利用結腸傳輸系統原理之藥物設計與應用   全文下載

The Design and Application of a Colon-specific Drug Delivery System

目前藥物在結腸傳輸系統之設計主要應用於結腸部位疾病之治療，另外也有藉結腸傳輸系統原理設計全身性作用藥物之劑型；不過此部份之研究成果尚未實際應用於臨床治療。藥物利用結腸傳輸系統原理設計依其所使用之介質、處方劑型設計不同，開發出不同種類的藥物；而這些藥物大多應用於與結腸部位有關疾病之治療。其中大部分與腸道用磺胺藥物 Sulphasalazine (SASP)之開發有密切關係。少部份係應用於其他藥物例如類固醇、非類固醇抗炎性止痛劑（NSAID）之開發上。另外亦有嘗試利用結腸傳輸系統原理之設計模式改變蛋白質與多胜?藥物之劑型設計。

A major application of colon-specific drug delivery system is one that is focused on treating colonic diseases. Nonetheless, there are some systemic drugs designed for a colon-specific delivery system. The design of a colon-specific drug delivery differs in its matrix, formulations or dosage forms, depending on the drug candidates being considered. Most of the specific designs are associated with the treatment of local colonic diseases. The first example is sulfasalazine(SASP). After oral administration, 70 to 75% of SASP passes unchanged through the small intestine and liberates the active 5-amino salicylic acid(5-ASA) by the reduction of the colon-specific diazo-reductase. Other applications include the colonic-delivering development of steroids or NSAID. For example, in clinical trial budesonide-β-D-glucuronide is more effective than pure budesonide without typical adverse reactions of glucocorticoids. There are also newer designs for proteins and polypeptides with a colon-specific delivery system. Among these designs, insulin-polymer complex constructed with styrene or hydroxyethyl-methacrylate can protect insulin from decomposing of digestive fluids, insulin then released, absorbed, and detected in blood plasma. Though the detail mechanism of the drug-complex releasing is still unknown, it reveals a new administration route other than traditional injective way.