황체호르몬 유리호르몬의 경점막 수송: 가토 점막균질액 중에서 중쇄지방산염의 LHRH에 대한 안정화 효과

• 영문명: Transmucosal Delivery of Luteinizing Hormone-Releasing Hormone: Effect of Medium Chain Fatty Acid Salts on Stabilization of LHRH in Mucosal Homogenates in vitro.
• 발행기관: 대한약학회
• 저자명: 한건(Kun Han) 박정숙(Jeong Sook Park)
• 간행물 정보: 『약학회지』제38권 제1호 (1994년), 67~77쪽, 전체 11쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1994.02.28

영문 초록

In order to investigate the feasibility of transmucosal delivery of the model peptide, LHRH, metabolism of LHRH and inhibition effect of medium chain fatty acid salts were studied in rabbit mucosal homogenate. LHRH incubated in homogenates of rectal(RE), nasal(NA) and vaginal(VA) mucosa were assayed by HPLC. Five to six degradation products of LHRH were detected and the degradation of LHRH(500mcg/ml) followed the first order kinetics. The main degradation products were found as LHRH1-5(M-I), LHRH1-3(M-II) and LHRH1-6(M-III) by the method of amino acid analysis. The half-lives of LHRH in the mucosal homogenates were found to be less than 20 min at protein concentration of 2.5mg/ml with the order of VA>NA>RE mucosal homogenate. Medium chain fatty acid salts such as sodium caprylate (C8), sodium caprate (C10) and sodium laurate (C12) at the concentration of 0.5%-1.O% inhibit the proteolysis of LHRH significantly. The addition of sodium laurate(O.5%) into the NA and VA mucosal homogenates protected LHRH completely from the degradation.

키워드

LHRH mucosal homogenate proteolysis medium chain fatty acid salts inhibition.