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口腔给药系统在已上市产品中的应用:患者价值和工业考量。

Oral Drug Delivery Systems Applied to Launched Products: Value for the Patients and Industrial Considerations.

机构信息

Pharmaceutical Research and Technology Laboratories, Astellas Pharma Inc, 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.

出版信息

Mol Pharm. 2023 Nov 6;20(11):5312-5331. doi: 10.1021/acs.molpharmaceut.3c00482. Epub 2023 Oct 19.


DOI:10.1021/acs.molpharmaceut.3c00482
PMID:37856863
Abstract

Drug delivery systems (DDS) control the amount, rate, and site of administration of drug substances in the body as well as their release and ADME (absorption, distribution, metabolism, excretion). Among the various types of DDS, amount-controlled DDS for solubilization and absorption increase the bioavailability. Time- and amount-controlled DDS are controlled release formulations classified as (1) membrane-type, (2) matrix-type, (3) osmotic-type, and (4) ion-exchange type. Timed-release formulations also control the time and amount of release and the absorption of drugs. Site- and amount-controlled DDS are characterized by colonic delivery and intestinal lymph-targeting to improve release and ADME of drug substances. Finally, site-, time-, and amount-controlled DDS are gastroretentive formulations and local delivery in the oral cavity to improve site retention, release, and ADME of drugs. DDS can enhance efficacy, reduce adverse effects, and optimize the dosing frequency of various drug products to increase patient value. This review focuses on patient value and industrial considerations of launched oral DDS. We provide a technological overview of candidate and marketed DDS, as well as the pros/cons of the technologies for industrialization with consideration to excipients, manufacturing, and storage stability. Moreover, to demonstrate the usefulness of the technology and support the selection and development of the best technologies for patients, we also describe patient value from clinical studies and analyses, particularly with regard to increased new medical options, higher efficacy, reduced adverse effects, reduced number of doses and clinic visits, easier administration, higher quality of life, greater adherence, and satisfaction.

摘要

药物传递系统(DDS)控制药物在体内的给药量、速率和部位,以及它们的释放和 ADME(吸收、分布、代谢、排泄)。在各种类型的 DDS 中,用于增溶和吸收的控释系统可以提高生物利用度。时间和剂量控制的 DDS 是控释制剂,分为(1)膜型、(2)基质型、(3)渗透型和(4)离子交换型。定时释放制剂还控制药物的释放和吸收的时间和剂量。部位和剂量控制的 DDS 的特点是结肠传递和肠淋巴靶向,以改善药物的释放和 ADME。最后,部位、时间和剂量控制的 DDS 是胃滞留制剂和口腔内局部给药,以提高药物的部位保留、释放和 ADME。DDS 可以提高疗效、减少不良反应,优化各种药物产品的给药频率,从而提高患者的价值。本文重点介绍已上市口服 DDS 的患者价值和工业考虑因素。我们提供了候选和上市 DDS 的技术概述,以及考虑赋形剂、制造和储存稳定性的技术工业化的优缺点。此外,为了展示技术的有用性,并支持为患者选择和开发最佳技术,我们还从临床研究和分析中描述了患者价值,特别是在增加新的医疗选择、提高疗效、减少不良反应、减少剂量和就诊次数、提高给药便利性、提高生活质量、提高依从性和满意度方面。

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