• Title/Summary/Keyword: lipophilic

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THE ACUTE TOXICITY TEST OF A NOVEL MICELLAR SOLUBILIZER FOR USE WITH INJECTABLE ANTICANCER AGENTS

  • Kim, Y.W.;Min, K.N.;Pan, S.R.;Ok, K.E.;Lee, M.J.;Kim, J.J.;Sheen, Y.Y.
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.05a
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    • pp.130-130
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    • 2001
  • The commercially available paclitaxel product, Taxol$\circledR$ is currently formulated in a vehicle containing approximately a 1:1 v/v mixture of polyoxyethylated castor oil (Cremophor EL) and ethanol. Cremophor EL, a commonly used surfactant for lipophilic compounds, has been associated with many issues, such as adverse effects particularly following rapid administration, stability with the possibility for drug precipitation upon dilution, and filtering requirements.(omitted)

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Effect of Suppository Bases on Absorption of Lithium Carbonate (좌제기제가 탄산리튬의 흡수에 미치는 영향)

  • Kim, Yong-Hyun
    • Journal of Pharmaceutical Investigation
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    • v.16 no.4
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    • pp.148-151
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    • 1986
  • This paper was designed to investigate the influence of different suppository bases on both the rectal absorption and dissolution rate of lithium carbonate, and to compare bioavailability from rectal administration with that from oral administration. The dissolution rates were in such order as PEG 4000, surfactant A (Witepsol 15+sodium lauryl sulfate), surfactant B (Witepsol 15+cholic acid), Witepsol 15 and cacao butter. Among various suppository bases, the blood level of lithium carbonate after rectal administration was increased in the following order: surfactant A>surfactant B>PEG 4000>Witepsol 15>cacao butter. When it comes to compare oral with rectal administration in AUC values, surfactants and PEG 4000 showed similar blood levels to oral administration, but lipophilic bases such as Witepsol 15 and cacao butter showed far lower blood level than oral administration. Peak time in oral administration was 2 hrs, but those in rectal administration using various suppository bases were $6{\sim}8$ hrs.

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Parenteral Docetaxel Emulsion System and Its Stability

  • Kim, Hyun-Jo
    • Journal of Pharmaceutical Investigation
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    • v.39 no.1
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    • pp.13-18
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    • 2009
  • Docetaxel is an anticancer agent with low aqueous solubility. More extensive clinical use of this drug is somewhat delayed due to lack of appropriate delivery vehicles. An attempt was made to adopt an o/w emulsion as the drug carrier which incorporated docetaxel in the propyleneglycerol stabilized by a mixed-emulsifier system. A suitable formulation was found in this study: 10 mg/mL docetaxel, 10% (w/v) oil blend, 4% (w/v) PG, 3% (w/v) Solutol HS 15 in 2.25% (w/v) glycerol solution. The formulated emulsion has very good stability when stored at $40^{\cird}C$, and the docetaxel containment efficiency can be maintained above 95% and the mean emulsion diameter around $10{\mu}m$ for at least 3 months. The formulated emulsion is a promising carrier for docetaxel and other lipophilic drugs.

Oxidations product of ${\alpha}-,\;{\gamma}-tocopherol$ and ${\gamma}-tocotrienol$ (${\alpha}-,\;{\gamma}-Tocopherol$${\gamma}-tocotrienol$의 산화 생성물)

  • Lee, Hyung-Ok
    • Applied Biological Chemistry
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    • v.36 no.1
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    • pp.33-37
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    • 1993
  • Oxidations products of ${\alpha}-tocopherol$, ${\gamma}-tocopherol$ and ${\gamma}-tocotrienol$ in lipophilic reaction media were studied. ${\alpha}-Tocopherylquinone$, ${\gamma}-tocopherylquinone$ and ${\gamma}-tocotrienylquinone$ were fractionated using micro column, isolated and identified by HPLC and MS.

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돼지 Cytochrome P450 Aromatase의 새로운 기능

  • 최인호
    • Proceedings of the KSAR Conference
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    • 2003.06a
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    • pp.3-5
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    • 2003
  • 여성호르몬으로 잘 알려진 estrogen은 난소의 granulosa 세포와 정소의 Sertoli 세포에서 주로 생성되는 것으로 알려져 있으며 최근엔 사람의 지방, 근육, 뇌, 뼈세포 등에서의 합성 가능성과 각 조직에서 생성되는 estrogen 의 생리학적인 기능에 관해 많은 관심이 모여져 왔다. 다른 steroid처럼 지방친화적인 (lipophilic) estrogen은 세포막과 핵막을 쉽게 통과하여 목표세포 (target cell)의 핵에 존재하는 estrogen receptor (ER)에 결합하여 특정 유전자를 발현에 관여하는 것으로 알려져 있다. Cytochrome P450 Aromatase (간략히, aromatase)는 steroid hormone을 합성하는 마지막 단계에서 androgens을 estrogens으로 전환시키는데 관여하는 효소이다. Aromatase의 substrate (기질)로 사용되는 androgen에는 androstenedione과 testosterone 등이 있으며, 최종 산물로써 estrone(E1)이나 17$\beta$-estradiol(E2) 등의 estrogen이 생성된다. Aromatase는 steroidogenic tissues의 세포내 골지체에 존재하는 것으로 알려져 있으며, NADPH-cytochrome P450 reductase와 함께 복합체로써 존재한다. NADPH-cytochrome P450 reductase는 다른 steroid hormone에 관여하는 효소들과도 복합체를 형성하여 다른 steroid hormone을 합성할 수 있으므로, 어떤 조직에서 여성호르몬이 만들어질 수 있느냐 하는 것은 그 조직에서 aromatase 단백질이 만들어지느냐에 따라서 결정된다.

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THE RELATIONSHIP OF INTESTINAL ABSORPTION CLEARANCE AND PARTITION COEFFICIENT OF NINE BETA-BLOCKERS IN RATS

  • Cho, Hea-Young;Lee, Suk;Kang, Hyun-Ah;Lee, Yong-Bok
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.411.3-412
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    • 2002
  • On the basis of recognizing that physicochemical properties (lipophilic/hydrophilic), intestinal absorption clearance and pharmacokinetic characteristics of drug are the fundamental parameters controlling the rate and the extent of drug absorption, the biopharmaceutics classification system for the correlation between drug lipid- solubility and intestinal absorption clearance is proposed. (omitted)

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Study on of Extraction Methods of Saponin in Ginseng Products (인삼제품의 Saponin 추출방법에 관한 연구)

  • 손현주;장진규
    • Journal of Ginseng Research
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    • v.8 no.1
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    • pp.32-37
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    • 1984
  • In order to shorten the extraction time of saponin in ginseng products, election with Extrelut column and phase-separation methods were compared. The results obtained are as follows. 1. Saponin of ginseng products was extracted completely within 3 hours by election method with Extrelut column, and the rate of removing glucose by the column was increased with increasing glucose content in ginseng products. 2. Stirring method was superior to refluxing method for removing sugars from ginseng products, and removing rate was deceased in the order of lactose, sucrose and glucose. 3. Extraction rate of ginsenoside from ginseng extracts by the elution method was nearly same as that of phase-separation method; however, the former was much higher than the latter in the case of ginseng teas. Therefore, the elution by Extrelut column is to be improper for extraction of saponin in ginseng tea which contains much sugar. It was necessary to remove lipophilic compounds for extraction of saponin from ginseng extracts by elution with Extrelut column.

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Effects of Polygonatum odoratum on Mercuric Chloride Induced Renal Failure Rats (둥굴레의 승홍으로 유도된 흰쥐 신부전에 미치는 영향)

  • Kim, Ju-Hyang;Yang, Ki-Sook
    • Korean Journal of Pharmacognosy
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    • v.33 no.3 s.130
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    • pp.200-206
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    • 2002
  • The rhizoma of Polygonatum odoratum (Liliaceae) has been used as the treatment of body fluid deficiency, dryness symptoms and hyper glycemia. To study effects on acute renal failure of P. odorati rhizoma, urinary volume, urinary electrolytes and serum factors associated with renal dysfunction were measured in $HgCl_2-induced$ acute renal failure rats. It was revealed that its ether ex. had significant diuretic effects, regulated hypoelectrolytes$(Na^+,\;K^+,\;Cl^-)$ and inhibited the increase of creatinine, BUN in acute renal failure rats. From the ether ex. which was more effective than MeOH ex., three lipophilic compounds were isolated and elucidated hydrocarbon(l), ${\beta}-sitosteryl$ stearate(2), ${\beta}-sitosterol$(3). The ${\beta}-sitosteryl$ stearate(2) were isolated from Polygonatum sp. at first.

Effect of the Cultivated Fruit body of Phellinus linteus on Low Density Lipoprotein Oxidation (배양상황버섯의 저밀도지질단백질 (LDL)산화에 미치는 영향)

  • 정은주;성재모;양기숙
    • YAKHAK HOEJI
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    • v.48 no.2
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    • pp.130-134
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    • 2004
  • Phellinus linteus (Hymenocaetaceae) has been used for the treatment of gastric cancer, noninsulin dependant diabetes, diarrhea, and menstrual irregularity. The antioxidative effect of cultivated fruit body of Phellinus linteus on low density lipoprotein oxidation was investigated. The MeOH and water extracts were examined by TEARS assay on human plasma LDL in vitro system. The MeOH ex. showed antioxidative activity, and then was fractionated into Precipitates, Water Insoluble fr., Water fro and ether fro The results showed that the lipophilic fractions, Water Insoluble fr. and Ether fr. of cu 1-tivated fruit body of Phellinus linteus, inhibited the oxidative modification of LDL.

Candelilla Wax Nanoemulsions Prepared by Phase Inversion Composition (PIC) Method

  • Kim, Eun-Hee;Cho, Wan-Goo
    • Journal of the Korean Applied Science and Technology
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    • v.31 no.2
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    • pp.203-209
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    • 2014
  • Candelilla wax-in-water nanoemulsions stabilized by Span 80/Tween 80 were prepared by the phase inversion composition (PIC) method. Stable nanoemulsions with droplet diameters below 50 nm could be formed when the hydrophilic-lipophilic balance (HLB) values were between 13.5 and 14.5, surfactant concentration was 5.0 wt%, and the surfactant-wax ratio was 1:1. Increased emulsification temperature and cooling rate were found to improve the emulsion properties. Process of PIC (adding aqueous phase to the wax phase) produced smaller droplet size nanoemulsion compared to the process of adding wax phase to the aqueous phase. The stability of these nanoemulsions was assessed by following the change in droplet diameters with time of storage at room temperature (${\sim}25^{\circ}C$). The size remained constant during 2 months storage time.