• Journal of Pharmaceutical Investigation
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• v.39 no.4
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• pp.249-255
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• 2009

The main object of this study was to prepare of w/o emulsion including glyceryl monooleate(GMO) and to evaluate its stability by using the recently developed $Turbiscan^{(R)}LAB$. GMO is the polar oily surfactant with the low HLB value, and it forms the gel phase of cubic structures after dissolves in aqueous media. Phosphate buffer solution (PBS) of pH 7.4 was prepared as the water phase and Marcol 52(mineral oil) was used as the oil phase in this study. GMO was used as the surfactant of W/O emulsion. W/O emulsion using GMO alone as a surfactant was very unstable. But the emulsion using both GMO and poloxamer 407 was more stable. The stability of W/O emulsions was evaluated after centrifuging the emulsions. But it was difficult with naked eye because an opaque and concentrated system like W/O emulsion was very turbid. So $Turbiscan^{(R)}LAB$ was used to detect the destabilization phenomena in non-diluted emulsion. As a result, the W/O emulsion using the proper amounts of GMO and poloxamer 407 was more stable among them using GMO of various amounts. But it seems that the other element for the stability of W/O emulsion including GMO was required. Furthermore, the $Turbiscan^{(R)}LAB$ was a very efficient analyzer for evaluating the physical stability of emulsion.

• YAKHAK HOEJI
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• v.51 no.1
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• pp.56-62
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• 2007

Twelve epoxy and hydroxydiosgenin derivatives (DI-1${\sim}$DI-12) were synthesized from diosgenin (25(R)-5-spirosten-3${\beta}$-ol). Diosgenin was epoxidized with m-chloroperoxybenzoic acid (mCPBA) to oxidize 25(R)-4${\alpha}$,5${\alpha}$-epoxyspirostane (DI-1). Diosgenin was reacted with DDQ to form 25(R)-1,4,6-spirostatrien-3-one (DI-2), which was treated with 30% H$_2$O$_2$ to give 25(R)-1${\alpha}$,2${\alpha}$-epoxy-4,6-spirostadien-3-one (DI-3) and treated with mCPBA to form 25(R)-6${\alpha}$,7${\alpha}$-epoxy-1,4-spirostadien-3-one (DI-7), respectively. DI-3 was reduced with NaBH$_4$ to afford 25(R) -1${\alpha}$,2 ${\alpha}$-epoxy-4,6-spirostadien-3${\beta}$-ol(DI-4) and reacted with Li metal in absolute ethanol to form 25(R)-2-ethoxy-1,4,6-spirostatrien-3-one (DI-5). DI-7 was reduced with NaBH$_4$ to produce 25(R)-3${\beta}$,7${\alpha}$-dihydroxy-4-spirostene (DI-8) and treated with Li metal in liquid ammonia to produce 25(R)-7${\alpha}$-hydroxy-4-spirosten-3-one (DI-9). DI-2 was reduced with NaBH$_4$ to form 25(R) -4,6-spirestadien-3${\beta}$-ol(DI-10), which was stirred with 30% H$_2$O$_2$ to synthesize 25(R)-4,6-spirostadien-3-one (DI-11) and reacted with mCPBA to give 25(R)-4${\beta}$,5${\beta}$ -epoxy-6-spirosten-3${\beta}$-ol (DI-12), respectively. The antinociceptive effects of synthesiz ed compounds were measured by hot plate method and compound DI-7 signifcantly exhibited antinociceptive effect. DI-2 decreased the serum triglyceride and total cholesterol levels in poloxamer P-407 injected rat.

• Archives of Pharmacal Research
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• v.29 no.10
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• pp.928-933
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• 2006

Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

• Journal of Pharmaceutical Investigation
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• v.27 no.4
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• pp.279-286
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• 1997

In order to formulate 2% ibuprofen solution, the effects of various solublizing agents, such as cosolvents (propylene glycol, polyethylene glycol, glycerin), a complexing agent $(CELDEX{\circledR}\;CH20)$, surfactants $(Poloxamers\;and\;Cremophor{\circledR}\;RH40)$ on the solubility of ibuprofen in aqueous solution were evaluated. Among them, Poloxamer 407 and $Cremophor{\circledR}$ RH40 showed the excellent capacity on the solubilization of ibuprofen. After 2% ibuprofen solution of choice were administered orally to rats, in reference to a 2% ibuprofen syrup in the market, the pharmacokinetic parameters were determined. The absorption rate of ibuprofen from the solution was higher than that from the suspension.

• Journal of Pharmaceutical Investigation
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• v.38 no.6
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• pp.393-398
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• 2008

A propofol delivery system was prepared using two biocompatible polymeric surfactants, poloxamer 407 and PEG 400. The nanoparticular stability of the micellar system was evaluated in terms of temperature change, storage time and composition. The particle size of the system was slightly increased with elevating temperature from $4^{\circ}C$ to $25^{\circ}C$, but its distribution was unimodal. At $40^{\circ}C$, the system presented a bimodal particle size distribution and the increase in the fraction of particles larger than 15 nm. This result might be due to the expansion of the nanoparticles through micellar swelling at the high temperature. It was found that propofol was gradually come out of the system, stored for a month at three different temperatures (4, 25 and $40^{\circ}C$). The drug loss was apparently dependent on temperature and the system composition. Increasing temperature induced the acceleration of the drug loss of $7{\sim}10%$ at $4^{\circ}C$ and $14{\sim}16 %$ at $40^{\circ}C$. This may be owing to the high diffusivity resulting from the swelling of the hydrophilic surface of the nanoparticle at high temperature. However, the addition of PEG 400 to the system led to the reduction of the drug loss. This result is associated with the previous investigation that PEG coverage decreased diffusion coefficient because of the formation of the denser structure on the surface of nanoparticulate. Nevertheless, the limited amount of PEG, less than 2% (w/v), should be used to prevent the precipitation and discoloration of the system.

• Journal of dental hygiene science
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• v.10 no.2
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• pp.79-83
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• 2010

This study manufactured hydrogel, which was contained NSAIDs(non-steroidal anti-inflammatory drugs) Ketorolac tromethamine and hydrolyzed products of gardeniae fructus extract, and experimented viscosity, surface tension, tensile strength and bio-adhesiveness by using hairless mouse. Thus, it was performed in expectation for being probably able to develop as effective auxiliary agent of periodontal disease after non-surgical or surgical periodontal treatment. As a result, the following conclusions were obtained. 1. Out of KGE and KGH gel materials, the content of ketorolac tromethamine was 1.02~0.97%. The content of geniposide was 0.34% in KGE gel A and C. However, it got lower to 0.11% in KGH gel B and D. The content of genipin wasn't shown in KGE gel A and C, but was shown with 0.13% in KGH gel B and D. 2. As for viscosity according to temperature in gel material, the gel, which used independently Carbopol 940 as gel inoculant, maintained the higher viscosity than the gel, which added Poloxamer 407. The surface tension in each material showed 34.77~40.58 dyne/cm at 37. As for tensile strength in material, KGH gel B was shown the higher tensile strength in about 3.5 times compared to the control group. 3. As for bio-adhesiveness, the back-skin upper part(epidermis) and abdomen skin were shown to be 50.62 N in KGH gel B, thereby having indicated higher value in about 5 times compared to control group. The back-skin lower part(dermis) and abdomen skin were shown to be 35.93 N in KGH gel B, thereby having indicated higher value in about 3.5 times compared to control group.

• Journal of the Korean Society of Food Science and Nutrition
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• v.40 no.4
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• pp.531-537
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• 2011

The effects of dietary supplementation of pacific saury on anti-hyperlipidemic activities were investigated using an animal test study in which normal rats were fed four different parts of saury, such as the whole body, meat, internal organs, or a mixture of head, caudal fin, and bone. Serum total lipid and triglyceride levels were significantly (p<0.05) reduced in rats fed saury meat at a dose of 200 mg/kg of body weight compared to hyperlipidemic control rats. There were also significant decreases in serum total cholesterol and LDL-cholesterol levels in the rats fed saury meat at 200 mg/kg of body weight. In addition, the atheroscrelosis index and superoxide dismutase in blood lipids were significantly (p<0.05) lowered in rats fed saury meat at 200 mg/kg of body weight compared to the control rats. In conclusion, our results indicate that saury meat contains unknown physiologically active components as than compared to other parts of saury, and has potential for use in the prevention of hyperlipidemic arteriosclerosis.

• Biomolecules & Therapeutics
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• v.6 no.1
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• pp.45-49
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• 1998

The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and E-lotion, which is a 3% ketoprofen lotion in the Japanese market was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, $C_{max}$ were 316 $\pm$22.3 ng/ml and 163 $\pm$ 12.2 ng/ml, respectively, at the same Tma of 2 hours postdose, while $C_{max}$ and $T_{max}$ after oral administration of the drug were 1,030$\pm$89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and I-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageeneninduced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while I-lotion showed 34.\\\\`r%. The calculated ED5o after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.n.n.n.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.6
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• pp.1528-1533
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• 2005

To evaluate the anti-hyperlipidemic effect of Brassica rapa L. and its major compound, $\beta$-sitosterol, the present study was undertaken, hypercholesterolemia was induced in rats with poloxamer-407, Triton WR-1339, 30% corn oil high cholesterol diet. The ethanol extract of Brassica rapa L. significantly decreased total cholesterol (TC), phospholipid, triglyceride at doses of 200 mg/kg, and $\beta$-sitosterol significantly exerted anti-hyperlipidemic activity at a dose of 15 mg/kg in rats with hyperlipidemia. Taken together, Brassica rapa L. and $\beta$-sitosterol can be useful agents for the prevention or treatment of hyperlipidemia.

• Journal of Pharmaceutical Investigation
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• v.39 no.4
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• pp.269-273
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• 2009

The objective of this investigation was to develop a gastro-retentive(GR) dosage form of gabapentin and was to evaluate of its dissolution characteristics. GR tablet consists of expandable core tablet matrix and semi-permeable membrane coating. Poloxamer 407 and sodium bicarbonate were used to prepare the core matrix. Polyvinly acetate dispersion (Kollicoat $SR30D^{(R)}$) and polyvinyl alcohol-polyethylene glycol copolymer ((Kollicoat $IR^{(R)}$)) were employed to form the semi-permeable membrane. The GR tablets significantly expanded up to fivefold in simulated gastrointestinal fluids with no apparent damage of the coating membrane over 12 hours. Also, the swelling rate was controllable with the amount of sodium bicarbonate. The drug release was observed to be substantially sustained based on coating level. The release rate of gabapentin from the GR tablet was gradually slowed down as the coasting amount was increased. The gabapentin GR tablet with 8% coating level showed a pseudo-zero order release kinetics over 12 hours. These results suggest that this swellable GR tablet system having semi-permeable membrane coating can be applicable for hydrophilic drug substances like gabapentin.