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저널/프로시딩 상세정보

권호별목차 / 소장처보기

H : 소장처정보

T : 목차정보

藥劑學會誌 = Journal of Korean pharmaceutical sciences 10건

  1. [국내논문]   시클로덱스트린과 소염진통제간의 포접복합체에 관한 연구 (II) : 2-히드록시프로필-${\beta}$-시클로덱스트린이 이부프로펜 좌제의 방출에 미치는 영향  

    오인준 (전남대학교 약학대학 ) , 이미영 (전남대학교 약학대학 ) , 이용복 (전남대학교 약학대학 ) , 신상철 (전남대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 165 - 171 , 1997 , 0259-2347 ,

    초록

    Ibuprofen, a nonsteroidal antiinflammatory, analgesic and antipyretic drug, has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. Effect of ibuprofen/ $2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ inclusion compound on release of suppository was investigated. Complex formation was confirmed by $^{1}H-\;and\;^{13}C-NMR$ spectroscopy. The release of ibuprofen from suppository base in vitro was significantly increased by the complexation with $HP{\beta}CD$ . The release of ibuprofen from hydrophilic base was faster than that from hydrophobic base. In vivo studies, the release rate of ibuprofen from suppository was accelerated after rectal administration in complex form. This results suggested that ibuprofen/ $HP{\beta}CD$ complex can be practically used for suppository to have faster effect of ibuprofen with reduced side effect.

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  2. [국내논문]   수용성 Dimethyl Dimethoxy Biphenylate 유도체의 간염 치료 효과  

    문전옥 (부산대학교 약학대학 ) , 정경욱 (부산대학교 약학대학 ) , 김수현 (부산대학교 약학대학 ) , 김남득 (부산대학교 약학대학 ) , 이성광 (부산대학교 의과대학 ) , 양희선 (환경부 환경정책실 ) , 이치호 (부산대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 173 - 179 , 1997 , 0259-2347 ,

    초록

    A water-soluble DDB derivative (Bis{2-(methylamino)ethyl}-4,4-dimethoxy-5,5',6,6'-dimethylenedioxy-biphenyl-2,2'-dicarboxylate, DDB-S) was synthesized and its therapeutic effects on the liver damage induced by carbon tetrachloride in rats were evaluated. Oral administration of DDB-S reduced the aspartate aminotransferase(AST) and alanine aminotransferase(ALT) activities and increased total protein and albumin contents in the serum of the carbon tetrachloride intoxicated rat. Therapeutic effects of DDB-S by intravenous injection was also investigated using carbon tetrachloride intoxicated rats. Histological studies showed that IV injection of DDB-S had improved the typical necrosis around centrilobular area in liver tissue due to the carbon tetrachloride intoxication and also prevented the elevation of liver weigh/body weight ratio. IV administration of DDB-S to $CCl_4-treated$ rats significantly decreased AST & ALT activities and also prevented the decrease of aniline hydroxylation activity of the liver. These results indicate that i.v. administration of DDB-S is very effective in recovering the liver function in $CCl_4-treated$ rats.

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  3. [국내논문]   Aspartate함유 복합성분과 Ethanol의 약물동태학적 거동  

    김태완 (강원대학교 약학대학 ) , 이범진 (강원대학교 약학대학 ) , 최한곤 (서울대학교 약학대학 ) , 김종국 (서울대학교 약학대학 ) , 신희종 (종근당 (주) ) , 김정우 (종근당 (주))
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 181 - 187 , 1997 , 0259-2347 ,

    초록

    The purpose of this work was to investigate pharmacokinetics of alcohol as a function of dose and time of administration of ethanol. The pharmacokinetics of alcohol 15 min after and before oral administration of aspartate-containing compositions to rats were also evaluated. The retention time of acetaldehyde, alcohol and isopropyl alcohol an internal standard in gas chromatogram was 3.6, 6.0 and 10.5 min, respectively. The maximum concentration of alcohol $(C_{max})$ and area under the blood concentration (AUC) were significanly increased as a function of ethanol dose in a nonlinear fashion. The significant diurnal variation of alcohol pharmacokinetics was also noted, showing fast metabolism and elimination when given orally in the night time. When APAP was given after administration alcohol (1g/kg) to rats, AUC and $C_{max}$ were increased when compared to alcohol only. However, AUC and $C_{max}$ were decreased when aspartate or standard complex compositions containing aceaminophen (APAP, 250mg). sodium L-aspartate(25 mg), dl-methionine (125 mg) and anhydrous caffeine (25 mg) was orally given by coupling malate/asparate shuttle in hepatocyte. The blood alcohol concentration profiles between aspartate and standard complex compositions were similar when given before or after administration alcohol (1g/kg) to rats. No significant difference of administration sequence was observed. However, it was noted that AUC and $C_{max}$ of standard complex compositions given before alcohol administration were significantly lower when compared with alcohol only. Based on these findings, dose, time of administration and composition of drugs to improve alcohol metabolism and elimination were considered to be important in the pharmacokinetics of alcohol. The administration sequence of drug compositions and alcohol might be also considerd.

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  4. [국내논문]   중쇄지방산염 함유 Eudispert hv 하이드로겔의 인슐린 직장 흡수증대효과  

    한건 (충북대학교 약학대학 ) , 김준식 (충북대학교 약학대학 ) , 유정희 (충북대학교 약학대학 ) , 정연복 (충북대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 189 - 198 , 1997 , 0259-2347 ,

    초록

    The purpose of the present study was to investigate the effect of medium chain fatty acid salts, reported as enhancers in insulin nasal absorption, on the rectal absorption of insulin in rats. The serum glucose and remained insulin level in perfusate were measured after rectal recirculation of insulin with or without sod. laurate, sod. caprate and sod. caprylate in situ. The addition of sod. laurate or sod. caprate reduced serum glucose concentration considerably. Sod. caprate (1.0%) showed the greatest promoting effect on the decrement of serum glucose. Eudispert hv hydrogels containing insulin with medium chain fatty acid salts were, thereby, prepared and evaluated. The release rate of insulin from Eudispert hv hydrogels was reduced with an increase in the content of Eudispert hv, and was raised with increasing NaOH concentration. Ten percent Eudispert hv hydrogels were offered for the rectal administration of insulin. The addition of 1.0% sod. caprate reduced serum glucose concentration remarkably after rectal administration of 10% Eudispert hv hydrogels containing insulin. The level of glucose decrement was greater by 30% compared to subcutaneous administration of insulin solution. From the above findings, Eudispert hv hydrogels would be used as useful rectal delivery systems of insulin.

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  5. [국내논문]   수용액중의 비페닐디메칠디카르복실레이트의 가용화  

    배준호 (성균관대학교 약학대학 ) , 박은석 (성균관대학교 약학대학 ) , 지상철 (성균관대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 199 - 205 , 1997 , 0259-2347 ,

    초록

    In order to formulate biphenyl dimethyl dicarboxylate(DDB) aqueous solutions, the effects of various solubilizing agents such as cosolvents(PG, PEG 400, glycerin, ethanol), surfactants, $(poloxamer\;407,\;Cremophor^{\circledR}\; RH40,\;Solutol^{\circledR},\;Tween\;80,\;sodium\;lauryl\;sulfate)$ , complexation agent $(CELDEX^{\circledR}\;CH-20)$ and others(urea, niacinamide, propylene carbonate, HPMC) on the solubility of DDB in water were evaluated. The solubility of DDB in water was about $0.21\;{\mu}g/ml\;at\;20^{\circ}C$ , while its solubility in PEG 400 was 5,000 times higher than that in water. 60% PEG 400 aqueous solution was selected as an optimum solvent system, and surfactants or other solubilizing agents were added to prevent DDB from recrystalization. The addition of surfactants in water increased the solubility of DDB from 15- to 34-fold, however, $CELDEX^{\circledR}\;CH-20$ and other agents studied showed negligible effects on the solubility of DDB in water. The 60% PEG 400 aqueous solution containing 5% $Cremophor^{\circledR}$ RH40 was appeared as the formula of choice. It showed acceptable physical stability after stored for 7 days at $4^{\circ}C$ .

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  6. [국내논문]   나부메톤 정의 생물학적 동등성 평가  

    이윤석 (성균관대학교 약학대학 ) , 박은석 (성균관대학교 약학대학 ) , 지상철 (성균관대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 207 - 212 , 1997 , 0259-2347 ,

    초록

    The bioequivalence of two nabumetone tablets was evaluated in 16 normal male volunteers $(age\;21{\sim}30\;yrs)$ following oral administration. Test product was 'Nacton tablet' made by Jin Yang Pharmaceutical Co. and reference product was 'Unimeton tablet' made by Dong Kwang Pharmaceutical Co.. After one tablet containing 500 mg of nabumetone was administered, blood was taken at predetermined time intervals and the concentration of 6-methoxy-2-naphthylacetic acid, active metabolite of nabumetone, in plasma was determined with an HPLC method using fluorescence detector. AUC, $C_{max}$ and $T_{max}$ were calculated and statistically analyzed for the bioequivalence of the two products. The results showed that the differences in AUC, $C_{max}$ and $T_{max}$ between two products were 3.66%, 6.87% and 1.85%, respectively. The powers $(1-{\beta})$ for AUC, $C_{max}$ and $T_{max}$ were 91.4%, 88.9% and 81.1%, respectively. Detectable differences $({\Delta})$ and confidence intervals were all less than 20%. All of these parameters met the criteria of FDA for bioequivalence, indicating that "Nacton tablet" is bioequivalent to 'Unimeton tablet'.

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  7. [국내논문]   Terfenadine-pseudoephedrine HCl의 이중정 및 유핵정의 비교 용출시험  

    최한곤 (동화약품공업 (주) 중앙연구소)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 213 - 217 , 1997 , 0259-2347 ,

    초록

    The present sustained-release terfenadine-pseudoephedrine HCl dosage form was the core tablet composed of outer (fast-release) layer containing 60 mg of terfenadine and l0mg of pseudoephedrine HCl, and inner (sustained-release) layer containing 110 mg of pseudoephedrine HCl. The purpose of this study was to investigate the possibility of formulating the terfenadine-pseudoephedrine HCl double-layered tablet which was bioequivalent to the core tablet. Its sustained-release and fast-release layer were formulated with disintegrating agents and polymers, respectively, varying with their kinds and amounts. The comparative dissolution test of double-layered and core tablet was carried out at pH 1.2, 4.0 and 6.8, leading to select composite of double-layered tablet whose dissolution pattern was similar to that of core tablet. It was composed of fast-release layer containing 60mg of terfenadine. 10 mg of pseudoephedrine HCl, sodium bicarbonate, microcrystalline cellulose and sodium starch glycolate, and sustained-release layer containing 110 mg of pseudoephedrine HCl and ethylcellulose/hydroxypropyl methylcellulose) (110/30 mg/tablet).

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  8. [국내논문]   테르페나딘-${\beta}$-시클로덱스트린 포접화합물의 제조방법 및 물리화학적 특성  

    최한곤 (동화약품공업 (주) 중앙연구소 ) , 유제만 (동화약품공업 (주) 중앙연구소 ) , 윤성준 (동화약품공업 (주) 중앙연구소)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 219 - 223 , 1997 , 0259-2347 ,

    초록

    Terfenadine, antihistaminic drug, is poorly soluble in water. The purpose of this study is to investigate the possibility of using $terfenadine-{\beta}-cyclodextrin$ inclusion compound, instead of terfenadine, as the active substance of solid dosage form by improving the solubility, dissolution and anti-histaminic activity of terfenadine. The solubility and binding characteristics of $terfenadine-{\beta}-cyclodextrin$ complex in pH $1.2{\sim}6.8$ were investigated. Furthermore, the preparing method of $terfenadine-{\beta}-\;cyclodextrin$ inclusion compound was setting up and its physico-chemical characteristics such as DSC curve, solubility, dissolution and anti-histaminic activity were investigated. In conclusion, the solubility of terfenadine was increasing ${\beta}-cyclodextrin$ and with the decreasing pH. $Terfenadine-{\beta}-cyclodextrin$ inclusion compound, whose yield is almost 100%, was prepared by neutralization method. This inclusion compound was 200-times as soluble as terfenadine in pH 1.2-6.8. In addition, it had the faster dissolution and anti-histaminic activity than terfenadine. Therefore, it is used to the active substance of solid dosage form such as tablet and capsule in stead of terfenadine.

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  9. [국내논문]   Naloxone의 Polyphosphazene 이식제제에 관한 연구  

    서성연 (이화여자대학교 약학대학 ) , 박주애 (이화여자대학교 약학대학 ) , 김길수 (이화여자대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 225 - 231 , 1997 , 0259-2347 ,

    초록

    For the effective administration of naloxone, we attempted to investigate the naloxone sustained-release implants. Using the biodegradable polymer, poly[(diethyl glutamate)-co-(ethyl glycinate)phosphazenes](PGGP), the implantable devices containing naloxone hydrochloride(NLX HCl) and naloxone base(NLX) were prepared. The release rates of NLX and NLX HCl were compared. Influences of NLX contents on release rates were examined. For pharmacokinetic studies, NLX and NLX HCl loaded devices were implanted subcutaneously in rabbits and then the plasma concentrations of NLX were determined by HPLC(ECD). NLX-containing devices were implanted with various doses and pharmacokinetic parameters according to dose were calculated. The relative bioavailabilities were evaluated and compared. Incorporation of NLX in the polymer leaded to a slow release. There were no differences of release rates based on drug contents. In pharmacokinetic parameters determined in 216 hours, NLX loaded devices resulted in enhanced bioavailability with the higher AUC (p

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  10. [국내논문]   글리벤클라미드 결정다형의 용출   피인용횟수: 1

    손영택 (덕성여자대학교 약학대학 ) , 엄보영 (덕성여자대학교 약학대학)
    藥劑學會誌 = Journal of Korean pharmaceutical sciences v.27 no.3 ,pp. 233 - 239 , 1997 , 0259-2347 ,

    초록

    Glibenclamide is a second generation sulfonylurea that is orally active as a hypoglycemic drug. It exists as a crystalline powder which is sparingly soluble in water. It was investigated that the potential of glibenclamide to exhibit polymorphism. Three polymorphic modifications (form 1, form 2 and form 3) and three pseudopolymorphic modifications (form 4, form 5 and form 6) were obtained by crystallization from different organic solvents. The isolated crystal forms were characterized by differential scanning calorimetry(DSC), thermogravimetric analysis(TGA) and X-ray crystallography powder diffraction studies. Form 1 was the most stable and melt at $175.4^{\circ}C$ . Form 2 was metastable and melt at $151.0^{\circ}C$ . Form 3 was a new polymorphic modification because it was different from form 1 and form 2 in X-ray crystallography powder diffraction data. Form 4 was a 1 : 7(toluene : glibenclamide) toluene solvate; form 5 was a 1 : 5(toluene : glibenclamide) toluene solvate; form 6 was a 3 : 8(pentanol : glibenclamide) pentanol solvate. All forms were stable in 3-month storage under 0% or 100% humidity condition. The dissolution rate of form 4 was highest; those of form 2, form 3, form 1, form 5 and form 6 followed.

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