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
Background Tamsulosin hydrochloride can significantly improve benign prostatic hyperplasia （BPH） symptoms after the first dose and achieve long-term efficacy in European and American populations; however, the coresp...Background Tamsulosin hydrochloride can significantly improve benign prostatic hyperplasia （BPH） symptoms after the first dose and achieve long-term efficacy in European and American populations; however, the coresponding studies from China are rarely seen. The purpose of this study was to evaluate the long-term efficacy and safety of tamsulosin hydrochloride 0.2 mg once daily in patients with lower urinary tract symptoms （LUTS） suggestive of BPH in China. Methods Chinese patients with LUTS suggestive of BPH were enrolled in a 4-week placebo run-in period and subsequent 60-week open-label study. Tamsulosin hydrochloride 0.2 mg was administered daily during the period of the study. The efficacy and safety parameters were evaluated at the end of treatment period I （0-12 weeks） and period II （13-60 weeks）. The BPH patients were divided into tamsulosin monotherapy group and combination therapy group which received concomitant medication of finasteride 5 mg once daily after the evaluation at the end of treatment period I. Results A total of 113 patients were recruited to the study. Eighty-two patients received tamsulosin monotherapy and twenty-nine received combination therapy during the treatment period I1. Tamsulosin hydrochloride produced a great improvement in mean maximum urinary flow rate （Qmax） （1.7 ml/s, 3 ml/s） and a significant decrease in mean international prostate symptom score （IPSS） （4.1,6.4） after 12-week and 60-week treatments, respectively. At the end of treatment period II, there were significant improvement in IPSS, quality of life （QOL） score, Qmax and average flow rate （eave） for combination therapy group compared with the treatment period I （all P 〈0.05）. No serious adverse events （SAE） were recorded during the study. Conclusion Long-term tamsulosin hydrochloride therapy is a safe, effective and well-tolerated method for the treatment for LUTS suggestive of BPH in China.展开更多
The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performe...The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.展开更多
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Background Tamsulosin hydrochloride can significantly improve benign prostatic hyperplasia （BPH） symptoms after the first dose and achieve long-term efficacy in European and American populations; however, the coresponding studies from China are rarely seen. The purpose of this study was to evaluate the long-term efficacy and safety of tamsulosin hydrochloride 0.2 mg once daily in patients with lower urinary tract symptoms （LUTS） suggestive of BPH in China. Methods Chinese patients with LUTS suggestive of BPH were enrolled in a 4-week placebo run-in period and subsequent 60-week open-label study. Tamsulosin hydrochloride 0.2 mg was administered daily during the period of the study. The efficacy and safety parameters were evaluated at the end of treatment period I （0-12 weeks） and period II （13-60 weeks）. The BPH patients were divided into tamsulosin monotherapy group and combination therapy group which received concomitant medication of finasteride 5 mg once daily after the evaluation at the end of treatment period I. Results A total of 113 patients were recruited to the study. Eighty-two patients received tamsulosin monotherapy and twenty-nine received combination therapy during the treatment period I1. Tamsulosin hydrochloride produced a great improvement in mean maximum urinary flow rate （Qmax） （1.7 ml/s, 3 ml/s） and a significant decrease in mean international prostate symptom score （IPSS） （4.1,6.4） after 12-week and 60-week treatments, respectively. At the end of treatment period II, there were significant improvement in IPSS, quality of life （QOL） score, Qmax and average flow rate （eave） for combination therapy group compared with the treatment period I （all P 〈0.05）. No serious adverse events （SAE） were recorded during the study. Conclusion Long-term tamsulosin hydrochloride therapy is a safe, effective and well-tolerated method for the treatment for LUTS suggestive of BPH in China.
文摘The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.
