Kaur Gurpreet, Jain Subheet, Tiwary Ashok K
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, India.
Recent Pat Drug Deliv Formul. 2007;1(3):222-9. doi: 10.2174/187221107782331665.
Colon delivery is especially required for drugs intended to act locally or for drugs that exhibit maximum systemic absorption from the colon. However, exposure to extreme pH conditions, gastric enzymes, bile salts and variation in gastric emptying makes the development of colon release dosage forms extremely challenging. The approaches generally used for formulating a colon release dosage form include use of pH dependent release polymers, time-release coatings, prodrugs and biodegradable polymers. Although, considerable choice exists while selecting a pH dependent release polymer, the drug release from these polymers is easily influenced by nature of diet and disease. In addition, while these polymers may prevent drug release in stomach (pH 1-3) and proximal small intestine (pH 6.5), the drug may be prematurely released in vivo in lower small intestine (pH 7.5). Similarly, variation in gastric transit time due to nature of diet and severity of disease often lead to reduced performance of time-release based colon delivery dosage forms. Therefore, new approaches are continuously being evaluated to ensure compliance with requirement of colon release and to reduce the variation in their performance. This article is aimed at studying the recent patents with a view to unveil new concepts being put into use for designing colon release dosage forms.
对于旨在局部起作用的药物或从结肠表现出最大全身吸收的药物,结肠给药尤为必要。然而,暴露于极端的pH条件、胃酶、胆汁盐以及胃排空的变化使得结肠释放剂型的开发极具挑战性。通常用于制备结肠释放剂型的方法包括使用pH依赖性释放聚合物、控释包衣、前体药物和可生物降解聚合物。尽管在选择pH依赖性释放聚合物时有相当多的选择,但这些聚合物的药物释放很容易受到饮食和疾病性质的影响。此外,虽然这些聚合物可能会阻止药物在胃(pH 1 - 3)和近端小肠(pH 6.5)中释放,但药物可能会在体内小肠下部(pH 7.5)过早释放。同样,由于饮食性质和疾病严重程度导致的胃转运时间变化,常常会导致基于控释的结肠给药剂型的性能下降。因此,人们不断评估新的方法,以确保符合结肠释放的要求并减少其性能变化。本文旨在研究近期的专利,以期揭示用于设计结肠释放剂型的新概念。