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首页> 外文学位 >1. Pharmacokinetic modeling and simulations of gastrointestinal transit effects on drug pharmacokinetics from enteric-coated pellet formulations and their applications. 2. Development of crushable enteric-coated formulations. 3. Development of leaky enteric-coated pellets formulations.
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1. Pharmacokinetic modeling and simulations of gastrointestinal transit effects on drug pharmacokinetics from enteric-coated pellet formulations and their applications. 2. Development of crushable enteric-coated formulations. 3. Development of leaky enteric-coated pellets formulations.

机译：1.胃肠道转运对肠溶微丸制剂中药物药代动力学的影响的药代动力学建模和模拟及其应用。 2.开发可压碎的肠溶衣制剂。 3.开发泄漏的肠溶丸剂。

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摘要

Effects of gastrointestinal transit on plasma concentrations of drugs from enteric-coated pellet formulations were demonstrated using pharmacokinetic models describing plasma concentrations of drugs from various enteric-coated pellet formulations. Gastric emptying time, lag time of emptying, and drug release rate from pellets in the small intestine, along with other pharmacokinetic parameters of drugs, were used to construct pharmacokinetic models. The models were then evaluated by comparing simulated plasma concentrations of model drugs from Monte Carlo simulations to observed plasma concentrations of these drugs from the literature. Results showed that the models described plasma concentrations of drugs from enteric-coated pellet formulations very well. Pharmacokinetic models describing plasma concentrations of drug from mixed immediate-release and enteric-coated pellet formulations were also used in simulations of bioequivalence studies. Results from the research are very useful in designing generic products of mixed pellet formulation and in refining or selecting the final product for actual bioequivalence study.; Development of crushable enteric-coated formulations was presented. Nonpareil sugar pellets were spray-loaded with mixed amphetamine salts. Drug-loaded pellets were subsequently spray-coated with enteric polymer, hydrophilic gel-forming polymer, enteric polymer and/or mixture of insoluble polymer and hydrophilic polymer. The resulting pellets were then spray-coated with disintegrant and compressed to form crushable tablets. Dissolution testing of both non-compacted crushable enteric-coated tablets and crushed tablets showed that the intact crushable tablet formulations and the crushed tablet formulations were able to prevent the majority of the drug from being released in a simulated gastric dissolution medium within the first 2 hours.; Concept and formulations of "leaky" enteric-coated pellets were presented. "Leaky enteric-coated pellets" formulation is defined as enteric-coated pellets that allow some of the drug to be released from the formulation in acidic dissolution medium. Different approaches of making leaky enteric-coated pellets using spray-coating techniques were presented. Plasma concentrations of drug from leaky enteric-coated pellet formulations were simulated using computer simulations. The present research was based on the hypothesis that leaky enteric-coated pellets formulations were able to provide sustained-release effect on plasma concentration profiles of drugs that have the absorption window without jeopardizing their bioavailability or with improved bioavailability.
机译：使用描述了各种肠溶丸剂配方药物血浆浓度的药代动力学模型证明了胃肠道转运对肠溶丸剂配方药物血浆浓度的影响。胃排空时间，排空滞后时间，小肠颗粒中药物的释放速率以及药物的其他药代动力学参数均用于构建药代动力学模型。然后通过比较来自蒙特卡洛模拟的模型药物的模拟血浆浓度与文献中观察到的这些药物的血浆浓度来评估模型。结果表明，该模型很好地描述了来自肠溶丸剂的血浆浓度。描述生物等效性研究的模拟中也使用了药动学模型，该药理学模型描述了混合速释和肠溶丸剂的血浆浓度。研究的结果对于设计混合颗粒配方的通用产品以及为实际生物等效性研究精制或选择最终产品非常有用。介绍了可压碎肠溶衣制剂的开发。将非pareil糖丸喷雾混合苯丙胺盐。随后用肠溶性聚合物，形成亲水性凝胶的聚合物，肠溶性聚合物和/或不溶性聚合物和亲水性聚合物的混合物对负载药物的小丸进行喷涂。然后将所得的丸剂用崩解剂喷雾包衣并压制成可压碎的片剂。对非压制的可压碎肠溶片和压制片的溶出度测试表明，完整的可压制片剂和压制片制剂能够防止大多数药物在最初的2小时内在模拟的胃溶媒中释放。;介绍了“渗漏”肠溶丸剂的概念和配方。 “渗漏的肠溶丸剂”制剂定义为允许某些药物在酸性溶出介质中从制剂中释放的肠溶丸剂。提出了使用喷涂技术制备泄漏的肠溶丸剂的不同方法。使用计算机模拟对泄漏的肠溶小丸制剂中药物的血浆浓度进行了模拟。本研究基于以下假设：泄漏的肠溶丸剂可以在不损害其生物利用度或生物利用度的情况下，对具有吸收窗口的药物的血浆浓度曲线提供缓释作用。

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  • 作者

    Watanalumlerd, Prapoch.;

  • 作者单位

    Oregon State University.;

  • 授予单位 Oregon State University.;
  • 学科 Health Sciences Pharmacy.
  • 学位 Ph.D.
  • 年度 2004
  • 页码 256 p.
  • 总页数 256
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药剂学;
  • 关键词

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