• 제목/요약/키워드: poloxamer

검색결과 117건 처리시간 0.022초

아세트아미노펜 액상좌제의 물리화학적 특성에 미치는 첨가제의 영향 (Effect of Additives on the Physicochemical Properties of Acetaminophen Liquid Suppository)

  • 최한곤;정재희;유제만;이미경;김인숙;이범진;김종국
    • 약학회지
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    • 제42권3호
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    • pp.290-295
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    • 1998
  • To optimize the formulation of acetaminophen liquid suppository, the effect of additives on the physicochemical properties of liquid suppository base was investigated. The physi cochemical properties of P 407/P 188 (15/15%) (abbreviated in 15/15) and P 407/P l88 (15/20%) (abbreviated in 15/20) were measured after the addition of following additives; 2.5% acetaminophen as an active ingredient, vehicle components (5% ethanol, 5% propylene glycol, 5% glycerin), preservatives (0.1% sodium benzoate, 0,1% methylparahydroxybenzoate, 0.1% propylparahydroxybenzoate) and 1% of sodium chloride as an ionic strength controlling agent. Poloxamer gel was prepared with three different buffer solutions (pH 1.2, 4.0 and 6.8) and the physicochemical properties, gelation temperature, gel strength and bioadhesive force, were determined. In the results, the effect of additives on the physicochemical properties was dependent on their bonding capacities including hydrogen bonding and cross-linking bonding. Because the hydrogen-bonding capacities of acetaminophen, ethanol and propylene glycol were smaller than that of poloxamer, the binding force of poloxamer gel became weak by their putting in between poloxamer gel. Therefore, the gelation temperature (15/15, $35.7^{\circ}C$ vs 37.0, 39.4 $38.2^{\circ}C$; 15/20, $29.2^{\circ}C$ vs 31.2, 32.0, $30.3^{\circ}C$) increased, and gel strength (15/15, 4.03 see vs 2.72, 2.08, 3.12sec; 15/20, 300g vs 50, 50, 200g) and bioadhesive force (15/15, $6.8{\times}10^2\;dyne/cm^2$ vs 3.2, 6.0, $6.0{\times}10^2\;dyne/cm^2$; 15/20, $97.3{\times}10^2\;dyne/cm^2$ vs 11.1, 89.5, $92.0{\times}10^2\;dyne/cm^2$) decreased. Furthermore, the binding force of poloxamer gel became strong due to the hydrogen-bonding capacities of glycerin and the cross-liking bonding of sodium salt. Then, the gelation temperature (15/15, 35.0, $32.1^{\circ}C$; 15/20, 26.0, $21.0^{\circ}C$) decreased, and gel strength (15/15, 6.51 see, 300g; 15/20, 500, 650g) and bioadhesive force (15/15, 7.2, $81.6{\times}10^2\;dyne/cm^2$; 15/20, 112.3, $309.2{\times}10^2\;dyne/cm^2$) increased. The effect of pH on the physicochemical properties of poloxamer gel was dependent on the ingredients with which the buffer solutions were prepared. Poloxamer gels prepared with pH 1.2 and 4.0 buffer solutions had the increasing gelation temperature (15/15, 37.5, $38.1^{\circ}C$; 15/20, 33.1, $34.0^{\circ}C$) and the decreasing gel strength (15/15, 2.98, 3.81sec; 15/20, 200, 200g) and bioadhesive force (15/15, $7.0{\times}10^2dyne/cm^2$; 15/20, $74.0{\sim}88.1{\times}10^2dyne/cm^2$) owing to HCl. Poloxamer gel prepared with pH 6.8 buffer solutions had the decreasing gelation temperature (15/15, $27.2^{\circ}C$; 15/20, $22.3^{\circ}C$) and the increasing gel strength (15/15, 400g; 15/20, 550g) and bioadhesive force (15/15, $207.0{\times}10^2dyne/cm^2$; 15/20, $215.0{\times}10^2dyne/cm^2$) due to the cross-linking bonding of $NaH_2PO_4\;and\;K_2HPO_4$.

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Lipid-lowering and Antioxidant Effects of Curcuma Radix in Poloxamer 407-induced Hyperlipidemia Model Rat Models

  • Park, So-Ae;Jo, Hyun-Kyung;Yoo, Ho-Ryong;Kim, Yoon-Sik;Seol, In-Chon;An, Joung-Jo
    • 대한한방내과학회지
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    • 제32권2호
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    • pp.243-258
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    • 2011
  • Objectives : This study investigated the hypolipidemic and antioxidant effects of Curcuma radix using a rat model induced by poloxamer 407 injection. Methods : Serum lipid parameters and oxidative stress-associated biomarkers were determined. Additionally, hepatic cholesterol and triglyceride as well as lipid metabolism-associated gene expressions were observed in hepatic tissue. Results : 1. Curcuma radix ameliorated elevation of serum cholesterol, triglyceride, LDL-cholesterol, MDA, hepatic cholesterol level, and reduction of serum TAC, SOD, GSH, GSH-reductase level. 2. Curcuma radix augmented up-regulated ACAT gene expression. 3. Curcuma radix almost completely ameliorated down-regulated CYP-7A1 but up-regulated HMG-CoA gene expression. Conclusions : The hypolipidemic and antioxidant properties of Curcuma radix were evidenced. This study provides a scientific basis for the clinical application of Curcuma radix and development of hypolipidemics using this herb in the future.

가시오갈피 줄기의 물 추출물이 지질대사에 미치는 영향 (Effects of the Water Extract from the Stem Bark of Acanthopanax senticosus on Hyperlipidemia in Rats)

  • 이연실;정상훈;임순성;지준;이상현;신국현
    • 생약학회지
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    • 제32권2호통권125호
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    • pp.103-107
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    • 2001
  • The effects of the water extract from the stem bark of Acanthopanax senticosus were evaluated on hyperlipidemic rats induced by lipid rich diet or poloxamer-407. The water extracts, when administered orally for 3 consecutive days in hyperlipidemic rats induced by poloxamer-407 (1 ml of 30%), was found to cause a significant decrease in plasma cholesterol and triglyceride concentrations. The water extracts, when treated orally for 5 consecutive days also showed a significant inhibition of serum total cholesterol and triglyceride level in rats treated with lipid rich diet (15% cholesterol, 1% sodium cholate and 84% com oil). HDL-cholesterol, however, was increased significantly.

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Preparation and Characterization of Quercetin-Loaded Solid Dispersion by Solvent Evaporation and Freeze-Drying Method

  • Park, Sang Hyun;Song, Im-Sook;Choi, Min-Koo
    • Mass Spectrometry Letters
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    • 제7권3호
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    • pp.79-83
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    • 2016
  • We prepared solid dispersion formulations of quercetin to enhance its solubility and dissolution rate. Various quercetin-loaded solid dispersion were tested with quercetin, poloxamer 407, and carrier such as hydroxypropyl methyl cellulose (HPMC), polyethylene glycol 8000 (PEG 8000), and polyvinylpyrrolidone K40 (PVP K40) using solvent evaporation and freeze drying methods in terms of both the aqueous solubility and the dissolution rates of quercetin. The solubility of quercetin as its solid dispersion formulations was markedly improved compared with that of quercetin powder. Especially, highest solubility of quercetin was observed when HPMC was used as a carrier. The cumulative dissolution of quercetin within 360 min from solid dispersion composed of quercetin, poloxamer 407, and HPMC was 8.8-fold higher than the dissolution of pure quercetin. The results of powder X-ray diffraction (XRD) and scanning electron microscope (SEM) indicated that quercetin transformed from a crystalline to an amorphous form through the solid dispersion formulation process. These results suggest that the solid dispersion formulation of quercetin with poloxamer 407 and HPMC could be a promising option for enhancing the solubility and dissolution rate of quercetin.

A Polymeric Micellar Carrier for the Solubilization of Biphenyl Dimethyl Dicarboxylate

  • Chi, Sang-Cheol;Yeom, Dae-Il;Kim, Sung-Chul;Park, Eun-Seok
    • Archives of Pharmacal Research
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    • 제26권2호
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    • pp.173-181
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    • 2003
  • A polymeric micelle drug delivery system was developed to enhance the solubility of poorly-water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The block copolymers consisting of poly(D,L-lactide) (PLA) as the hydrophobic segment and methoxy poly(ethylene glycol) (mPEG) as the hydrophilic segment were synthesized and characterized by NMR, DSC and MALDI-TOF mass spectroscopy. The size of the polymeric micelles measured by dynamic light scattering showed a narrow monodisperse size distribution with the average diameter less than 50 nm. The MW of mPEG-PLA, 3000 (MW of mPEG, 2 K; MW of PLA, 1K), and the presence of hydrophilic and hydrophobic segments on the polymeric micelles were confirmed by MALDI-TOF mass spectroscopy and NMR, respectively. Polymeric micelle solutions of DDB were prepared by three different methods, i.e. the matrix method, emulsion method and dialysis method. In the matrix method, DDB solubility was reached to 13.29 mg/mL. The mPEG-PLA 2K-1K micelle system was compared with the poloxamer 407 micelle system for their critical micelle concentration, micelle size, solubilizing capacity, stability in dilution and physical state. DDB loaded-polymeric micelles prepared by the matrix method showed a significantly increased aqueous solubility (>5000 fold over intrinsic solubility) and were found to be superior to the poloxamer 407 micelles as a drug carrier.

개에서 Poloxamer / Sodium Alginate 혼합물의 복강 유착 방지 효과 (The Effects of Poloxamer/Sodium Alginate Mixture Barriers on Prevention of Post-Operative Peritoneal Adhesion in Dogs)

  • 김지훈;장광호
    • 한국임상수의학회지
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    • 제26권4호
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    • pp.324-330
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    • 2009
  • 이 실험의 목적은 개에서 poloxamer/sodium alginate 혼합물(PX/SA)의 수술 후 복강 유착 방지 효과를 알아보는 것이다. 잡종견 15마리를 무처치군, 2% Sodium carboxymethylcellulose(SCMC)처치군, PX/SA 처치군으로 각각 5마리씩 배치하였다. 유착은 돌창자의 창자간막 대측에 1 ${\times}$ 1 cm 크기로 미세 점상 출혈 찰과상을 일으켜 유도하였다. SCMC 용액은 카테터를 통하여 복강내 주입하였고, PX/SA는 찰과상 부위에 단순히 도포하였다. 수술 전 1일과 수술 후 1일, 4일, 7일, 14일에 정맥에서 혈액을 채취하여 적혈구수, 총백혈구수, 섬유소원농도를 분석하고, 수술 후 21일에 유착정도를 computerized tensiometer를 이용하여 분석하였다. 적혈구수, 총백혈구수, 섬유소원농도는 각 군간에 유의성은 없다. 유착부 분리에 필요한 평균 장력은 무처치군에서 173.05 ${\pm}$ 113.48 gf, SCMC 처치군에서 111.42 ${\pm}$ 38.25 gf, PX/SA 처치군에서 69.00 ${\pm}$ 45.07 gf였다. PX/SA 처치군의 평균 분리 장력이 다른 두 군에 비하여 유의성 있게 낮았다 (p < 0.05). 본 실험 결과로 PX/SA는 SCMC용액과 비교하여 복강유착을 감소시키는 것으로 보아 PX/SA를 개에서 복강 수술 후 유착 방지에 적용 가능한 것으로 생각한다.

Antioxidant and Lipid-lowering Effects of Artemisia capillaris on a Rat Model of Hyperlipidemia

  • Jang, Woo-Seok;Kim, Yoon-Sik;Seol, In-Chan
    • 대한한의학회지
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    • 제33권2호
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    • pp.11-24
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    • 2012
  • Objectives: This study was designed to evaluate lipid-lowering and antioxidant effects of Artemisia capillaris(A. capillaris) using a model of hyperlipidemic rats induced by poloxamer-407. Methods: Rats were previously treated by A. capillaris water extract, and intraperitoneally injected by poloxamer-407 to induce hyperlipidemia. Parameters of serum lipid and oxidative stress biomarkers were determined. Results: 1. A. capillaris ameliorated the elevation of serum total cholesterol, triglyceride, LDL-cholesterol and MDA level. 2. A. capillaris ameliorated the reduction of serum TAC and SOD activities. 3. A. capillaris ameliorated the reduction of serum GSH and GSH-reductase level. Conclusions: According to these results, A. capillaris can be used to treat hyperlipidemia or as basis for making new drugs for treating hyperlipidemia in the future.

Enhanced Dissolution of Coenzyme Q10 using Solid Dispersions Prepared by Low Temperature Melting Method

  • Kang, Jun-Heok;Yan, Yi-Dong;Kim, Hyun-Chan;Lee, Sung-Neung;Yong, Chul-Soon;Choi, Han-Gon
    • Journal of Pharmaceutical Investigation
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    • 제40권5호
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    • pp.277-283
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    • 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.

Poloxamer-407로 유도한 고지혈증 동물모델에서 Quercetin-3-O-rhamnoside 및 어성초 분획물의 항고지혈증 효과 (Anti-hyperlipidemic Effect of the Isolated Component, Quercetin-3-O-rhamnoside and the Fractions from the Extract of Houttuynia Cordata in Mice)

  • 김도국;김세건;암릿파우델;정태숙;정현주
    • 생약학회지
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    • 제43권2호
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    • pp.101-106
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    • 2012
  • The anti-hyperlipidemic effect of Houttuynia cordata was assessed in poloxamer-407 induced hyperlipidemic mice model. The butanol fraction and its isolated compound, quercetin-3-O-rhamnoside, significantly reduced the blood triglyceride and total-cholesterol level and increased the blood HDL-cholesterol level. They also showed the significant reductive effect on the blood AST and ALT level, rising in proportion to the liver damage, in hyperlipidemic mice.

PLGA 나노파티클로부터 수용성 블루 덱스트란의 서방성 방출 (Sustained Release of Water-Soluble Blue Dextran from PLGA Nanoparticles)

  • 류상화;황성주;박정숙
    • Journal of Pharmaceutical Investigation
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    • 제36권2호
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    • pp.109-114
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    • 2006
  • Biodegradable poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles were developed for sustained delivery of water-soluble macromolecules. PLGA nanoparticles were fabricated by spontaneous emulsification solvent diffusion method generating negatively charged particles and heterogeneous size distribution. As a model drug, blue dextran was encapsulated in PLGA nanoparticles. In addition, nanoparticles were also prepared with varying ratio of poloxamer 188 (P188) and poloxamer 407 (P407), and coating with poly(vinyl alcohol) (PVA). Then, the particle size, zeta potential and encapsulation efficiency of nanoparticles containing blue dextran were studied. In vitro release of blue dextran from nanoparticles was also investigated. The surface and morphology of nanoparticles were characterized by scanning electron microscopy (SEM). In case of nanoparticles prepared with PLGA, P407, and different organic solvents, particle size was in the range of $230{\sim}320\;nm$ and zeta potentials of nanoparticles were negative. The SEM images showed that ethyl acetate is suitable for the formulation of PLGA nanoparticles with good appearance. Moreover, ethyl acetate showed higher encapsulation efficiency than other solvents. The addition of P188 to formulation did not affect the particle size of PLGA nanoparticles but altered the release patterns of blue dextran from nanoparticles. However, PVA, as a coating material, altered the particle size with increasing the PVA concentration. The nanoparticles were physically stable in the change of particle size during long-term storage. From the results, the PLGA nanoparticles prepared with various contents of poloxamers and PVA, could modulate the particles size of nanoparticles, in vitro release pattern, and encapsulation of water-soluble macromolecules.