Physiological parameters for oral delivery and in vitro testing.
Physiological parameters for oral delivery and in vitro testing.
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DOI：
10.1021/mp100149j
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发表时间：
2010-10-04
影响因子：
4.9
通讯作者：
Amidon GE
中科院分区：
文献类型：
--
作者：
Mudie DM;Amidon GL;Amidon GE
药物固体口服剂型必须在胃肠道肠液中溶解，才能被吸收并进入体循环。因此，溶出是给药过程的关键部分。药物溶出和吸收的速度和程度取决于活性成分的特性以及剂型的性质。同样重要的是，生理环境的特征，如缓冲液种类、pH值、胆汁盐、胃排空率、肠道运动和流体动力学等，也会显著影响溶解和吸收。虽然自1970年首次引入药典溶出度测试（USP器械1）以来取得了重大进展，但目前的溶出度测试并没有充分利用现有的广泛生理信息。为了质量控制的目的，如果问题是批次间性能的一致性，使用非生理性测试条件，使药物和剂型特性与实际溶出介质和仪器相匹配，可能是合适的。然而，当需要体外-体内相关性时，考虑和利用体内条件的知识是合乎逻辑的。本出版物批判性地回顾了与人类口服药物递送有关的文献。生理学上的相关信息必须作为设计更能代表人体状况的溶出度测试方法和系统的基础。随着体外方法在生理相关性方面的进步，更好的体外-体内相关性将成为可能。反过来，这将导致可用于更有效地设计具有改进和更一致的口服生物性能的剂型的体外系统。
Pharmaceutical solid oral dosage forms must undergo dissolution in the intestinal fluids of the gastrointestinal tract before they can be absorbed and reach the systemic circulation. Therefore, dissolution is a critical part of the drug-delivery process. The rate and extent of drug dissolution and absorption depend on the characteristics of the active ingredient as well as properties of the dosage form. Just as importantly, characteristics of the physiological environment such as buffer species, pH, bile salts, gastric emptying rate, intestinal motility, and hydrodynamics can significantly impact dissolution and absorption. While significant progress has been made since 1970 when the first compendial dissolution test was introduced (USP Apparatus 1), current dissolution testing does not take full advantage of the extensive physiologic information that is available. For quality control purposes, where the question is one of lot-to-lot consistency in performance, using nonphysiologic test conditions that match drug and dosage form properties with practical dissolution media and apparatus may be appropriate. However, where in vitro – in vivo correlations are desired, it is logical to consider and utilize knowledge of the in vivo condition. This publication critically reviews the literature that is relevant to oral human drug delivery. Physiologically relevant information must serve as a basis for the design of dissolution test methods and systems that are more representative of the human condition. As in vitro methods advance in their physiological relevance, better in vitro - in vivo correlations will be possible. This will, in turn, lead to in vitro systems that can be utilized to more effectively design dosage forms that have improved and more consistent oral bioperformance.
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影响因子：
4.5
作者：
Baxter, JL;Kukura, J;Muzzio, FJ
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