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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.
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.
Salmonella typhi KNIH100으로부터 aroA 유전자의 클로닝과 염기서열 분석
길영식,신희정,김영창 한국미생물학회 2000 미생물학회지 Vol.36 No.1
장티푸스는 Salmonella typhi에 의해 유발되는 장감염성 질환으로 사람과 동물에 공통되는 질병이다. 본 연구에서는 국립보건원과 공동연구를 수행하여 한국형 장티푸스 유발균인 S. typhi KNIH100을 분리하였다. 분리된 S. typhi KNIH100의 염색체 DNA로부터 방향족 아미노산의 생합성에 관여하는 효소인 5-enolpyruvylshikimate-3-phosphate synthetase를 암호화하는 aroA 유전자를 포함하는 약 5.0 kb의 SalI절편을 pBluescriptII SK(+) vector와 aroA 돌연변이주인 E. coli CGSC2829를 이용하여 클로닝하였다. 그리고 이 클론을 pSAL80이라 명명하였다. 클로닝된 재조합 plasmid인 pSAL80에는 ATG 개시코돈과 TGA 종결코돈을 포함하는 1,284 염기로 구성된 aroA 유전자가 위치하고 있었으며, 다른 장내세균과 마찬가지로 serC와 하나의 오페론을 구성하고 있음을 밝혔다. 또한 S. typhi Ty2, S. typhimurium, 그리고 E. coli 등 다른 장내세균의 aroA 유전자와 상동성을 비교하여 본 결과 각각 99%, 95%, 77%의 상동성을 나타내었다. Salmonella typhi is one of important causes of human enteric infections. S. typhi KNIH100 was isolated from a patient of typhoid fever in Korea. We cloned a 5.0 kb SalⅠ fragment containing the aroA gene encoding a 5-enolpyruvylshikimate-3-phosphate synthetase from chromosomal DNA of this strain. This recombinant plasmid was named pSAL80. E. coli CGSC2829, an aroA- mutant, was not grown on the M9 minimal medium but E. coli CGSC2829 (pSAL80) was grown on the M9 minimal medium. The aroA gene was composed of 1,284 base pairs with ATG initiation codon and TAA termination codon. Sequence comparison of the aroA gene exhibited 99%, 98%, and 77% identity with those of S. typhi Ty2, S. typhimurium, and E. coli respectively. As in the cases of Shigella sonnei and E. coli, the serC and aroA genes lie in a single operonic structure.
Salmonella typhi KNIH100으로부터 aroD 유전자의 클로닝과 염기서열 분석
길영식,전형규,신희정,김영창 한국미생물학회 2000 미생물학회지 Vol.36 No.3
장티푸스는 Salmonella typhi 에 의해 유발되는 장감염성 질환으로 사람과 동물에 공통되는 질병이다. 본 연구에서는 기 보고된Salmonella typhi KNH100의 염색체 DNA로부 터 방향족 아미노산의 생합성에 관여하는 효소인 3-dehydroquinate hydratase(3- dehydroquinate)를 암호화하는 aroD 유전자를 포함하는 약 3.2 kb의 Sal I 절편을 pSAL62 이라 명명하였다. 클로닝된 재조합 plasmid인 pSAL61에는 ATG 개시코돈과 TGA 종결코돈 을 포함하는 759 염기로 구성된 aroD 유전자가 위치하고 있었다. 또한 S. typhi Ty2, Shigella dysenteriae, 그리고 Escherichia coli 등 다른 장내 세균의 aroD 유전자와 상동성을 비교하여 본 결과 각각 90%, 72.7% 그리고 73%의 상동성을 나타내었다. Sulmonella gyhi is one of important causes of human enteric infections. S @phi I<NIN100 was isolated from a patient of typhoid fever in Korea. We cloned a 3.2 kb Soil fi-aggmeiit coniainlng the uroD gene encoding a 3- dehydroqninaie hydratase(3-dehydroquinase) from chroinosomal DNA of this stram. This recoinbinant plasmid w-as named pSAL62. E. coli CGSC2848. an nroD m~~tant, was not grown on Ule M9 minimal medium but E coli CGSC2848 (pSAL62) was grown on the M9 ininiinal medium. The UIIOD gene was coinposed of 759 base pairs with ATG mitiation codon and TGA tem~inatiou codon. Sequence comparison of the moD gene exhibited 98%, 72.756, and 73% identity w i h Urose o f S typhi Ty2, S. rlyserrte~ine, and E call, respectively.
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.