不同氢溴酸右美沙芬口服固体制剂的溶出度考察

目的：对6个厂家不同氢溴酸右美沙芬口服固体制剂进行体外溶出度考察，比较体外溶出情况，为临床用药提供参考。方法：采用转篮法，转速100 r·min^-1，用高效液相色谱法测定氢溴酸右美沙芬口服固体制剂在0.1 mol·L^-1盐酸溶液中的溶出曲线；以威布尔方程拟合溶出参数T₅₀、T_d、m，并对参数进行方差分析。结果：氢溴酸右美沙普通片、分散片、胶囊以及软胶囊的平均累积溶出度分别为94.3%、101.3%、105.2%、93.4%。溶出参数T₅₀、T_d差异较大，其中T₅₀最大的是最小的13.4倍。结论：氢溴酸右美沙片、分散片、胶囊以及软胶囊体外溶出行为差别大，产品质量存在较大差异。     

反相高效液相色谱法测定血浆中氢溴酸右美沙芬浓度

本文报道采用反相高效液相色谱法测定人血浆中氢溴酸右美沙芬的浓度。采用ＹＷＧ－Ｃ１８Ｈ３７分析柱，以乙腈－水－乙酸（５０：４９：１，三乙胺调节ｐＨ至４．３）为流动相，利多卡因作内标，在２７８ｎｍ波长处监测洗提液。本法简便，灵敏，专属性好，适用于氢溴酸右美沙芬血药浓度测定及药代动力学研究 。     

Memory Deficits in Aged Cebus Monkeys and Facilitation With Central Cholinomimetics

Cebus monkeys of 3 different age groups were trained to perform an automated behavioral task (delayed response), intended to measure recent memory ability. In in initial study, the aged monkeys (18 years and older) exhibit prprogressively greater performance impairments (relative to young monkeys) as they were required to remember the location of a visual stimulus for increasingly longer durations (0 to 20 sec). This deficits replicated previously published results from aged Rhesus monkeys and appeared similar to the primary memory deficits reported in elderly humans and demented patients. In subsequent studies, the effects of three different cholinomimetics were evaluated for their ability to improve the aged monkey's performance on this task. Each monkey was tested under several acute doses of the cholinergic precursor, choline, the anticholinesterase, physostigmine, and the cholinergic muscarinic receptor agonist, arecoline. The results revealed clear differences in the ability of these drugs to improve performance on this task. Choline exerted no apparent effects in the aged monkeys at any dose tested. Physostigmine clearly enhanced performance in certain aged monkeys, but the optimal dose varied dramatically between subjects, replicating previously published results with aged Rhesus monkeys and humans. Arecoline produced clear improvement within a restricted dose range, with little variation in optimal dose between subjects. In addition to demonstrating differences in the effects of different cholinomimetics on memory performance in aged primates, these data also suggest a possible rationale for future investigations. Assuming that each of these drugs primarily affected cholinergic function in the manner conventionally attributed, these data suggest that, within the cholinergic system, the more directly one stimulates the receptor, the more one might expect robust and consistent effects on memory performance in aged subjects.     

高效液相色谱法测定氢溴酸樟柳碱含量

目的：建立了高效液相色谱法测定氢溴酸樟柳碱的含量。方法：采用ＯＤＳ柱,以０．２％十二烷基硫酸钠的甲醇－０．０１ｍｏｌ．Ｌ^-1磷酸二拚钾（用磷酸调节ｐＨ为３．５（ ６０：４０）为流动相,对羟基苯甲酸丁酯为内标物,用紫外检测器于２１０ｎｍ波长处检测。结果：氢溴酸樟柳碱进样量在０．５～３μｇ范围内有良好线笥关系（ｒ＝０．９９９９）。平均回收率为９９．５％,ＲＳＤ为２．６％（ｎ＝３）。最低检出量为０．００６     

Noradrenergic influences on catalepsy

Widespread depletion of forebrain noradrenaline, produced by the intracerebral injection of 4 g of 6-hydroxydopamine into the fibres of the dorsal noradrenergic bundle, potentiated the catalepsy induced by 20 mg/kg of morphine and severely attenuated the catalepsy induced by two separate cholinergic agonists, arecoline and pilocarpine. It did not, however, affect haloperidol catalepsy at any of the four doses tested. These results suggest that cholinergic catalepsy may be critically dependent on an intact noradrenergic substrate, perhaps through cholinergic receptors located either presynaptically on noradrenergic terminals or on the cell bodies of origin in the locus coeruleus. Noradrenaline appears to play a modulatory role in morphine catalepsy, although other sites of action must also be involved. Ascending noradrenergic systems do not appear to influence haloperidol catalepsy.     

氢溴酸右美沙芬片健康人体生物等效性

目的 :研究氢溴酸右美沙芬片在健康人体的药动学及相对生物利用度。方法 :8名健康受试者单剂量随机交叉口服氢溴酸右美沙芬片参比制剂和被试制剂 6 0mg ,采用HPLC法测定用药后不同时间的血药浓度。结果 :2种制剂的体内过程均符合一房室开放模型 ,参比制剂和被试制剂的tmax分别为 (2 72± 0 2 1)h和 (2 74± 0 19)h ,cmax分别为 (5 5 1± 0 4 4) μg·L-1和(5 5 8± 0 2 7) μg·L-1,AUC分别为 (4 5 3± 2 9) μg·h·L-1和 (4 5 7± 3 0 ) μg·h·L-1,被试制剂的相对生物利用度为 (10 1±5 9) %。结论 :2种制剂具有生物等效性。     

HPLC法测定氢溴酸加兰他敏分散片的含量

目的 :建立氢溴酸加兰他敏及其分散片的HPLC分析方法。方法 :采用ODS色谱柱 (15 0mm× 4 .6mm ,5 μm) ,以甲醇 水 冰醋酸 (75∶92 5∶10 )为流动相 ;流速 :1.0ml·min-1,检测波长 :2 89nm ;采用外标法测定氢溴酸加兰他敏分散片的含量。结果 :氢溴酸加兰他敏在 10～ 10 0 μg·ml-1范围内 ,线性关系良好 (r =0 .9998) ;平均回收率为 10 0 .2 % ;日内精密度(RSD =0 .6 % ,n =5 )良好。结论 :本法适用于氢溴酸加兰他敏及其分散片的含量测定 ,方法简便、准确、快速。     

复方制剂珮夫人小儿咳露中主药成分的含量测定

目的 :建立一种采用高效液相色谱检测复方制剂中氢溴酸美沙芬、愈创木酚甘油醚和马来酸氯苯那敏含量的方法。方法 :采用C1 8色谱柱 ,以 0 .0 0 2 5mol·L- 1 IPR -B6 甲醇溶液∶水 (含 2 %三乙胺 )∶磷酸 (12 0∶10 0∶1)为流动相 ,检测波长为 2 5 7nm。结果 :氢溴酸美沙芬、愈创木酚甘油醚和马来酸氯苯那敏 3种成分的回收率分别为10 0 .5 % ,99.5 % ,10 0 .6% ;RSD分别为 2 .2 % ,1.6% ,1.9% (n =7)。结论 :本方法简便 ,结果准确可靠     

氢溴酸高乌甲素氯化钠注射液细菌内毒素的鲎试验研究

目的:探讨氢溴酸高乌甲素氯化钠注射液进行细菌内毒素检查的可行性.方法:采用凝胶法鲎试验对样品中的细菌内毒素进行检测.结果:6批氢溴酸高乌甲素氯化钠注射液及其2倍稀释液对细菌内毒素检查均无干扰作用;所测样品的细菌内毒素含量均<0.5EU·mL-1 .结论:可建立氢溴酸高乌甲素氯化钠注射液的细菌内毒素检查法,日常细菌内毒素检查时可将样品稀释2倍以排除其干扰作用.     

愈美分散片的HPLC测定

建立了HPLC法测定愈美分散片中愈创木酚甘油醚和氢溴酸右美沙芬的含量.采用ODS柱,流动相为乙腈-甲醇-0.01%三乙胺溶液(18:15:67,pH3.5),流速1.0ml/min,检测波长276nm.愈创木酚甘油醚和氢溴酸右美沙芬的线性范围分别为6～72μg/ml和4.2～51μg/ml,平均回收率分别为99.0%和102.6%,RSD分别为1.2%和1.5%.