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내인성 N1- methylnicotinamide 를 이용한 신혈장유량측정
심창구 한국약제학회 1983 Journal of Pharmaceutical Investigation Vol.13 No.1
Renal plasma flow (RPF) was estimated from the extraction ratio (E.R.) and renal plasma clearance of the endogenous N¹-methylnicotinamide(NMN) in the experimental renal failure (ERF) rat, and was compared with that of healthy rats. PRE of ERF-rats was not different from that of the healthy rat significantly and dependened upon E. R, or intrinsic clearance of the kidney. This NMN method seemed to be superior to the conventional p-aminohippuric acid (PAH) method clinically.
위내체류를 목적으로 한 알부민 가교 PVP 하이드로겔의 팽윤특성
심창구,여소현 한국약제학회 1993 Journal of Pharmaceutical Investigation Vol.23 No.3
Retaining a drug in the stomach by some means is sometimes necessary to extend the G1 absorption time of the drug more than 6-8 hrs. Hydrogel has often been examined for its feasibility as a dosage form, so called platform, that could be retained in the stomach due to its excellent swelling properties in the gastric fluid. In this study, polyvinylpyrrolidone (PVP) hydrogel crosslinked by albumin or acrylated albumin was synthesized in a tablet form and evaluated for its possibility as the platform. The synthesis of the hydrogel was performed by ^(60)Co γ-ray irradiation of N-vinyl-2-pyrrolidone (monomer) in the presence of a crosslinking agent: aqueous solution of albumin or acrylated albumin. Synthetic conditions such as radiation dose, dose rate and concentration of crosslinking agent were varied in order to optimize the swelling and mechanical properties of the hydrogels. Degree of swelling of albumin-crosslinked PVP (Al-PVP) was highly dependent on radiation dose, dose rate and albumin concentration: it was decreased as they increased. On the other hand, that of acrylated albumin-crosslinked PVP (Acryl-PVP) was almost independent on them except dose rate: it was decreased as the radiation dose rate increased. The compressive strength of the two hydrogels was decreased as the dose rate increased. Digestion of both PVP in artificial gastric fluid containing pepsin was delayed by the γ-ray irradiation. In conclusion, Al-PVP and Acry-PVP with diverse swelling and mechanical properties could be obtained by controlling synthetic conditions, mainly the irradiation dose rate.
심창구,한용해,김현지 한국약제학회 1993 Journal of Pharmaceutical Investigation Vol.23 No.3
The effect of omeprazole (OPZ) suppository on rat rectal mucosa was investigated microscopically. The suppository was prepared with Witepsol H15 base by molding method. Rectal irritation was evaluated according to defined pathological features. The suppository produced a slight damage to the rectal mucosa at 1 hr after the interectal administration, which was almost completely recovered within 24 hr. The damage was not due to OPZ but due to suppository base, Witepsol H15, itself, since Witepsol H15 suppository without OPZ produced the same damage. Therefore, it was concluded that OPZ itself has no rectal mucosa-irritating effect and thus can be developed as a suppository dosage form without any further toxicity problems.
경구투여된 약물의 혈장중 농도곡선에 나타나는 다중피크 현상의 해석
심창구,이혜원 한국약제학회 1991 Journal of Pharmaceutical Investigation Vol.21 No.4
There are many drugs reproted to show unusual pharmacokinetic behavior by producing a significant secondary peak in the plasma concentration-time curve after oral administration. The drugs are ranitidine. cimetidine, acetaminophen, aspirin, furosemide, bumetanide, piretanide, veralipride, sobrerol, penicillamine and doxycycline etc. Enterohepatic circulation-, two absorption site-, biphasic gastric emptying-, tissue deposition- and multi-fraction absorption theories have been suggested for the mechanisms of this phenomenon. Here, the theories were reviewed and critisized for their validity as a possible mechanism of the multiple peak phenomenon.
상피세포 성장인자의 경피흡수 : 정상피부 , 각질제거피부 및 화상피부에 있어서
심창구,조애리,이정욱,안병락,정주영,고여욱 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.1
In vivo and in vitro skin permeation of recombinant ^(125)I-EGF through normal. stripped and the first degree burn skin were studied. The in vitro skin permeation rate through the first degree burn skin (296 cpm/㎠/hr) and the stripped skin (1131 cpm/㎠/hr) were 3.5 times and 13 times higher, respectively, as compared with the one through normal skin. In vivo absorption study with the first degree burn skin, the peak concentration of EGF in the skin was achieved at 1-3 hr and decreased afterward up to 8 hr with an elimination constant of 1.31 × 10³g/㎖/hr. To investigate the higher elimination rate of EGF in burn skin, binding and metabolism studies were conducted. No significant metabolism of EGF in burn skin (100℃, 5second burning) was observed. With the presence of unlabelled-EGF, ^(125)I-EGF permeation through the burn skin showed higher permeation rate than the one without unlabelled-EGF. The result may indicate that EGF-receptor binding play a role in determining the skin permeation rate.
아르기닌 또는 인산일수소나트륨이 수용액중에서 오메프라졸의 안정성에 미치는 영향 비교
심창구,한용해,우종수,이창현 한국약제학회 1993 Journal of Pharmaceutical Investigation Vol.23 No.4
The stability of omeprazole in the aqueous solutions containing arginine or sodium phosphate dibasic(SPD) was examined at 30, 40 and 50℃. Arginine or anhydrous SPD was added to omeprazoie solution (200㎍/㎖ in distilled water) to yield 100㎍/㎖ concentration of each. Then, the solution was kept at 30, 40 or 50℃ for 90 hrs. Aliquots of the solution were withdrawn at specified time intervals and assayed by HPLC for intact omeprazole. The remaining percentage-time curves revealed that omeprazole was degraded rapidly as functions of time and temperature following pseudo first-order kinetics. The rate constant in the SPD solution was much higher than in the arginine solution. In other words. the degradation half-lives of omeprazole at 30℃, for example, was 148 and 76 hr in arginine and SPD solutions respectively. The initial pH of the solution containing 100㎍/㎖ of arginine or SPD was 9.7 or 8.7, respectively. Since omeprazole is more stable as the pH of its solution becomes more alkaline, the longer half-life of omeprazole in arginine solution could be explained by the more alkaline characteristics of arginine than SPD In the solution. The activation energy necessary for the degradation reaction was almost identical in both solutions, indicating similar degradation mechanisms of omeprazole in the solutions. In conclusion, omprazole was more stable in the presence of arginine than of SPD.