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이부프로펜 리지네이트의 직장흡수에 미치는 좌제기제 및 첨가제의 영향
전홍렬,박동우,이승목,이정우,최영욱,Jeon, Hong-Ryeol,Park, Dong-Woo,Lee, Seung-Mok,Yi, Jung-Woo,Choi, Young-Wook 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.3
Ibuprofen is an effective non-steroidal anti-inflammatory drug (NSAID), but it has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. A water-soluble salt of ibuprofen, ibuprofen Iysinate, has been synthesized to overcome these shortcomings, and it was formulated as suppository for rectal administration. Witepsol and polyethylene glycols were employed as suppository bases for either ibuprofen or ibuprofen Iysinate, in order to compare the bioavailability in rabbits. The plasma concentrations of ibuprofen were assayed by HPLC after a rectal administration of ibuprofen and ibuprofen Iysinate, respectively. In addition to the comparison of two suppository bases, the other factors which affect on rectal absorption were also evaluated, especially in the point of not only particle size and shape of ibuprofen Iysinate but also effects of additives such as stearic acid, cetyl alcohol and capric acid. And pharmacokinetic parameters such as AUC, $C_{max}$, and $T_{max}$ were also compared. In conclusion, spray-dried ibuprofen Iysinate which was polyporous and spherical shape gave an increased absorption from the rectal formulations with Witepsol Hl5 and stearic acid.
Loxoprofen sodium 플라스타의 소염 , 진통 작용 및 혈중 약물 농도에 대한 연구
채주병(Joo Byung Chae),전홍렬(Hong Ryeol Jeon),이승목(Seung Mok Lee),정남주(Nam Joo Jeong),김수균(Soo Kyun Kim),조길도(Kil Do Cho),김동연(Dong Yeun Kim) 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.2
Loxoprofen-Na (sodium 2-[4-(2-oxocyclopentylmethyl)phenyl]propionate dihydrate) is a potent analgesic drug. We developed loxoprofen-Na plasters to extend duration time of analgesic activity and to reduce side effect on gastrointestinal tract. Analgesic effect of Loxoprofen-Na plasters was investigated. Loxoprofen-Na plaster had good analgesic effect in rat paw pressure test, Tail-flick latency test and acetic acid-induced writhing test. Also, it had anti-inflammatory effect on carrageenan-induced rat hind paw edema. In pharmacokinetic study of Loxoprofen-Na, plasters dosage form showed that plasma drug concentration was prolonged up to 14 hours. So, we can conclude that loxoprofen-Na plasters, when applied on skin, will he a new type of drug for controlling the various local pain or inflammation.
생분해성 폴리락티드/글리콜리드 미립구를 이용한 재조합 소 성장호르몬(rBST)의 지속성주사제 설계
전홍렬,이봉상,권도우,윤미경,전현주,신택환,최영욱 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.3
In order to develope a sustained release formulation of bovine somatotropin(BST), which has been used to increase the body weight of oxen or the milk production of dairy cows, poly(D,L-lactide-co-glyceride)(PLGA) microspheres were made by W/O/W multiple emulsification method and solvent extraction method. Physical properties including particle size, drug entrapment, drug release, protein denaturation, and in vivo body weight increase in rats were characterized. The size of the microspheres was increased as the molecular weight of PLGA increased. When Span 65 and stearic acid during preparation were added, the size was decreased but the amount of surface protein was increased, resulting in a high loading efficiency, with fast release of BST from the microspheres. Aggregation of fragmentation of BST by SDS-PAGE during microspheres preparation and drug release study was not observed. Body weight of Sprague-Dawley's male rats was significantly increased after subcutaneous administrations of BST-loaded PLGA microspheres. There was a good correlation between in vivo weight gain and vitro release rate of microspheres. PLGA microspheres with a high surface protein ratio could be a good candidate for the sustained delivery of BST.
이영재,최영욱,전홍렬,박동우,권석형 한국약제학회 2000 Journal of Pharmaceutical Investigation Vol.30 No.1
A new technique has been developed for the preparation of Lactobacillus microcapsules to enhance the stability against high temperature, humidity, gastric acid and bile acid. Employing fluidized bed coating, primary sub-coating was processed in non-organic solvent system, so that Lactobacillus did not directly contact with organic solvent. Secondary enteric-coating was processed in organic solvent with low temperature (below 33℃) technique, which minimized the heat labilability of Lactobacillus. Survival rate of Lactobacillus within microcapsule was not less than 95% and acid tolerance was above 30% in the artificial gastric acid. Further more it was dissolved in the artificial intestine juice within 2∼3 hr. Average size of Lactobacillus microcapsules was 450 ㎛(25-50 mesh) and its viability was above 90% in the direct tableting.
이부프로펜 리지네이트의 직장흡수에 미치는 좌제기제 및 첨가제의 영향
이승목,최영욱,이정우,전홍렬,박동우 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.3
Ibuprofen is an effective non-steroidal anti-inflammatory drug (NSAID), but it has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. A water-soluble salt of ibuprofen, ibuprofen lysinate, has been synthesized to overcome these shortcomings, and it was formulated as suppository for rectal administration. Witepsol and polyethylene glycols were employed as suppository bases for either ibuprofen or ibuprofen lysinate, in order to compare the bioavailability in rabbits. The plasma concentrations of ibuprofen were assayed by HPLC after a rectal administration of ibuprofen and ibuprofen lysinate, respectively. In addition to the comparison of two suppository bases, the other factors which affect on rectal absorption were also evaluated, especially in the point of not only particle size and shape of ibuprofen lysinate but also effects of additives such as stearic acid, cetyl alcohol and capric acid. And pharmacokinetic parameters such as AUC, C_(max), and t_(max) were also compared. In conclusion, spray-dried ibuprofen lysinate which was polyporous and spherical shape gave an increased absorption from the rectal formulations with Witepsol H15 and stearic acid.