• Journal of Pharmaceutical Investigation
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• v.1 no.1
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• pp.70-77
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• 1971

The ointment, had discovered and used from the ancient, have not ever defined to qualitity as the hardness concerned with the absorned With the absorption of the effect of durg through the skin. Auther, for the first time, suggest the apparent logarithmic hardness against the penetration of ointment registered on the pharmacopeia of the Republic of Korea, the results are as the followings. 1. The speciality of this apparent logarithmic hardness ie in proportion for the solidity on the contrary to the penetration of oiniment, and the distribution range of it are between 1.68 to 3.53 for their ointments examined. 2. The specific gravity of the verious ointments according to the apparent logarithmic hardness may be ignore on the calculaiotn, the mean valve of the samples was 2.9303. 3. The determination of apparent logarithmic hardness(H) by the penetration method follows the under equation. $H=log_{10}({\frac{P-0.545h^3}{0.855h^2}})$ where, the h is the penetrate length described centimeter, and p is the weight of the cone.

• Journal of Pharmaceutical Investigation
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• v.40 no.3
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• pp.187-192
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• 2010

We aimed to evaluate the effect of temperature, pH, and light conditions on the stability of porcine placental extract (PPE)-loaded liposomes with different surface charges. The size distribution profiles and in vitro release patterns were investigated by dynamic light scattering method and spectrophotometry. The stability of PPE-loaded liposomes was affected by the surface charges of the liposomes. As compared to neutral and anionic liposomes, cationic liposome formulations showed significantly lower physical stability. At the test storage conditions of different temperatures and pHs, the mean sizes of cationic PPE-loaded liposomes substantially increased. In contrast, neutral and anionic liposomes did not reveal significant changes in mean sizes upon various storage conditions. The neutral and anionic liposomes showed no significant differences in the release profiles of PPE after storage at various temperatures and pHs. Our results indicate that anionic and neutral liposome compositions might be more suitable for the formulations of PPE providing the higher stability.

• Journal of Pharmaceutical Investigation
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• v.28 no.3
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• pp.141-149
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• 1998

In order to reduce systemic side effects following administration, flurbiprofen was formulated as O/W microemulsion consisting of the surfactant, oil phase and aqueous phase. Particle size distribution, apparent viscosity, solubility and skin permeation of flurbiprofen in various vehicles and microemulsion were evaluated. The domain of O/W microemulsion s phase diagram had difference between oil types and the area of O/W microemulsion was wide distributed by adding to PG and cosurfactant than that of water alone. As increasing 10, 15 and 20% of Brij 97 content and 1, 2.5, 5% of oil content, the solubility of flurbiprofen in O/W microemulsions and various vehicles was $400{\sim}1,000$ and $10{\sim}500$ times higher than that of control. Also, apparent viscosity of soybean oil microemulsions was higher than that of IPM microemulsions and that of vehicle were increased as increasing vehicle content. Since skin permeation of flurbiprofen decreased as increasing viscosity, in each vehicle, it was not affected 2% ${\beta}-CD$ and decreased as increasing PG content and to 2, 5 and 10% of $HP-{\beta}-CD$. In O/W microemulsion, 5% soybean oil. 20% Brij 97 and 75% water(A-1) with high viscosity showed low skin penetration.

• Journal of Pharmaceutical Investigation
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• v.35 no.5
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• pp.349-353
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• 2005

This study reports the pharmacokinetics of a novel histone deacetylase inhibitor, SD-0542, in rats after i..v. and oral administration. SD-0542 was injected intravenously at doses of 10, 20, and 40 mg/kg. The terminal elimination half-life $(t_{1/2})$, systemic clearance (Cl), and steady-state volume of distribution $(V_{ss})$ remained unaltered as a function of dose, with their values ranging from 2.0-2.5 hr, 157.2-214.1 ml/min/kg, and 11.1-17.5 L/kg, respectively, whereas, the initial serum concentration $(C_0)$ and AUC increased linearly as the dose was increased. Renal excretion of SD-0542 was minimal. Oral pharmacokinetic studies were conducted in rats at a dose of 20 mg/kg. The $T_{max}$, Cl/F, $V_{z}/F$, and $t_{1/2}$ were 2.0 hr, 92864 ml/min/kg, 16331 L/kg, and 2.0 hr, respectively. Taken together, SD-0542 showed linear pharmacokinetics over the i.v. bolus dose range studied. SD-0542 was poorly absorbed, with the absolute oral bioavailability of 0.9%.

• Food Science of Animal Resources
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• v.37 no.6
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• pp.813-822
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• 2017

The aim of this study was to prepare diacylglycerol (DAG) by enzymatic glycerolysis of lard. The effects of reaction parameters such as lipase type, reaction temperature, enzyme amount, substrate molar ratio (lard/glycerol), reaction time, and magnetic stirring speed were investigated. Lipozyme RMIM was found to be a more active biocatalyst than Novozym 435, and the optimal reaction conditions were 14:100 (W/W) of enzyme to lard substrate ratio, 1:1 of lard to glycerol molar ratio, and 500 rpm magnetic stirring speed. The reaction mixture was first incubated at $65^{\circ}C$ for 2 h and then transferred to $45^{\circ}C$ for 8 h. At the optimum reaction conditions, the conversion rate of triacylglycerol (TAG) and the content of DAG in the reaction mixture reached 76.26% and 61.76%, respectively, and the DAG content in purified glycerolized lard was 82.03% by molecular distillation. The distribution of fatty acids and Fourier transform infrared spectra in glycerolized lard samples were similar to those in lard samples. The results revealed that enzymatic glycerolysis and molecular distillation can be used to prepare more highly purified DAG from lard.

• Journal of Pharmaceutical Investigation
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• v.28 no.4
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• pp.249-255
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• 1998

Solid Lipid Nanoparticle(SLN), one of the colloidal carrier systems, has many advantages such as good biocompatibility, low toxicity and stability. In this paper, the effects of drug lipophilicity and surfactant on the drug loading capacity, particle size and drug release profile were examined. SLNs were prepared by homogenization of melted lipid dispersed in an aqueous surfactant solution. Ketoprofen, ibuprofen and pranoprofen were used as model drugs and tweens and poloxamers were tested for the effect of surfactant. Mean particle size of prepared SLNs was ranged from 100 to 150nm. The drug loading capacity was improved with the most lipophilic drug and low concentration of surfactant. Particle size and polydispersity of SLNs were changed according to the used lipid and surfactant. The rates of drug release were controlled by the loading drug and surfactant concentration. SLN system with effective drug loading efficiency and proper particle size for the intravenous or oral formulation can be prepared by selecting optimum drug and surfactant.

• Journal of Pharmaceutical Investigation
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• v.31 no.4
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• pp.257-263
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• 2001

The microspheres have been developed as a new drug delivery system. Although many particulate drug carriers, such as liposome, niosome and emulsion, have been introduced, injectable and biodegradable microspheres appears to be a particularly ideal delivery system because the local anesthesia is not necessary for the insertion of large implants and for the removal of the device after the drug release is finished. Biodegradable microspheres with nicotine and triamcinolone acetonide are prepared and evaluated. As biodegradible polymers, PLA (M.W. 15,000, PLA-0015), PLGA (M.W. 17,000, RG 502) and PLGA (M.W. 8,600, RG 502H) are used. This study attempted to prepare and evaluate the nicotine and triamcinolone acetonide-incorporated microspheres, which were prepared by two methods, solvent-evaporation and spray-drying methods. The microspheres, as a disperse system for injections, were evaluated by particle size, size distribution, entrapment efficiency, and in vitro drug release patterns. The differences of preparation method, partition coefficient, types of polymer, and preparation conditions of microspheres influence the particle size, entrapment efficiency, and in vitro drug release patterns.

• Journal of Pharmaceutical Investigation
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• v.30 no.1
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• pp.13-19
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• 2000

$Stealth^{\circledR}$ liposomes entrapped with streptokinase were prepared to improve the physical stability of conventional liposomes. The particle size distribution, dissolution rate and entrapping efficiency of the $Stealth^{\circledR}$ liposomes were studied. The entrapping efficiency of streptokinase into conventional liposomes was proportional to the total lipid and cholesterol amounts. In $Stealth^{\circledR}$ liposomes, the entrapping efficiency of streptokinase was increased with the increase of DPPE-PEG(5,000) amount. The particle size of $Stealth^{\circledR}$ liposomes decreased with the increase of DPPE-PEG(5,000) amount. The dissolution rate of streptokinase from conventional liposomes was decreased by addition of cholesterol. The dissolution rate of streptokinase from the $Stealth^{\circledR}$ liposomes was also decreased by addition of DPPE-PEG(5,000).

• Journal of Pharmaceutical Investigation
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• v.36 no.5
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• pp.309-314
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• 2006

The multicellular layers(MCL) of human cancer cells is a three dimensional(3D) in vitro model for human solid tumors which has been used primarily for the assessment of avascular penetration of anti-cancer drugs. For anti-cancer drugs with penetration problem, MCL represents a good experimental model that can provide clinically relevant data. Calcein-AM is a fluorescent dye that demonstrates the cellular vitality in a graded manner in cancer cell culture system. In the present study, we evaluated the use of calcein-AM for determination of anti-proliferative activity of anti-cancer agents in MCL model of DLD-1 human colorectal cancer cells. Optical sectioning of confocal imaging was compromised with photonic attenuation and penetration barrier in the deep layers of MCL. By contrast, fluorescent measurement on the cryo-sections provided a feasible alternative. Cold pre-incubation did not enhance the calcein-AM distribution to a significant degree in MCL of DLD-1 cells. However, the simultaneous determination of drug penetration and cellular vitality appeared to be possible in drug treated MCL. In conclusion, these data suggest that calcein-AM can be used for the simultaneous determination of drug-induced anti-proliferative effect and drug penetration in MCL model.

• Journal of Pharmaceutical Investigation
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• v.38 no.6
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• pp.399-403
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• 2008

The aim of this study was to evaluate the difference of analytical methods for the pharmacokinetic study of bromosulfophthalein (BSP), an indicator of hepatobiliary function. The plasma and bile concentrations of BSP after intravenous administration were measured according to custom UV spectroscopy and HPLC, respectively. Plasma concentration of BSP measured by UV spectroscopy was similar to that measured by HPLC. There was no significant difference in the distribution volume, total body clearance, area under the curve and mean residence time of BSP between different analytical method groups. However, bile concentration of BSP measured by UV spectroscopy was overestimated compared with concentration measured by HPLC method. Biliary clearance of BSP obtained from UV spectroscopy method was almost 3 times higher than that obtained from HPLC method. Thus, a feasibility of UV spectroscopy method for high throughput pharmacokinetic evaluation of BSP was limited to the study based on the plasma concentration of BSP, not bile concentration.