Stuchlík M, Zák S
Research, Development and Clinical Department, IVAX-CR a.s., Ostravská 29, 747 70 Opava 9, Czech Republic.
Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2001 Dec;145(2):17-26.
With an increasing number of lipophilic drugs under development, homolipids and heterolipids have gained renewed interests as excipients for oral drug delivery systems. Oral administration has many advantages for chronic drug therapy. It is relatively safe, convenient for the patient and allows self administration. This article is not intended to review the broad area of lipid-based vehicle for oral drug delivery comprehensively. The rationale behind choosing lipids materials for pharmaceutical dosage forms and their applications is discussed. It also comments on the methods for monitoring the physicochemical properties of vehicles and formulations and describes a range of pharmacopoeial excipients suitable for these purposes. The excipients selected here are pharmacopoeial in European Pharmacopoeia 4th Ed., United States Pharmacopoeia 24th Ed./National Formulary 19th Ed. and Japanese Pharmacopoeia 13th Ed. or are drafted in Pharmaeuropa and Pharmacopoeial Forum. Widening availability of lipidic excipients with specific characteristics offer flexibility of application with respect to improving the bioavailability of poorly water-soluble drugs and manipulating release profiles.
随着越来越多的亲脂性药物处于研发阶段,同脂质和异脂质作为口服给药系统的辅料重新引起了人们的关注。口服给药对于慢性药物治疗具有诸多优势。它相对安全,对患者方便且允许自我给药。本文并非旨在全面综述基于脂质的口服给药载体这一广泛领域。讨论了选择脂质材料用于药物剂型的基本原理及其应用。还对监测载体和制剂物理化学性质的方法进行了评论,并描述了一系列适用于这些目的的药典辅料。此处所选的辅料在《欧洲药典》第4版、《美国药典》第24版/《国家处方集》第19版和《日本药典》第13版中是药典收载的,或者是在《欧洲制药杂志》和《药典论坛》中起草的。具有特定特性的脂质辅料可用性的拓宽,在提高难溶性药物的生物利用度和控制释放曲线方面提供了应用灵活性。