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首页> 外文学位 >Evaluation of Hakea gibbosa as a sustained-release and mucoadhesive component of buccal tablets.
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Evaluation of Hakea gibbosa as a sustained-release and mucoadhesive component of buccal tablets.

机译：评估作为一种颊片的缓释和粘膜粘附性成分的Hakea gibbosa。

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摘要

Oral administration of peptides and proteins results in poor bioavailability. Parenteral route, on the other hand, needs frequent administration because of short elimination half-life. Sustained buccal delivery represents an attractive alternative mode of delivery. The overall objective of this research project was to evaluate the mucoadhesive and sustained-release properties of the water-soluble gum obtained from Hakea gibbosa (Hakea) in buccal tablets, both in vitro and in vivo, using chlorpheniramine maleate and salmon calcitonin as model therapeutic agents.; Dissolution studies indicated that the direct compression technique was more efficient in sustaining the release of chlorpheniramine maleate than the wet granulation technique. The mechanism of sustained release was more likely due to hindered diffusion of chlorpheniramine maleate through the hydrated Hakea, rather than chemical interaction. The in vitro calcitonin release profiles were sigmoidal in nature and indicated super case-II transport as the primary mechanism of release. Following the application of the mucoadhesive chlorpheniramine maleate and calcitonin buccal tablets, not only were the peak plasma concentrations achieved rapidly, but were also maintained throughout the period of application showing the in vivo efficacy of the Hakea gum to sustain the release of incorporated model drugs. Serum calcium concentrations indicated that biologically active calcitonin was delivered across the rabbit buccal mucosa. The strength of mucoadhesion of the tablets in terms of the force of detachment indicated the excellent mucoadhesive properties of the gum and suggested that the mucoadhesive strength can be modulated by altering either the amount of Hakea per tablet or the force used to apply the tablet. The effect of the Hakea gum on the activity of a model protease enzyme pyroglutamate aminopeptidase was investigated by performing enzyme kinetic studies. The mechanism for the inhibition of the enzyme by Hakea appeared to be a mixed-linear type (non-competitive inhibition).; Thus, the natural gum may be a promising additive not only for its sustained-release and mucoadhesive properties, but also for its ability to retard the enzymatic degradation of therapeutic polypeptides incorporated in dosage forms. The mucoadhesive buccal tablets evaluated represent an improved transbuccal delivery system for both conventional drug substances and peptides.
机译：肽和蛋白质的口服给药导致生物利用度差。另一方面，由于消除半衰期短，肠胃外途径需要频繁给药。持续的颊部分娩代表了一种有吸引力的分娩方式。该研究项目的总体目标是评估从 Hakea gibbosa （Hakea）口腔颊片中获得的水溶性胶的粘膜粘附和缓释特性，两者均在体外>和 in vivo ，使用马来酸氯苯那敏和鲑鱼降钙素作为模型治疗剂。溶出度研究表明，直接压片技术在维持马来酸氯苯那敏释放方面比湿法制粒技术更有效。持续释放的机制更可能是由于马来酸氯苯那敏通过水合Hakea扩散的阻碍，而不是化学相互作用。降钙素的体外释放曲线本质上是S形的，并表明超级病例II转运是释放的主要机制。粘膜粘附性马来酸氯苯那敏和降钙素颊片应用后，不仅峰值血浆浓度迅速达到，而且在整个应用过程中也保持不变，显示出哈卡阿胶维持生命的体内功效。释放纳入模型的药物。血清钙浓度表明，具有生物活性的降钙素通过兔颊粘膜递送。就剥离力而言，片剂的粘膜粘附强度表明了口香糖的优异的粘膜粘附特性​​，并暗示可以通过改变每片Hakea的量或施加片剂的力来调节粘膜粘附强度。通过进行酶动力学研究，研究了哈卡阿胶对模型蛋白酶焦谷氨酸氨基肽酶活性的影响。 Hakea抑制酶的机制似乎是混合线性类型（非竞争性抑制）。因此，天然树胶不仅因为其持续释放和粘膜粘附特性​​，而且由于其能够抑制掺入剂型的治疗性多肽的酶促降解的能力而可能是有前途的添加剂。所评估的粘膜粘附颊片剂代表了针对常规药物和肽的改进的经颊递送系统。

著录项

  • 作者

    Alur, Hemant Hanumant.;

  • 作者单位

    University of Missouri - Kansas City.;

  • 授予单位 University of Missouri - Kansas City.;
  • 学科 Health Sciences Pharmacology.
  • 学位 Ph.D.
  • 年度 2001
  • 页码 159 p.
  • 总页数 159
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药理学;
  • 关键词

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