• Title/Summary/Keyword: Drug content

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Preparation of the Dexamethasone-incorporated Lipid Nanosphere: Characteristics of Lipid Nanosphere by Varying Species and Ratio of Lipid (덱사메타손이 봉입된 지질나노입자의 제조: 지질의 종류와 함량 변화에 따른 지질나노입자의 특성)

  • Jeong, Seok-Hyeon;Lee, Jeong-Eun;Seong, Ha-Su;Sin, Byeong-Cheol
    • Journal of the Korean Chemical Society
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    • v.50 no.6
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    • pp.464-470
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    • 2006
  • the coricosteroid drug dexamethasone is an efficacious antiinflammatory drug, it is difficult to formulate in an injectable formulation due to its poor aqueous solubility. A lipid-based nanosphere formulation containing dexamethasone was designed for solubilization of the drug in aqueous solution and sustained release of the drug from the nanosphere. The lipid nanospheres, composed of phospholipid, cholesterol and cationic lipid, were prepared by self emulsification-solvent diffusion method followed by diafiltration. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated according to the variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter 80-120 nm and dexamethasone loading efficiency of greater than 80%. The drug loading efficiency increased with the increase of the length of aliphatic chain attached to the phospholipid. However, the drug loading efficiency was inversely proportional to the increase of cholesterol content in the lipid composition. The lipid nanosphere could not be prepared without the use of cationic lipid and the drug loading efficiency was proportional to the increase of cationic lipid content. The lipid nanospheres containing dexamethasone are a promising novel drug carrier for an injectable formulation of the poorly water-soluble drugs.

Guideline for Bioequivalence Studies of Controlled Release Products (서방성 제제의 생물학적동등성시험을 위한 가이드라인)

  • Seo, Hyun-Ok;Kim, So-Hee;Ahn, Mee-Ryung;Ahn, Choong-Yul;Park, Hye-Jin;Oh, Eun-Kyung;Lee, Eun-Ju;Kim, Bo-Yeon;Kim, Min-Jeong;Woo, Na-Ry;Seo, Hee-Won;Chung, Soo-Youn
    • Journal of Pharmaceutical Investigation
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    • v.40 no.1
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    • pp.63-66
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    • 2010
  • The "Guidance Document for Bioequivalence Study" was revised for adding to bioequivalence studies of controlled-release products after meal(Korea Food & Drug Administration Notification #2008-22, 2008.5.7). The bioequivalence study design for controlled-release products is $2{\times}2$ crossover under fast and fed condition in respect. For studies of controlled-release products under fed study, the same high-fat diet should be taken within 20 minutes in at least a 10-hour fasting state. The drug products should be administered 30 minutes after the meal started. A high-fat(more than 35 percent of total caloric content of the meal) and high-calorie(over 900 calories) meal is recommended as a test meal for fed BE studies.

Study on the Variation of Components from Scutellariae Radix by Processing and Storage Condition (황금(黃芩)의 포제 및 보관조건에 따른 성분변화 연구)

  • Ham, In-Hye;Maeng, Won-Mo;Yang, Gab-Sik;Kim, Dal-Hwan;Kim, Do-Hoon;Cho, Jung-Hee;Choi, Ho-Young
    • The Korea Journal of Herbology
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    • v.22 no.2
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    • pp.189-199
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    • 2007
  • Objective : This study was observed the variation of components from Scutellariae Radix (SR) by processing and storage. Methods : The main component of SR is analysed after various processing and also storage condition by HPLC. Result : 1. In wine-fried SR, the contents of baicalein, wogonin and oroxylin-A was significantly increased. However, the content of baicalin was decreased slightly. In charred SR, the contents of baicalein, wogonin and oroxylin- A was significantly increased. However, the content of baicalin was decreased greatly. 2. The contents variation of SR was not almost changed in room and cold condition. But in accelerated condition, the content of baicalin was slightly decreased, and the contents of baicalein, wogonin and oroxylin-A was significantly increased. 3. The contents variation of wine-fried SR was not almost changed in room and cold condition. But in accelerated condition, the content of baicalin was signifjcantly decreased. 4. The contents variation of charred SR was not almost changed in all conditions. Conclusion : The bioactivity of SR and wine fried SR might be changed by the contents varition during longterm storage. charred SR can be preserved more than two years in room and cold condition.

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Effect of Poloxamer Content on Dissolution of Diltiazem Hydrochloride from Core Pellets (딜티아젬 함유 코아 펠렛으로부터 약물의 용출에 미치는 폴록사머 함량의 영향)

  • Lee, Seung-Woo;Kam, Sung-Hoon;Hong, Ji-Woong;Choi, Ki-Song;Park, Eun-Seok;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.32 no.4
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    • pp.305-311
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    • 2002
  • In order to evaluate the effect of poloxamer 407 content on the dissolution profiles of pellets, diltiazem HCl (DTL) core pellets were prepared with poloxamer 407 (50-90% w/w, with lactose as filler) using an extruder and a spheronizer. Any possible interaction between the drug and excipients was evaluated using DSC, IR and TLC. Dissolution tests were performed using USP basket method. In addition, scanning electron micrograph was performed to examine the surface roughness and cross sections. The release of DTL from the core pellets was decreased with increasing poloxamer 407 content. Cracks appeared on the surface of the core pellets with increasing the poloxamer 407 content, which may play a role on the retardation of the release of DTL from core pellets. There was no any significant interaction between the drug and excipients employed to prepare the core pellets.

Effects of Methods of Adding Barley Malt in the Production of Kanjang (Korean traditional soy sauce) on it's Chemical Compositions and Sensory Characteristics (한국 전통간장 제조시 맥아첨가방법이 간장의 성분과 식미에 미치는 영향)

  • Kwon, Kwang-Il;Lee, Jong-Gu;Lee, Ryun-Kyung;Choi, Jong-Dong;Ryu, Mun-Kyun;Im, Moo-Hyeog;Kim, Ki-Ju;Hong, Yeong-Pyo;An, Yeong-Sun;Choi, Kwang-Soo
    • Applied Biological Chemistry
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    • v.46 no.3
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    • pp.195-200
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    • 2003
  • Methods of adding barley malt as source of carbohydrates and enzymes in the production of kanjang in order to improve it's tastes and qualities were investigated. Soybean meju, soybean-malt meju and soybean meju cummalt was mashed with 20% salt brine in the ratio of 1:3 respectively, matured and analyzed the chemical compositions of the soy sauce mash samples for 150 days of maturing. Organoleptic evaluations for the matured soy sauce samples were done. The higher total nitrogen, TCA soluble nitrogen, O.D. at 500 nm, pure extract and lactic acid content could be observed with the soy sauce mash made of soybean-malt meju than those of contrast one from the beginning of the mashing throughout to the whole maturing period of 150 days. The higher the content of malt in the soybean-malt meju, the higher those content in the mash. But the lower content of those compositions in the soy sauce mash made of soybean meju cum malt than those in the contrast was found. The highest scores in all the sensory characteristics including 7.56 points, which were significantly different from that of contrast soy sauce at 5% level, in overall palatability were obtained by the soy sauce made of soybean-malt meju added with 30% malt in the organoleptic evaluations.

Evaluation of Methyl Methacrylate-Butyl Methacrylate Copolymer Films and Kinetics of Nitrofurazone Release (메칠메타크릴레이트-부틸메타크릴레이트 공중합체 필름의 평가 및 니트로푸라존 방출의 속도론적 연구)

  • Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.17 no.3
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    • pp.111-126
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    • 1987
  • Methyl methacrylate-butyl methacrylate copolymer (MMBM)-dibutyl phthalate (DBP) films were investigated as a potential topical drug delivery system for the controlled release of nitrofurazone. The kinetic analysis of release data indicated that drug release followed a diffusion-controlled granular matrix model, where the quantity released per unit area is proportional to the square root of time. DBP of several hydrophobic plasticizers selected was found to give the highest release of nitrofurazone. However, hydrophilic plasticizers such as propylene glycol and polyethylene glycol 400 had no controlled release properties and acceptable film formation. The effects of changes in film composition, drug concentration, film thickness, pH of release medium, and temperature on the in vitro release of nitrofurazone were analyzed both theoretically and experimentally. The release rate constant (k') was found to be proportional to DBP content, pH, and the temperature of release medium, but independent of film thickness, and drug concentration in a range of 0.1-0.4% by weight. The linear relationship was found to exist between the log k' and DBP content. The release of nitrofurazone from MMBM-DBP (8:2) films was found to be an energy-linked process. Two energy terms were calculated ; the activation energy for matrix diffusion was 13.45 kcal/mole, and the heat of drug crystal solvation was 27.26-29.34 kcal/mole. Observation of scanning electron micrographs and microscopic photographs showed that the incorporation of DBP in films increased markedly the particle size of nitrofurazone dispersed in the film matrix, comparing with the fine dispersion of nitrofurazone in pure MMBM film alone.

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Alginate/Carboxymethyl Scleroglucan Hydrogels for Controlled Release of Protein Drugs

  • Lee, Chang-Moon;Jeong, Hwan-Jeong;Kim, Dong-Woon;Lee, Ki-Young
    • Macromolecular Research
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    • v.16 no.5
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    • pp.429-433
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    • 2008
  • Alginate/carboxymethyl scleroglucan (CMSG) hydrogels were suggested as a novel carrier for the controlled release of protein drugs. The drug release characteristics of alginate hydrogels were improved by CMSG addition. Scleroglucan (Sclg) was carboxymethylated using monochloroacetic acid in aqueous alkaline medium. Alginate/CMSG hydrogels were prepared by dropping the mixture solution of alginate/CMSG into calcium chloride solution. The swelling behaviors and drug release characteristics of the hydrogels were investigated in the buffers of pH 1.2 or 7.4. As the CMSG content increased in the hydrogels, the swelling ratio of the alginate/CMSG hydrogel increased rapidly in the buffer of pH 7.4. At pH 1.2, however, the swelling ratio significantly decreased compared to that at pH 7.4. According to in vitro release tests, only 15% of ovalbumin, investigated as a model protein drug, was released from the alginate/CMSG hydrogels at pH 1.2 within 6 h. At pH 7.4, however, the drug release significantly increased due to the rapid swelling of the hydrogels. The release and swelling behaviors of the hydrogels could be controlled by changing the CMSG content in the hydrogels. These results supported the use of alginate/CMSG hydrogels as a suitable carrier for the controlled release of protein drugs in a pH responsive manner.

Identification of Cinnamon Components and Quantitative Determination of Cinnamlc Acid from Crude Drug Drink Preparations (생약복방 드링크제 중 계피성분의 확인 및 계피산의 분리정량)

  • 고성룡;김나미
    • Journal of Ginseng Research
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    • v.15 no.1
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    • pp.1-5
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    • 1991
  • For the quality control of crude drug drink preparations, methods for identification of cinnamon components and quantitative determination of cinnamic acid were established. Cinnamon components were identified by TLC with benzene/ethyl acetate (1:1, v/v) on silica gel plate by spraying p-anisaldehyde-sulfuric acid. Cinnamic acid contents were determined at UV 280 nm by HPLC on $\mu$-Bondapak Cls column with acetonitrile/water/acetic acid (40:60:2, v/v). Recoveries of cinnamic acid in three crude drug drink preparations were between 84.1-90.2% compared to the content of the cinnamon extract.

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Formulation and Pharmaceutical Properties of Mucoadhesive Film Containing Dipotassium Glycyrrhizate (구내염증 치료용 구강점막 필름제의 제제설계와 약제학적 성질)

  • Rhee, Gye-Ju;Lee, Duk-Keun;Sin, Kwang-Hyun;Park, Chong-Bum
    • Journal of Pharmaceutical Investigation
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    • v.29 no.2
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    • pp.127-136
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    • 1999
  • In order to eliminate demerits of conventional dosage forms, dipotassium glycyrrhizate was formulated as a slim mucoadhesive film type dosage form. The mucoadhesive drug layer gel containing dipotassium glycyrrhizate was prepared using $Noveon^{\circledR}$ AA-1, hydroxypropylcellulose-M, ethylcellulose N 100 and citric acid, and the protective layer gel by using ethylcellulose N 100, $Eudragit^{\circledR}$ RS and castor oil. The viscosity of drug layer gel of mucoadhesive film was enhanced as the increased amount of $Noveon^{\circledR}$ AA-1 or hydroxypropyl cellulose-M. The drug content was unifonnly $1160{\pm}14.6\;{\mu}g$, and was varied within 3.5%. The optimum film dosage form showed a good fluidity and malleability of drug layer, with 179 g of thickness, pH 5.7, 411 min of in vitro adhesion time and 172 g in gravity adhesive strength. The release time of drug from the mucoadhesive film was significantly shorter but was delayed when polymers such as ethylcellulose was added. From these results, the new mucoadhesive film may be effective for the treatment of aphthous stomatitis.

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Preparation of Nanoparticles in Drug Delivery System Using Guar Derivatives and Dialysis Method

  • Na, Kun;Kim, Yu-Eun;Lee, Ki-Young
    • Journal of Microbiology and Biotechnology
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    • v.9 no.1
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    • pp.50-55
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    • 1999
  • To develop a new form of controlled release dosage for administering for indomethacin (IND), two formulations of IND-loaded nanoparticles were designed based on polysaccharide (guar) derivatives. Nanoparticles prepared by the dialysis method were characterized with respect to morphology, size distribution, drug content, and in vitro drug release. Morphological studies by scanning electron microscopy (SEM) indicated that guar acetate (GA) nanoparticles were spherical in shape and had a smooth surface. The particle size distributions of formulation I (40mg of GA) and formulation II (80mg of GA) were shown to be $250.78\pm185.13nm$ and $718\pm145.90nm$ in distilled water ($20$^{\circ}C$), respectively. The drug loading efficiencies of nanoparticles were approximately 26% and 31% for formulations I and II, respectively. The differential scanning calorimetry (DSC) results indicated that the IND was perfectly distributed within GA nanoparticles. We also found, from the X-ray diffractometry analysis, that a decrease in the degree of crystallinity of the drug occurred in the nanoparticles. No changes between the original IND and the released IND from GA nanoparticles were detected by FT-IR. Using guar acetate, it is possible to design nanoparticles which allow the controlled release of IND over an extended period of time.

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