아세트아미노펜 액상좌제의 물리화학적 특성에 미치는 첨가제의 영향

• 영문명: Effect of Additives on the Physicochemical Properties of Acetaminophen Liquid Suppository
• 발행기관: 대한약학회
• 저자명: 최한곤(Han Gon Choi) 정재희(Jae Hee Jung) 유제만(Jei Man Ryu) 이미경(Mi Kyung Lee) 김인숙(In Sook Kim) 이범진(Beom Jin Lee) 김종국(Chong Kook Kim)
• 간행물 정보: 『약학회지』제42권 제3호 (1998년), 290~295쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.06.30

영문 초록

To optimize the formulation of acetaminophen liquid suppository, the effect of additives on the physicochemical properties of liquid suppository base was investigated. The physicochemical properties of P 407/P 188 (15/15%) (abbreviated in 15/15) and P 407/P l88 (15/20%) (abbreviated in 15/20) were measured after the addition of following additives; 2.5% acetaminophen as an active ingredient, vehicle components (5% ethanol, 5% propylene glycol, 5% glycerin), preservatives (0.1% sodium benzoate, 0,1% methylparahydroxybenzoate, 0.1% propylparahydroxybenzoate) and 1% of sodium chloride as an ionic strength controlling agent. Poloxamer gel was prepared with three different buffer solutions (pH 1.2, 4.0 and 6.8) and the physicochemical properties, gelation temperature, gel strength and bioadhesive force, were determined. In the results, the effect of additives on the physicochemical properties was dependent on their bonding capacities including hydrogen bonding and cross-linking bonding. Because the hydrogen-bonding capacities of acetaminophen, ethanol and propylene glycol were smaller than that of poloxamer, the binding force of poloxamer gel became weak by their putting in between poloxamer gel. Therefore, the gelation temperature (15/15, 35.7oC vs 37.0, 39.4 38.2oC; 15/20, 29.2oC vs 31.2, 32.0, 30.3 oC) increased, and gel strength (15/15, 4.03 see vs 2.72, 2.08, 3.12sec; 15/20, 300g vs 50, 50, 200g) and bioadhesive force (15/15, 6.8 X 102 dyne/cm2 vs 3.2, 6.0, 6.0 X 102 dyne/cm2; 15/20, 97.3 X 102 dyne/cm vs 11.1, 89.5, 92.0 X 102 dyne/cm2) decreased. Furthermore, the binding force of poloxamer gel became strong due to the hydrogen-bonding capacities of glycerin and the cross-liking bonding of sodium salt. Then, the gelation temperature (15/15, 35.0, 32.1oC; 15/20, 26.0, 21.0oC) decreased, and gel strength (15/15, 6.51 see, 300g; 15/20, 500, 650g) and bioadhesive force (15/15, 7.2, 81.6 X 102 dyne/cm2; 15/20, 112.3, 309.2 X 102 dyne/cm2) increased. The effect of pH on the physicochemical properties of poloxamer gel was dependent on the ingredients with which the buffer solutions were prepared. Poloxamer gels prepared with pH 1.2 and 4.0 buffer solutions had the increasing gelation temperature (15/15, 37.5, 38.1oC; 15/20, 33.1, 34.0oC) and the decreasing gel strength (15/15, 2.98, 3.81sec; 15/20, 200, 200g) and bioadhesive force (15/15, 7.0 X 102dyne/cm2; 15/20, 74.0-88.1 X 102dyne/cm2) owing to HCl. Poloxamer gel prepared with pH 6.8 buffer solutions had the decreasing gelation temperature (15/15, 27.2oC; 15/20, 22.3oC) and the increasing gel strength (15/15, 400g; 15/20, 550g) and bioadhesive force (15/15, 207.0 X 102dyne/cm2; 15/20, 215.0 X 102dyne/cm2) due to the cross-linking bonding of NaH2PO4 and K2HPO4.

키워드

Acetaminophen Liquid suppository Gelation temperature Gel strength Bioadhesive force.