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首页> 外文学位 >Assessing the permeability of a potent antipsychotic drug (Risperidone) through human cadaver skin: Effect of permeability enhancers and formulation variables.
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Assessing the permeability of a potent antipsychotic drug (Risperidone) through human cadaver skin: Effect of permeability enhancers and formulation variables.

机译：评估有效的抗精神病药物（利培酮）通过人尸体皮肤的渗透性：渗透性增强剂和制剂变量的影响。

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摘要

The novel approaches of drug delivery are continuously being introduced, which help for minimizing the drug doses and maximizing the biological availability of drug. Transdermal delivery of drug is a very interesting phenomenon as the drug avoids first pass metabolism, therefore the direct entry of drug into the systemic circulation will take place with increased biological availability. The system that release drug at zero order rate, for it frequency of dosing is not much important than the capacity of the system i.e. the quantity of drug for transdermal system. There are very less chances of over or under dosing with transdermal delivery as the result of prolonged preprogrammed delivery of drug at the required therapeutic rate. Such delivery is easily accessible for self medication, and hence it is well acceptable by the patients. Administration and even termination of drug both can be possible whenever desired.;In this study, a transdermal formulation of a potent antipsychotic drug Risperidone was developed and optimized using different gelling agents and permeability enhancers. Risperidone is mainly used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in people with autism. It is available in forms of tablets, orally disintegrating tablets and oral solution. An HPLC method for the drug Risperidone was developed and validated, which was used to carry out the assay of a formulation. In-vitro permeability studies were carried out using modified Franz cells with cellulose membrane as a barrier to optimize the gelling agents and their concentrations. Furthermore, to assess the in-vivo drug release/permeation of the drug the formulation exhibiting optimum drug release was evaluated using human cadaver skin as a barrier. Here, permeability enhancers were incorporated in formulations to analyze the effect of enhancers on the permeability of the drug.;Mass balance and accelerated stability studies of the formulations were carried out including stability assays; viscosity and pH of the formulations were studied.;From the studies it was found that drug permeation depends on the type and concentration of the gelling agents. Incorporation of permeability enhancers creates the physiological changes to the human cadaver skin and it changes the drug permeation. Accelerated stability studies data helped to determine the long term stability of a product. It is concluded that effect of temperature and relative humidity modifies the viscosity and pH of the formulation as well as the change in drug concentration was also altered.
机译：不断地引入新的药物递送方法，这有助于最小化药物剂量并最大化药物的生物利用度。药物的透皮递送是非常有趣的现象，因为药物避免了首过代谢，因此，随着生物利用度的增加，药物将直接进入体循环。以零级速率释放药物的系统，因为它的给药频率并不比系统的容量（即透皮系统的药物量）重要。由于以所需的治疗速率延长了药物的预编程递送，因此透皮给药的过量或不足的机会非常少。这种递送对于自我药物治疗是容易获得的，因此被患者很好地接受。无论何时需要，都可以给药甚至终止药物。在这项研究中，开发了有效的抗精神病药物利培酮的透皮制剂，并使用了不同的胶凝剂和通透性增强剂进行了优化。利培酮主要用于治疗精神分裂症（包括青少年精神分裂症），精神分裂症，与躁郁症有关的躁狂和躁狂状态以及自闭症患者的易怒性。它有片剂，口服崩解片剂和口服溶液形式。开发并验证了利培酮的高效液相色谱方法，该方法用于进行制剂测定。体外渗透性研究是使用改良的Franz细胞和纤维素膜作为屏障进行的，以优化胶凝剂及其浓度。此外，为了评估药物的体内药物释放/渗透，使用人尸体皮肤作为屏障来评估表现出最佳药物释放的制剂。在此，将通透性增强剂掺入制剂中以分析增强剂对药物通透性的影响。进行了制剂的质量平衡和加速稳定性研究，包括稳定性测定；研究了制剂的粘度和pH。从这些研究中发现，药物渗透取决于胶凝剂的类型和浓度。掺入渗透性增强剂会导致人体尸体皮肤发生生理变化，并会改变药物的渗透性。加速的稳定性研究数据有助于确定产品的长期稳定性。结论是温度和相对湿度的影响改变了制剂的粘度和pH，并且药物浓度的变化也被改变。

著录项

  • 作者

    Shah, Jaimin Rajnikant.;

  • 作者单位

    Long Island University, The Brooklyn Center.;

  • 授予单位 Long Island University, The Brooklyn Center.;
  • 学科 Health Sciences Pharmacy.
  • 学位 M.S.
  • 年度 2014
  • 页码 135 p.
  • 总页数 135
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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