肤渗透释药实验,不同时间取样,测定接受液中双氯芬酸钠的浓度,计算累积透过量、稳态流量、渗透系数和滞后时间等指标.结果松节油对双氯芬酸钠促透作用较氮酮弱,但其时滞较氮酮短(P<0.05).两种促透剂均减弱双氯芬酸钠的储库效应,其中松节油减弱程度没有氮酮大;两种促透剂对双氯芬酸钠的时滞均有延长,松节油延长更明显(P<0.05).结论松节油对双氯芬酸钠有一定的促透作用.     

Ezetimibe

Ezetimibe is a cholesterol absorption inhibitor that significantly lowers low- density lipoprotein cholesterol (LDL-C), and favourably affects triglyceride and high-density lipoprotein cholesterol blood levels in monotherapy and in combination with statins. Hepatic and extrahepatic (peripheral) cholesterol synthesis are well-known sources of cholesterol found in LDL-C. However, the emergence of ezetimibe has highlighted intestinal cholesterol absorption as an additional, important source of cholesterol in LDL-C, and has better illuminated how genetic factors, dietary content, pharmaceutical agents, and nuclear receptor activation (such as liver X receptors) all influence the relative contribution of these important cholesterol sources to LDL-C. In fact, investigations into ezetimibe have sometimes challenged existing scientific dogma, has prompted reconsideration of older data, and has helped create ‘new’ paradigms in cholesterol metabolism. Thus, ezetimibe's efficacy, excellent tolerability, and safety has not only expanded potential treatment options for dyslipidaemic patients, but also has promoted exploration of new frontiers of lipid research towards a better understanding of cholesterol metabolism.     

氢溴酸高乌甲素大鼠在体胃肠的吸收动力学研究

 目的：考察氢溴酸高乌甲素(LH)在大鼠胃肠道的吸收动力学特征及促进剂对其的吸收促进效果。方法：采用大鼠在体胃肠吸收实验模型,用HPLC法测定循环液中药物的浓度。结果：LH在胃、十二指肠、空肠、回肠、结肠的吸收百分率分别为9.67%,19.61%,11.83%,12.95%,9.51%;不同质量浓度的LH(10～40 mg?L-1)与小肠吸收量呈线性关系,吸收速率常数Ka几乎不变。P-糖蛋白抑制剂维拉帕米可增加药物从小肠的吸收。促进剂对药物在小肠内的吸收促进效果均比较明显,癸酸钠吸收促进效果最好。组织病理学观察结果显示,癸酸钠对小肠黏膜造成的损伤最小。结论：药物在整个胃肠道中的吸收均比较有限,在小肠中的吸收呈一级动力学过程,吸收机制有可能为被动扩散;吸收促进剂癸酸钠吸收促进效果最好,且毒性最小,有望作为药用辅料用于口服制剂中提高LH的生物利用度。