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1985年在英国利物浦召开的国际专题会上讨论两类口服缓释制剂:骨架片(Matrix tablet)和多粒小丸制剂(Multiparticulate solid dosage systems)的优缺点,肯定了小丸剂具有如下优点。1.小肠是药物吸收的主要部位。多粒小丸剂和片剂在胃肠道经过时间均约为4 h。骨架片常常停留于幽门括约肌处,易产生胃肠道副反应,而多粒剂则可避免此种副反应;2.含刺激性的药物制成多粒小丸剂型尤为有效。作为一种缓释剂型,与片剂相比,多粒制剂具有能使剂量倾泻分散化(Dumping)、胃肠道经过时间较长以及血药浓度个体间差异较小等优点;3.体外试验表
Two major types of oral sustained-release preparations, Matrix tablets and Multiparticulate solid dosage systems, were discussed at an international symposium held in Liverpool, England in 1985, affirming that the pellets have the following advantages. 1. The small intestine is the main site of drug absorption. Multi-particle pellets and tablets in the gastrointestinal tract are about 4 h. Skeleton tablets often stay in the pylorus sphincter, easy to produce gastrointestinal side effects, and more tablets can avoid such side effects; 2. Containing irritating drugs made of multi-particle pellets form is particularly effective. As a sustained-release dosage form, the multiparticulate has the advantages of being able to disperse the dose, dispersing the gastrointestinal tract, and having smaller differences in plasma concentrations than the tablets; 3. In vitro tests table