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점막 추출액중 치로트로핀 유리호르몬의 효소적 분해 및 안정화
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  • 점막 추출액중 치로트로핀 유리호르몬의 효소적 분해 및 안정화
저자명
전인구,신동원,Chun. In-Koo,Shin. Dong-Won
간행물명
藥劑學會誌
권/호정보
1997년|27권 2호|pp.99-108 (10 pages)
발행정보
한국약제학회
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정기간행물|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

To evaluate the feasibility of mucosal delivery of thyrotropin releasing hormone (TRH) through various mucosae, enzymatic degradation and stabilization of TRH in the nasal, rectal and duodenal extracts of rabbits were studied. TRH in the extracts was assayed by HPLC and its degradation was found to follow apparent first-order kinetics. The residual concentrations of TRH in the mucosal extracts of nasal, rectal and duodenal segments after 24 hr of incubation were found to be $65.1({pm}1.1),;19.7({pm}2.7)$ and 0%, and in the serosal extracts, $65.6({pm}5.5),;75.2({pm}1.1)$ and $68.7({pm}1.4)%$, respectively. This result suggests that there is a significant difference in the activity of TRH-degrading enzymes among the sites of administration. The inhibition of TRH degradation in the mucosa extracts was kinetically investigated using various additives such as thimerosal, benzalkonium chloride, disodium edetate, ${sigma}-phenanthroline$, dithiothreitol and dithioerythritol, and $IC_{50}$ values of inhibitors were calculated. The results obtained showed that thimerosal (0.5 mM) and benzalkonium chloride (0.141 mM) protected TRH from the enzymatic degradation in all the mucosa extracts more than 95% after 24 hr of incubation.