• Journal of the Korean Applied Science and Technology
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• v.28 no.2
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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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• v.6 no.3
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• pp.48-57
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• 1976

An enhancement in the dissolution rate of the drug should facilitate its GI absorption if the absorption process is dissolution rate limited. One of the need for the techniques that can potentially enhance the dissolution rate and extent of absorption of hydrophobic drugs is the formation of coprecipitates with pharmacologically inert, polymeric materials. The physicochemical modification offers the advantage of possibly enabling one to administer the drug orally in a form from which it is most available for GI absorption. Several $investigation^{1-15)}$ demonstrated that the formation of solid dispersions or coprecipitates of relatively water-insoluble drugs with various pharmacologically inert carriers can increase singnificantly their in vitro dissolution rates. However, little information is available in the literature related to the dissolution rate patterns of furosemide, a water-insoluble diurectices, with respect to the sort of copolymer and the ratio of coprecipitates as a function of time, respectively. The purpose of the present investigation was to ascertain, the general applicability of the copolymers to use fore more fast, enhanced dissolution techniques of furosemide. To accomplish the need for enhancement in the dissolution rate of furosemide, varying ratio coprecipitates with different water-soluble polymers, such as polyvinylpyrrolidone (PVP), polyethylene glycol 4000(PEG 4000), and polyethylene glycol 6000 (PEG 6000), were quantitatively studied by comparing their dissolution characteristics of furosemide. The dissolution patterns of pure furosemide, varying ratio furosemide-PVP coprecipitates, (1:2, 1:5, and 1:9(w/w)), furosemide-PEG 4000 coprecipitates (1:4, 1:9, and 1:19(w/w), furosemide-PEG 6000 coprecipitates(1:4, 1:9, and 1:19(w/w)), and the same ratio physical mixtures, respectively, were compared by the amount dissolved as a function of time.

• Journal of Pharmaceutical Investigation
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• v.22 no.3
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• pp.1-15
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• 1992

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2004.05a
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• pp.27-29
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• 2004

Drug transporters play an essential role in the absorption, distribution and elimination of clinical drugs, nutrients and toxicants. The importance of the transporters is exampled by therapeutic failure in cancer chemotherapy that is mainly caused by the overexpression of multidrug resistance (MDR)-related transporters. In addition, the transporters may involve in drug-drug interactions that lead to serious adverse drug responses and some transporters also contribute to inter-individual variation in drug responses. As an effort to understand the mechanism underlying the inter-individual variation of transporters activity, genetic and environmental factors influencing the expression or function of the transporters have extensively explored through last decade. Among them, genetic polymorphism of drug transporter encoding genes has generated much interest since the discovery of functional single nucleotide polymorphisms (SNP) of MDR1 gene. Besides drug transporters, xenobiotic receptors also modulate drug disposition by regulating the transcription of drug metabolizing enzymes and drug transporters. Among many xenobiotic receptors, pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are two most well characterized since these receptors show wide substrate specificities and regulate the expression of various enzymes involved in drug disposition. Recently, several functional genetic polymorphisms were reported in PXR coding gene. In the present study, genetic polymorphisms of two drug transporters, MDR1 and BCRP, and two xenobiotic receptors, PXR and CAR, were investigated in Korean population.

• Proceedings of the Korean Society of Toxicology Conference
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• 2004.05a
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• pp.27-29
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• 2004

Drug transporters play an essential role in the absorption, distribution and elimination of clinical drugs, nutrients and toxicants. The importance of the transporters is exampled by therapeutic failure in cancer chemotherapy that is mainly caused by the overexpression of multidrug resistance (MDR)-related transporters. In addition, the transporters may involve in drug-drug interactions that lead to serious adverse drug responses and some transporters also contribute to inter-individual variation in drug responses. As an effort to understand the mechanism underlying the inter-individual variation of transporters activity, genetic and environmental factors influencing the expression or function of the transporters have extensively explored through last decade. Among them, genetic polymorphism of drug transporter encoding genes has generated much interest since the discovery of functional single nucleotide polymorphisms (SNP) of MDRl gene. Besides drug transporters, xenobiotic receptors also modulate drug disposition by regulating the transcription of drug metabolizing enzymes and drug transporters. Among many xenobiotic receptors, pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are two most well characterized since these receptors show wide substrate specificities and regulate the expression of various enzymes involved in drug disposition. Recently, several functional genetic polymorphisms were reported in PXR coding gene. In the present study, genetic polymorph isms of two drug transporters, MDR1 and BCRP, and two xenobiotic receptors, PXR and CAR, were investigated in Korean population.

• YAKHAK HOEJI
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• v.31 no.5
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• pp.286-295
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• 1987

The relationship between in vitro release and in vivo bioavailability of acetaminophen from suppositories was investigated. Effect of glycyrrhizin on the drug release and rectal absorption in rats was also examined. Suppositories containing 25mg of acetaminophen were prepared with Wecobee FS (fatty base) or PEG (water-soluble base) bases. The release from the suppositories were determined with USP rotating basket dissolution apparatus and with the suppository release tester. The temperature of the dissolution medium was very critical for the dissolution of acetaminophen from Wecobee FS suppositories. The bioavailability of acetaminophen was calculated from the plasma concentration-time curve after rectal administration of the suppositories to the rats. There were no significant differences in AUC following rectal administration of Wecobee FS and PEG suppositories, but the release and absorption from the Wecobee FS suppositories were faster than those from PEG suppositories. The dissolution rate obtained by the suppository release tester was better correlated with in vivo absorption rate constant than that by the USP dissolution apparatus. It suggests that the partitioning between rectal fluid and suppository base is the rate-limiting step in the rectal absorption of acetaminophen from suppositories. Glycyrrhizin was found not to affect in vitro dissolution and rectal absorption of acetaminophen.

• YAKHAK HOEJI
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• v.40 no.4
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• pp.400-410
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• 1996

In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.

• Journal of Radiation Protection and Research
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• v.31 no.1
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• pp.47-52
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• 2006

A self-absorption correction is important issue for the exact radioactivity determination of gamma emitting radionuclides in environmental samples which have the range of apparent density from $0.3g/cm^3$ up to $1.5g/cm^3$. In this paper, a practical and simple method without radioactive standard solutions having various densities is proposed for the self-absorption correction of environmental samples by a developed outside beaker surrounding Marinelli beaker. For the densities of 0.8, 1.0, $1.3g/cm^3$, the corrected efficiencies by the new method and the measured those by radioactive standard solutions of the three densities showed good agreement within 4 %.

• YAKHAK HOEJI
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• v.12 no.1_2
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• pp.16-31
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• 1968

Comparative studies were made on some sulfonamides, used individually and combined with parasympatholytic agents as regards (1) the absorption rate through isolated rat small intestine (in vitro), (2) the absorption rate through rat small intestine (in vivo), and (3) the blood concentration of sulfonamides were examined by its oral administration with each combined drug to rabbits, and the following effects were found, parasympatholytic agents inhibit the absorption of sulfonamides from the small intestinal tract. Comparison of the inhibitic efficiency of parasympatholytic agents is as follows: oxazepam, oxyphencyclimine hydrochloride, probantheline bromide, atropine sulfate (The examples are from the weakest to the strongest). Decrement of the absorption rate of sulfonamides is as follows: sulfadiazine, sulfathiazole, sulfamethoxypyridazine, sulfadimethoxine, sulfamerazine, sulfamethazine (The example are from the strongest to the weakest). Additionally, it is assumed that if the combined drugs were absorbed from the small intestine in the original form, those inhibitic effects should be best regarding to their sulfonamide per parasympatholytic agent combined rate "25:1" than to their any other rates.her rates.

• Journal of Pharmaceutical Investigation
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• v.16 no.1
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• pp.31-35
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• 1986

Effect of ethanol on the absorption rate, blood level and bioavailability of sulfamethazine (SM) in rats was determined. Absorption rate of SM was determined both by the in vitro and in situ experiment. In vitro, absorption rate of SM in rat small intestine was increased by 0.3, 1.0 and 3.0% ethanol. In situ, absorption rate of SM was increased by 0.3 and 1.0% ethanol but not by 3.0% ethanol. After oral administration, blood level of SM was elevated and relative bioavailability was significantly increased to 114.8% at the dose of 0.6g/kg ethanol but not significantly at the dose of 3.0g/kg ethanol. The time for attainment of peak blood level was changed from 2.5 to 1.5hr. Ethanol enhanced absorption rate constant of SM significantly and reduced elimination rate constant of SM administered orally at the dose of 0.6g/kg ethanol.