The main purpose of the present study was to prepare duloxetine hydrochloride(DXH) entericcoated pellets using different enteric polymers. Three layers(drug-loaded layer, barrier layer,and enteric-coated layer) were a...The main purpose of the present study was to prepare duloxetine hydrochloride(DXH) entericcoated pellets using different enteric polymers. Three layers(drug-loaded layer, barrier layer,and enteric-coated layer) were applied to the inert core pellets, successively. The optimal formulation was manufactured by employing suspension layering method in fluidized bed processor(FBP) with varieties of enteric polymers like Aqoat? AS-LF, Eudragit? L30D55 and HPMCP-HP55. The prepared pellets were measured for physical characterization and the in vitro dissolution profile. Scanning electron microscopy(SEM) was conducted to observe the morphology of pellets, and different kinetic models were applied to analyze the release mechanism of Cymbalta? and home-made pellets. The coating weight gain of enteric-coated layer containing Eudragit? L30D55, Aqoat? AS-LF and HP-55 were determined to be 35%, 26% and 24%, respectively. The similarity factors(f2) of self-made capsules with above polymers and commercially available capsules(Cymbalta?) were above 50 in the dissolution medium of pH 6.8 phosphate buffer solution(PBS). SEM figures showed the smooth surfaces of selfprepared pellets using Eudragit? L30D55 and Aqoat? AS-LF, whereas rough surface was found in the HP-55 pellets at day 0, and an impurity was appearing in the condition of 40 ℃/75% relative humidity for 1 month. In conclusion, the pellets prepared by utilizing Eudragit? L30D55 and Aqoat?AS-LF were the optimal preparations based on the dissolution profile and stability.展开更多
The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques.Centrifugal granulator and fluidizedbed coater were employed to prepare drug-loaded ...The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques.Centrifugal granulator and fluidizedbed coater were employed to prepare drug-loaded pellets and to employ two-layered membrane coating respectively.The prepared pellets were evaluated for physicochemical characterization,subjected to differential scanning calorimetry(DSC)and in vitro release of different pH.Different release models and scanning electron microscopy(SEM)were utilized to analyze the release mechanism of Harnual■ and home-made pellets.By comparing the dissolution profiles,the ratio and coating weight gain of Eudragit■ NE30D and Eudragit■ L30D55 which constitute the inside membrane were identified as 18:1 and 10%-11%.The coating amount of outside membrane containing Eudragit■ L30D55 was determined to be 0.8%.The similarity factors(f_(2))of home-made capsule and commercially available product(Harnual■)were above 50 in different dissolution media.DSC studies confirmed that drug and excipients had good compatibility and SEM photographs showed the similarities and differences of coating surface between Harnual■ and self-made pellets before and after dissolution.According to Ritger-Peppas model,the two dosage form had different release mechanism.展开更多
目的:建立盐酸雷尼替丁胶囊溶出度的测定方法。方法:采用HPLC法测定盐酸雷尼替丁胶囊溶出度,色谱柱为JADE PAK C_(18)(4.6 mm×250 mm, 5μm),流动相为0.1%甲酸的乙腈溶液-5 mmol·L^(-1)甲酸铵溶液(10∶90),柱温为35℃,波长为3...目的:建立盐酸雷尼替丁胶囊溶出度的测定方法。方法:采用HPLC法测定盐酸雷尼替丁胶囊溶出度,色谱柱为JADE PAK C_(18)(4.6 mm×250 mm, 5μm),流动相为0.1%甲酸的乙腈溶液-5 mmol·L^(-1)甲酸铵溶液(10∶90),柱温为35℃,波长为314 nm。结果:雷尼替丁在27.189~203.91μg·mL^(-1)范围内,线性关系良好(r=0.999 8),平均回收率为100.3%,RSD为0.6%(n=9)。测定13家企业158批次样品,其中56批次与参比制剂溶出行为不一致。结论:该方法经方法学验证,可用于盐酸雷尼替丁胶囊的溶出度测定。展开更多
文摘The main purpose of the present study was to prepare duloxetine hydrochloride(DXH) entericcoated pellets using different enteric polymers. Three layers(drug-loaded layer, barrier layer,and enteric-coated layer) were applied to the inert core pellets, successively. The optimal formulation was manufactured by employing suspension layering method in fluidized bed processor(FBP) with varieties of enteric polymers like Aqoat? AS-LF, Eudragit? L30D55 and HPMCP-HP55. The prepared pellets were measured for physical characterization and the in vitro dissolution profile. Scanning electron microscopy(SEM) was conducted to observe the morphology of pellets, and different kinetic models were applied to analyze the release mechanism of Cymbalta? and home-made pellets. The coating weight gain of enteric-coated layer containing Eudragit? L30D55, Aqoat? AS-LF and HP-55 were determined to be 35%, 26% and 24%, respectively. The similarity factors(f2) of self-made capsules with above polymers and commercially available capsules(Cymbalta?) were above 50 in the dissolution medium of pH 6.8 phosphate buffer solution(PBS). SEM figures showed the smooth surfaces of selfprepared pellets using Eudragit? L30D55 and Aqoat? AS-LF, whereas rough surface was found in the HP-55 pellets at day 0, and an impurity was appearing in the condition of 40 ℃/75% relative humidity for 1 month. In conclusion, the pellets prepared by utilizing Eudragit? L30D55 and Aqoat?AS-LF were the optimal preparations based on the dissolution profile and stability.
文摘The aim of the present study was to develop tamsulosin hydrochloride sustained-release pellets using two-layered membrane techniques.Centrifugal granulator and fluidizedbed coater were employed to prepare drug-loaded pellets and to employ two-layered membrane coating respectively.The prepared pellets were evaluated for physicochemical characterization,subjected to differential scanning calorimetry(DSC)and in vitro release of different pH.Different release models and scanning electron microscopy(SEM)were utilized to analyze the release mechanism of Harnual■ and home-made pellets.By comparing the dissolution profiles,the ratio and coating weight gain of Eudragit■ NE30D and Eudragit■ L30D55 which constitute the inside membrane were identified as 18:1 and 10%-11%.The coating amount of outside membrane containing Eudragit■ L30D55 was determined to be 0.8%.The similarity factors(f_(2))of home-made capsule and commercially available product(Harnual■)were above 50 in different dissolution media.DSC studies confirmed that drug and excipients had good compatibility and SEM photographs showed the similarities and differences of coating surface between Harnual■ and self-made pellets before and after dissolution.According to Ritger-Peppas model,the two dosage form had different release mechanism.
文摘目的:建立盐酸雷尼替丁胶囊溶出度的测定方法。方法:采用HPLC法测定盐酸雷尼替丁胶囊溶出度,色谱柱为JADE PAK C_(18)(4.6 mm×250 mm, 5μm),流动相为0.1%甲酸的乙腈溶液-5 mmol·L^(-1)甲酸铵溶液(10∶90),柱温为35℃,波长为314 nm。结果:雷尼替丁在27.189~203.91μg·mL^(-1)范围内,线性关系良好(r=0.999 8),平均回收率为100.3%,RSD为0.6%(n=9)。测定13家企业158批次样品,其中56批次与参比制剂溶出行为不一致。结论:该方法经方法学验证,可用于盐酸雷尼替丁胶囊的溶出度测定。
