• Title/Summary/Keyword: poloxamer-407

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Preparation and Evaluation of Liquid Suppository Containing Prostaglandin $E_1-loaded$ Microemulsion (프로스타글란딘 $E_1$ 마이크로에멀젼이 함유된 액상좌제의 제조 및 평가)

  • Kim, Chung-Hwan;Lee, Sa-Won;Park, Kyung-Mi;Choi, Han-Gon;Kim, Chong-Kook
    • Journal of Pharmaceutical Investigation
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    • v.30 no.3
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    • pp.167-172
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    • 2000
  • The purpose of this study is to develop a transurethral liquid suppository containing prostaglandin $E_1\;(PGE_1)-loaded$ microemulsion, which undergoes a phase transition to gels at body temperature. The effects of oils, ethanol as solvent and HCl as pH-controlling agent on the physicochemical properties of liquid suppositories composed of poloxamer P 407, P 188 and carbopol was investigated. The stability of $PGE_1$ and release of $PGE_1$ from liquid suppository were evaluated. Oils such as Neobee and soybean oil significantly decreased the gelation temperature but increased the gel strength of liquid suppository due to their strongly binding with the components of liquid suppository base. However, ethanol slightly did the opposite. The pH of liquid suppositories hardly affected the gelation temperature and gel strength due to addition of very small HCl (0.005-0.01%). A liquid suppository [$PGE_1/P$ 407/P 188/carbopol/Neobee/ethanol/HCl (0.2/14/14/0.4/7/2/0.005%)], which had the gelation temperature $(34.2{\pm}0.6^{\circ}C)$ and gel strength $(31.35{\pm}4.37\;sec)$ suitable for liquid suppository system, was easily administered and not leak out from the body. About 60% of $PGE_1$ was released out within 2 h from this formulation. It was shown that the release of $PGE_1$ was proportional to the square root of time, indicating that $PGE_1$ might be released from the suppository by Fickian diffusion. It was stable at $4^{\circ}C$ for at least 2 months. The results suggest that transurethral liquid suppository containing prostaglandin $E_1-loaded$ microemulsion is thought to be a convenient, safe and effective dosage form for $PGE_1$. However, it should be further developed as a more convenient and stable dosage form for $PGE_1$.

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Effect of Allium Victorialis Var. platyphyllum Leaves on Triton WR-1339-Induced and Poloxamer-407-Induced Hyperlipidemic Rats and on Diet-Induced Obesity Rats (식이성 고지혈 및 비만에 대한 산마늘 추출물의 효과)

  • Choi, Jong-Won;Lee, Kyung-Tae;Kim, Won-Bae;Park, Kwang-Kyun;Chung, Won-Yun;Lee, Jin-Ha;Lim, Sang-Cheol;Jung, Hyun-Ju;Park, Hee-Juhn
    • Korean Journal of Pharmacognosy
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    • v.36 no.2 s.141
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    • pp.109-115
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    • 2005
  • The herb of Allium victorialis var. platyphyllum (Liliaceae) has been used as an edible wild herb and to treat heart failure and gastritis. We have already reported antihyperlipidemic anti-tumor effects of this plant. To enlarge the commercial availability of this food, it was investigated whether the extracts of A. victorialis var. platyphyllum reduce hyperlipidemia and obesity or not. The plants tested in this experiment were collected from two eco-types of Is. Ullung and Mt. Odae cultivated at Pyongchang. Extracts were prepared by extracting the fresh leaves and those dried at $36^{\circ}C$ and $90^{\circ}C$, respectively. Pretreatment with the ethanolic extracts for two weeks(p.o.) reduced serum triglyceride-, total cholesterol- and LDL-cholesterol contents in rats induced by Triton WR-1339, respectively. Furthermore, oral administration of the extracts also inhibited the hyperlipidemia induced with oral diet of 30% corn oil. In the other attempt to find to alleviate the obesity, the model rats with obesity were induced by the high fat-diet for six weeks. Post-treatment with the extracts for two weeks significantly reduced the hyperlipidemia. Retroperitoneal-, epidymal- and total abdominal fat pad weights were considerably reduced at 100 mg/kg oral administration of the extracts. Increased feces lipid contents were also found in the rat treated with the extracts. The extract may lead to the higher activity in treatment of hyperlipidemia and obesity than of the dried one.