...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>American Journal of Drug Discovery and Development >Formulation and Evaluation of Simvastatin Injectable in situ Implants
【24h】

Formulation and Evaluation of Simvastatin Injectable in situ Implants

机译：辛伐他汀可注射原位植入物的配制与评价

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Simvastatin is anti-hyperlipidemic drug which is used to control elevated cholesterol or hypercholesterolemia. The drug undergoes extensive first pass metabolism and has a t1/2 of 3 h. It has poor bioavailability (about 5%) and high protein binding (>95%).The dosage form currently available is conventional uncoated tablet administered once daily. The objective of the present study was to improve the bioavailability of the drug by formulating an intraperitoneal implant and to sustain the drug release for atleast 15 days. The formulation was prepared by polymer precipitation method. In this method, the polymer drug solution is injected into the aqueous buffer from which the solvent dissipates into buffer and forms a solid implant. The optimized formulations were evaluated for drug content, cumulative percentage drug release, solvent ratio, surface morphology and drug interactions. From our studies, it was observed that the drug entrapment efficiency increased and the burst release decreased with increase in the polymer concentration. We could achieve sustained release of the drug with optimized formulation. The formulation with 20% polymer concentration exhibited moderate burst release and sustained release for 15 days. The in situ implants showed no drug polymer interactions. The SEM configurations showed polymer precipitation and the crosslinking of the polymer. Pharmacokinetic studies performed on rats confirmed sustained drug release up to 15 days. The bioavailability of the drug was also found to be improved and showed a 3 fold increase when compared to control tablets (ZOCOR 10 mg). Hence in addition to our studies, further research and clinical investigations can certainly help in proposing Simvastatin in situ implants as a treatment alternative in hyperlipidemic patients.
机译：辛伐他汀是一种抗高血脂药，用于控制胆固醇升高或高胆固醇血症。该药物经历大量的首过代谢，t1 / 2为3小时。它具有较低的生物利用度（约5％）和高蛋白结合（> 95％）。目前可用的剂型是常规的非包衣片剂，每天一次。本研究的目的是通过配制腹膜内植入物来改善药物的生物利用度，并将药物释放至少维持15天。该制剂通过聚合物沉淀法制备。在这种方法中，将聚合物药物溶液注入水性缓冲液中，溶剂从该水性缓冲液中分散到缓冲液中并形成固体植入物。评价了优化的制剂的药物含量，累积药物释放百分比，溶剂比率，表面形态和药物相互作用。从我们的研究中，观察到随着聚合物浓度的增加，药物的包封效率增加，而突释释放减少。我们可以通过优化配方实现药物的持续释放。聚合物浓度为20％的制剂表现出适度的突释和持续释放15天。原位植入物未显示药物聚合物相互作用。 SEM构型显示出聚合物沉淀和聚合物的交联。对大鼠进行的药代动力学研究证实药物可持续释放长达15天。与对照片剂（ZOCOR 10 mg）相比，还发现该药物的生物利用度得到改善，并显示出3倍的增加。因此，除了我们的研究之外，进一步的研究和临床研究当然可以帮助提出辛伐他汀原位植入物作为高脂血症患者的治疗选择。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号