消化道酶类药物剂型研究：乳糖酶复合微囊

研制成功一种在胃和肠液中对酶类药物均具有保护作用的复合微囊剂型。方法是先将酶包埋,制成半透性微囊,再用肠溶材料将半透性微囊包埋。该复合微囊经口服进入肠道后释出半透性微囊,后者允许小分子底物自由通透,被膜内酶作用;而屏蔽肠道蛋白酶。将酵母乳糖酶制成复合微囊后,在人工胃液2h内可保留65％以上的剩余活性;在含胰酶人工肠液中6h内其活性也达60％以上。而游离乳糖酶在同样条件下很快失活。

An Approach to the Preparation of Digestive Enzyme-drug for Oral Administration: Complex Lactase Microcapsules

Complex microcapsules which could protect enzyme drugs from inactivation in both the stomach and intestine were prepared. In the process, semipermeable microcapsules were first formed by enveloping the enzymes within spherical, ul-trathin semipermeable membranes. To resist gastric juice, the semipermeable microcapsules were further encapsulated by enteric-soluble materials to form complex microcapsules. When the preparations were taken into the intestine, the semipermeable microcapsules were released and small molecular substrates could then equilibrate rapidly across the semipermeable membrane to be acted on by the enveloped enzymes, while alimentary proteases remained outside. This complex microca-psulated lactase could retain over 65% of its activity after simulation in gastric juice for 2h, and over 60% of its activity was retained after 6h in pancreatin-containing simulated intestinal juics. On the contrary, unencapsulated lactase lost all activities immediately under the same conditions.