11厂家国产头孢氨苄片的溶出度比较

目的:比较国内11个厂家头孢氨苄片的溶出情况。方法:参照《中国药典》2005年版和日本在"药品品质再评价"拟定流程中对溶出度试验条件的规定,分别考察不同批次头孢氨苄片在水、pH1.2人工胃液、pH4.0醋酸盐缓冲液、pH6.8磷酸盐缓冲液4种溶出介质中的体外溶出度,溶出方法采用转篮法,转速为100r·min-1,测定方法为紫外分光光度法,检测波长为262nm;以其中溶出效果最优的E厂家样品为对照采用相似因子法进行各厂家样品间溶出行为的比较。结果:在上述4种溶出介质中,分别只有4个、3个、5个、8个厂家的样品在45min时累积溶出度在80%以上;多数厂家样品的相似因子结果都远小于50。结论:不同厂家样品的溶出行为不但有显著性差异,且溶出度不符合质量要求。     

六个厂家的氧氟沙星片体外溶出度比较

目的：比较不同厂家氧氟沙星片的体外溶出度.方法：以转篮法测定溶出度,紫外分光光度法测定氧氟沙星含量.结果：六个厂家的氧氟沙星片溶出度均符合《中国药典》对片剂溶出度的要求,但在1,5,10,15,25,45 min的药物累积溶出率径方差分析表明差异有显著性.结论：六个厂家的样品溶出度差异有显著性.     

硝苯地平片的溶出度研究

本文采用来法对国产6个厂家7个批号的硝苯地平片进行了溶出度测定。结果表明：不同厂家及同一厂家不同批号样品的溶出参数（T50、Td、m）有显著性差别。建议对该产品进行溶出度检查，以控制产品质量，保证临床疗效。     

五厂家罗红霉素制剂的溶出度比较

目的：比较不同厂家罗红霉素制剂的溶出度。方法：以对二甲氨基苯甲醛为显色剂，用分光光度法测罗红霉素的含量并用转篮法测罗红霉素的溶出度，计算溶出参数并进行方差分析。结果：B，C，D，E厂的样品均在30min内溶出80%以上，T50分别为5.24,2.28,2.05,0.001min,Td分别为8.56,3.06,2.37,0.05min，A厂样品在1h内未崩解。结论：B、C、D，E厂的样品溶出度无显差异，A厂样品溶出度不合格。     

不同厂家头孢克肟胶囊体外溶出度与含量测定

目的 比较3个常用厂家头孢克肟胶囊的体外溶出度和含量,为临床用药提供参考. 方法 采用转篮法进行体外溶出度实验,对不同厂家的样品溶出参数进行方差分析,以高效液相色谱法对样品进行含量测定. 结果3个厂家头孢克肟胶囊的体外溶出参数（t50、td、m）具有统计学差异（P＜0.05＝.头孢克肟胶囊的含量分别为99.17%,90.47%,98.43%. 结论 不同厂家头孢克肟胶囊的溶出度及含量差异有显著性,临床用药时应加以注意.     

两种条件下实时测定硝苯地平片溶出度研究

目的对比中国药典法与日本橙皮书法条件下硝苯地平片溶出度测定结果,为本品质量控制、溶出度评价提供依据。方法随机取6个市售不同厂家硝苯地平片,采用光纤药物溶出度实时测定仪进行溶出度测定,并将2种条件下测定的结果进行比较分析。结果 6个厂家样品采用中国药典法条件测定的溶出度在60 min时均能达到75%以上,符合中国药典标准规定,但6个厂家样品溶出行为存在差异;采用日本橙皮书法条件测定的溶出度30min时均小于70%,达不到日本橙皮书标准规定,且60 min时均未达到溶出平台。结论硝苯地平片溶出度在2种条件下检测的结果存在显著性差异,6厂家样品质量存在差异,且中国药典法溶出条件比日本橙皮书法宽松。     

4个厂家甲睾酮片体外溶出度的比较

目的建立甲睾酮片溶出度的HPLc测定方法,比较4个厂家甲睾酮片在4种不同溶出介质中的溶出曲线,对全国范围市售的甲睾酮片溶出度质量进行合理分析。方法采用美国FDA推荐的4种溶出介质（水、pH4．5磷酸盐缓冲液、pH6．8磷酸盐缓冲液、pH1．0盐酸溶液）比较4个厂家甲睾酮片的溶出曲线,通过考察在同一种溶出介质中不同厂家样品的溶出曲线,筛选能区分各厂家样品溶出质量优劣的溶出条件;通过比较同一厂家在4种不同溶出介质中的溶出曲线,对各厂家的甲睾酮片的产品质量进行区分,筛选工艺稳定、质量优良、适宜病人服用的产品。设定其中1个厂家（厂家D）的样品作为参考制剂。其余3个厂家的样品作为受试制剂,进行溶出曲线的比较,用AV法考察参考制剂与受试制剂溶出曲线的相似性。结果4个厂家的甲睾酮片均符合《中国药典》（2010版）标准中规定的溶出度要求,但在4种溶出介质中的溶出曲线存在差异,只有厂家D生产的甲睾酮片具有“非pH依赖性”,其余3个厂家的产品（除厂家C的一个批号产品）与之均不相似。结论建立的溶出度测定方法能有效区分不同厂家的甲睾酮片溶出情况,不同厂家的甲睾酮片产品质量有区别,建议临床使用时加以注意。     

不同厂家特非那丁片溶出度考察

:采用高效液相色谱法测定不同厂家生产的特非那丁片溶出度 ,以考察其质量。结果表明 :3个厂家 4个批号样品溶出度存在显著性差异。     

溶出度评价不同厂家拉米夫定片的内在质量

目的:考察不同厂家拉米夫定片体外溶出度曲线,比较不同厂家药品的内在质量,为药品质量控制和临床用药提供参考.方法:采用光纤药物溶出度实时测定仪,测定4个厂家拉米夫定片在水、0.1 mol·L-1盐酸溶液、pH4.0醋酸盐缓冲液和pH6.8磷酸盐缓冲液4种溶出介质中的溶出过程,并对溶出曲线进行了比较分析.结果:原研企业样品均一性良好,国内仿制样品均一性较差.在4种溶出介质中,有2个厂家与原研制剂溶出曲线相似,1个厂家相似性较差.结论:不同pH介质中的实时溶出度可全面反映药物在不同体内环境下的溶出行为,能更有效地评价制剂的内在质量.     

盐酸雷尼替丁胶囊体外溶出度考察

目的 对不同厂家、不同批号的盐酸雷尼替丁胶囊进行溶出度考察.方法 以蒸馏水为溶出介质,采用转篮法对3个厂家4个批号的盐酸雷尼替丁胶囊进行溶出度测定,测得结果用Weibull分布模型提取参数进行方差分析,并采用相似因子法评价不同厂家药品溶出度的相似程度.结果 不同厂家的药品溶出参数存在显著性差异（P＜0.01）;相似因子分析发现不同厂家药品溶出度存在差异,同一厂家不同批号药品溶出度相似.结论 生产单位应对产品进行溶出度检查,并与国内外同类产品进行溶出度比较,以便更好地控制药品质量.     

盐酸胺碘酮固体分散体的制备及溶出度测定

目的制备盐酸胺碘酮固体分散体,测定其体外溶出度,同时与普通胶囊剂的体外溶出度比较。方法以聚乙二醇6000(PEG6000)为载体,溶剂熔融法制备盐酸胺碘酮固体分散体,用紫外分光光度法测定体外溶出度。结果盐酸胺碘酮固体分散体的体外溶出度比普通胶囊剂显著提高。结论成功制备了盐酸胺碘酮固体分散体。     

Is there variability in drug release and physical characteristics of amiodarone chloride from different commercially available tablets? Possible therapeutic implications

Objectives Amiodarone is a low‐solubility, high‐permeability drug with a narrow therapeutic index and reported bioavailability problems associated with switching formulations. The aim of this study was to identify whether there is variability in drug release and physical characteristics of different commercially available amiodarone hydrochloride formulations in Australia. Methods Four available formulations (innovator Cordarone (COR) and generic products G1, G2 and G3) were tested for drug dissolution, content uniformity, hardness, weight variation, friability and disintegration in accordance with the US Pharmacopeia specifications. Key findings The tested formulations exhibited variable dissolution behaviours: G1 and G3 exhibited the fastest dissolution, G2 dissolution was the slowest and Cordarone showed a medium dissolution. After 3 months' exposure to high temperature (40 ± 2°C) and relative humidity (75 ± 5%), the products exhibited a higher degree of disparity, with drug‐release profiles of the generics being markedly different from that of Cordarone. This suggests possible implications on bioequivalence for patients who live in warm/tropical regional areas. Most products met the US Pharmacopeia specifications for drug‐content uniformity and other test physical characteristics. Conclusions The results suggested that variability in drug release profiles in vitro of amiodarone formulations might be a potential indicator of compromised bioavailability, causing possible interference with the therapeutic response of the drug.     

Comparative in vitro and in vivo evaluation of three tablet formulations of amiodarone in healthy subjects

Background and the purpose of the study

The relative in vivo bioavailability and in vitro dissolution studies of three chemically equivalent amiodarone generic products in healthy volunteers was evaluated in three separate occasions. The possibility of a correlation between in vitro and in vivo performances of these tablet formulations was also evaluated.

Methods

The bioequivalence studies were conducted based on a single dose, two-sequence, cross over randomized design. The bioavailability was compared using AUC_0–72, AUC_0–8, C_max and T_max. Similarity factor, dissolution efficiency (DE), and mean dissolution time (MDT) was used to compare the dissolution profiles. Polynomial linear correlation models were tested using either MDT vs mean residence time (MRT) or fraction of the drug dissolved (FRD) vs fraction of the drug absorbed (FRA).

Results

Significant differences were found in the dissolution performances of the tested formulations and therefore they were included in the development of the correlation. The 90% confidence intervals of the log-transformed AUC0-72, AUC_0–8, and C_max of each two formulations in each bioequivalence studies were within the acceptable range of 80–125%. Differences were not observed between the untransformed T_max values. Poor correlation was found between MRT and MDT of the products. A point-to-point correlation which is essential for a reliable correlation was not obtained between pooled FRD and FRA. The dissolution condition which was used for amiodarone tablets failed for formulations which were bioequivalent in vivo and significant difference between the dissolution characteristics of products (f2<50) did not reflect their in vivo properties.

Major conclusions

Bioequivalence studies should be considered as the only acceptable way to ensure the interchangeability and in vivo equivalence of amiodarone generic drug products. The dissolution conditions used of the present study could be used for routine and in-process quality control of amiodarone tablet formulations.     

46批氟康唑胶囊溶出度的评价

目的:对46批氟康唑胶囊溶出过程进行评价.方法:采用篮法,以盐酸溶液(9→1 000)500 ml为溶出介质,转速100r·min-1,采用高效液相色谱法测定溶出曲线,采用f2因子法对其进行评价.结果:从溶出曲线比较来看,部分国产氟康唑胶囊的溶出曲线与进口氟康唑胶囊存在较大差异,仅少数国产产品溶出曲线与进口产品相似.结论:单点溶出度测定方法对质量可控性较差,需加强对药品溶出曲线的评价,确保药品质量的稳定性与均一性,确保用药质量及临床疗效的一致性.     

Beyond-Use Dates Assignment for Pharmaceutical Preparations: Example of Low-Dose Amiodarone Capsules

Background: Beyond-use dates (BUDs) in compounding practice are assigned from stability studies. The United States Pharmacopoeia (USP 42 NF 37) suggested to assign a 6 months BUD for dry oral forms. A new pediatric formula of amiodarone capsules was implemented in our hospital, with 3 dosages (5 mg, 20 mg, and 50 mg). Objective: BUD of these new formulas had to be determined by stability study. Methods: The method for the determination of amiodarone content was validated to be stability indicating, and a stability study was performed. Different excipients commonly used for capsule compounding were compared. Results: We found that, with microcrystalline cellulose as excipient, 50 mg amiodarone capsules were stable for 1 year, whereas 5 mg and 20 mg capsules were not. This difference was studied, and lactose or mannitol were found to be better excipients for 5 mg amiodarone capsules, despite their potential side effects. A potential drug-excipient interaction between microcrystalline cellulose and amiodarone hydrochloride is described. Conclusion: Amiodarone hydrochloride/microcrystalline cellulose capsules have a BUD of 1 month for 5 mg capsules, 6 months for 20 mg, and 1 year for 50 mg.     

高效液相色谱法测定人血清中胺碘酮浓度

目的建立以高效液相色谱法测定人血清中胺碘酮浓度的方法。方法色谱柱为ShimadzuShim-packVP-ODS,流动相为甲醇∶乙腈∶醋酸-醋酸钠缓冲液(80∶10∶10),流速为0.8mL.min-1,紫外检测波长为241nm,内标为枸橼酸他莫昔芬。结果胺碘酮检测浓度在0.4～3.2mg·L-1范围内线性关系良好(r=0.9997),方法回收率为101.4%～109.0%,绝对回收率为79.5%～87.0%,日内和日间RSD<10%。结论本方法快速、专一,可用于人血清中胺碘酮浓度的测定。     

盐酸胺碘酮分析方法进展

本文综述光谱分析、电化学分析和色谱分析测定在制剂和血液中盐酸胺碘酮的含量及其溶出度测定方法的研究进展，引用文献30篇。     

功劳去火片的溶出度考察

目的 :对功劳去火片中的黄芩苷溶出度进行考察 ,为评价和控制药品质量提供依据和参数。方法 :以水为释放介质 ,用高效液相色谱法对功劳去火片的溶出度进行测定和比较。结果 :功劳去火片的T50 为106min～220min ,不同批号样品的溶出参数 (T50、Td、m)有显著性差异 (P<0 01)。结论 :有必要对每批产品进行溶出度检查 ,以保证临床疗效     

盐酸曲美他嗪片仿制药与原研药的体外溶出度一致性评价

目的：比较国内三个厂家盐酸曲美他嗪片与原研药的体外溶出度。方法：以水、pH 1.0盐酸溶液、pH 6.8磷酸盐缓冲液为溶出介质,浆法,转速为50 r·min-1,溶出介质体积为900 mL,采用紫外分光光度法,检测波长232 nm,进行溶出度测定。通过相似因子f2法评价仿制药与原研药溶出曲线的相似性。结果：其中丙厂的仿制药在3种介质中与进口药物的溶出曲线均相似,甲乙两厂的仿制药仅在水中的溶出曲线与原研药相似,但在另两种介质中较原研药溶出更快。结论：三厂家的盐酸曲美他嗪片的溶出度均符合《中国药典》规定,但较多仿制药与原研药的体外溶出行为有差异,需进一步结合生物等效性结果考察仿制药质量。     

An alternative method to the evaluation of similarity factor in dissolution testing

This paper addresses an alternative method to the evaluation of similarity factor f₂ as a criterion for assessment of similarity between two in-vitro dissolution profiles as proposed in the SUPAC-IR Guidance (1995). Diltiazem hydrochloride Sustained-Release (SR) tablets were tested and the following independent-model dissolution parameters were used: t_10% dissolution time, t_25% dissolution time, t_50% dissolution time, mean dissolution time (MDT), dissolution efficiency (DE) at t₁₂₀, and at t₃₆₀. To compare the dissolution profiles, several release models were tested such as Higuchi, zero order, first order, Baker-Lonsdale, Hixson-Crowell, Weibull and Korsmeyer-Peppas. The similarities between two in-vitro dissolution profiles were assessed by pair-wise independent-model procedures such as difference factor (f₁), similarity factor (f₂) and Rescigno index (ξ₁ and ξ₂). The in vitro release kinetics of diltiazem hydrochloride sustained release tablets were evaluated using USP apparatus 2.