• Journal of Pharmaceutical Investigation
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• 제22권1호
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• pp.63-68
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• 1992

An HPLC procedure with UV detection has been developed for the quantitation of flurbiprofen released into isopropyl myristate used as the receptor phase in an in vitro membraneless drug diffusion cell. The drug and the internal standard (oxaprozin) were extracted from isopropyl myristate with a mixture of dimethylsulfoxide:methanol:water (2:1:1) and quantitated using a reverse phase $C_{18}$ column. The chromatograms were completely free from interfering peaks, and the relative retention times of flurbiprofen and the internal standard were 4.9 and 6.8 min, respectively. Calibration plots were linear over the concentration range of $1-200\;{\mu}g/ml$ of flurbiprofen with correlation coefficients, all higher than 0.99. The mean intra-day precision and accuracy among three replicate sets of the assay in a day were 4.26 and 4.52%, respectively, whereas the mean inter-day precision and accuracy were 3.35 and 3.64%, respectively. The mean recovery of the drug was 92.5% over the calibration range. The method was simple, reliable and accurate for the quantitation of flurbiprofen in unpurified isopropyl myristate.

• 한국동물위생학회지
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• 제36권1호
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• pp.1-6
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• 2013

Since the 1980's, several kinds of inactivated bovine viral diarrhea virus (BVDV) vaccines have been used to immunize domestic animals such as cattle and goat in Korea. Immunogenicity of the BVDV vaccines has been checked by the Korean Veterinary Authority using laboratory animals. In this study, we applied a molecular method to investigate the genetic characterization of the BVDV genes in six commercial inactivated BVDV vaccines, and determined the efficiency of two extraction reagents (i.e., sodium citrate or isopropyl myristate) to separate the vaccine antigens from the antigen/adjuvant complexes. Six partial non-coding regions (288 bp) were successfully amplified with specific primer sets, which demonstrated that sodium citrate is more efficient in extracting viral RNA from inactivated gel vaccines than isopropyl myristae. In addition, we identified the virus strains from the vaccines by analyzing the nucleotide sequences of the 5' non-coding region (NCR) of BVDV. The nucleotide similarity of the partial 5' NCR ranged from 95.1 to 100% among BVDV vaccine strains, respectively, indicating that a few manufacturers used different BVDV strains to produce their vaccines.

• Journal of Pharmaceutical Investigation
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• 제33권2호
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• pp.141-144
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• 2003

The transdermal therapeutic system (TTS) of scopolamine has various advantages over its oral dosage forms. The ideal scopolamine TTS requires high skin permeation rate in short time after it is applied on the skin. In order to increase the initial skin permeation rate of scopolamine from TTS, various permeation enhancers were employed. Enhancers employed were fatty acids (oleic and linolenic acids), cyclic monoterpenes (menthol, camphor, cineole and limonene) and others (isopropyl myristate, sodium lauryl sulfate and glyceryl monostearate). The concentration of enhancers in the base were fixed to 5% (w/w). While fatty acids had little enhancing effect on the skin permeation of scopolamine, cyclic monoterpenes, isopropyl myristate and sodium lauryl sulfate resulted in $1.5{\sim}2.6-fold$ higher skin permeation rate of the drug compared to the control. However, lag time was not affected by enhancers studied.

• 대한화장품학회지
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• 제19권1호
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• pp.127-138
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• 1993

고압유화 장치인 Microflridizer를 이용하여 4성분계의 emulsion을 제조하기 위한 최적조건을 알아보았다. Oil은 squalane, isopropyl myristate, PPG-15 stearyl benzoate ester를 사용하였으며, surfactant는 POE(20) sorbitan monolaurate, POE(20) sorbitan monopalmitate, POE(20) sorbitan monostearate를, cosuractant는 glycerine을 사용하여 Micro-fluidizer의 작업압력 및 순환횟수, oil의 종류 및 농도, cosurfactant의 농도에 따른 eumlsion의 상태를 비교하였다. 입자의 크기는 작업압력 및 순환횟수가 증가함에 따라 감소율이 점점 둔화되었으며 이 때의 적정압력은 1400bar 정도, 순환횟수는 4회 정도임을 알았다. 또한 cosurfactant인 glycerine의 농도가 30wt.%일 때 가장 작은 emulsion입자를 얻을 수 있었고, oil의 농도가 증가할수록 입자의 크기는 증가하는 현상을 나타내었다.

• Archives of Pharmacal Research
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• 제24권3호
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• pp.224-228
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• 2001

DA-5018, a recently synthesized capsaicin analog, appears to possess potent analgesic activity when administered topically. The objective of this study is to test the feasibility of the topical administration of this compound. Specifically, our goal was to identify vehicle system that permit a reasonable transdermal permeation of the compound in mice. Among the vehicles examined, isopropyl myristate (IPM) showed the largest in vitro permeability across the intact skin (83.6 ${\pm}$ 5.42${\mu}$l/$\textrm{cm}^2$/h ). However, due to the limited solubility of DA-5018 in IPM (0.53 mg/ml), the maximal flux from the IPM medium remained at only 44.3 ${\pm}2.87{\mu}$g/$\textrm{cm}^2$/hr. In order to increase the flux, addition of better solvents for DA-5018 was attempted, under the assumption that flux is the result of both solubility and permeability. Ethoxydiglycol (EG) and oleic acid (OA) were selected as examples of food solvents. The addition of IC or OA to IPM at a 1:1 volume ratio resulted in a comparable increase in the solubility of the compound (i.e., to 61.1 and 50.2 mg/ml for EG and OA, respectively). However, the addition of EG at a 1:1 volume ratio, for example, increased the flux 6.3 fold (i.e., $279{\mu}$g/$\textrm{cm}^2$/hr), while OA, at a 1:1 volume ratio, decreased the flux 5 fold (i.e., $9.26{\mu}$g/$\textrm{cm}^2$//hr). The mechanism of this discrepancy between EG and OA was investigated by measuring the permeabilty of DA-5018 across the stratum corneum-removed skin of the mouse, under the hypothesis that the viable skin layer may serve as a barrier for the permeation of lipophilic substances such as DA 5018. The permeability of DA-5018, from the medium of EG or OA, across the viable skin differed greatly for EG ($0.41{\mu}$l/$\textrm{cm}^2$/hr) and OA ($0.086{\mu}$l/$\textrm{cm}^2$/hr), suggesting that a higher permeability across the viable skin layer is needed for the second solvents. The maximum flux across the intact skin was achieved for DA-5018 when EG was added to IPM at a 1:1 volume ratio. Thus, the use of a binary system appears to be the best approach for realizing the transdermal delivery of DA-5018 at a reasonable rate.

• 대한화장품학회지
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• 제10권1호
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• pp.8-12
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• 1984

Increasing the oil volume in the oil : water mixtures using isopropyl myristate, oleic acid as oils, the solubilities of methyl, propyl and butyl parabens and the MICs (minimum hibitory concentrations) to E. coli were increased. But in liquid paraffin, the solubility was reversed. The relation between MIC and solubility of parabens had constant factor of 0.7 as saturation fraction percent. The solubility of methyl paraben was crossed over in those of propyl and butyl parabens, when the oil volume was increased. When the oil was used over the cross-over point, methyl paraven was useful to preserve the systems, and below the cross-over point the more lipophilic propyl and/or butyl parabens were effective.

• Journal of Pharmaceutical Investigation
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• 제41권1호
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• pp.9-17
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• 2011

The objective of this work is to study transdermal delivery of calcitonin using iontophoresis and to evaluate various factors which affect the transdermal transport. We have studied the effect of polarity, current density, drug concentration, penetration enhancers (isopropyl myristate [IPM] and ethanol) and laser treatment on transdermal flux and the results were compared. We also investigated the iontophoretic flux from microemulsions containing calcitonin together with oleic acid (OA) or IPM. In vitro flux study was performed at $33^{\circ}C$, using side-by-side diffusion cell and full thickness hairless mouse skin. Anodal delivery at pH 3.0 was much larger than cathodal and passive delivery, due to the positive charge of calcitonin. Cumulative amount delivered (CUM) by cathodal or passive delivery was close to zero for 10 hours. The pretreatment of skin by neat IPM markedly increased the CUM anodically. CUM increased as the current density, drug concentration or the duration of IPM treatment increased. Microemulsion containing IPM or oleic acid was prepared and the phase diagram was constructed. CUM also increased when IPM was incorporated into a microemulsion. OA microemulsion showed similar enhancing effect to IPM microemulsion. The delivery of calcitonin from 70% (v/v) ethanol aqueous solution showed a large increase in flux. Laser treatment of skin before flux experiment exhibited about 2 fold increase in total calcitonin amount transported for 12 hours, when compared to that delivered by IPM microemulsion. Based on these results, we have evaluated the possibility of delivering enough amount of calcitonin to reach the therapeutic level. The data suggest that it is highly possible to deliver clinically effective amount of calcitonin using iontophoresis patch with small area (<10 $cm^2$).

• Journal of Pharmaceutical Investigation
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• 제38권3호
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• pp.171-176
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• 2008

Talniflumate is a nonsteroidal anti-inflammatory drug (NSAID), which has been used treat of rheumatoid diseases, is insoluble in water, therefore it has low bioavailability after oral administration. The purposes of this study were to prepare O/W or W/O microemulsions for solubilization of poorly water soluble drug, talniflumate and to formulate into other dosage form. For this purpose, we made O/W or W/O microemulsion with oil(soybean oil, IPM), surfactant (Cremophor $EL^{(R)}$, Tween 80) and water or propylene glycol and evaluated solubility of talniflumate. The microemulsion systems were very stable and showed transmittance above 95% without flocculation or aggregation. Especially, the solubility of talniflumate in the formulation B-1 containing 18% of isopropyl myristate and 71% of tween 80 was 10 times higher than that of other O/W microemulsions. The addition of propylene glycol and N-methylglutamine to the fomulation B-1 showed excellent capacity on the solubilization of talniflumate and the percentage was almost 2.0%. These results suggest that the microemulsion system may be promising for the solubility improvement of talniflumate.

• Archives of Pharmacal Research
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• 제17권4호
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• pp.240-243
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• 1994

Release rates of flurbiprofen from transdermal gels made of poloxamer 407 were evaluated using a membraneless diffusion cell in order to study the effects of formulation variables on flurbiprofen release such as poloxamer 407 (17.5-25%) drug (0.1-1.0%), ethanol (10-20%), PG or PEF 300 (5-15%) concentrations and gel pH(3-7). Isopropyl myristate was employed as a receptor medium for the drug released from the gel. The diffusion coefficient of flurbiprofen decreased linearly as the amount of poloxamer 407 and the drug in the gel increased. The release rate of flurbiprofen was gel increased. The The addition of more ethanol in the gel increased the drug release, resulting from the increase of the thermodynamic activity of the drug in the aqueous phase of the gel. However, the concentration effects of PG and PEG 300 on the release rate of flurbiprofen were negligible over the concentration range used.

• Journal of Pharmaceutical Investigation
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• 제34권1호
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• pp.29-34
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• 2004

The solubility and stability of quercetin in various vehicles were determined. The solubility of quercetin at $28^{\circ}C$ increased in the rank order of isopropyl myristate < oleyl alcohol < propylene glycol monolaurate < oleoyl macrogol­6 glycerides < linoleoyl macrogol-6 glycerides < propylene glycol laurate (PGL) < propylene glycol monocaprylate (PGMC) < polyethylene glycol-8 glyceryl linoleate < caprylocaproyl macrogol-6 glycerides < diethylene glycol mono ethyl ether (DGME). The addition of DGME to non-aqueous vehicles such as PGL ad PGMC markedly increased the solubility of quercetin. From the stability studies, it was found that quercetin was unstable due to rapid oxidation by dissoved oxygen. The addition of a combination of ascorbic acid and edetic acid (EDTA) at 0.1 % markedly decreased the degradation rates of quercetin in 40% polyethylene glycol 400 in saline. Quercetin was relatively unstable in non-aqueous vehicles such as PGL and PGMC alone, and PGL-PGMC co-solvent The degradation of quercetin in such non-aqueous vehicles was fast, depending on temperature. The addition of butylated, hydroxytoluene, butylated hydroxyanisole, citric acid and/or EDTA at 0.1 % was effective in retarding the degradation of quercetin.