• Toxicological Research
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• v.30 no.4
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• pp.251-260
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• 2014

The number of farmers who have suffered from non-fatal acute pesticide poisoning has been reported to vary from 5.7% to 86.7% in South Korea since 1975. Absorption through the skin is the main route of exposure to pesticides for farmers who operate with them. Several in vitro tests using the skins of humans or animal and in vivo tests using laboratory animals are introduced for the assessment of human dermal absorption level of pesticides. The objective of this study is to evaluate and compare international guidelines and strategies of dermal absorption assessments and to propose unique approaches for applications into pesticide registration process in our situation. Until present in our situation, pesticide exposure level to operator is determined just using default value of 10 as for skin absorption ratio because of data shortage. Dermal absorption tests are requested to get exposure level of pesticides and to ultimately know the safety of pesticides for operators through the comparison with the value of AOEL. When the exposure level is higher than AOEL, the pesticide cannot be approved. We reviewed the skin absorption test guidelines recommended by OECD, EFSA and EPA. The EPA recommends assessment of skin absorption of pesticides for humans through the TPA which includes all the results of in vitro human and animal and animal in vivo skin absorption studies. OECD and EFSA, employ a tiered approach, which the requirement of further study depends on the results of the former stage study. OECD guidelines accept the analysis of pesticide level absorbed through skin without radioisotope when the recovery using the non-labeled method is within 80~120%. Various factors are reviewed in this study, including the origin of skin (gender, animal species and sites of skin), thickness, temperature and, etc., which can influence the integrity of results.

• YAKHAK HOEJI
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• v.30 no.2
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• pp.96-99
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• 1986

Absorption enhancing effect of 5 MSA-Na at the mucous memberanes of the rectum and duodenum was studied via in vitro sac test. There were no significant differences between two membranes. Effect of 5MSA-Na on the transfer of CMZ to the tissue was also studied via in situ loop method. There was no significant difference at the duodenum, compared to the control when CMZ was administered intravenously. Transfer of CMZ to the loop of the rectum was increased in the presence of 5MSA-Na compared to the control, which might be attributed to the enhanced permeability of the mucous memberane of the rectum.

• Archives of Pharmacal Research
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• v.11 no.3
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• pp.185-196
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• 1988

The inflence of hydrophilic vehicles on percutaneous absorption rate of griseofulvin was studied using intact skin of full thickness of hairless rat. The in vitro absorption rates were used as the characteristics for deciding the optimum formula of ointment vehicles. The optimum formula of vehicle compositions for maximum absorption rate was obtained from the polynomial regression equation and the two graphical techniques, contour graph and partial derivative graph. It was composed of sodium lauryl sulfate (1.65 W /W%), white petrolatum (16.5 W /W%), propylene glycol (12.0 W /W%), and stearyl alcohol (19.6W /W%). The experimental value obtained from the optimum formula and the prediction value were 33.99 and 33.87 ${\mu}g/\sqrt{min}$, respectively. From these results, it was believed that optimum formula for semisolid dosage forms could be obtained from the application of the optimization technique used in this study.

• Journal of Pharmaceutical Investigation
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• v.27 no.1
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• pp.57-64
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• 1997

$Amino-{\beta}-lactam$ antibiotics are absorbed by the dipeptide transporter in the small intestine. These uptakes are coupled to a proton influx. The inward proton gradient is partly induced by the $Na^+/H^+$ exchanger and calcium ion is involved in control of this antiport. Interaction between ampicillin which is one of the $Amino-{\beta}-lactam$ antibiotics and nifedipine which is one of calcium channel blocking agents was studied in rats in vivo and with rabbit jejunum mounted on the Sweetana/Grass diffusion cells in vitro. Bioavailability of ampicillin was increased significantly when nifedipine was co-administered orally in rats. There were no differences in the distribution phase and the elimination phase when ampicillin was given either alone or with nifedipine intravenously. Conditions for in vitro experiments were determined. The lift rate of $O_2/CO_2$ gas was controlled to 3 bubbles/sec and ampicillin was stable in the Kreb's buffer at pH 6.0. Absorption of ampicillin was the greatest when the completely-stripped serosal membrane was used. Transport of ampicillin from mucosal to serosal side in the rabbit jejunum was enhanced by 32% in the presence of nifedipine (p=0.059). Above results suggest that nifedipine might increase the plasma level of ampicillin via the improved absorption in the intestine rather than the reduction in the elimination or/and alteration in the distribution.

• Korean Journal of Food Science and Technology
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• v.26 no.4
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• pp.348-354
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• 1994

Chitin and chitosan samples prepared from crab's shells under different conditions were compared for their physicochemical properties; and functionality in gastrointestinal tract by in vitro test. Their bulk density was in the range of $127{\sim}208\;mg/ml$, and their viscosity was $80{\sim}581\;cP$ in 0.1 chitin and $80{\sim}3,670\;cP$ in 0.5% chitosan solution, showing a wide variation. The degree of deacetylation in chitosan samples as determined by IR spectral analysis was relatively high, showing $81{\sim}93%$. At the same alkali concentration and reaction temperature, a longer reaction period gave an increased degree of deacetylation and lower viscosity. The water holding capacity of chitic substance became greater at higher soaking temperature; chitosan D at $37^{\circ}C$ showed the greatest value. Chitic substance with lower bulk density showed the higher water holding capacity. The retardation effect toward glucose absorption was higher in critic substances of lower density and higher water holding capacity; chitosan D showed the highest value of 38%. The retardation index toward bile acid absorption after 1 hour dialysis was $15{\sim}34%$ in chitic substances, 39% in pectin and 9% in cellulose. The retarding effect showed the highest value of 34% in chitosan D at 3% concentration.

• Archives of Pharmacal Research
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• v.18 no.4
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• pp.219-223
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• 1995

Rectal absorption of opeprazole, a proton pump inhibitor, from suppositories was studied in rabbits. The suppositories were prepared by the conventional melting method with two types of bases, water-soluble polyethylene glycol (PEG) 4000 and oil-soluble Witepsol H15 bases, and administered intractally (ir) to rabbits at a dose of 10 mg omeprazole/kg. The plasma omeprazole concentration-time profiles of the two suppositories were compared with those following intravenous 9iv) administration of the same dose. There were no significant differences between the two suppositories in bioabailabilities and peak plasma concentrations $(C_{max})$. Bioavaiabilities and $C_{max}$ of PEG- and Witpsol suppositories were 30.3 and 33.9%, and 7.0 and $5.6\mug/ml$, resepectively. However, PEG suppository showed significantly (p<0.05) shorter time to reach peak plasma concentration $(T_{max})$ mean absorption time (MAT) and mean residence time in the plasma (MRT) than Witepsol suppository. The $T_{max}$ MRT nad MAT were 25.0, 83.0 and 38.5 min for PEG syppository, but were 90.0, 122.5 and 78.0 min for Wiepsol supposiotory, respectively. These differences between thw two suppositories could be explanined by the difference in the in vitro dissolution rates between the suppositories. The dissolution of omeprazole form PEG suppository was reportedly much faster than that from Witepsol suppository. It suggests that plasma profiles of omeprazole, especially $C_{max}$ MAT and MRT, could be controlled by modifying the in vitro dissolution rate of the drug from the suppositories. Above results suggest that rectal suppository is worth developing as an alternative dosage form of omeprazole to the conventional oral preparations which need sophisticated treatments, such as enterix coating, to prevent acid degradation of the drug in the stomach fluid.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.45 no.2
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• pp.139-150
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• 2019

This study is investigated sunscreen formulation that enhances UV absorption efficiency by UV light. Ethylhexyl methoxycinnamate (OMC) is one of the most common UV filters. Many studies have been conducted about photostability of OMC. It is well known that under the UV exposure, trans-OMC could turn to cis-OMC, or produce various photoproducts including its dimers. Those chemical structure changes were understood as the reason of a decrease in UV absorption efficiency upon UV exposure. However, it was found that OMC and isoamyl p-methoxycinnamate (IMC) could even enhance its UV absorption efficiency when it was exposed to UV light in an environment similar to actual use. In order to develop sunscreen formulation that enhances UV absorption efficiency by UV light, emollient with high polarity and compatibility should be avoided from the formular. Those emollient seemed to prevent OMC or IMC from producing photoproducts under UV light. Finally, a sunscreen formulation (UV sensing SPF boosting formular) enhancing UV absorption efficiency by UV was developed by the UV activated SPF boosting technology, and the effect of the sunscreen was evaluated. in vitro SPF of the sunscreen was increased from 50.69 to 72.33 when it was exposed to UV light and its in vivo SPF (53.7) was 56.10% higher than that of the control sunscreen (below 34.4).

• KSBB Journal
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• v.28 no.5
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• pp.319-326
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• 2013

This study was carried out to investigate the in vitro and in vivo moisturizing properties and percutaneous absorption of PEG-impregnated Aloe vera gel. The PEG-i-Aloe gel was obtained from dewatering and impregnation by soaking (DIS) of Aloe vera leaf slice. The moisturizing property of the obtained sample was evaluated by moisture determination using gravimetric method in desiccator under different RH% and by water sorption-desorption test on human skin. The transdermal penetration characteristics of PEG-i-Aloe gel was investigated by Franz diffusion cell in vitro transdermal absorption method. PEG-i-Aloe gel had high moisture retention ability and could significantly lead the enhancing skin hydration status as well as reducing the skin water loss due to the film formation as a skin barrier. The skin penetration rate of PEGi- Aloe gel at steady state was 9.76 ${\mu}g/(h{\cdot}cm^2)$ and the quantity of the transdermal absorption was 144 ${\mu}g/cm^2$ in 9 hr. The penetration mechanism was well fitted with Higuchi model ($R^2$ = 0.974-0.994). The results show that PEG-i-Aloe gel has the significant moisturizing effect and strong penetration of the animal skin. It could be used as the moisturizing additive in cosmetic skin products.

• Journal of the Korean Applied Science and Technology
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• v.29 no.4
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• pp.552-560
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• 2012

Drug delivery technologies are patent protected formulation technologies that modify drug release profile, absorption, distribution, and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stop if the drug dosage lead to side effect. Polysaccharide, such as karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO) were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, tacrine contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in tacrine such as lipophilic drug in vitro. We used glycerin, PEG 400, and PEG 800 as enhancers. Therefore, transdermal absorption of tacrine could be improved by changing vehicle composition or by using penetration enhancers. Especially it would be anticipated that the high permeation efficacy could be obtained by using vehicle that has enhancing effect for itself and by adding enhancers to it.

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.7 no.2
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• pp.279-288
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• 1997

The penetrating speeds of organic solvents into the nude mouse skin were measured by in vitro methods(diffusion cell methods) and in vivo methods(measuring internal residues of the organic solvents). The results were as follows: 1. The penetrating speeds of toluene, m-xylene, MEK, MIBK, ethanol, IPA and 2-bromopropane into the skin were $0.4832mg/cm^2/h$, $0.1738mg/cm^2/h$, $1.124mg/cm^2/h$, $0.6627mg/cm^2/h$, $1.747mg/cm^2/h$, $1.359mg/cm^2/h$, and 2-bromopropane $4.165mg/cm^2/h$ respectively. 2. The penetrating speeds of the mixtures of two, toluene and m-xylene, the mixture of three, IPA, ethyl acetate, and MIBK, the mixture of five, toluene, m-xylene, IPA, ethyl acetate, and MIBK were $0.172mg/cm^2/h$, $1.431mg/cm^2/h$, and $2.983mg/cm^2/h$ respectively. 3. The absorption speeds of 2-bromopropane and styrene which were measured by in vivo processes were $3.12mg/cm^2/h$ and $1.44mg/cm^2/h$ respectively. The absorption speed of 2-bromopropane mesured in vivo was 74.9% of that measured by in vitro methods, $4.165mg/cm^2/h$.