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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.  相似文献   

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克拉霉素5种片剂体外溶出度比较   总被引:2,自引:0,他引:2  
目的 :比较 5种克拉霉素片剂体外溶出度。方法 :利用HPLC测定克拉霉素片剂含量 ,按USP2 3版采用转篮法测定克拉霉素片剂在醋酸钠缓冲液中的溶出度。结果 :9min平均累积溶出百分率产品A ,C >D ,E >B。A和C ,E和D差别无显著意义 (P >0 .0 5) ,余存在极显著差异 (P <0 .0 1)。 18min时 ,产品A已基本溶出完全 ,其余产品在 4 5min时仍未完全溶出。 5个厂家生产克拉霉素片剂 4 5min时在醋酸钠缓冲液中的溶出量均大于标示量的70 % ,符合中国药典 1995版的规定。结论 :A厂产品溶出度优于其他产品 ,C厂产品 30min前溶出度优于D ,E ,B。  相似文献   

4.
目的:考察不同药厂亚叶酸钙片的溶出度,评价其内在质量。方法:按中国药典2000版溶出度测定方法,即以水为介质,采用转篮法,检测波长为282nm,用紫外分光光度法测定溶出液的含量,同时对4种来源的片剂进行溶出度比较,计算各时间的累积溶出百分率,并提取溶出参数及方差分析。结果:各片剂在30min时的溶出量均大于75%,威布尔参数T50,Td和m值,除C片与D片间比较P>0.05外,其余两两间比较P均<0.01。结论:采用溶出度测定方法,表明亚叶酸钙片剂间存在显著性差异。  相似文献   

5.
The dissolution behaviour of four commercial and two experimental formulations of frusemide tablets has been investigated using the USP rotating basket apparatus and pH 5.0 buffer at 37 degrees C as the test medium. There is a linear relationship between the percentage dissolution in 30 min and the bioavailability relative to an oral solution of frusemide over the bioavailability range 76-97%. Predicted bioavailabilities differed by no more than 2% from the measured values.  相似文献   

6.
The main objective of this research was to develop an experimental method to apply well-defined flow fields to solid dosage forms, to study the rate process underlying tablet dissolution, and to better understand the role of external hydrodynamic condition on mass transfer rate and film thickness during dissolution. Two drugs models, Theophylline (class 1) and Naproxen (class 2), were selected and formulated into conventional tablets containing 105 mg Theophylline or 300 mg Naproxen using the wet granulation method. Tablets were tested for dissolution using both the basket and paddle methods at different rotational speed of 25, 50, 75, and 100 rpm. In general, the paddle method gave higher dissolution rates than the basket method and as the velocity of rotation was increased, drug release was also increased. Six different paddles and a tablet holder were designed and used to test dissolution rate. The rate of dissolution was dependent on the tablet surface area exposed to the dissolution medium, and on the shape, diameter, and area of the paddles used. Theophylline tablets showed increased mass transfer rate and decreased film thickness as basket rotation speed was increased. At 25 rpm, the mass transfer coefficient was 0.684 x 10(-4) cm/sec and film thickness was 12.003 x 10(-2) cm; at 100 rpm, the mass transfer coefficient was 3.884 x 10(-4) cm/sec and film thickness was 2.114 x 10(-2) cm. Paddle values tested at the same speed showed higher mass transfer coefficient and lower film thickness for Theophylline and Naproxen tablets. P values obtained by modification of the Stokes-Einstein equation showed that diffusion is the rate-limiting step to drug release and not mass transfer. This study demonstrated that hydrodynamic condition, type of dissolution testing used, and design of the paddles have an effect on dissolution rate, mass transfer rate, and the film thickness underlying the dissolution process.  相似文献   

7.
The main objective of this research was to develop an experimental method to apply well‐defined flow fields to solid dosage forms, to study the rate process underlying tablet dissolution, and to better understand the role of external hydrodynamic condition on mass transfer rate and film thickness during dissolution. Two drugs models, Theophylline (class 1) and Naproxen (class 2), were selected and formulated into conventional tablets containing 105 mg Theophylline or 300 mg Naproxen using the wet granulation method. Tablets were tested for dissolution using both the basket and paddle methods at different rotational speed of 25, 50, 75, and 100 rpm. In general, the paddle method gave higher dissolution rates than the basket method and as the velocity of rotation was increased, drug release was also increased. Six different paddles and a tablet holder were designed and used to test dissolution rate. The rate of dissolution was dependent on the tablet surface area exposed to the dissolution medium, and on the shape, diameter, and area of the paddles used. Theophylline tablets showed increased mass transfer rate and decreased film thickness as basket rotation speed was increased. At 25 rpm, the mass transfer coefficient was 0.684 × 10? 4 cm/sec and film thickness was 12.003 × 10? 2 cm; at 100 rpm, the mass transfer coefficient was 3.884 × 10? 4 cm/sec and film thickness was 2.114 × 10? 2 cm. Paddle values tested at the same speed showed higher mass transfer coefficient and lower film thickness for Theophylline and Naproxen tablets. P values obtained by modification of the Stokes‐Einstein equation showed that diffusion is the rate‐limiting step to drug release and not mass transfer. This study demonstrated that hydrodynamic condition, type of dissolution testing used, and design of the paddles have an effect on dissolution rate, mass transfer rate, and the film thickness underlying the dissolution process.  相似文献   

8.
目的:采用计算机模拟技术结合Caco-2细胞模型和溶出度试验,对国产盐酸曲美他嗪生物等效性进行研究。方法:首先基于Caco-2单层细胞膜模型考察盐酸曲美他嗪的渗透性,获得其表观渗透系数Papp;第二步采用HPLC法测定溶出曲线来比较10家国产企业与原研生产的盐酸曲美他嗪片在5种不同pH条件下体外溶出行为的差异;最后采用Gastrol PlusTM软件,导入本试验实测Papp,通过该软件转化为Peff值,建立准确的体外溶出曲线与体内药动学曲线之间的相关性模型,基于该模型预测国产盐酸曲美他嗪片的药动学曲线,对其生物等效性进行体内外相关的研究。HPLC测定法:C18柱,以0.287%无水庚烷磺酸钠-甲醇(55:45)为流动相,检测波长为231 nm,流速1.0 mL·min-1;溶出度方法:分别以0.05 mol·L-1盐酸溶液,pH 1.2、pH 4.0、pH 6.8缓冲盐溶液和水为溶出介质,桨法50 r·min-1,溶出体积900 mL,分别考察片剂在上述5种溶出介质中5,10,5,20,30,45,60,90 min取样的溶出曲线。结果:盐酸曲美他嗪的表观渗透系数Papp值随着药物浓度的增加反而下降,属于中等渗透的药物;不同pH的溶出介质对盐酸曲美他嗪片的溶出行为无区分性;但在每种溶出介质中,国外原研片剂溶出较慢,与国产片剂的溶出行为存在明显差异,多数国产片剂快速溶出;采用Gastrol PlusTM软件从药物在体内具有不同释放速率时的体内吸收情况与通过体外溶出曲线模拟体内吸收情况两个方面进行模拟研究,结果显示现有的国产盐酸曲美他嗪片与原研片剂在体内能够生物等效。结论:尽管国产盐酸曲美他嗪片的体外溶出曲线与原研片剂存在差别,但体内生物等效的可能性极大。Gastrol PlusTM软件能够预测口服固体制剂与原研制剂的生物等效性,可在一致性评价工作中推广应用。  相似文献   

9.
In order to improve the predictability of dissolution testing new apparatuses have been proposed that mimic hydrodynamic and mechanical conditions in the gastrointestinal tract. In this study tested were four different nifedipine extended release (ER) formulations using the paddle apparatus and the reciprocating cylinder as pharmacopoeial test devices as well as two newly developed test apparatuses: the rotating beaker apparatus and the dissolution stress test apparatus. Investigated were Adalat OROS in strengths of 30 and 60 mg, and two hydrophilic matrix formulations: 60 mg nifedipine Coral and Nifedipin Sandoz 40 mg retard. The results demonstrate that the dissolution characteristic of the ER tablets is strongly dependent on the applied test conditions. The dosage form related food effects for Coral 60 mg tablets that were previously observed in human bioequivalence studies could be predicted with the two non-compendial dissolution test devices. The dissolution of Sandoz 40 mg tablets was very sensitive to all applied test conditions. The stable drug delivery characteristics of Adalat OROS observed in numerous in vivo studies was also observed in all of the dissolution tests. In conclusion, the present study shows that besides pH dependency the aspect of the mechanical robustness may be an essential factor affecting the dissolution characteristic of hydrogel matrix formulations.  相似文献   

10.
Torrado JJ 《Die Pharmazie》2003,58(9):636-638
Although most commercial valerian formulations are coated tablets not any comparison study of their drug release profiles has been published so far. The main objective of this work is to establish a drug release test suitable for studying and comparing different valerian tablets. Thus, hydroxyvalerenic and valerenic acid concentrations were assayed by HPLC using a C18 Kromasil (200 x 4.6 mm, 5 microm) column and a mobile phase containing methanol and an orthophosphoric acid solution 0.5% v/v in water at a ratio of 75:25 at a constant flow rate of 1 ml/min. Saturation solubilities for hydroxyvalerenic and valerenic acid at pH 6.8 were 26 +/- 5.1 and 1 +/- 0.6 microg/ml, respectively. Usually for drugs with such low solubility values, their oral absorption and hence bioavailability are limited by their dissolution characteristics. A dissolution test was conducted according to the general method 2 (paddles) of USP 24 using 500 ml buffer medium (pH 6.8) at 50 rpm. Five different formulations were studied and compared: one uncoated tablet formulation and four marketed coated tablets. The uncoated tablet formulation had the fastest release profile, whereas the coated tablets manifested very different release patterns, depending on the type of formulation. Because of these differences in drug release pattern not every tablet formulation may be appropriate for the same clinical indications. Clinical data are required to confirm the correlation between drug release pattern and the therapeutically value of each formulation.  相似文献   

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