• 약학회지
• /
• 제41권5호
• /
• pp.607-614
• /
• 1997

Flurbiprofen- and flurbiprofen axetil-loaded microemulsions composed of soybean oil, poloxamer 407, glycerine and water were prepared by generator-type homgenizer and ultrasoni c probe system. The particle size of microemulsions was measured by the dynamic light scattering method. The pharmacokinetics and organ distribution of flurbiprofen were investigated after intravenous injection of flurbiprofen solution, flurbiprofen-loaded microemulsion and flurbiprofen axetil-loaded microemulsions equivalent to 10mg/kg of flurbiprofen to rats. Blood samples were collected from the anterior ciliary artery of rats for 24hr, and flurbiprofen in plasma and organs was analyzed by HPLC. Stable microemulsions were prepared. Even though there is a little change in droplet size just after the preparation, no creaming and no separation were occured during the storage period for 6 months at 4, 21, 37 and 45$^{\circ}C$. Pharmacokinetic parameters and organ distribution of flurbiprofen after intravenous injection of flurbiprofen- and flurbiprofen axetil-loaded microemulsions emulsified with poloxamer 407 were not significantly different from those of commercial lipid microemulsion emulsified with lecithin. Therefore, it is concluded that flurbiprofen- and flurbiprofen axetil-loaded microemulsion prepared with poloxamer 407 could be used as a parenteral formulation.

• Journal of Pharmaceutical Investigation
• /
• 제37권1호
• /
• pp.39-43
• /
• 2007

Previously, we have reported that PLGA nanoparticles were prepared for sustained release of water-soluble blue dextran and the particle size, in vitro release pattern and encapsulation were modulated by varying polymers. This study was designed to encapsulate plasmid DNA in PLGA nanoparticles and to investigate the effect of Polymers and temperatures. PLGA nanoparticles were fabricated with poloxamer 188 (P188) or poloxamer 407 (P407) by using spontaneous emulsification solvent diffusion method. As a model plasmid DNA, pCMV-Taq2B/1L-18 was encapsulated in PLGA nanoparticles. Then, the particle size, zeta potential and encapsulation efficiency of nanoparticles containing plasmid DNA were investigated. Particle sizes of PLGA nanoparticles prepared with P188 and P407 were in the range of 200-330 nm and 250-290 nm, respectively. Zeta potentials of nanoparticles were negative regardless of nanoparticle compositions. Encapsulation efficiency of P407 nanoparticles prepared at $30^{\circ}C$ was higher than those at other preparation condition. From the results, the PLGA nanoparticles prepared with poloxamers at different temperature, could modulate the particles size of nanoparticles, and encapsulation efficiency of plasmid DNA.

• 대한한방내과학회지
• /
• 제26권4호
• /
• pp.820-827
• /
• 2005

연구목적: 본 연구는 Poloxamer-407로 유발시킨 고지혈증에 대한 청간탕의 효과를 알아보기 위해 수행되어졌다. 실험방법: Poloxamer-407로 쥐에 고지혈증을 유발시킨후 청간탕과 Lipidil을 경구 투여하여 혈청 cholesterol, 고밀도 지단백, 중성지질을 측정하였으며, 지질대사와 관련된 ACAT, DGAT, $CYP7{\alpha}H$, LDL receptor의 gene expression을 RT-PCR를 통해 비교 분석하였다. 실험결과: 청간탕 투여군은 혈청 콜레스테롤을 각각 32% 와 65% (p<0.05)로, 혈청 중성지방을 각각 21% 와 51% (p<0.05)로 감소시켰다. 또한, 청간탕은 LDL 수용체와 $CYP7{\alpha}H$ 유전자 발현을 증가시켰다. 결론: 이상의 연구로부터 우리는 청간탕이 지질의 흡수, 저장을 억제하고 콜레스테롤의 분비를 촉진함으로써 고지혈증에 일정한 효과가 있음을 알 수 있었다.

• 한국식품영양과학회지
• /
• 제32권7호
• /
• pp.1126-1131
• /
• 2003

인류는 질병에 대한 예방 및 치료에 주로 합성 의약품을 사용하여 왔으나 근래에 이르러 여러 가지 합성 의약품의 부작용 또는 독성이 밝혀짐에 따라 세계적으로 천연자원으로부터의 의약품 개발이 활발히 추진되고 있다. 한편, 우리나라를 위시한 동양에서는 오랜 시일을 통하여 많은 식물을 치료제로 사용하여 왔으나 약화학적 및 약리학적 검토 자료는 지금에 와서 많이 도출되고 있으며 다양한 연구가 이루어지고 있는 실정이다. 본 연구에서는 해양생물로부터 생리활성을 검색할 목적으로 검은 밀복으로부터 제독처리하여 추출, 정제한 검은 밀복 간유를 대상으로 항피로효과, 간기능에 미치는 영향 및 poloxamer-407로 유도되는 고지혈증에 대한 효과를 검색한 결과, 다음과 같은 결론을 얻었다. 첫째, 식품위생학적 안전성 여부를 조사하기 위하여 검은밀복 간유의 정제품을 mouse assay로 그 잔류 독성을 조사한 결과 모두 무독하였다. 둘째, 생쥐를 유영하게 하여 사망하는 시간을 측정하여 본 결과 정상 생쥐에서는 사망시간보다 복어간유를 용량별로 2주일간 경구투여하였을때 사망 시간은 용량 의존적으로 증가되었다. 셋째, 간장해의 유발 약물로 사염화탄소 및 D-galactosamine(GaIN)을 사용하여 복어로부터 추출한 복어간유를 투여한 결과 사염화탄소 및 GaIN을 투여하였을 때 혈중 AST, ALT 및 SDH의 활성이 정상군에 비하여 현저히 증가되던 것이 복어간유의 전처리로 현저히 억제되었다. 넷째, 혈청 중 중성지방 및 total cholesterol의 함량은 정상군에 비하여 poloxamer-407의 투여로 증가되던 것이 복어간유를 용량별로 투여함으로써 현저히 감소되었다. 한편 poloxamer-407로 유도된 고지혈증의 실험동물의 bleeding time이 복어간유의 투여로 연장되었으며 plasma clotting time도 증가되었다.

• 생약학회지
• /
• 제35권2호통권137호
• /
• pp.143-146
• /
• 2004

The effects of the MeOH and water extracts from the marine algae Pelvetia siliquosa were evaluated on hyperlipidemic rats induced by cholesterol rich diet or poloxamer-407. The MeOH and water extracts, when administered orally for 3 consecutive days in hyperlipidemic rats induced by poloxamer-407 (1 ml of 30%), were found to cause a significant decrease in plasma cholesterol and triglyceride concentrations. Both extracts also showed a significant inhibition of serum total cholesterol and triglyceride level in rats treated with cholesterol rich diet. HDL-cholesterol, however, was increased significantly.

• 식품보건융합연구
• /
• 제4권4호
• /
• pp.1-9
• /
• 2018

To determine the effect of Vitex doniana (leaves stem and root bark) ethanolic extracts on lipid profiles of Poloxamer 407 (P407) induced hyperlipidemic and normal rats. Fifty four mixed sex rats weighing 100-200g were divided into nine groups comprising six animals per group. At the end of the 21 day, the animals were sacrificed and blood sample were collected for determination of serum levels of: Total cholesterol (TC), Triacylglycerides (TAG), High-density lipoprotein cholesterol (HDL-c) and Low-density lipoprotein cholesterol (LDL-c). The studies showed that all induced treated groups significantly (P<0.05) lower serum levels of TC, TAG, LDL-c and significantly (P<0.05) increased HDL-c when compared to the P407 induced hyperlipidemic control. The normal treated groups showed no significant (P>0.05) difference in the serum levels of TC, TAG, LDL and HDL when compared to the normal control group. Calculation of atherogenic risk predictor indices of the induced treated groups showed that all the extracts significantly (P<0.05) lowered the LDL-c/HDL-c, log (TAG/HDL-c) and significantly (P<0.05) increased HDL-c/TC ratio when compared to the P407 induced hyperlipidemic control group. The atherogenic risk predictor indices of normal treated groups showed no significant difference (P>0.05) in LDL-c/HDL-c, Log (TAG/HDL-c) and HDL-c/TC ratio when compared to the normal control group. The study demonstrates the phytotherapeutic effect of Vitex doniana (leaves, stem and root bark) ethanolic extract in poloxamer 407 induced hyperlipidemia.

• Journal of Pharmaceutical Investigation
• /
• 제25권2호
• /
• pp.129-136
• /
• 1995

In order to reduce the systemic side effects and the gastrointestinal irritation of indomethacin following its oral administration, the drug was formulated as a transdermal gel using poloxamer 407. In vitro diffusion cells fitted with excised rat skins were used to evaluate the effects of formulation variables on skin permeation of indomethacin from poloxamer gels. The formulation variables were the concentrations of indomethacin, poloxamer 407 and ethanol, and the gel pH. The increase of the drug amount in the gel from 0.5% to 2.0% induced a direct but nonlinear increase in the skin permeation rate of indomethacin. The increase of poloxamer concentration from 17.5% to 25% in the gel resulted in a decrease of skin permeation rate of indomethacin, which was due to a reduction in the amount of free drug molecules available for permeation through skin by entrapping more drug molecules within the micelles formed by poloxamer. The increase of ethanol concentration from 10% to 20% in the gel resulted in a linear increase of permeation rate of indomethacin through skin, possibly due to the penetration enhancing effect of ethanol. The skin permeation of indomethacin was substantially influenced by the gel pH, exhibiting a maximum at pH 4.

• Journal of Pharmaceutical Investigation
• /
• 제25권3호
• /
• pp.177-184
• /
• 1995

In order to formulate an aqueous topical preparation of epidermal growth factor(EGF) for the treatment of open wound and bum, the stability of EGF in aqueous vehicles containing various stabilizers was evaluated and the pharmacological activity of gel preparations formulated with poloxamer 407 was determined with wound model. Various additives, which are known as potent stabilizers for proteins and polypeptides so far, were used to increase the stability of EGF in aqueous vehicles. The contents of EGF in the vehicles containing stabilizers were determined with an HPLC method after the storage at $37^{\circ}C$. EGF was more stable in ultrapure water than RO water or saline. All the additives studied resulted in deleterious effects on EGF stability. Therefore, it was speculated that any additives or impurities in the vehicle made EGF unstable. However, nitrogen purge of solution increased the stability of EGF in aqueous vehicles. The aqueous topical preparations of EGF were formulated with poloxamer 407 as a gel base in saline. Gelatin or amastatin was employed as a protease inhibitor. The pharmacological effect of EGF gel was studied with open wound model in mice. EGF preparations, made of oleaginous base or poloxamer gel base, showed significant healing effect compared to the control group(p<0.05). The addition of protease inhibitor in poloxamer 407 gel resulted in significant healing effect compared to the gel without it(p<0.05). Body weights of mice treated with EGF preparation were increased at the first day after the formation of open wound, while those of the control group were decreased. The EGF gel made of poloxamer 407 containing a pretense inhibitor would be a promising aqueous topical preparation for EGF.

• Journal of Pharmaceutical Investigation
• /
• 제40권5호
• /
• pp.277-283
• /
• 2010

CoQ with low melting temperature was exploited to improve its solubility by preparing its solid dispersions (SDs) with a meltable polymer, poloxamer 407 (P 407). P407 can be utilized for a relatively simple, quick, inexpensive, reproducible and potentially scalable manner in the low temperature melting method. CoQ 10 solubility and dissolution increased with increasing concentrations of P 407 in SDs. Comparison of the enhanced dissolution of CoQ 10 from different poloxamers suggested that the preparation of CoQ 10 SDs using P 407 as a meltable hydrophilic polymer carrier could be a promising approach to improve its dissolution.

• Journal of Pharmaceutical Investigation
• /
• 제32권4호
• /
• pp.299-303
• /
• 2002

The oral bioavailability of itraconazole is variable and low in fasting state. This is mainly due to the low solubility of this drug. Bioavailability can be improved by changing the formulation and it is general that the liquid preparations show greater bioavailability than the solid dosage forms such as tablets and capsules do. Benzyl alcohol-water binary mixture showed the excellent solubilizing capacity for itraconazole but the release of the drug from the preparation needs to be enhanced. In this study, various nonionic surfactants and hydrophilic polymers, poloxamers, were screened to investigate their effects on the releasε of itraconazole from the liquid preparations. Poloxamer 407 showed the most enhancing effect on the drug release and the release rate was proportional to thε amount of poloxamer 407 added. A liquid preparation of itraconazole, consisting of benzyl alcohol/water/poloxamer 407 ternary solvent system, releasεd more than 80% of the total drug amount at 5 min and showεd the possibility of a new formulation development.