• Journal of Pharmaceutical Investigation
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• 제22권2호
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• pp.97-104
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• 1992

The purpose of this study was (i) to determine whether protease inhibition by medium chain fatty acids such as sodium caprate, sodium caprylate and sodium laurate led to suppression of insulin proteolysis over a range of insulin concentrations and (ii) elucidate preventing effect of the enhancers on molecular self-association of insulin in pH 7.4 phosphate buffer isotonic solution. To this end, the rate of insulin proteolysis in nasal tissue supernatants of the albino rabbits was determined in the presence of $0.1{\sim}2%$ sodium caprylate, sodium caprate and sodium laurate at insulin concentrations ranging from $5\;to\;100\;{\mu}M$. At fatty acid salts concentration lower than 0.5%, insulin proteolysis was accelerated but the enhancers of high concentration (>1%) reduced the rate of insulin proteolysis. These effects were dependent upon insulin concentration and chain length of fatty acid salts. Circular dichroism spectra of insulin solutions were then determined. Monomer fraction of insulin was increased with increasing sodium caprate. Therefore, half-life decrease of insulin at low concentrations of the enhancers was attributed to deaggregation of insulin by the enhancers, increasing the proportion of monomers available for nasal proteolysis. And the increase of half-life at high concentration of the enhancers was attributed to inhibitory effect on protease rather than the effect of monomer fraction.

• 한국응용과학기술학회지
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• 제27권4호
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• pp.407-414
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• 2010

New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.

• Journal of Pharmaceutical Investigation
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• 제31권3호
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• pp.181-184
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• 2001

The purpose of this study was to develop transdermal drug delivery system (TDDS) for the combination of physostigmine and procyclidine. The effects of various pressure sensitive adhesives (PSA) on the percutaneous absorption of procyclidine across hairless mouse skin were evaluated to select an appropriate PSA. In addition, the influences of various vehicles on the percutaneous absorption of procyclidine from PSA matrix across hairless mouse skin were evaluated using flow-through diffusion cell system at $37^{\circ}C$. Physostigmine did not have any influence on the permeation rate of procyclidine. The flux of procyclidine was the highest in silicone and PIB and was relatively lower in SIS, Acryl, and SBS adhesive matrices, however, their use was limited by the crystallization of the drug in the matrix. Among acrylic adhesives, the permeability of procyclidine was the highest from poly (ethylene oxide) grafted acrylic adhesive. Some enhancers show different enhancing effect depending on the drug, however, many of the tested enhancers showed enhancing effect for the permeation of both procyclidine and physostigmine to some extent. $Crovol^{\circledR}$ EP 40 showed the highest enhancing effect on the permeation of both compounds. The size of TDDS to provide required permeation rate was estimated to be $35\;cm^2$ based on available information.

• Archives of Pharmacal Research
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• 제24권6호
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• pp.578-583
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• 2001

To investigate the feasibility of developing a new tenoxicam plaster, the effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from a pressure-sensititre adhesive (PSA) matrices across the dorsal hairless mouse skin were studied. Vehicles employed in this study were propylene glycol (PC)-oleyl alcohol (OAI), PG-oleic acid (OA), and diethylene glycol monoethyl ether (DCMI)-propylene glycol monolaurate (PCML) cosolvents with/without fatty acids. In this studys amines such as triethanolamine (TEA) and tromethamine (TM) were additionally used as a solubilized. Among PSAs used, $Duro-Tak^{\circledR}$87-2510 showed much higher release rate than either $Duro-Tak^{\circledR}$ 87-2100 or $Duro-Tak^{\circledR}$87-2196. The relatively high flux rate was obtained with the formulation of DCMI-PCML (40:60, v/v) with 3% OA and 5% TM, and the flux increased as a function of the dose;the initial flux up to 12 h was $4.98{\pm}1.38{\;}{\mu\textrm{g}}/{\textrm{cm}^2}/h$ at the tenoxicam dose of $50{\;} mg/70{\;}{\textrm{cm}^2}$. This flux was much higher than that of a commercial piroxicam patch ($Trast^{\circledR}$) ($1.24{\pm}0.73{\;}{\mu\textrm{g}}/$\textrm{cm}^2/hr$) with almost only one-third that of the commercial patch. Therefore, these observations indicated that these composition of tenoxicam plaster may be practically applicable.

• 대한지역사회영양학회지
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• 제9권2호
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• pp.142-150
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• 2004

To increase both iron and enhancers for iron absorption through diets should be a basic strategy to sufficiently provide increased iron for pregnancy. Previous studies reported that iron intakes of Korean pregnant women were short and their iron status deteriorated as pregnancy progressed. However, there is little data about the bioavailability of dietary iron during pregnancy. Therefore, this study was conducted to determine the changes of dietary iron intakes, its bioavailability and iron status during pregnancy longitudinally in Korean women. A total of 151 pregnant women in their first trimester of pregnancy voluntarily participated. Among them, 72 women finished the research protocol during the second trimester and 55 did it during the third trimester. Dietary intakes of total iron, both non-heme and heme iron, as well as enhancers, both MPF (meat, poulty, and fish) and vitamin C, increased significantly as pregnancy progressed. As the results, bioavailability of dietary iron and iron absorbed increased significantly as pregnancy progressed. However, the amount of iron absorbed at each trimester did not meet considerably the iron needed during pregnancy. All five indices examined in the study, Hb level, Hct, serum concentrations of ferritin and sTfR (soluble transferrin receptor), and sTfR: ferritin ratio, showed that iron status of the subjects deteriorated as pregnancy progressed. The rate of anemia of the subjects increased as pregnancy progressed although more than 80% of the subjects took iron supplements after the 20th week of pregnancy. These results imply that it is needed to provide more iron especially, heme iron and dietary enhancers to prevent the deterioration of iron status during pregnancy. Future research on bioavailability of supplemental iron should be performed to determine the iron balance precisely.

• 한국응용과학기술학회지
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• 제28권2호
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• pp.170-177
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• 2011

Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. 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 stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.189-198
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• 1997

The purpose of the present study was to investigate the effect of medium chain fatty acid salts, reported as enhancers in insulin nasal absorption, on the rectal absorption of insulin in rats. The serum glucose and remained insulin level in perfusate were measured after rectal recirculation of insulin with or without sod. laurate, sod. caprate and sod. caprylate in situ. The addition of sod. laurate or sod. caprate reduced serum glucose concentration considerably. Sod. caprate (1.0%) showed the greatest promoting effect on the decrement of serum glucose. Eudispert hv hydrogels containing insulin with medium chain fatty acid salts were, thereby, prepared and evaluated. The release rate of insulin from Eudispert hv hydrogels was reduced with an increase in the content of Eudispert hv, and was raised with increasing NaOH concentration. Ten percent Eudispert hv hydrogels were offered for the rectal administration of insulin. The addition of 1.0% sod. caprate reduced serum glucose concentration remarkably after rectal administration of 10% Eudispert hv hydrogels containing insulin. The level of glucose decrement was greater by 30% compared to subcutaneous administration of insulin solution. From the above findings, Eudispert hv hydrogels would be used as useful rectal delivery systems of insulin.

• 한국식품영양과학회지
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• 제22권3호
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• pp.349-358
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• 1993

철분 결핍은 아직도 전 세계적으로 공통적인 영양장애중 하나이다. 특히 개발도상국에서는 식이로부터의 철분 생이용도가 매우 낮은데 이는 nonheme 철분 흡수를 매개하는 식이성분의 양이 매우 적은 것이 주원인이다. 식이에 함유된 철분의 양, 개체의 철분 영양상태, 그리고 식이성분 등은 철분흡수에 영향을 주는 주 요소들이다. 식이로부터 부적당한 철분의 섭취는 칼로리가 낮은 식이, 제한된 음식물 섭취, 단조로운 식이로부터 오기 쉽다. Ascorbic acid, 육류, 생선, 닭고기 등은 식이에서 nonheme 철분의 흡수를 증가시키는 매우 중요한 요소이며, ascorbic acid와 육류는 여러 연구에서 철분 생이용도 증가 효과를 일정하게 보여 주었다. Phytate, polyphenols, dietary fiber는 nonheme 철분 흡수의 주요 저해 요소로서 인지되어 왔다. 또한 nonheme 철분의 생이용도는 함께 섭취한 식품의 성분에 의해 크게 영향을 받을 수 있으므로 어떤 조합에 의한 식품의 섭취는 철분 흡수를 상승 또는 저해시킬 수 있다.

• 약학회지
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• 제60권1호
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• pp.36-45
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• 2016

This study was aimed to enhance the percutaneous absorption of tizanidine hydrochloride (TZ) across Strat-M$^{TM}$ artificial membrane and excised hairless mouse skin using various vehicles and chemical permeation enhancers. Solubility studies were performed using hydrophilic and lipophilic vehicles. To initially evaluate vehicle effects on skin permeation, Strat-M$^{TM}$ membrane was adopted using Franz-type diffusion cells loaded with 0.4 mg donor dose. Effects of fatty acids on the permeation of TZ from PG and PGMC were compared, and the effects of various hydrophilic vehicles in the presence of linoleic acid were studied using excised hairless mouse skin specimens. The mean solubility (mg/ml) of TZ in hydrophilic vehicles was higher: water > PG > DMSO > ethanol > PEG 200 > NMP > PEG 300 > PEG 400 > DGME, and solubilities in lipophilic vehicles such as PGMC, PGMC, IPM, Captex 200 and Captex 300 were much less than 1.0 mg/ml. Permeation rates through StratTM membrane from pure vehicles were in the rank order: PGMC ${\geq}$ LBF > DMSO ${\geq}$ NMP ${\geq}$ PGML ${\geq}$ PG ${\geq}$ PEG 200 ${\geq}$ DGME ${\geq}$ EtOH. However, permeation rates of TZ through hairless mouse skin from pure vehicles were very low, although PG showed the highest flux ($1.66{\pm}0.28{\mu}g/cm^2{\cdot}hr$). Therefore, PG was selected in further studies. Addition of enhancers (3 v/v%) into PG markedly increased the flux (${\mu}g/cm^2{\cdot}hr$): oleyl alcohol ($14.9{\pm}3.1$) ${\geq}$ oleic acid ($14.5{\pm}1.6$) ${\geq}$ linoleic acid ($13.7{\pm}1.3$) > capric acid ($4.4{\pm}0.6$) > caprylic acid ($2.1{\pm}0.4$). Among hydrophilic vehicles with linoleic acid, PG and DMSO revealed relatively higher permeation for TZ. Increase of donor dose in PG resulted in dose-dependent permeation fluxes. These results suggest that permeation properties of TZ from nonaqueous solutions are markedly different between Strat-$M^{TM}$ membrane and excised hairless mouse skin, and transdermal delivery of TZ would be feasible with a combination of PG and enhancers.

• Journal of Animal Science and Technology
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• 제62권5호
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• pp.692-701
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• 2020

This study evaluated the quality characteristics of crust derived from dry-aged Holstein and Hanwoo loins and their effects on food as additives. With respect to physicochemical properties, we examined the proximate composition, pH value, salinity, color, water and fat absorption, emulsifying capacity, and swelling yield. The protein and ash contents in the Holstein crust were significantly higher than those in the Hanwoo crust (p < 0.0001). The fat content in the Hanwoo crust was significantly higher than that in the Holstein crust (p < 0.01). The salinity, lightness, and yellowness of the Hanwoo crust were significantly lower than those of the Holstein crust (p < 0.001). Furthermore, the pH value and emulsifying capacity of the Hanwoo crust were significantly higher than those of the Holstein crust (p < 0.001). The fat absorption of the Holstein crust was significantly higher than that of the Hanwoo crust (p < 0.001). The swelling yield of the Holstein crust was significantly higher than that of the Hanwoo crust at pH 3 and 4 (p < 0.001), whereas the swelling yield of the Hanwoo crust was significantly higher than that of the Holstein crust at pH 7 (p < 0.001). Principal component analysis of dry-aged Hanwoo, Holstein, and non-aged Holstein showed different flavor patterns for each sample. Finally, the results showed that the crusts derived from dry-aged Hanwoo and Holstein loins were suitable flavor enhancers.