硝苯地平缓释片释放度研究

目的建立硝苯地平缓释片的释放度试验方法，对5个厂家生产的硝苯地平缓释片的含量和释放度进行测定。方法以0．5％吐温-80水溶液（900mL）作为溶出介质，采用桨法测定溶出度，转速为100r／min，温度为（37．0±0．5）℃；用反相高效液相色谱法测定含量，测定波长为333nm。结果用建立的方法可以准确地测定各厂家硝苯地平缓释片的释放度，不同厂家生产的硝苯地平缓释片释放速度差别较大。结论对不同厂家生产的硝苯地平缓释片释放度进行检查，有助于控制产品质量。     

尼莫地平缓释胶囊的释放度与其普通片的溶出度比较

目的　在相同介质中将尼莫地平缓释胶囊的释放度与普通片的溶出度作比较。方法　利用ZRS 8C型药物智能释放仪 ,采用转篮法 ,溶出介质为 0 5 5 %的十二烷基硫酸钠水溶液 ,溶出杯内温度为 ( 37± 0 5 )℃ ,转速为 5 0± 1r/min ,分别在不同的时间点取样 ,在波长为 36 0nm处测定吸收度 ,计算出释放度和溶出度。结果　尼莫地平缓释胶囊在 6 0min的累积释放率为 4 4 17% ,而普通片的累积溶出率达到了 90 91%。结论　尼莫地平缓释胶囊与普通片相比 ,血药浓度明显平稳 ,从而使药效延长 ,达到了提高人体生物利用度的目的     

硫酸沙丁胺醇控释胶囊释放度的HPLC测定

目的　建立HPLC测定硫酸沙丁胺醇控释小丸胶囊释放度的方法。方法　采用腈基键合硅胶柱 (SpherisorbCN 2 5cm× 4.6mm) ;以水 - 0 0 5mol ml醋酸铵 -异丙醇 (30 ∶6 5 ∶5 )为流动相 ;流速为 2ml min ;检测波长为 2 76nm。结果　线性范围为 0 48～19 2 0 μg ml,r=1 0 0 0 ;回收率为 95 3%～ 99 5 % ,RSD <1 31% (n =6 )。 结论　本方法快捷、简便、准确 ,适合于本品释放度的检测     

5-单硝酸异山梨酯控释小丸胶囊释放度的HPLC测定

目的　建立HPLC法测定 5 -单硝酸异山梨酯 (5 -ISMN)控释小丸胶囊的释放度。方法　采用C1 8BDS柱 (4.6×2 50mm ,5μ) ,流动相为甲醇 -水 (1∶ 1 ) ,流速为 1ml/min ,检测波长 2 2 0nm。结果　线性范围为 5～ 1 0 0 μg/ml,方法回收率为99 .0 % ,RSD为 1 .76 % (n =6)。结论　本方法灵敏、简便、快速 ,适用于该制剂释放度检测     

双氯芬酸钠贴片体外释放度测定

目的：建立双氯酚酸钠释放度测定方法。方法：采用0．5％十二烷基硫酸钠为溶出介质．照分光光度法在不同时间点测定样品中双氯酚酸钠的释放度。结果：贴片体外释放度研究表明双氯芬酸钠体外释药随时间为一递增过程,符合Higuchi方程。结论：本方法药物溶出均匀,操作方便,重现性好,适合于双氯芬酸钠贴片释放度测定。     

硫酸吗啡控释片在人工肠液中的释放度考察

为了考察硫酸吗啡控释片 (CRM)在人工肠液中的释放度 ,以推测直肠给药是否安全 ,以水介质为对照用紫外分光光度法考察 CRM在人工肠液中的释放度。结果 CRM在两种不同介质中的累积释放度无差异 (P >0 .0 5 ) ,而所有的释放度参数均有极显著性差异 (P <0 .0 1)。结果表明 CRM在人工肠液中的释放度在不同时间点均有推迟 ,直肠给药有可能蓄积中毒     

黄杨宁缓释胶囊释放度的研究

目的研究自制的黄杨宁缓释胶囊的体外释放度。方法采用酸性染料染色分光光度法测定黄杨宁缓释胶囊的释放度,0．05mol·L^-1的磷酸二氢钠缓冲溶液为释放介质,转速为100r·min^-1。结果平均回收率98．5％,RSD=3．39％,3批样品在1,4,8h的平均累计释放度分别为23．10％,57．39％和85．86％,释放度符合要求。结论自制黄杨宁缓释胶囊有较好的释药性能。本试验建立的释放度测定方法可以作为该制剂的质控方法。     

比色法测定潲丁胺醇包合物缓释片的释放度

目的 :建立沙丁胺醇包合物缓释片释放度的测定方法。方法 :用比色法于波长 (5 0 6± 1)nm处测定释放介质水中沙丁胺醇的浓度。结果 :沙丁胺醇平均回收率为 (10 1.2±1.1) %。结论 :该方法简便、准确、稳定性好 ,可用于沙丁胺醇释放度的测定。     

盐酸二甲双胍缓释片的体外释放特性

目的:考察盐酸二甲双胍缓释片体外释放影响因素,建立其释放度测定方法。方法:采用UV法测定盐酸二甲双胍缓释片在不同溶出递质、不同方法和不同转速的释放度。结果:UV法测定盐酸二甲双胍缓释片释放度线性关系良好,r=0.9999(n=5),线性范围为2~10mg·L-1,回收率和稳定性均良好。药物释放受释放方法和递质的影响。盐酸二甲双胍缓释片体外释放曲线在t=0~12h范围内较符合一级动力学方程。结论:方法简便,结果可靠,可作为盐酸二甲双胍缓释制剂生产过程的质量控制依据。     

高效液相色谱法测定可待敏缓释胶囊的释放度

目的建立测定复方制剂可待敏缓释胶囊释放度的高效液相色谱法。方法按照2010年版《中国药典（二部）》释放度测定法中的第一法,以水900mL为介质,转速为10017／rain,分别在l,4,8h时采样,以高效液相色谱法测定。色谱柱为DiamonsilC18柱（150mm×4．6mm,5μm）;流动相为0．05mol／L磷酸二氢钾,加入0．01％的己烷磺酸钠溶液（离子对试剂）和0．5％三乙胺,用磷酸调pH至6．0,与甲醇以（50：55）的比例配成流动相并调节pH至7．0～7．5;流速为1．0mL／min;检测波长为220nm。结果可待敏缓释胶囊在12h内缓慢释放,在12h时释放较完全。结论该方法简便,结果准确可靠。     

硝酸甘油透皮给药系统体外释药速率测试方法的研究

随着透皮吸收研究的兴起,先后已有东茛菪碱、硝酸甘油、硝酸异山梨醇、可乐定和雌二醇等透皮给药系统进入市场。各生产单位对这些产品都有一定的质量控制项目,主要有药物含量、粘附力及药物释放速率,其中药物的释放速率是一个较重要的质量控制项目。虽然现在上市的透皮给药系统     

Stability of nitroglycerin tablets submitted by U.S. hospitals

The stability of nitroglycerin tablets that had been stored in hospitals across the United States was studied. Through a voluntary FDA drug stability program, all hospital pharmacies in the United States were asked in October 1981 to complete a response card indicating information about nitroglycerin tablets they had in stock. Based on the responses, FDA selected 167 samples (representing three manufacturers and all available tablet strengths) from pharmacies that represented an adequate cross section of the country. The samples were analyzed for content uniformity, strength, identification, and disintegration; samples that left a residue on the screen of the tablet disintegration basket were tested for dissolution by three methods and compared with samples that did not leave a residue. All samples met USP requirements for content uniformity, strength, and disintegration. Six samples that showed unusual disintegration characteristics dissolved slowly by one or more methods; however, other samples also showed slow dissolution. Nitroglycerin tablets appear to be stable when stored under actual marketplace conditions. The USP disintegration test will not distinguish between rapidly and slowly dissolving tablets.     

乌拉地尔、硝酸甘油用于高血压急症院前急救的临床分析

目的观察乌拉地尔、硝酸甘油注射液对高血压急症的临床疗效,并分析其对心率的影响。方法将80例高血压急症患者随机分为乌拉地尔组与硝酸甘油组各40例。乌拉地尔组给予乌拉地尔注射液25mg用0．9％氯化钠注射液20mL稀释,5min内静脉推注,随后用乌拉地尔50mg加入0．9％氯化钠注射液250mL中静脉滴注,初始速度为0．5mL／min（100μg／min）;硝酸甘油组给予硝酸甘油注射液5mg加入0．9％氯化钠注射液250mL中静脉滴注,初始速度为0．5mL／min（10μg／min）。比较两组给药前后血压、心率变化。结果乌拉地尔组、硝酸甘油组均可明显降低高血压急症患者血压．达到治疗目标．两组间疗效比较无明显差异,硝酸甘油组治疗后心率明显增快,不良反应较多。结论乌拉地尔作用迅速、降压平稳．不良反应轻微．是高血压急症院前急救的理想药物。     

Optimization and statistical evaluation of dissolution tests for indinavir sulfate capsules

An optimization, statistically based on t-student test, to set up dissolution test conditions for indinavir sulfate capsules is presented. Three dissolution media, including that reported in United States Pharmacopeial Forum, and two apparatus, paddle and basket, were applied. Two different indinavir sulfate capsules, products A and B, were evaluated. For a reliable statistical analysis eighteen capsules were assayed in each condition based on the combination of dissolution medium and apparatus. All tested media were statistically equivalent (P > 0.05) for both drug products when paddle apparatus was employed at the stirring speed of 50 rpm. The use of basket apparatus at the stirring speed of 50 rpm caused significant decrease in the drug release percent for the product B (P < 0.05). The best dissolution conditions tested, for products A and B, were applied to evaluate capsules dissolution profiles. Twelve dosage units were assayed and dissolution efficiency concept was used, for each condition, to obtain results with statistical significance (P > 0.05). Optimal conditions to carry out the dissolution test were 900 ml of 0.1 M hydrochloric acid as dissolution medium, basket at 100 rpm stirring speed and 260 nm ultraviolet detection.     

不同介质中头孢地尼干混悬剂溶出曲线相似性比较的研究

目的：评价自制头孢地尼干混悬剂与市售原研品头孢地尼胶囊体外溶出行为的相似性,同时为难溶性药物制剂质量判断提供参考.方法：分别考查自制试验制剂头孢地尼干混悬和参比制剂头孢地尼胶囊在纯水、pH 1.2人工胃液、pH 4.0与pH 6.8磷酸盐缓冲液4种溶出介质中的体外溶出行为,以紫外-可见分光光度法进行测定,并采用f2相似因子法评价受试制剂和市售参比制剂溶出曲线的相似性.结果：在4种介质中,自制样品与参比制剂相似因子f2均大于50.结论：在这4种介质中,自制试验制剂与参比制剂溶出行为相似,说明受试制剂的处方工艺合理.     

Release Liner Removal Method For Transdermal Drug Delivery Systems (TDDS)

A release liner removal test is a valuable test for assessing the quality of a transdermal drug delivery system (i.e., TDDS, patch). This test measures the force required to remove the release liner from a patch. The objective of the present study was to establish sample preparation and instrument parameters for measuring release liner removal adhesion for TDDS. Ten TDDS were evaluated (six drugs for a total of 29 lots). Patches which had a ratecontrolling membrane were run as-is, since they could not be cut to a precise width without sacrificing their structural integrity. Patches that were square or rectangular in shape were run as-is, and the width of these patches was determined using a digital caliper. Patches which were not square or rectangular in shape and did not have a rate-controlling membrane were cut to a precise width using a specimen cutter. Double-sided tape was used to adhere the liner side of the transdermal system to a clean stainless steel test panel. A release liner peel adhesion method for TDDS is proposed using a dwell time of approximately 3 min, a peel angle of 90°, and a peel speed of 300 mm/min.     

尼群地平片溶出度测定

目的采用不同方法考察市售尼群地平口服片剂和软胶囊的溶出度 ,并提出尼群地平溶出度检查的标准。方法用含不同浓度的十二烷基硫酸钠 (SDS)醋酸盐缓冲液 (pH 4 5 )为溶出介质 ,采用紫外分光光度法检查 ,比较不同厂家尼群地平片和尼群地平软胶囊的体外溶出度。用相似因子法对片剂溶出度数据进行统计分析。结果用 0 3 %SDS醋酸盐缓冲液 (pH 4 5 ) ,除B片和D片之间的 (B片 D片 )相似因子F2 >5 0外 ,其余的F2 ≤ 5 0 ,可以显示出不同厂家生产的尼群地平片的溶出度差异。而用 0 1 %SDS醋酸盐缓冲液可以显示出尼群地平软胶囊与片剂的溶出度差异。结论不同厂家生产的尼群地平片的溶出度存在较大的差异 ,尼群地平片和软胶囊在溶出度方面整体存在较大差异 ,建议《中华人民共和国药典》规定尼群地平片剂的溶出度检查     

Dissolution test for citalopram in tablets and comparison of in vitro dissolution profiles.

A dissolution test for tablets containing 20 mg of citalopram was developed and validated using a reverse-phase liquid chromatographic method and this dissolution test was applied to compare dissolution profiles. The sink conditions, filters, stability of the drug and specificity on different dissolution media were tested to choose a discriminatory dissolution method which uses USP apparatus 1 with baskets rotating at 50 rpm, 900 ml of deaerated 0.1 M hydrochloric acid (HCl) as the dissolution medium. The quantitation method was also adapted and validated. The parameters of difference factor, similar factor, according to current FDA guidelines, and dissolution efficiency were employed to compare dissolution profiles. The dissolution test developed and validated was adequate for its purposes and could be applied for quality control of citalopram tablets, since there is no monograph to citalopram in tablets, this work can be used to help pharmocopoeias.     

阿齐沙坦片国产品溶出度试验方法的建立及与原研品体外溶出行为比较

目的:建立阿齐沙坦片的溶出度试验方法,并将国产品与原研品进行溶出曲线比较,评价二者体外溶出行为的一致性。方法:筛选各溶出参数,采用紫外-可见分光光度法在246 nm波长处测定吸光度并计算溶出度;分别考察两种产品在pH 6.8磷酸盐缓冲液、pH 4.5醋酸盐缓冲液、0.1 mol/L盐酸、水4种溶出介质中的溶出曲线,采用相似因子f2法与AV值法比较二者的溶出行为。结果:溶出方法采用桨法,转速为50 r/min,溶出介质为pH 6.8磷酸盐缓冲液;阿齐沙坦检测质量浓度线性范围为1.07¹2.80μg/ml(r=0.999 8),平均回收率为99.32%(RSD=0.75%,n=3);在4种溶出介质中,两种产品的f2值均在5012.80μg/ml(r=0.999 8),平均回收率为99.32%(RSD=0.75%,n=3);在4种溶出介质中,两种产品的f2值均在50¹00,AV平均值均小于15,表明二者相似性好。结论:建立的溶出度试验方法专属性强、灵敏、简便,能有效控制阿齐沙坦片的质量;同时国产品与原研品的体外溶出行为一致。