• Proceedings of the PSK Conference
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• 2000.10a
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• pp.209.2-209.2
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• 2000

• Journal of Pharmaceutical Investigation
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• v.41 no.4
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• pp.233-238
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• 2011

DEET, N,N'-diethyl-m-toluamide, is the most commonly used mosquito repellent. However, it can easily permeate through skin leading to toxic effects. A recent study showed that the ortho analogue of DEET showed enhanced repellency with reduced permeation compared to the commercially used meta analogue. Thus, in order to understand the differences in properties and effectiveness among the m-, o- and p-analogues of DEET, an HPLC-UV method was developed for separately analyzing the three analogues. Moreover, stability profiles at temperatures ranging from $30^{\circ}C$ to $70^{\circ}C$ as well as pH ranging from pH 3 to pH 9 have been determined. All three analogues were stable with no degradation observed during the 5 day period. o-DEET therefore could be further developed into a safer and more effective mosquito repellent.

• Journal of Pharmaceutical Investigation
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• v.24 no.4
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• pp.273-279
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• 1994

The stability of three oximes, Hl-6 [(4-carbamoyl-2'[(hydroxyimino)-methyl]- 1,1'-oxydimethylenedi-(pyridinium chloride)], Hl-CN [(4 cyano-2'-[(hydroxyimino)-methyl] -1,1'-oxydimethylene-di-(pyridinium chloride)], and 2-PAM [pralidoxime chloride] in aqueous solutions was evaluated by HPLC assay. The rate of degradation is dependent on the pH as well as the temperature at which the solution is stored. The optimum pH for the stability of these oximes was pH 2 to 3. The degradation rate constant for 2-PAM ($k\;at\;70^{\circ}C$, $2.07{\times}10^{-4}/hr;\;E_a\;value$, 27.2 kcal/mol) was smaller than those for bis-pyridiniumoximes, Hl-6 ($k\;at\;70^{\circ}C$, $3.38{\times}10^{-3}/hr$) and Hl-CN ($k\;at\;70^{\circ}C$, $8.66{\times}10^{-3}/hr;\;Ea\;value$, 20.7 kcal/mol). In mechanistic analyses, it was found that Hl-CN was decomposed through not only the hydrolysis of nitrile group but also the cleavage of methylene ether bridge, in contrast to Hl-6 which was degraded mainly through the cleavage of methylene ether bridge.

• Journal of Pharmaceutical Investigation
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• v.34 no.1
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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.

• Journal of Pharmaceutical Investigation
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• v.35 no.5
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• pp.333-336
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• 2005

The objective of this study was to investigate the stability of tetracycline HCl on encapsulation into and inside reverse micelles. To do so, tetracycline HCl was first mixed with cetyltrimethylammonium bromide, water and ethyl formate to make reverse micelles. The degradation kinetics of tetracycline HCl inside the reverse micelles was then assessed by scrutinizing its stability data. Under our experimental conditions, the reverse micelles formed spontaneously in absence of any mixing devices. During the preparation of the reverse micelles, however, considerable portions of tetracycline HCl underwent a chemical reaction (e.g., epimerization). For instance, $51.4{\pm}0.6%$ of an initial concentration of tetracycline HCl was transformed into a degradation product. Once dissolved inside the reverse micelles, the degradation of tetracycline HCl followed an exponential decay pattern. The plot of log{the degradation rate of tetracycline HCl} versus log{tetracycline HCl concentration} made it possible to determine the order of degradation reaction and rate constant. It was proven that the degradation of tetracycline HCl inside the reverse micelles followed a first order kinetics with a rate constant of 0.0027 $hour^{-1}$. Meriting further investigation might be formulation studies to stabilize tetracycline HCl on encapsulation into and inside the reverse micelles.

• Journal of Pharmaceutical Investigation
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• v.20 no.2
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• pp.55-64
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• 1990

Soybean fatty acid, the largest byproduct in the production of soybean oil, was formulated for hand cream, oil in water emulsion base, to improve the suppleness and elasticity of skin. The stability of emulsion observed by a macroscopic method was used as a characteristic index for deciding an optimum formula of hand creams. The optimum formula of the most stable hand cream was obtained from polynomial regression equation, contour graphs and partial derivative graphs. The values of soybean fatty acid and stearyl alcohol in the obtained optimum formula were 9.75 and 14.75 w/w%, respectively, and sodium lauryl sulfate was not needed. Experimental value for the stability of hand cream prepared according to the optimum formula was 76,14 days, and the prediction value by computation method was 73.25 days. From the results of accelerated tests by elevated temperature, the stability of hand cream by optimum formula was 1.7 year at room temperature $(25^{\circ}C)$. The hand cream containing soybean fatty acid was found to be free of primary irritant substance to the skin by Draize technique.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.20 no.12
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• pp.555-562
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• 2019

This study was undertaken to develop a stable self-microemulsifying drug delivery system (SMEDDS) for trans-cinnamaldehyde, a known antibacterial and antifungal agent. A simultaneous analytical method was established for quantification of trans-cinnamaldehyde and its degradant, cinnamic acid. Various surfactants were applied to assess their effect on the aqueous solubility of trans-cinnamaldehyde, and pseudo-ternary phase diagrams were plotted. Of the various formulations tested, the liquid SMEDDS composed of trans-cinnamaldehyde (oil), Cremophor EL (surfactant) and Transcutol P (cosurfactant) at a volume ratio of 10/70/20, produced the smallest emulsion droplet size (around 23 nm). The stability test determined the superior stability of the trans-cinnamaldehyde SMEDDS with constant trans-cinnamaldehyde content and z-average diameter of emulsion, under accelerated and heat stressed condition. Thus, we believe that this novel trans-cinnamaldehyde SMEDDS formulation has the potential to be applied for the development of trans-cinnamaldehyde medicines in the pharmaceutical industry.

• Journal of Pharmaceutical Investigation
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• v.40 no.4
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• pp.255-261
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• 2010

Pluronic as pharmaceutical excipients are listed in the US and British Pharmacopoeia. In particular, Pluronics exist as different compositions and display abundant phases as self-assembling into polymeric micelles with various morphologies depending on the aqueous solvent quality, the composition of structure, and hydrophilic-lipophilic balance (HLB). Pluronics were also known as a P-gp modulator, which was exploited as a reversal molecule of multi-drug resistant (MDR) cancers. We selected a lamella forming Pluronic L92 which has high hydrophobicity and relatively long PEO block among L series of Pluronics. The dispersion of L92 showed great size particles and low stability. To increase the stability and to decrease the particle size, secondary Pluronics (F68, F88, F98, F127, P85, P105, and P123) with relatively long PEO chain were added into 0.1 wt% Pluronic L92 dispersion. The stability of binary systems was increased due to incorporated long PEO chain. Their particle sizes slightly decreased to over 200~400 nm and their solubilization capacity of binary systems didn't change except Pluronic L92/P123 mixtures. The L92/P123 systems showed ca. 100 nm sizes and lowest turbidity among the all systems. The solubilization capacity of 0.1 wt% L92/0.1 wt% P123 was slightly increased compared to 0.1 wt% L92 mono system and other binary systems. These nano-sized binary systems may have potential as alternative drug delivery systems with simple preparation method and overcome the drawbacks of mono systems such as low stability and loading capacity.

• Journal of Pharmaceutical Investigation
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• v.38 no.1
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• pp.9-14
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• 2008

Cation exchange resin complex of amlodipine free base has been investigated to improve the stability and dissolution profile. The complex was prepared by reacting amlodipine solution with activated cation exchange resin, and amlodipine content in the complex was 31.6% calculated by HPLC determination. Its product was not physical mixture but the complex formed by ionic bond, which was identified by microscope system, differential scanning calorimetry and X-ray diffractometry. Each tablet containing amlodipine free base(I) and its complex(II) was prepared for the accelerated stability test ($40^{\circ}C$, 75%RH) and dissolution test in the pH 1.2 buffer solution and purified water media. Dissolution patterns of formulation II in both media were similar to those of $Norvasc^{(R)}$ tablet, but the pattern of formulation I in purified water was different. After 6 months storage under stability test, amlodipine content of formulation I, II and $Norvasc^{(R)}$ tablet were $99.3{\pm}1.2%,\;98.9{\pm}1.4%\;and\;83.9{\pm}3.4%$, respectively. While amlodipine free base was unstable at the condition, its complex was not only significantly stable, but also similar in the dissolution pattern. These results suggest the usefulness of complex as a stable carrier for amlodipine free base.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.276-276
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• 1996

합성한 BR-8702-2의 시험결과 원소분석에서는 이론치와 실험치가 잘 일치하였고, 구조확인을 위한 FT-IR 및 FT-NMR(H$^1$)등의 시험에서도 구조와 일치하는 결과치를 나타내었다. 합성물질의 정량법을 HPLC 및 구성원소인 P와 N을 이용한 정량법에서도 유의성있는 결과를 얻을 수 있었다. 또한 분말상태인 이 물질의 안정성은 고온 고습하에서도 양호하였으며, 각종 완충수용액에서 pH가 분해에 미치는 영향을 pH-rate profile로 나타낸 결과 pH7, 8, 9에서 안정하였고 pH8에서 k=1.3$\times$$10^{-4}$day으로 가장 안정하여 shelf life는 807일이었다. 광에 대해서도 k=5.8$\times$$10^{-4}$day로 매우 안정하였다.