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피막과 팽윤을 이용한 고분자 기질에서의 약물의 조절방출
Controlled Drug Release by Polymeric Matrix Formulation by Coating and Swelling
HWAHAK KONGHAK, August 1989, 27(4), 561-567(7), NONE
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Abstract
약물의 열적 불안정성과 용매와의 반응성을 피하기 위하여 고분자 기질을 팽윤시켜 약물을 봉입하는 방법을 고안하여 고분자 기질로 된 약제를 제조하였다. 고분자 기질은 hydrogel인 p-HEMA로 제조하여 모델약물인 citidine diphosphate coline(중추신경제)의 방출기전을 연구하였다. 또한 고분자사슬에 이온을 갖지 않는 p-HEMA와 음이온을 갖는 polyacrylate에 대한 pH에 따른 약물 방출기전의 차이를 분석하였다. 그 결과 p-HEMA는 팽윤이 일어남으로써 약물 방출곡선에 분계점이 나타났으며 polyacrylate는 음이온을 가짐으로써 pH에 따라 팽윤도가 변하였고 pH가 높을수록 팽윤도와 약물의 방출속도가 증가하였다. HEMA와 methylmethacrylate의 공중합체에 생체분해성 고분자인 polylactide로 코팅 막을 형성한 제형을 제시하였으며 이 시스템에서의 약물 방출기전 및 고분자 기질의 두께에 따른 변화를 고찰하였다. 이 제형은 생체분해성 막이 초기의 약물 방출속도를 억제함으로써 sustained release pattern을 유도하였다.
In order to avoid a thermal instability and a reaction of drug with solvents, a method was devised to load a drug in a polymer matrix by swelling. Using p-HEMA hydrogel as polymer matrix, the release mechanism of a model drug, citidine diphosphate coline(CNS stimulant),was studied. Also analyzed was the difference in the pH-related release mechanism of p-HEMA which has a non-ionic polymer chain and polyacrylate which has negative ions on the polymer side chain. For p-HEMA, ist break-point on the drug release curve occured due to swelling and degree of swelling did not change pH. On the other hand, swelling polyacrylate differed pH:the higher the pH, the higher the degree of swelling and faster the release rate. A formulation with a bioerodible coating membrane of polylactide was in-troduced to the co-polymer of HEMA and methylmethacylate. The difference in the drug release mechanism and changes relative to the polymer thickness in this system was observed. The formulation allows the bioerodible mem-brane to suppress the initial rate of drug release mechanism, which led to the sustained release pattern.