PDF(Pubmed)
Abstract：
UNASSIGNED: There is evidence that vaginal cabergoline can help to prevent ovarian hyperstimulation syndrome. Therefore, the vaginal suppository may be a good choice because it can be administered directly into the vagina and has no adverse effects on the stomach. In this regard we developed a cabergoline suppository as an alternative to cabergoline tablets. Design-Expert was used to determine the most suitable concentrations of PEG 6000/400, and Tween 80 to obtain a stable suppository. Specific ratios of PEG6000/400 and Tween 80 were entered as factors, and release, melting time, and hardness were evaluated as responses. In addition, the final formulation was evaluated for weight changes, pH, drug content, degradation time, deformation time, in vitro drug release, DSC analysis, infrared spectroscopy, and stability properties.
UNASSIGNED: The suppositories were all smooth and white. They all had a weight that averaged less than 5 %. The formulations showed a pH between 6 and 6.5. The active ingredient content ranged between 79.666 ± 8.54 % and 99.67 ± 6.55 %. Suppository stiffness was between 2.74 ± 0.04 and 4.20 ± 0.03. The decomposition time of the suppositories varied between 11.25 ± 0.15 to 20.19 ± 0.08 min. The deformation time was between 26.11 ± 0.06 to 38.59 ± 0.47 min. Cabergoline content was released over 45 min from formulations of F10 (∼46 %), F2 (∼64 %), F6 (∼69 %), F4 (∼79 %), F1 (∼88 %), and F7 (∼93 %). However, other formulations released more than 95 % within 45 min.
UNASSIGNED: All variables except melting time significantly affected our responses. In vitro studies have indicated that the optimized cabergoline formula could be an excellent alternative to cabergoline oral formulations.
UNASSIGNED: The suppositories were all smooth and white. They all had a weight that averaged less than 5 %. The formulations showed a pH between 6 and 6.5. The active ingredient content ranged between 79.666 ± 8.54 % and 99.67 ± 6.55 %. Suppository stiffness was between 2.74 ± 0.04 and 4.20 ± 0.03. The decomposition time of the suppositories varied between 11.25 ± 0.15 to 20.19 ± 0.08 min. The deformation time was between 26.11 ± 0.06 to 38.59 ± 0.47 min. Cabergoline content was released over 45 min from formulations of F10 (∼46 %), F2 (∼64 %), F6 (∼69 %), F4 (∼79 %), F1 (∼88 %), and F7 (∼93 %). However, other formulations released more than 95 % within 45 min.
UNASSIGNED: All variables except melting time significantly affected our responses. In vitro studies have indicated that the optimized cabergoline formula could be an excellent alternative to cabergoline oral formulations.
摘要：
■有证据表明阴道卡麦角林可以帮助预防卵巢过度刺激综合征。因此,阴道栓剂可能是一个很好的选择，因为它可以直接进入阴道，对胃没有副作用。在这方面，我们开发了卡麦角林栓剂作为卡麦角林片剂的替代品。使用Design-Expert确定PEG6000/400和吐温80的最合适浓度以获得稳定的栓剂。PEG6000/400和吐温80的具体比率被输入为因子，和释放，熔化时间,和硬度被评估为响应。此外,评估最终配方的重量变化，pH值,药物含量,降解时间,变形时间,体外药物释放，DSC分析,红外光谱,和稳定性。
■栓剂都是光滑和白色的。它们都具有平均小于5%的重量。制剂显示pH在6和6.5之间。活性成分含量介于79.666±8.54%和99.67±6.55%之间。栓剂硬度在2.74±0.04和4.20±0.03之间。栓剂的分解时间在11.25±0.15至20.19±0.08分钟之间变化。变形时间在26.11±0.06至38.59±0.47分钟之间。卡麦角林的含量在45分钟内从F10的配方中释放（〜46％），F2（~64%），F6(~69%)，F4（~79%），F1(~88%)，和F7（~93%）。然而,其他制剂在45分钟内释放超过95％。
■除熔化时间外的所有变量都显着影响我们的响应。体外研究表明，优化的卡麦角林配方可能是卡麦角林口服制剂的极好替代品。
■栓剂都是光滑和白色的。它们都具有平均小于5%的重量。制剂显示pH在6和6.5之间。活性成分含量介于79.666±8.54%和99.67±6.55%之间。栓剂硬度在2.74±0.04和4.20±0.03之间。栓剂的分解时间在11.25±0.15至20.19±0.08分钟之间变化。变形时间在26.11±0.06至38.59±0.47分钟之间。卡麦角林的含量在45分钟内从F10的配方中释放（〜46％），F2（~64%），F6(~69%)，F4（~79%），F1(~88%)，和F7（~93%）。然而,其他制剂在45分钟内释放超过95％。
■除熔化时间外的所有变量都显着影响我们的响应。体外研究表明，优化的卡麦角林配方可能是卡麦角林口服制剂的极好替代品。
