감마선 조사법으로 합성한 PVP하이드로겔의 팽윤과 약물방출특성

• 영문명: Swelling and Drug Release Characteristics of PVP Hydrogel Polymerized by gammar-Irradiation Method
• 발행기관: 대한약학회
• 저자명: 심창구(Chang Koo Shim) 오정숙(Chung Sook Oh) 신병철(Byung Chul Shin)
• 간행물 정보: 『약학회지』제37권 제5호 (1993년), 511~519쪽, 전체 9쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1993.10.30

영문 초록

The short and variable transit of drug throught GI tract and the inter-and intra-subject variations of the transit restrict the sustained drug absorption after oral adminstration. These restrictions may be solved by retaining the dosage forms in the stomach. Then the dosage form will act as a platform which releases the drug slowly and makes the GI absorption occur for a long time. In this study, as the platforms, PVP hydrogels were synthesized by chemical and gammar-irradiation method in the cylindrical test tube. The chemical method means the synthesis of the hydrogel by heating the mixed solution of N-vinyl-2-pyrrolidone [monomer], acrylated albumin [crosslinking agent], 2,2''-agobis(2-methylpropionitrile) [initiator] and proxyphylline [drug] at 65oC for 5 hr. The gammar-irradiation method means the synthesis of the hydrogel by irradiation with 60Co gammar-ray of the mixed solution of the monomer, acrylated albumin, and flurbiprofen [drug] at room temperature with total 0.2Mrad for 3 hr. Our intention is to design the hydrogel tablet (diameter : 1.20cm, thickness : 0.60cm) which swells in the gastric fluid after oral administration to such a size that passing through the pylorus could be inhibited during the period of drug release. After releasing drug, the hydrogel should be degraded by the enzymeatic digestion in the stomach, or by hydrolysis and eventually solubilized. Thus, in vitro tests were performed to examine the factors that affect swelling and drug release from the PVP hydrogels. Experimental results show that the hydrogels swell to a size larger than the diameter of the pylorus(1.3 +/- 0.7cm) and the hydrogel prepared by the chemical method is digested by pepsin. But the hydrogel prepared by the gammar-irradiation method was not digested by the pepsin and just collapsed with time. Thus, the swelling of the hydrogel synthesized by gammar-irradiation was independent albumin acrylation time and pepsin concentration. But drug content and radiation dose affected the swelling and drug release kinetics of the hydrogel. Drug release from the hydrigels was prolonged up to about 24 hr. Therefore, it was concluded that by adjusting these factors, the albumin-crosslinked PVP hydrogel synthesized by gammar-irradiation method is expected to be retained in the stomach for up to 60 hr and be a potential platform of drugs for long-term GI absorption.

키워드

Hydrogel PVP swelling release proxyphylline flurbiprofen chemical method y-irradiation method acrylation albumin gastric emptying.