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카페인의 비강 분무액의 제제설계 및 점막 투과 증진
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  • 카페인의 비강 분무액의 제제설계 및 점막 투과 증진
저자명
노은선,전인구,Noh. Eun-Sun,Chun. In-Koo
간행물명
藥劑學會誌
권/호정보
2004년|34권 2호|pp.131-138 (8 pages)
발행정보
한국약제학회
파일정보
정기간행물|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

This study was aimed to investigate the feasibility of nasal delivery of caffeine for the elimination of sleepiness. The effects of various vehicles, solubilizers, and enhancers on the permeation of caffeine through rabbit nasal mucosa was observed. The permeation study was carried out using a Franz-type permeation system at $37^{circ}C$, and the amount of caffeine permeated though the rabbit nasal mucosa was determined by a validated HPLC. The apparent solubility and phys iochemical stability of caffeine in various nasal formulations were was determined. The effect of hydrotropes and modified cyclodextrins on the solubility of caffeine in water was determined by equilibrium solubility method. The solubility of caffeine in water was 29 mg/mL at $30^{circ}C$. The addition of sodium benzoate and nicotinamide at 10% improved the solubility of caffeine (115 and 132 mg/mL, respectively) in aqueous solution. The flux of caffeine though the nasal mucosa from aqueous solution was $2.1{pm}0.26;mg/cm^2/hr$. The addition of sodium benzoate reduced its permeation $(1.4{pm}0.01;mg/cm^2/hr)$, but sodium benzoate with 5% $2HP{eta}CD$ and 0.03% monoterpenes increased its permeation $(2.4{pm}0.04;mg/cm^2/hr)$ markedly. The addition of nicotinamide also increased also increased its permeation $(2.5{pm}0.36;mg/cm^2/hr)$. markedly. As the concentration of caffeine in nasal formulation increased, the permeation flux increased linearly. Caffeine was stable physicochemically and enzymatically in the nasal mucosa extract at $37^{circ}C$. These results suggest that caffeine can be efficiently delivered nasally and the development of nasal formulation will be feasible.