- 오플록사신 및 리도카인 함유 수분 감응성 구강점막 패취제의 제조 및 방출 특성
- ㆍ 저자명
- 곽혜선,송연화,전인구,Gwak. Hye-Sun,Song. Yeon-Hwa,Chun. In-Koo
- ㆍ 간행물명
- 藥劑學會誌
- ㆍ 권/호정보
- 2005년|35권 6호|pp.417-422 (6 pages)
- ㆍ 발행정보
- 한국약제학회
- ㆍ 파일정보
- 정기간행물| PDF텍스트
- ㆍ 주제분야
- 기타
This study was aimed to design and formulate the moisture-activated patches containing ofloxacin and lidocaine for antibacterial and local anesthetic action. The solubility of lidocaine at $32^{circ}C$ in various vehicles decreased in the rank order of PG $759.5{pm}44.5;mg/mL$ > PGL > IPM > PEG 300 > PEG 400 > Ethanol > PGMC > DGME > PGML > OA > $Captex^{circledR};300$ > $Captex^{circledR};200$ > water $(4.0{pm}0.1;mg/mL)$. Ofloxacin revealed very low solubility, which the highest solubility was obtained from PEG 400 $(18.7{pm}6.3;mg/mL)$ among the vehicles used. The addition of lactic acid increased the solubility of ofloxacin dramatically; the solubility at 5% lactic acid was $133.7{pm}9.7;mg/mL$. As $2-hydroxypropyl-{eta}-cyclodextrin$ was added at the concentrations of 40, 80, 120, 160 and 200 mM, the solubilities of lidocaine and ofloxacin were enhanced up to three and two times, respectively, with concentration-dependent pattern. Gel intermediates for filmtype patches were prepared with mucoadhesive polymer, viscosity builders, lidocaine or ofloxacin at pH values from 5 to 7. Gels were cast onto a release liner and dried at room temperature. Dried patch was attached onto an adhesive backing layer, thus forming a patch system. Patches containing a single drug component were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane. The release study was carried out at $37^{circ}C$ using a Franz-type cell. Receptor solutions were isotonic phosphate buffers (pH 7.4). Samples $(100;{mu}L)$ were taken over 24 hours and quantitated by a verified HPLC method. The releases from all tested were proportional to the square root of time. The release rates were 0.9, 157.3 and $281.7;{mu}g/cm^{2}/min^{1/2}$ for the lidocaine patches and 19.8,37.2 and $50.7;{mu}g/cm^{2}/min^{1/2}$ for the ofloxacin patches at the concentrations of 0.3, 0.5 and 1 %, respectively. The release rates were dose dependent in both drug patches $(R^{2};=;0.9077;for;lidocaine;;R^{2};=;0.9949;for;ofloxacin)$ and those were also thickness-dependent $(R^{2};=;0.9246;for;lidocaine;;R^{2};=;0.9512;for;ofloxacin)$.