http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
DRUG METABOLISM IN TRANSDERMAL DRUG DELIVERY
최후균 전남대학교 약품개발연구소 1997 약품개발연구지 Vol.6 No.1
In the most recent two decades, a large number of investigations have been directed toward transdermal delivery of drugs to achieve systemic effects. Scopolamine, nitroglycerine, fentanyl, clonidine, estradiol, and testosterone have been shown to have clinically significant transdermal permeabilities (1,2). One of the major difficulties in attempting io deliver a drug through the human skin into the systemic circulation is the selective barrier property of the skin, especially for polar compounds. This impermeability holds the percutaneous absorption of many dings, including amino acid analogues and bioactive peptides, to levels less than required for pharmacological activity. Due to the inherently low permeability of the skin, many investigators have used radio-labeled compounds in percutaneous absorption studies, based on the ease of detecting such compounds and on the low detection. limit achievable when using liquid scintillation counting as the method for analysis. However, scintillation counting can not differentiate metabolites and/or degradates from the parent compound, therefore, results from scintillation counting can sometimes be misleading. The transdermal route has been thought to have little proteolytic enzyme activity (3) and thus considered as a useful approach to solve the delivery problems associated with bioactive peptides. The objectives of this presentation are io demonstrate existence of metabolism and/or degradation pathway in the skin. Using samples from a leucine-enkephalin percutaneous penetration study and from a percutaneous absorption study involving a compound with hydroxyl group, it was found that there was a tremendous difference in detected penetrant when using scintillation counting versus HPLC assay as the method of analysis. Enzymatic metabolism of penetrants during the course of their diffusion across the skin also has been studied by many other investigators (4-7).
Effect of Enhancers and Pressure Sensitive Adhesives on the Transdermal Delivery of Fentanyl
최후균,이지영,장준호 한국약제학회 2008 Journal of Pharmaceutical Investigation Vol.38 No.4
The purpose of this study was to investigate the feasibility of developing transdermal drug delivery system (TDDS) for fentanyl used for the management of chronic cancer pain. The effect of type of pressure sensitive adhesive on the permeation of fentanyl from polyisobutylene (PIB), silicone and acrylic adhesive was evaluated. Due to the good adhesive force and relatively steady flux for 3 days, both acrylic and PIB adhesives were chosen for further study. The permeation rate of fentanyl was the highest from acrylic adhesive with hydroxyl functional group. Permeation rate increased linearly as the concentration of fentanyl in acrylic adhesive was increased from 2.5% to 10%. In case of PIB adhesive, crystals of fentanyl were developed above 5% drug load. CrovolR A40, CrovolR PK40 and Plurol oleiqueR provided higher flux of fentanyl.
조영주,최후균 조선대학교 약학연구소 1998 藥學硏究誌 Vol.19 No.1
Tacrine (9-amino-l,2,3,4-tetrahydroacridine), a reversible acetylcholinesterase inhibitor, is used for treating the symptoms of mild to moderate Alzheimer's disease. On per oral administraton, however, tacrine appears to exhibit side-effects such as dose-dependent and reversible hepatotoxicity. To overcome this disadvantage, we investigated the feasibility of developing transdermal drug delivery system for tacrine. The effects of various solvents on the permeation rate of tacrine salt across hairless mouse skin were examined using flow-through diffusion cell system. The solubility of tacrine salt in the solvents used in percutaneous absorption study was obtained using equilibrium solubility method. Among tested vehicles, octanol and propylene glycol/oleyl alcohol mixtures showed the highest permeability of tacrine salt. Theoretically, the higher the solubility, the lower the permeation rate. However, it was not possible to demonstrate any correlationship between the solubility and the percutaneous absorption rate of tacrine salt. The results indicate that some of the solvents may change the barrier property of the skin and/or carrier mechanism may be involved.
생체 피부조직을 이용한 피부보호제 in-vitro 시험평가
이은영,최후균,김상웅,서동성,조혜은,유치호,김창환,조영 한국군사과학기술학회 2022 한국군사과학기술학회지 Vol.25 No.4
Highly toxic chemical warfare agents(CWA) could be used in chemical warfare and terrorism. The protection of skin is crucial for civilians and soldiers, because the primary routes of exposure to CWA are inhalation and skin absorption. Thus, topical skin protectants(TSP) have been studied and developed in many countries to complement protective equipments. In this study, in-vitro test procedure was optimized and established using a flow-through diffusion cell system containing excised hairless mouse skin in an attempt to assess the effectiveness of various TSP formulations against nerve agent simulants. In addition, the test results on the formulations including the ingredients used in SERPACWA(Skin Exposure Reduction Paste Against Chemical Warfare Agent) and IB-1(TSP of Israel) were included, indicating that the formulations with perfluorinated compounds were more effective than the glycerin-based formulations.