Liposome 과 그 제제에의 응용

구영순 한국약제학회 1981 Journal of Pharmaceutical Investigation Vol.11 No.4

항암제의 조절투여성 약제개발에 관한 연구(제2보) : 2-hydroxyethyl methacrylate-styrene 공중합체 매트릭스로부터 Tegafur의 조절방출 Controlled Release of Tegafur from 2-hydroxy ethyl methacrylate-styrene Copolymer Matrices

具永順,金吉洙,李承晋 梨花女子大學校 藥學硏究所 1991 藥學硏究論文集 Vol.- No.1

HEMA-styrene 공중합체 매트릭스를 활용한 항암제인 Tegafur의 조절 방출에 관하여 검토하였다. HEMA-styrene 공중합체를 styrene의 조성비를 달리하여 합성한 후 약물 전달체를 제조하고, 팽윤도 실험 및 약물 방출 실험을 수행하였다. 고분자의 팽윤도는 소수성 변조에 따라 광범위한 조절이 가능 하였으며 Tegafur의 방출은 고분자의 친수-소수성 정도에 따라 조절 가능하였다. In a attempt to develop anti-cancer drug delivery systems, controlled release of Tegafur from 2-hydroxyethyl methacrylate(HEMA)-styrene copolymer matrices was investigated. HEMA-styrene copolymer was synthesized at different monomer composition. Swelling of the copolymers decreased as the styrene content increased. Release rates of Tegafur from the copolymer matrices were controlled by their hydrophilic-hydrophobic balances. As the copoymer hydrophobicity increased, the drug release rates retarded and approached to zero-order release pattern. The release kinetics was attributed to the polymer relaxation control mechanism.

염산 프로프라놀롤-고체 분산계-폴리비닐알코올 하이드로겔 중공좌제로부터의 약물방출

구영순,정진훈,이정연 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.4

In order to develop the controlled release of a drug from the suppsitories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppository forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The polyvinyl alcohol(PVA) hydrogel as a base, and propranolol·HCl(PPH) as a model drug were employed. In vitro drug dissolution studies showed that the dissolved amounts(%) of PPH from PPH-methylcellulose(MC)-SDS and PPH-ethylcellulose(EC)-SDS reached 100% and 63% in 4.5-hours. respectively. In the relative strength test fox PVA hydrogel. PVA hydrogel became harder and more rigid when the number of freezing-thawing cycles and the ratio of PVA 2000 were increased. In vitro drug release profile revealed that the release rate(%) of PPH from PPH-EC-SDS and PPH-MC-SDS hollow type suppositories were sustained. The release amount(%) of PPH from PPH-EC-SDS hollow type suppositories was not affected by storage time, but since the use of hydrophilic MC made PPH diffuse into the hydrogel after it absorbed the water of base, the various release patterns were appeared as the storage time went by. In vivo absorption experiments with rabbits showed that PPH-EC-SDS(PPH : EC=1:3) hollow type suppository delayed the absorption of PPH, significantly. The C_(max). AUC_(0·8) and MRT of PPH powder hollow type suppository were 196.37±5.63ng/㎖. 1105.26ng/㎖/min and 8.66min. respectively. The C_(max), AUC_(0·8) and MRT of PPH-EC-SDS(PPH : EC=1:3) were 91.30±14.14 ng/㎖. 554.69 ng/㎖/min, 235.99 min, respectively.

Sulfamerazine-Sugar Glass Dispersion의 용출속도에 관한 연구

구영순,성경수 梨花女子大學校 藥學硏究所 1991 藥學硏究論文集 Vol.- No.1

Three sugar glass dispersions of sulfamerazine were prepared using dextrose, galactose and sucrose as the carriers, with the ratio of the drug to the carrier was 1:9. The chemical stability of sulfamerazine in the glass dispersion system was studied using TLC. TLC revealed no additional spot and there was good correspondence with the Sulfamerazine itself. While time required to dissolve 50%(T_50%) of sulfamerazine powder was 390 min that of dextrose glass dispersion system was 1.5min. and galactose system was 4.0min. in distilled water 23) T_50% of physical mixture with dextrose, galactose and sucrose were 26.4min., 26.5min., and 26.0min. respectively in distilled water. T_50% of control was 54min. and those of all of the glass dispersion systems were within 1min. in 0.1N HCI. The dissolution rates of sulfamerazine from sugar glass dispersion system in distilled water was greater than that in 0.1N HCI.

Solvent Deposition Method 를 이용한 Furosemide 제제의 용출증대와 Rat 에서의 이용효과에 관한 연구

구영순,한규정 한국약제학회 1983 Journal of Pharmaceutical Investigation Vol.13 No.2

The matrix affects the dissolution of furosemide, which is almost insoluble in the dissolution medium. In order to understand the effect of the matrix on the dissolution of furosemide, lactose, starch, Avicel ^ⓡpH 101, Avicel ^ⓡpH 301, SiO₂ and talc were used as the matrix and the solvent deposition method were used. The dissolution characteristics of four dissolution medium were compared to each other using various ratio of drug-to-matrix. The results are as follows: 1) Lactose was shown to be superior and talc was to be inferior to the other matrixes investigated. 2) A maximum dissolution rate and dissolution amount of furosemide were observed in 1 : 10 ratio of the drug-to-matrix. 3) T_(80%) of 1 : 10 ratio of the drug-to-matrix in pH 7.2 was 1 min. from FM-lactose and 30 min. from FM-talc. T_(50%) in pH 4.2 is 2 min. from furosemide-lactose and 150 min. from furosemide-talc. Total amount of furosemide in pH 1.2 at 30 min. were enhanced 13.3 fold in furosemide-lactose and 3.5 fold in furosemide-talc compared to the control. Diuretic action of those furosemide-lactose and furosemide-talc was also evaluated by monitoring changes in urinary excretion of sodium, potassium and urine volume in rat. The accumulated urine volume were enhanced 1.7 fold in furosemide-lactose (1.5) compared to the furosemide.

Solvent Deposition Method를 이용(利用)한 Furosemide 제제(製劑)의 용출증대(溶出增大) Rat에서의 이용효과(利用效果)에 관한 연구(硏究)

구영순,한규정,Ku, Young-Soon,Han, Gyu-Jung 한국약제학회 1983 Journal of Pharmaceutical Investigation Vol.13 No.2

The matrix affects the dissolution of furosemide, which is almost insoluble in the dissolution medium. In order to understand the effect of the matrix on the dissolution of furosemide, lactose, starch, $Avicel\;^{\circledR}pH\;101$, $Avicel\;^{\circledR}pH\;301$, $SiO_2$ and talc were used as the matrix and the solvent deposition method were used. The dissolution characteristics of four dissolution medium were compared to each other using various ratio of drug-to-matrix. The results are as follows: 1) Lactose was shown to be superior and talc was to be inferior to the other matrixes investigated. 2) A maximum dissolution rate and dissolution amount of furosemide were observed in 1 : 10 ratio of the drug-to-matrix. 3) $T_{80%}$ of 1 : 10 ratio of the drug-to-matrix in pH 7.2 was 1 min. from FM-lactose and 30 min. from FM-talc. $T_{50%}$ in pH 4.2 is 2 min. from furosemide-lactose and 150 min. from furosemide-talc. Total amount of furosemide in pH 1.2 at 30 min. were enhanced 13.3 fold in furosemide-lactose and 3.5 fold in furosemide-talc compared to the control. Diuretic action of those furosemide-lactose and furosemide-talc was also evaluated by monitoring changes in urinary excretion of sodium, potassium and urine volume in rat. The accumulated urine volume were enhanced 1.7 fold in furosemide-lactose (1.5) compared to the furosemide.

Nalidixic Acid의 Eudragit RL Microencapsulation에 관한 연구

구영순,최경주 梨花女子大學校 藥學硏究所 1991 藥學硏究論文集 Vol.- No.1

Microencapsulation of nalidixic acid using Eudragit RI, a methacrylic acid copolymer was investigated. Microcapsules were prepared by dispersing the drug solution in liquid paraffing using aluminium tristearate as dispersing agent. The preparation of the microcapsules showed high reprodulibility in particle size, shape and the drug content. The dissolution rates of Nalidixic acid from the these microcapsules considerably decreased as compared with that from Nalidixic acid powder and Nalidixic acid-Eudragit RL solid dispersions. The release of Nalidixic acid increased with increased with increasing percentage of aluminium tristearate added to the microcapsules.

Sodium salicylate 나일론 마이크로캅셀 제조에 미치는 Matrix의 영향

구영순,유정희,Ku, Young-Soon,Yoo, Jung-Hoo 대한약학회 1984 약학회지 Vol.28 No.4

Nylon microcapsules of sodium salicylate containing three different matrixes, acacia, gelatin and formalized gelatin, were prepared by interfacial polymerization and the effect of the matrix on the dissolution rate of sodium salicylate from its nylon microcapsule was investigated. The microcapsules were spherical and their particle diameter increased in proportion to the amount of matrix. The surface was different from each other according to the kind and the amount of matrix when observed by the scanning electron microscopy. The dissolution rate of sodium salicylate from its microcapsules was decreased by increase of the amount of matrix and the formalized gelatin most decreased the dissolution rate of drugs.

Promethazine·HCI-gel 형성부형제 Coprecipitate의 용출성에 관한 연구

具永順,張惠慶 梨花女子大學校 韓國生活科學硏究院 1990 韓國生活科學硏究院 論叢 Vol.46 No.-

The coprecipitates of promethazine hydrochloride, a cationic water-soluble as a model drug used drug, with pectin, chondroitin-Na-sulfate and sodium alginate, the gel forming excipients, were studied to determine their dissolution profiles in distilled water and 0.1 N HCI medium by means of the KP dissolution method. The dissolution rates of the coprecipitate tables were very slow, especially promethazine-alginate coprecipitate tablet in comparison with the intact drug, suggesting that it may be useful for sustained-release preparations. The formation of the coprecipitates was conformed by powder X-ray diffractometry.

Propranolol.HCl의 Cellulose Acetate Phthalate Microencapsulation에 관한 연구

구영순,김재연,Ku, Young-Soon,Kim, Jae-Youn 대한약학회 1989 약학회지 Vol.33 No.5

Microcapsule of Propranolol HCl with Cellulose Acetate Phthalate (CAP) by coacervation-phase separation method was studied. Encapsulation was carried out in the CAP-liquid paraffin-acetone ethanol solvent system. The optimum weight ratio for microencapsulation in the CAP-liquid paraffin-solvent system was 1.32:89.18:9.50 or 1.65:89.42:8.93. The wall thickness of microcapsules increased according to increasing of CAP concentration, but dissolution rate decreased. The dissolution of propranolol-HCl in simulated gastric and intestinal fluid test solution was completed within 3 min., but T50% of propranolol HCl from 10.0% CAP-microcapsules were 390 min. and 210 min. respectively. The released amount from 12.5% CAP-microcapsules was 41.8% within 720 min. in simulatd gastric fluid test solution and T50% of those in simulated intestinal fluid test solution was 250 min.