尼美舒利颗粒剂的溶出度方法研究

目的 建立尼美舒利颗粒剂溶出度的测定方法.方法 采用浆法,以磷酸缓冲液(pH8.0)为溶出介质;溶出量采用高效液相色谱的方法测定.以Diamond C18柱(250 mm×4.6 mm,5 μm),流动相为0.1%磷酸溶液-甲醇(45∶55),流速为1 mL·min-1,检测波长299 nm.结果 在15 min内不同厂家生产的尼美舒利颗粒剂的溶出度均能达到75%.结论 方法简单,准确可靠,可用于尼美舒利颗粒剂的溶出度测定.     

尼美舒利片溶出度测定方法的研究

目的:建立尼美舒利片溶出度测定方法.方法:以pH8.80磷酸盐缓冲液为溶出介质,采用桨法进行溶出度测定,转速:75 r·min-1,用紫外分光光度法在393 nm波长处测定.结果:尼美舒利在2～30 mg·L-1线性关系良好(r=1.00).结论:测定方法简便、准确度高、可用于尼美舒利片溶出度质量控制.     

尼美舒利胶囊剂的制备和质量控制

目的:制备尼美舒利胶囊剂并建立其质量标准。方法:考察填充剂和润滑剂对尼美舒利胶囊内容物流动性的影响,采用单因素试验优化尼美舒利胶囊剂处方,测定溶出度,进行含量测定的分析方法验证。结果:加入预胶化淀粉(62.7%)和微粉硅胶(4%)制得的尼美舒利胶囊剂囊内容物流动性良好,溶出均一性、溶出重复性,含量测定合格。结论:获得的尼美舒利胶囊剂的处方工艺适合产业化,建立的质量标准能够控制产品质量。     

尼美舒利片在不同介质中的溶出度比较

目的考察尼美舒利普通片剂在3种不同缓冲液(pH9.0)中的溶出度。方法按中国药典1995年版二部溶出度测定第一法,采用三羟甲基氨基甲烷缓冲液(Ⅰ)、硼酸缓冲液(Ⅱ)和硼砂缓冲液(Ⅲ)3种缓冲液作为溶出介质,UV法测定溶出度。结果尼美舒利片在3种介质中的累积溶出百分率差异无显著性(P＞0.05)。结论测定尼美舒利片剂的溶出度时,可采用介质(Ⅱ)、(Ⅲ)替代介质(Ⅰ)。     

尼美舒利干混悬剂溶出度检查方法研究

目的：建立尼美舒利干混悬剂溶出度检查方法。方法：参照中国药典2005年版二部溶出度测定法第二法，以磷酸盐缓冲液（pH8．8）为溶出介质，40min时取样，用紫外-可见分光光度法检测溶出量，检测波长为393nm。结果：尼美舒利在2-20mg·L^-1范围内溶液浓度与吸收值呈良好线性关系（r=0．9999）；平均回收率为99．6％（n=9，RSD为0．51％）；测定溶液在8h内稳定；样品的溶出均一性良好，RSD为3．86％，40min时平均溶出率为88．2％。结论：该方法简便易行、准确可靠，可用于尼美舒利干混悬剂溶出度检查.     

高速搅拌切割制粒法与摇摆式制湿粒法制备尼美舒利片的实验对比研究

以高速搅拌切割制粒法与摇摆式制湿粒法分别制备尼美舒利片,并比较两方法所得颗粒的性质、片剂溶出度、片重差异等。结果表明以高速搅拌切割制粒法制备尼美舒利片,颗粒致密均匀,片剂溶出度平均提高9%,片重差异更易于控制。     

高速搅拌切割制粒法与摇摆式制湿粒法制备尼美舒利片的实验对比研究

以高速搅拌切割制粒法与摇摆式制湿粒法分别制备尼美舒利片,并比较两方法所得颗粒的性质、片剂溶出度、片重差异等。结果表明以高速搅拌切割制粒法制备尼美舒利片,颗粒致密均匀,片剂溶出度平均提高9%,片重差异更易于控制。     

PVP在尼美舒利片中的应用

本文对PVP作为尼美舒利片粘合剂的浓度与溶出度的关系进行了考察。结果表明;PVP作为尼美舒利片粘合剂,其水溶液浓度在6-7%范围尼美舒利片的溶出度均符合规定。     

尼美舒利片溶出度测定方法的研究

目的 建立尼美舒利片的溶出度测定方法。方法 以pH8.80±0.05为溶出介质,采用浆法进行溶出度测定,转速为60 r／ min,温度为(37±0.5)℃,进行累积溶出百分率测定,用紫外分光光度法在392 nm的波长处测定。结果 该方法线性关系良好, 回归方程为:C=22.2239A-0.1124 r=0.9999。结论 测定方法简便,结果准确可靠,可适用于该制剂的溶出度质量控制。     

尼美舒利片溶出度测定方法的研究

目的建立尼美舒利片的溶出度测定方法.方法以pH8.80±0.05为溶出介质,采用浆法进行溶出度测定,转速为60 r/min,温度为(37±0.5) ℃,进行累积溶出百分率测定,用紫外分光光度法在392 nm的波长处测定.结果该方法线性关系良好,回归方程为: C=22.2239A-0.1124 r=0.9999.结论测定方法简便,结果准确可靠,可适用于该制剂的溶出度质量控制.     

Post-marketing survey of nimesulide in the short-term treatment of osteoarthritis

A multicentric trial was carried out to assess the therapeutic efficacy and tolerability of nimesulide in the treatment of patients with osteoarthritis. The trial involved 1600 general practitioners, 80 orthopedists and 88 specialists in internal medicine. A total of 22,938 ambulatory patients was admitted to the trial. Patients were given nimesulide tablets (40%) or granules (60%) from 100 to 400 mg/day for a length of time ranging from 1 to 3 weeks. The treatment was effective in relieving spontaneous pain and morning stiffness. The level of patients with adverse reactions, presumably related to nimesulide and mostly involving the gastro-intestinal tract, was 8%. The results of this study suggest that nimesulide is effective and well tolerated in the short-term treatment of a large number of patients with osteoarthritis.     

尼美舒利颗粒在中国健康人体的生物等效性

目的评价2种国产尼美舒利颗粒在中国健康人体的生物等效性。方法20名健康男性受试者随机交叉单剂量口服试验药物或对照药物,各100 mg。用高效液相色谱法测定血浆中尼美舒利浓度;用DAS 2.1软件计算主要药代动力学参数,并对2种药物进行生物等效性评价。结果试验药物和对照药物的主要药代动力学参数:Cmax分别为(6.67±1.80)和(6.50±1.72)μg.mL-1;Tmax分别为(1.88±0.81)和(2.25±0.66)h;t1/2分别为(2.99±0.72)和(2.70±0.58)h;AUC0-24分别为(33.67±12.16)和(33.93±12.99)μg.h.mL-1。AUC0-24、AUC0-∞、Cmax的90%可信区间分别为86.2%～116.3%,86.6%～116.7%和86.8%～120.7%。试验药物相对于对照药物的生物利用度F为(106.9±40.2)%。结论试验药物和对照药物生物等效。     

塞克硝唑胶囊溶出度测定方法研究

目的 建立塞克硝唑胶囊溶出度测定方法.方法 采用高效液相色谱法(HPLC)测定塞克硝唑胶囊的溶出度.溶出条件为中国药典2005年版溶出度测定法第一法,溶出介质为盐酸溶液(1→1 000).结果 绘制的溶出曲线表明45 min内塞克硝唑胶囊可溶出80%以上,确定的溶出时间为45 min,限度为80%.结论 该法快速准确,...     

市售阿奇霉素固体制剂的溶出行为

目的考察不同制药公司生产的阿奇霉素制剂(片剂、颗粒剂、干混悬剂)的体外溶出度。方法以硫酸溶液(φ=73.5%)为显色剂,用分光光度法测定阿奇霉素溶出度。结果不同制药公司及同一公司生产的不同批号的片剂、干混悬剂的溶出度基本上能达到《中华人民共和国药典》规定标准(即45 min溶出度分别≥80%)。各公司生产的颗粒剂,其溶出度差异显著。结论建议对颗粒剂制定溶出度标准。     

尼美舒利颗粒在健康人体的生物等效性

目的：评价2种国产尼美舒利颗粒在中国健康人体的生物等效性。方法：18名健康男性受试者随机交叉单剂量口服试验制药或参比制剂各200 mg。用高效液相色谱法测定血浆中尼美舒利的浓度;用DAS2.1软件计算主要药动学参数,并对2种药物进行生物等效性评价。结果：试验制药和参比制剂的主要药动学参数：Cmax分别为（9.28±2.05）和（9.41±2.31）μg·ml-1;Tmax分别为（3.50±1.86）和（3.56±1.65）h;T1/2分别为（3.43±0.85）和（3.38±0.68）h;AUC0-24分别为（77.78±18.42）和（81.69±23.50）μg·ml·h-1;AUC（0-∞）分别为（79.07±19.21）和（82.92±24.11）μg·ml·h-1。ln（AUC0-24）、ln（AUC0-∞）、ln（Cmax）的90%可信区间分别为90.7%~107.9%、90.6%~111.2%和90.7%~103.0%。试验制药相对于参比制剂的生物利用度F为（96.7±37.6）%。结论：受试制剂和参比制剂生物等效。     

Evaluation of a new pharmaceutical form of nimesulide for the treatment of influenza

In 39 outpatients suffering from a seasonal epidemic influenza, the antipyretic, analgesic and anti-inflammatory activity of nimesulide granules was compared with that of aspirin + vitamin C granules. The drugs were administered b.i.d., dispensed in one-dose sachets containing either 100 mg of nimesulide or 500 mg aspirin + 300 mg vitamin C. The efficacy of the two treatments was comparable: both drugs brought about a rapid complete recovery in all treated patients. However, nimesulide was better tolerated: only one case of slight gastralgia was recorded in the nimesulide group vs the six cases of side-effects complained of in the aspirin + vitamin C group.     

尼美舒利固体分散体的制备及其性质考察

目的提高尼美舒利释放速率及生物利用度。方法分别以聚乙二醇(PEG)、聚乙烯吡咯烷酮(PVP k30)及泊洛沙姆188为载体,采用熔融法、溶剂法及溶剂-熔融法等制备尼美舒利固体分散体;考察载体类别及载体-药物质量比对释放的影响;配合差示扫描量热(DSC)分析与电子扫描电镜(SEM)观察考察药物在载体中的存在状态。结果尼美舒利以无定型状态存在于固体分散体中,载体类别不同、载体-药物质量比不同,药物的释放度不同。结论将尼美舒利制成固体分散体能显著增加尼美舒利的体外释放度。     

Surfactant effect on the dissolution of sulfanilamide granules

Polysorbate 80 incorporated in sulfanilamide granules was found to depress the dissolution of sulfanilamide. The largest decrease corresponded to the lowest concentration of surfactant used. Sulfanilamide granules formulated with either starch or microcrystalline cellulose also decreased the release of the drug. The effect of starch depressing sulfanilamide dissolution was greater with higher starch content in the granules. However, addition of polysorbate 80 improved the dissolution of sulfanilamide granules containing starch but not those with microcrystalline cellulose. This difference was found to be related to the ability of starch to swell and cause granule disintegration. The inclusion of polysorbate 80 in starch-containing granules produced softer and more densely packed granules which were more responsive to the swelling effect of starch.     

Supercritical antisolvent precipitation of nimesulide: preliminary experiments

The purpose of this preliminary study was to investigate the physico-chemical properties of nimesulide precipitated by continuous supercritical antisolvent (SAS) from different organic solvents like acetone, chloroform and dichloromethane at 40 degrees C and 80, 85 and 88 bar, respectively. Scanning electron microscopy, differential scanning calorimetry, X-Ray diffractometry and in vitro dissolution tests were employed to study how the technological process and the solvent nature would affect the final product. SAS-processed nimesulide particles showed dramatic morphological change in crystalline structure if compared to native nimesulide, resulting in needle and thin rods shaped crystals. The solid state analysis showed that using chloroform or dichloromethane as a solvent the drug solid state remained substantially unchanged, whilst if using acetone the applied method caused a transition from the starting form I to the meta-stable form II. So as to identify which process was responsible for this result, nimesulide was further precipitated from the same solvent by conventional evaporation method (RV-sample). On the basis of this comparison, the solvent was found to be responsible for the re-organization into the different polymorphic form and the potential of the SAS process to produce micronic needle shaped particles, with an enhanced dissolution rate if compared to the to the pure drug, was ascertained. Finally, the stability of the nimesulide form II, checked by DSC analysis, was ruled on over a period of 15 months.     

头孢克洛颗粒及干混悬剂溶出度的研究

目的研究测定头孢克洛颗粒以及干混悬剂溶出度的方法。方法采用浆法,以水为溶出介质,转速为50r/min,紫外-可见分光光度法264nm波长处测定吸光度。结果头孢克洛颗粒和干混悬剂在5min的溶出量均不少于80%。结论方法准确可靠,能满足质量控制要求。