New preparation for oral administration of digestive enzyme. Lactase complex microcapsules.

Abstract

Complex microcapsules which could protect therapeutic enzymes from inactivation in both the stomach and intestine were prepared. Thus, semipermeable microcapsules were first formed by enveloping the enzymes within spherical, ultrathin semipermeable membranes. To resist to the gastric juice, the semipermeable microcapsules were further encapsulated by enteric-soluble materials to form complex microcapsules. When the preparation passes into the intestine, the semipermeable microcapsules are released, thus the small molecules of substrates equilibrate rapidly across the semipermeable membrane to be reacted by the enveloped enzymes, and alimentary proteases remain outside. This complex microencapsulated lactase remained over 65% of its activity after 2 h simulation in gastric juice, and over 65% of its activity was retained after 6 h contact with pancreatin-containing simulated intestinal juice. By contrary, unencapsulated lactase lost immediately all of its activity under similar conditions.