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H : 소장처정보

T : 목차정보

藥劑學會誌 = Journal of Korean pharmaceutical sciences 8건

  1. [국내논문]   트리메부틴의 N-모노데스메칠 트리메부틴으로의 대사동태  

    이용복 (전남대학교 약학대학 ) , 장우익 ((주)대웅제약 중앙연구소 ) , 고익배 (전남대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 73 - 80 , 1998 , 0259-2347 ,

    초록

    In order to elucidate the effect of N-demethylation on the in vivo metabolite kinetics, especially hepatic first-pass effect of trimebutine(TMB), the N-demethylation of TMB to N-monodesmethyl trimebutine(N-TMB) was studied in rats. TMB(10 mg/kg) and N-TMB(10 mg/kg) were injected into the femoral and the portal vein, respectively. And the pharmacokinetic parameters were obtained from the plasma concentration-time profiles of TMB and N-TMB determined by the simultaneous analysis using high-performance liquid chromatography. It was supposed that these drugs were almost metabolized in vivo because the urinary and biliary excreated amounts of TMB and N-TMB were lower than 0.1% of the administered dose. According to the hepatic biotransformation model and metabolic pathways of TMB proposed, it was found that the fraction of systemic clearance of TMB which formed N-TMB in liver $(G_{mi})$ was 0.826, that of TMB which furnishes the available N-TMB to the systemic circulation $(F_{mi})$ was 0.083, and the absolute hepatic bioavailability of N-TMB formed trom TMB $(F_{mi.p})$ was 0.1. These results showed that TMB was suspected of the sequential hepatic first-pass metabolism and N-demethylated by 82.6%. Therefore, the residue would be hydrolyzed by the esterase in the liver. That is, the ability of N-demethylation of TMB was 4.75-fold larger than that of hydrolysis by the esterase in rats.

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  2. [국내논문]   세포탁심나트륨의 결정형의 용출  

    손영택 (덕성여자대학교 약학대학 ) , 김희경 (덕성여자대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 81 - 85 , 1998 , 0259-2347 ,

    초록

    Three polymorphic modifications and two pseudopolymorphic modifications of cefotaxime sodium were obtained by crystallization from different organic solvents. The isolated crystal forms were characterized by UV spectrophotometry, DSC, TGA and X-ray crystallography. Crystal forms of cefotaxime sodium were also compared by dissolution rate. The dissolution rate of form 1 was the highest, followed by form 2, form 4, form 6, form 5 and form 3. Among these polymorphic modifications the dissolution rate of form 3 and form 5 was much slower than that of cefotaxime sodium on the market. All forms showed no change after 2-month storage test in the silica gel desiccator. But after the storage of 2-month at 95% relative humidity condition, all forms were deliquesced by hygroscopic property except form 1 that showed the highest dissolution rate. At 52% relative humidity condition, form 1, form 2 and form 6 had no evidence of phase transformation, but form 3, form 4 and form 5 were also deliquesced.

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  3. [국내논문]   외용겔 및 다중유제크림의 코지산 방출특성과 피부자극성  

    유성운 (중앙대학교 약학대학 ) , 박은우 (중앙대학교 약학대학 ) , 최영욱 (중앙대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 87 - 92 , 1998 , 0259-2347 ,

    초록

    Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p

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  4. [국내논문]   안정성 및 Transfection 효율이 우수한 양이온성 리포좀 유전자 전달시스템의 개발  

    김경미 (원광대학교 약품연구소 ) , 남방현 (약학대학 ) , 손동환 (약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 93 - 98 , 1998 , 0259-2347 ,

    초록

    We have developed liposomes which can be easily prepared with inexpensive lipid, have enhanced stability, and can efficiently deliver DNA into the COS-l cells, Liposome formulations were prepared using cationic materials such as dimethyldioctadecyl ammonium bromide (DDAB), cetyltrimethyl ammonium bromide(CTAB), We investigated the effect of cationic liposome formulations on in vitro DNA transfection, DDAB-containing liposomes showed increased transfection efficiency which was 3.2-fold as much as that by $Lipofectin^{\circledR}$ , but CTAB-containing liposomes were inactive in gene transfection. The effect of colipid of DDAB-containing liposome was also investegated. As a colipid, dioleylphosphatidylethanolamine(DOPE) and cholesterol did altered the transfection efficiency of DDAB-containing liposomes. And increased DDAB concentration lowered the transfection efficiency. The optimum amount of liposomal formulation was $10\;{\mu}M$ for $1\;{\mu}g$ of DNA. In the experiment of stability, DOPE-containing liposomes formulation showed a broad size distribution and separation of two major peaks on a 5th day of preparation, but liposomes containing cholesterol was stable for 10 days. DDAB-containing liposomal DNA delivery system was prepared easily and was stable.

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  5. [국내논문]   재조합 상피세포성장인자를 함유한 경구 점착성 겔제의 위궤양 치유효과  

    한건 (충북대학교 약학대학 ) , 이수진 (충북대학교 약학대학 ) , 김재환 (대웅제약 ) , 정연복 (충북대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 99 - 107 , 1998 , 0259-2347 ,

    초록

    The objective of this study was to develop effective oral formulations of rhEGF for gastric ulcer healing using polycarbophil. hydroxypropylcellulose(HPC) and sucralfate as its bioadhesive bases. Cytoprotective effects of rhEGF, cell proliferation and differentiation. on the ulcers induced by ethanol or acetic acid in rats were studied. rhEGF release from HPC formulation was much faster than that from polycarbophil formulation. HPC formulation combined with small amount of sucralfate showed much slower release of rhEGF than only HPC base only. rhEGF preparations with bioadhesive polymers showed better effects on the healing of gastric ulcers than EGF solution when administered orally. When rhEGF preparations were administered at once and the animals were under starvation, polycarbophil formulation showed better effect on gastric ulcers than HPC formulation. Otherwise, when rhEGF preparations were given more than three times and the rats were fed normally, HPC formulation showed good healing efficacy of ulcers compared to polycarbophil formulation. rhEGF showed dose-dependent effect on the healing of both chronic and acute ulcers.

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  6. [국내논문]   피라세탐의 방출조절 및 생체이용률  

    강진양 (삼육대학교 약학대학 ) , 이경태 (경희대학교 약학대학 ) , 서성훈 (경희대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 109 - 113 , 1998 , 0259-2347 ,

    초록

    This study is purposed to develop the sustained release and bioavailability of piracetam (PA). The use of alginate beads as a means to achieve sustained release of piracetam was evaluated in comparison with that of piracetam alone. In the PA-sodium alginate(SA) beads was confirmed by differential scanning calorimetry thermogram(DSC), indicating a relative shift of an endometric peak of PA to higher temperature. The changes in dissolution rates from PA-SA beads and PASA beads coated by chitosan(CHO) were significantly slower than that of intact PA. The release rate of PA-SA in the gastric fluid was markedly decreased compared with that in the intestinal fluid, suggesting that PA is mostly released in the intestinal fluid. However, the PA/SA ratio scarcely affected the release profile. The blood concentration- time curves of PA, PA-SA and PA-SA-CHO were obtained by oral administration to rats. $T_{max}$ of PA, PA-SA and PA-SA-CHO were 1, 10 and 6 hours, respectively. It was confirmed that the release of PA was prolonged by the formulation of PA-SA beads and PA-SA-CHO beads.

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  7. [국내논문]   세프라딘의 용출에 미치는 결정형의 영향  

    손영택 (덕성여자대학교 약학대학 ) , 김지선 (덕성여자대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 115 - 119 , 1998 , 0259-2347 ,

    초록

    Five polymorphic modifications of Cephradin were prepared by recrystallization from organic solvents. The isolated crystal forms were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and X-ray crystallography powder diffractometry. Modificaition 1 was the most stable form and decomposed at $201.3^{\circ}C$ . Modification 3 and 4 were metastable. The dissolution of modification 3 and 4 was faster than that of marketed form.

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  8. [국내논문]   수용액중 염산카로베린의 용해성 및 안정성  

    곽혜선 (동덕여자대학교 약학대학 ) , 이동수 (환인제약(주) 중앙연구소 ) , 전인구 (동덕여자대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.28 no.2 ,pp. 121 - 126 , 1998 , 0259-2347 ,

    초록

    The solubility and physicochemical stability of caroverine hydrochloride (CRV), an antispasmodic, in buffered aqueous solutions were studied using a reverse phase high performance liquid chromatography. The solubilty of the drug at pH 2.76-5.40 was similar at the range 31.9-36.2 mg/ml $(34^{circ}C)$ , but, at the pH higher than 6.0, markedly decreased. The use of polyethylene glycol 400 as a cosolvent did not increase the solubility at any compositions examined. Moreover. increasing molar concentration of aqueous phosphate buffer from 0 to 0.5 M remarkably decreased the solubility. The degradation of CRY followed the apparent first-order kinetics. The degradation was accelerated with decreasing pH and increasing storage temperature. The half-lives for the degradation of CRY (1.0 mg/ml) at pH 1.28. 4.01 and 5.93 $(45^{\circ}C)$ were 2.8, 31.4 and 124 hr. respectively. The pHs of incubated solutions were to some extent lowered perhaps due to the formation of acidic degradation products. The addition of disodium edetate (0.01%) to the CRY solution (pH 4.95) retarded 2.5 times the degradation rate at $45^{\circ}C$ , but the use of sodium bisulfite (0.1%) accelerated 2.9 times the rate. The activation energy for the CRY solution (20 mg/ml. pH 5.4) containing 0.01% EDTA was calculated to be 5.98 kcal/mole. When the solution was stored under nitrogen displacement in ampoule, there was no significant degradation even after 3 months at $40^{\circ}C$ , indicating that protection from oxidation by air (oxygen) is essential for the complete stabilization of CRY solution.

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