Zhaopeng H, Kimura G, Yoshikawa Y, Takada K
Department of Pharmaceutics and Pharmacokinetics, Kyoto Pharmaceutical University.
Nihon Rinsho. 1998 Mar;56(3):595-600.
Although many proteins and peptides were produced by gene-technology, their administration routes are limited to be i.v. route. To increase the clinical use of these products, oral dosage form is required. However, in the case of oral administration, proteins are degraded by digestive fluid having strong protease activity. To decrease the protease activity, protease inhibitors are administered concomitantly with proteins. Aprotinin, soybean trypsin inhibitors and gel-forming polymer such as Polycarbophil are representative protease inhibitors. Gel-forming polymers have both protease inhibiting activity and absorption enhancing effect on protein/peptides. The usefulness of these protease inhibitors have been suggested as an additive for the oral delivery of G-CSF and vasopressin derivatives.
尽管许多蛋白质和肽是通过基因技术生产的，但它们的给药途径仅限于静脉注射途径。为了增加这些产品的临床应用，需要口服剂型。然而，在口服给药的情况下，蛋白质会被具有强大蛋白酶活性的消化液降解。为了降低蛋白酶活性，蛋白酶抑制剂与蛋白质同时给药。抑肽酶、大豆胰蛋白酶抑制剂和诸如聚卡波非等凝胶形成聚合物是典型的蛋白酶抑制剂。凝胶形成聚合物对蛋白质/肽既有蛋白酶抑制活性又有吸收增强作用。这些蛋白酶抑制剂作为G-CSF和加压素衍生物口服给药的添加剂的有效性已得到证实。
