依那普利制剂体外溶出度对比研究

目的:以进口片剂为对照,对三种国产马来酸依那普利制剂溶出度进行对比研究.方法:采用高效液相色谱法测定依那普利浓度,参照USP(ⅩⅩⅢ)溶出度测定Ⅱ法进行溶出度试验. 结果:三种国产制剂30min累积溶出百分率分别为85.2%、101.9%和26.3%,经统计学检验有显著性差异.进口片剂30min累积溶出百分率为100.6%,国产制剂中仅有一种片剂30min 累积溶出百分率与之相当.结论:国内生产的马来酸依那普利制剂,其质量参差不齐,某些产品体外溶出与进口片剂相比存在较大差距.     

依那普利制剂体外溶出度对比研究

目的:以进口片剂为对照,对三种国产马来酸依那普利制剂溶出度进行对比研究.方法:采用高效液相色谱法测定依那普利浓度,参照USP(ⅩⅩⅢ)溶出度测定Ⅱ法进行溶出度试验. 结果:三种国产制剂30min累积溶出百分率分别为85.2%、101.9%和26.3%,经统计学检验有显著性差异.进口片剂30min累积溶出百分率为100.6%,国产制剂中仅有一种片剂30min 累积溶出百分率与之相当.结论:国内生产的马来酸依那普利制剂,其质量参差不齐,某些产品体外溶出与进口片剂相比存在较大差距.     

美洛昔康片的工艺研究与质量控制

目的制备美洛昔康片,并测定美洛昔康片的含量和溶出度。方法采用正交试验法,以溶出度作为指标,对处方中碱化剂、黏合剂和崩解剂进行筛选,采用紫外分光光度法测定美洛昔康片的含量和溶出度。结果美洛昔康片的最佳处方是每片含柠檬酸钠20mg,聚维酮K30 18mg,交联聚维酮12mg。美洛昔康线测定性范围为1.96~19.6μg.mL-1,回收率为99.84%,RSD为0.81%。自制片溶出度能在45min内能达到75%以上,与对照片莫比克相比,两者溶出相似。结论美洛昔康片工艺可行,且质量稳定。     

不同厂家奈韦拉平片的溶出度对比研究

目的 考察国产奈韦拉平片与进口制剂的体外溶出度情况,并比较其体外溶出相似性.方法 分别考察各厂家奈韦拉平片在pH 2.0磷酸盐缓冲液中的溶出度,并比较了国产奈韦拉平片与进口制剂分别在pH 1.2盐酸水溶液、pH 2.0磷酸盐缓冲液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液4种介质中溶出行为相似性.结果 各厂家奈韦拉平片在pH 2.0磷酸盐缓冲液60min时溶出度均高于75%;有3个厂家的奈韦拉平片在4种溶出介质中的溶出曲线与进口制剂相似.结论不同厂家生产的奈韦拉平片溶出行为有显著差异,可能会影响药物在体内的生物利用度.     

国产与进口尼莫地平片的溶出度考察

目的:考察国产与进口尼莫地平片的溶出度,为控制国产制剂质量提供依据。方法:参考2005年版《中国药典》相关标准,利用光纤药物溶出度实时测定仪绘制实时溶出曲线,对国产(B、C、D、E)与进口(A)5厂家共5批次尼莫地平片进行考察。结果:5厂家尼莫地平片30min时的溶出度均符合2005年版《中国药典》的规定,其平均累积溶出百分率均在89以上;但溶出速率明显不同,在6min时A、B、C、D、E5厂家产品平均累积溶出百分率分别为29.22、46.83、55.10、71.84、45.72。结论:国产与进口尼莫地平片的溶出过程存在差异,国产厂家应积极改进现有工艺,严格控制药物的溶出速率。     

不同厂家布洛芬混悬液的溶出度对比研究

摘 要 目的：比较国产布洛芬混悬液和进口制剂的溶出曲线相似性,为全面评价布洛芬混悬液的质量提供依据。方法: 分别考察各厂家布洛芬混悬液在pH 7.2磷酸盐缓冲液中的溶出度,并比较国内3个厂家布洛芬混悬液与进口制剂分别在pH 1.2盐酸溶液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液、pH 7.2磷酸盐缓冲液和水5种溶出介质中溶出行为相似性。结果: 各厂家布洛芬混悬液在pH 7.2磷酸盐缓冲液60 min时溶出度均达到80%以上;3个厂家的布洛芬混悬液溶出曲线与进口制剂溶出曲线相比较,有两个厂家的制剂与进口制剂相似性达到要求。结论:不同厂家生产的布洛芬混悬液,其溶出行为有明显差异。     

美洛昔康片剂与胶囊剂溶出度的比较

目的　测定 5个不同厂家的美洛昔康片剂与胶囊剂的溶出度 ,考察产品质量。方法　采用紫外分光光度法测定美洛昔康片剂与胶囊剂的溶出度。结果　 5个不同厂家的美洛昔康片剂及胶囊剂 4 5min内均溶出 70 %以上 ,溶出度参数T50 、Td、T80 、m及溶出速率常数Kr均存在显著性差异 (P <0 0 1)。结论　不同厂家产品的内在质量存在差异 ,提示临床用药时应加以注意     

醒脑静不同口服固体制剂的溶出度对比研究

目的:对醒脑静不同口服固体制剂进行溶出度考察,对比其有效成分的体外溶出特点,为优选醒脑静口服剂型提供依据。方法:采用小杯法,转速100r·min-1,以蒸馏水为溶出介质。采用高效液相色谱法测定不同口服固体制剂中有效成分栀子苷和龙脑的溶出度,计算累积溶出度,用相似因子进行释放曲线的相似性比较,对溶出曲线进行多种数学模型拟合。结果:不同口服固体制剂中,除水溶性包衣片和胶囊中栀子苷溶出曲线有一定相似性外,各制剂中栀子苷溶出曲线、龙脑溶出曲线均有较大差异,各剂型有效成分溶出曲线基本符合一级动力学方程。结论:醒脑静不同口服固体制剂中有效成分溶出度15min之内均可达到90%以上;栀子苷在胶囊中溶出最快,龙脑在水溶性包衣片中溶出最快。     

美洛昔康胶囊溶出度的测定

目的　测定美洛昔康胶囊的溶出度。方法　采用浆法测定溶出度 ,以pH 7.6的磷酸缓冲溶液作溶出介质 ,转速为10 0r·min-1。结果　 4 5min时溶出度均大于 70 % ,线性范围 2～ 16 μg·ml-1(r=0 .9999) ,平均回收率为 99.88% ,RSD =1.5 7%。结论　所用方法简便、准确、重复性好     

尼美舒利不同口服制剂溶出度比较

目的比较尼美舒利口腔崩解片与其他口服制剂的溶出度。方法采用转篮法和紫外分光光度法。结果4种制剂均可在规定时间达到溶出度的要求,但B片初始溶出缓慢。结论尼美舒利口腔崩解片溶出较好,崩解迅速。     

Investigation of preparation parameters to improve the dissolution of poorly water-soluble meloxicam

The rate of dissolution of drugs remains one of the most challenging aspects in formulation development of poorly water-soluble drugs. The meloxicam, a low molecular analgetic for oral administration, exhibits a slow dissolution. To improve the dissolution rate, the drug was formulated in a nanosuspension by using an emulsion–diffusion method, high-pressure homogenization or sonication. Optimization of the technological parameters (organic solvents, stabilizers, homogenization procedure and recovery of particles) allowed the formation of nanosuspensions with a particle size of 200–900 nm. SEM imaging confirmed the nanosized drug particles. Use of an SMCR method on the XRPD patterns of the nanosuspensions revealed the crystalline form of the drug and the strong interaction between meloxicam and the stabilizer. The rate of dissolution of the dried meloxicam nanosuspension was enhanced (90% in 5 min), relative to that of raw meloxicam (15% in 5 min), mainly due to the formation of nanosized particles. These results indicate the suitability of formulation procedure for preparation of nanosized poorly water-soluble drug with significantly improved in vitro dissolution rate, and thus possibly enhance fast onset of therapeutic drug effect.     

Development and Validation of a Dissolution Test for Meloxicam and Pridinol Mesylate from Combined Tablet Formulation

The association of meloxicam and pridinol is indicated for treating muscular contractures and low back pain. A dissolution test for the meloxicam-pridinol combined tablet formulation was developed and validated, using a suitable HPLC method for simultaneously quantitating both dissolved drugs. The optimized conditions include the use of USP apparatus 2 at a paddle rotation rate of 75 rpm and 900 ml of 50 mM phosphate buffer (pH= 7.5) as dissolution medium, at 37.0±0.5°. The test, which demonstrated to be robust against small changes in bath temperature, paddle rotation speed and pH of the dissolution medium, was applied to two different brands of tablets; the corresponding dissolution profiles were constructed and both brands showed to dissolve at least 75% of the drugs at the 45 min time point.     

Improved absorption of meloxicam via salt formation with ethanolamines.

The present study aimed to investigate the effect of ethanolamine salt formation on the dissolution as well as in vivo pharmacokinetics of meloxicam. Three meloxicam-ethanolamine salts were prepared and their in vitro dissolution profiles were examined at pH 1.2 and 6.8. The pharmacokinetic profiles of meloxicam following an oral administration of meloxicam or its ethanolamine salts were also evaluated in rats. The dissolution rates of meloxicam and its ethanolamine salts were similarly slow at pH 1.2, however, at pH 6.8, ethanolamine salt formation significantly enhanced the dissolution rate of meloxicam. Meloxicam diethanolamine salt exhibited the highest dissolution rate at pH 6.8. The faster dissolution of meloxicam via ethanolamine salt formation at pH 6.8 appeared to be correlated well with more rapid absorption of meloxicam in rats. Tmax of meloxicam was significantly (p<0.05) shortened following an oral administration of ethanolamine salts. Furthermore, ethanolamine salts exhibited a trend toward the increase in AUC0-4 (initial exposure), while the overall exposure (AUC0-24) was similar between meloxicam and its salts. In conclusion, the ethanolamine salts of meloxicam, particularly diethanolamine salt of meloxicam, facilitated the rapid absorption of meloxicam while maintaining the prolonged exposure and may be used for the earlier onset of action for meloxicam.     

美洛昔康片剂溶出度测定方法的研究

目的：建立完善美洛昔康片的溶出度测定方法。方法：按要求根据中华人民共和国药典1995年版二部附录XC第二法测定溶出度。结果：美洛昔康片在30min时，累积溶出接近平衡，累计溶出量在90％以上，回收率101．8％，RSD为0．6％。结论：该方法简便，可靠，可用于美洛昔康片的溶出度测定。     

自制与进口盐酸左西替利嗪片溶出度比较

目的评价自制与进口盐酸左西替利嗪片体外溶出行为的相似性。方法依据2010年版《中华人民共和国药典(二部)》标准和参照日本《医疗用药品品质情报集》中的溶出度试验条件,采用紫外分光光度法,分别以水、0.1 mol/L的盐酸、pH=4.0的醋酸盐缓冲液、pH=6.8的磷酸盐缓冲液为溶出介质进行测定,溶出方法为桨法,转速为50 r/min,并通过f2相似因子法评价自制与进口盐酸左西替利嗪片溶出曲线的相似性。结果 3个批号的自制片在不同溶出介质中30 min溶出度均大于90%,与进口片的相似因子大于50%。结论自制片与进口片的溶出曲线相似,提示该试验药品处方合理,生产工艺稳定可靠。     

Pharmacokinetics of meloxicam administered as regular and fast dissolving formulations to the rat: Influence of gastrointestinal dysfunction on the relative bioavailability of two formulations

It is believed that acute pain suppresses nervus vagus, thereby, influencing gastrointestinal secretion and motility, which are the two factors that are necessary for disintegration and dissolution of solid dosage forms. We studied the pharmacokinetics of meloxicam and the effect of vagal suppression on the oral bioavailability and bioequivalence using a marketed (Brand) and a fast dissolving (FD) formulation. In simulated gastric juice, FD was disintegrated in 30 s and released 30% of its meloxicam in 15 min and 60% in 2 h. Brand was disintegrated in 4.5 min with a dissolution rate of 5.6% in 30 min that stayed plateau for the 2 h experiment time. To suppress the vagus nerve, intraperitoneal injection of 20 mg/kg propantheline 1 and 2 h before meloxicam administration was used. Meloxicam (0.9 mg/kg) was administered to both control and vagally suppressed rats i.v. (n = 4–6/group) as well as orally in a paired random fashion as broken pieces of Brand or FD tablets (n = 7/ group). Serial (0–48 h) blood samples were collected for pharmacokinetic and bioavailability studies. Relative bioavailability was measured according to a method in use for bioequivalence assessments. Systemic pharmacokinetics of meloxicam was not affected by vagal suppression. Absolute bioavailability of meloxicam, based on 0–48 h measurement, was >0.68 regardless of the type of formulation and treatment. Vagal suppression, however, significantly reduced AUC_0–24 (μg h mL⁻¹) for Brand (control, 58.8 ± 22.0 vs treated, 22.1 ± 9.7) but not for FD (control, 63.5 ± 17.9 vs treated, 64.6 ± 8.9) indicating a reduced absorption rate for the former. The peak time for Brand was also significantly delayed by over 20 h for Brand and not for FD. Relative bioavailability was confirmed between FD and Brand that were in control but not in the vagally suppressed rats, indicating a disease-dependent bioequivalence. The effect of vagal suppression on the drug absorption rate can be obviated if the disintegration and dissolution become independent of gastrointestinal motility and secretion.     

4种抗生素治疗非淋菌性尿道(宫颈)炎的成本-效果分析

目的:评价4种口服抗生素治疗非淋菌性尿道(宫颈)炎(NGU)的成本-效果。方法:收集口服国产阿奇霉素与司帕沙星、进口阿奇霉素与司帕沙星治疗NGU的临床资料,进行成本-效果分析。结果:国产阿奇霉素与司帕沙星、进口阿奇霉素与司帕沙星治疗NGU的治愈率分别为89.6%与83.2%、95.5%与88.3%;成本-效果比分别为39与139、140与220。结论:国产与进口阿奇霉素、国产与进口司帕沙星均能有效治疗NGU,但国产阿奇霉素的成本-效果优于国产司帕沙星,进口阿奇霉素的成本-效果亦优于进口司帕沙星。     

布洛芬片剂的溶出度研究

本文对国内外10个厂家的布洛芬片剂进行了体外溶出度测定。各厂布洛芬片在30分钟的溶出度均大于50%,符合美国药典21版规定。但其体外平均溶解时间(MDT)有明显区别。三种国外布洛芬片的MDT分别为5.9,6.2和14.2。国内除山东某厂布洛芬片的MDT为3.5属最低外,多数比国外产品长。本文并对改善布洛芬片溶出度的方法作了初步探讨。     

复方盐酸二甲双胍片溶出度测定方法的研究

目的　考察复方盐酸二甲双胍片体外释放行为,制定合理的溶出度测定条件。方法　(1)以 10 0 0ml水为溶出介质,转速 75rpm,4 5min时取样,采用UV法于 2 33nm的波长处测定。(2 )以 0 0 2 %三(羟甲基)氨基甲烷 2 5 0ml为介质,转速为75rpm时,4 5min取样,采用HPLC法于 2 2 8nm测定格列本脲的溶出度。结果　盐酸二甲双胍的水溶液在 1 6 2～ 8 12 μg·ml-1浓度范围内,吸收度与浓度呈良好的线性关系;平均回收率 99 80 %。格列本脲溶出液在 4 10～ 6 16 μg·ml-1浓度范围内,吸收度与浓度呈良好的线性关系;平均回收率 10 0 16 %。结论　本品溶出迅速,主药在 4 5min内均可完全溶出,且均一性好,达到了很好的体外释放效果