고체분산체에 의한 펠로디핀의 용출율 개선과 서방성 경구제제

길영식,홍석천,유창훈,신현종,김종성,Gil, Young-Sig,Hong, Seok-Cheon,Yu, Chang-Hun,Shin, Hyun-Jong,Kim, Jong-Sung 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.3

To improve the solubility of poorly water-soluble drug and to develop a sustained release tablets, the need for the technique, the formation of solid dispersion with polymeric materials that can potentially enhance the dissolution rate and extent of drug absorption was considered in this study. The 1:1, 1:4, and 1:5 solid dispersions were prepared by spray drying method using PVP K30, ethanol and methylene chloride. The dissolution test was carried out at in phosphate buffer solution at $37^{\circ}C$ in 100 rpm. Solid dispersed drugs were examined using differential scanning calorimetry and scanning electron microscopy, wherein it was found that felodipine is amorphous in the PVP K30 solid dispersion. Felodifine SR tablets were prepared by direct compressing the powder mixture composed of solid dispersed felodipine, lactose, Eudragit and magnesium stearate using a single punch press. In order to develop a sustained-release preparation containing solid dispersed felodipine, a comparative dissolution study was done using commercially existing product as control. The dissolution rate of intact felodipine, solid dispersed felodipine and its physical mixture, respectively, were compared by the dissolution rates for 30 minutes. The dissolution rates of felodipine for 30 minutes from 1:1, 1:4, 1:5 PVP K30 solid dispersion were 70%, 78% and 90%. However, dissolution rate offelodipine from the physical mixture was 5% of drug for 30 minutes. Our developed product Felodipine SR Tablet showed dissolution of 17%, 50% and 89% for 1, 4, and 7 hours. This designed oral delivery system is easy to manufacture, and drug releases behavior is highly reproducible and offers advantages over the existing commercial product. The dissolution rate of felodipine was significantly enhanced, following the formation of solid dispersion. The solid dispersion technique with water-soluble polymer could be used to develop a solid dispersed felodipine SR tablet.

나프록센 함유 방출제어형 패취의 제제설계 및 평가

이계주(Gye Ju Rhee),홍석천(Seok Cheon Hong),황성주(Sung Joo Hwang) 한국약제학회 1999 Journal of Pharmaceutical Investigation Vol.29 No.4

The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressure-sensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIB) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSA-type patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIB-based PSA-type patch with various loading doses fitted Higuchi`s diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn`t fit the zero-order kinetics

소염진통제의 경피투여 제제의 개발과 평가

이계주(Gye Ju Lee),홍석천(Seok Cheon Hong),우종수(Jong Su Woo),이덕근(Duck Kun Lee),김은희(Eun Hee Kim),남진경(Jin Kyung Nam),박종범(Jong Bum Park),황성주(Sung Joo Hwang) 한국약제학회 1998 한국약제학회 총회 및 학술대회 요지집 Vol.- No.28

N/A N/A

L-아르기닌 복합체를 이용한 피록시캄의 용해도 및 생체이용률의 증가

홍석천,유창훈,조동현,신현종,길영식 한국약제학회 2003 Journal of Pharmaceutical Investigation Vol.33 No.2

Piroxicam-arginine complex was prepared to improve the solubility and dissolution rate of poorly water-soluble piroxicam. Its formation was identified by infrared spectrophotometry, differential thermal analysis and dissolution rate. Piroxicam complex dispersible tablets, commercial Feldene^?? dispersible tablets and piroxicam physical mixture hard capsules were prepared to compare dissolution rate in water. Dissolved amounts (%) after 15 mins of piroxicam complex dispersible tablets, commercial Feldene^?? dispersible tablets and piroxicam physical mixture hard capsules were 98%, 45% and 10%, respectively. The solubility of complex in water was significantly higher than that of piroxicam itself. In vivo, pharmacokinetic parameters were obtained after oral administrations of piroxicam complex and physical mixture at a does of 2㎎ to New Zealand White Rabbit. The C_max of piroxicam complex was similar to that of piroxicam. However, there were much difference between the two formulations with regard to T_max and AUC. The T_max of piroxicam alone was 4 hours, but that of piroxicam complex was 0.8 hours. In addition, the AUC of piroxicam complex was 1.38 times greater than that of piroxicam alone.

나프록센 함유 방출제어형 패취의 제제설계 및 평가

이계주,홍석천,황성주 충남대학교 약학대학 의약품개발연구소 1999 藥學論文集 Vol.15 No.-

The purpose of this study is to prepare he controlled release adhesive patch containing naproxen. Pressure-sensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIB) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSA-type patch. The membrane was mainly composed of Eugragit. polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIB-based PSA-type patch with various loading dosed fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics.

고체분산체에 의한 펠로디핀의 용출을 개선과 서방성 경구제제

길영식,홍석천,유창훈,신현종,김종성 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.3

To improve the solubility of poorly water-soluble drug and to develop a sustained release tablets, the need for the technique, the formation of solid dispersion with polymeric materials that can potentially enhance the dissolution rate and extent of drug absorption was considered in this study. The 1:1, 1:4, and 1:5 solid dispersions were prepared by spray drying method using PVP K30, ethanol and methylene chloride. The dissolution test was carried out at in phosphate buffer solution at 37℃ in 100 rpm. solid dispersed drugs were examined using differential scanning calorimetry and scanning electron microscopy, wherein it was found that felodipine is amorphous in the PVP K30 solid dispersion. Felodifine SR tablets were prepared by direct compressing the powder mixture composed of solid dispersed felodipine, lactose, Eudragit and magnesium stearate using a single punch press. In order to develop a sustained-release preparation containing solid dispersed felodipine, a comparative dissolution study was done using commercially existing product as control. The dissolution rate of intact felodipine, solid dispersed felodipine and its physical mixture, respectively, were compared by the dissolution rates for 30 minutes. The dissolution rates of felodipine for 30 minutes from 1:1, 1:4, 1:5 PVP K30 solid dispersion were 70%, 78% and 90%. However, dissolution rate offelodipine from the physical mixture was 5% of drug for 30 minutes. Our developed product Felodipine SR Tablet showed dissolution of 17%, 50% and 89% for 1, 4, and 7 hours. This designed oral delivery system is easy to manufacture, and drug releases behavior is highly reproducible and offers advantages over the existing commercial product. The dissolution rate of felodipine was significantly enhanced. following the formation of solid dispersion. The solid dispersion technique with water-soluble polymer could be used to develop a solid dispersed felodipine SR tablet.