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。     

Modeling in Frequency Domain Used for Assessment of In Vivo Dissolution Profile

Purpose. To present a model-dependent approach for the assessment of the in vivo drug dissolution profile based on in vitrodata for the multiple unit dosage form, as an alternative to the numerical method proposed in the study by Hayashi et al, Pharm. Res. 12:1333–1337 (1995). Methods. The data for aspirin granules administered to healthy subjects obtained in the above mentioned study were re-evaluated. The subject dissolution system was considered to consist of two subsystems connected in series, i.e. the subsystem describing the gastric-emptying process and the subsystem describing the intestinal dissolution process. The frequency response method was used to model the subject dissolution system. Results. The model in vivodissolution profile of aspirin, assessed as the integral of the model weighting function of the subject dissolution system, was in agreement with the in vivo cumulative absorption profile calculated by the Wagner-Nelson method. Conclusions. Comparison of dynamic properties of the subject dissolution system with the subsystem describing the gastric-emptying process yielded quantitative confirmation of the decisive role of the gastric-emptying process in the in vivodrug dissolution after administration in the multi unit dosage form.     

盐酸吗啡普通片及硫酸吗啡控释片在不同溶剂中溶释过程的对照研究

本文采用紫外分光光度法对国产盐酸吗啡普通片及合资厂产硫酸吗啡控释片于蒸馏水、人工胃液、人工肠液中进行体外溶出度和释放度测定。结果表明，两种片剂的溶释均符合中国药典９５版标准，控释片在人工肠液中溶释参数Ｔ５０、Ｔｄ、ｍ与在蒸馏水及人工胃液中的溶释参数差异具显著性（Ｐ＜０．０１），在人工肠液中的释放过程明显缓慢。     

依西美坦片在不同介质中的溶出特性

目的:考察新药依西美坦片在3种不同介质中的溶出特性,以研究影响其口服吸收速率的主要因素和规律。方法:建立HPLC法检测其制剂含量和溶出液浓度,色谱柱:HypersilC18(150mm×4.6mm,5μm);流动相:甲醇:0.05mol/LKH2PO4溶液(60:40);检测波长:247nm。溶出介质选用水、0.1mol/L盐酸溶液及0.5%十二烷基硫酸钠溶液,采用转篮法,转速100r/min。结果:依西美坦片在水和0.1mol/L盐酸溶液中的溶出较差,在0.5%十二烷基硫酸钠溶液巾溶出迅速完全,60min时在3种介质中的溶出百分率分别为(60.25±3.76)%、(47.57±1.20)%和(82.24±0.96)%。结论:依西美坦片可能主要在肠道溶出,其溶出速率受介质影响大。     

尼莫地平片溶出度的研究

采用转篮法对尼莫地平国产市售片，进口片和自制片在不同介质、不同转速和ＰＨ条件下的溶出度进行测试。结果表明，介质对尼莫地平溶出具有很大的影响，而最佳测定方法是以０．１％的十二烷基硫酸钠水溶液为介质，转速１５０ｒ／ｍｉｎ。     

尼莫地平控释片释放度试验研究

本文研究了尼莫地平控释片的释放度试验方法——转篮法，释放介质为含有２２％异丙醇的０．１ｍｏｌ·Ｌ－１盐酸液；磷酸盐缓冲液（ｐＨ５．８）和ｐＨ７．２的溶液。含量测定方法：紫外分光光度法，在三种介质中尼莫地平分别在１～３０μｇ·ｍｌ－１，１０～５０μｇ·ｍｌ－１和１０～５０μｇ·ｍｌ－１的范围内，浓度与吸收度有较好的线性关系。回归方程分别为Ａ＝０．６１５Ｃ＋０．０２３（ｒ＝０．９９９９）；Ａ＝０．０６１４Ｃ＋０．０１２（ｒ＝０．９９９５）；Ａ＝０．０６１２Ｃ＋０．００８８（ｒ＝０．９９９９）。平均回收率分别为９９．６３％，９９．９８％及１００．７７％，ＲＳＤ（％）分别为１．３４％，１．５９％及１．４１％。本方法的体外释放百分率与体内吸收分数有较好的相关性（ｒ＝０．９９１）。     

UROLITHIASIS IN AUSTRALIAN ABORIGINAL CHILDREN

Thirty-six Australian Aboriginal children with urolithiasis were reviewed. Males dominated the series. The age distribution ranged from 8 months to 12 years and nearly 70% were 2 years or younger. Thirty-five patients had upper tract stones. Ultrasound was diagnostic in 35 patients and was falsely negative in one. Dietary factors, dehydration and recurrent diarrhoea are incriminated in the aetiology, because ammonium urate and oxalate were the main constituents of the stones. Malformations of the urinary tract were rare and known metabolic disorders were not seen. Chemical dissolution of the stones was found to be a safe and effective adjuvant in the management of urate stones.     

复方盐酸伪麻黄碱缓释片的研究

应用反相ＨＰＬＣ法测定血药浓度，对复方盐酸伪麻黄碱缓释片的体外溶出及兔灌服一次的药物动力学进行了研究，并与自制普通片进行对照。结果表明缓释片维持体内有效血药浓度的时间较长，其相对生长利用度为１２２．４８％。体内外显著相关。理论值与实测值基本相符。     

Symptoms, diagnosis and endoscopic management of common bile duct stones

Symptomatic BDS commonly cause significant morbidity and attempt at stone removal should be attempted if possible. Complications of CBDS include biliary colic, jaundice, cholangitis and pancreatitis. Investigations aimed to predict the presence of stones within the bile duct include serum bilirubin, AST, ALP, common bile duct diameter and age as independent predictors of choledocholithiasis. TUS is a sensitive test in detecting bile duct dilatation but the sensitivity is reduced in its ability to detect choledocholithiasis. A NIH consensus statement found that ERC, MRC and EUS were comparable in their sensitivities, specificities and accuracy rates for detection of choledocholithiasis. ERC and stone removal using a balloon or basket is often performed following EST. EBD may be performed if patients have uncorrected coagulopathies but the risk of pancreatitis is higher than for EST (although the risk of bleeding complications is lower for EBD). ML is often required in difficult to remove CBDS and using this device, CBDS can be removed in 90–95% of cases. Other forms of lithotripsy including laser lithotripsy and EHL are confined to specialised centres and the evidence for their use is based on small studies. ESWL may clear stones from the bile duct in up to 93% of patients but frequently ERC and stone fragment removal is required post ESWL. The role of medical therapy in difficult to remove CBDS (or in CBDS in patients with severe co-morbid illness preventing ERC + stone removal) is still currently uncertain due to a lack of large randomised control trials.     

卡马西平片体外溶出度与体内吸收相关性

目的：考察卡马西平（ＣＢＺ）片溶出度与体内吸收的相关性。方法：应用ＺＲＳ－４溶出度仪测定卡马西平片的溶出度。４名男性健康志愿性ｐｏ单剂量２００ｍｇＣＢＺ用ＴＤｘ分析仪测定血药浓度，并按照Ｗａｇｎｅｒ－Ｎｅｌｓｏｎ公式计算药物吸收分数。结果：体外溶出度与体内药物吸收分数的相关系数ｒ＝０．９２６１，体外溶出度与体内药物吸收分数的相关系数ｒ＝０．９９７７。结论：ＣＢＺ片体外溶出度与体内吸收有较好的相关性