Lorazepam 제제의 용출에 관한 연구

양재헌 한국약제학회 1984 Journal of Pharmaceutical Investigation Vol.14 No.4

The tests of dissolution and bioavailability of six formulas of lorazepam tablet under various binders were performed. Lorazepam can be seperated in pharmaceutical preparation and biological plasma by high performance liquid chromatograph. Dissolution process of lorazepam tablet was largely influenced by binder and the dissolution rate was increased by sodium starch glycolate and microcrystalline cellulose, the slower dissolution rate in starch. Bioavailability of lorazepam tablet got relationship with dissolution rate, because tablets containing sodium starch glycolate and microcrystalline cellulose as binder maintained higher plasma level than other binders.

바이칼린 함유 생약의 제제화 및 생체 이용률 (제 2보) : 황금 및 황련 공침물의 장내 흡수 및 항균 효과 Gastro-Intestinal Absorption and Antibacterial Effect of Coprecipitated Product of Scutellariae Radix and Coptidis Rhizoma

양재헌,김동수,류희두,이남희 우석대학교 의약품개발연구소 1996 藥學硏究誌 Vol.1 No.-

Precipitation was formed during the preparation of decoction from mixure of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine, the active ingredients of the two herbal medicine were identified in coprecipitated product. Pills were prepared using the coprecipitated product and various binders. The dissolution rate of baicalin and berberine from pills was increased in at pH1.2 when acacia or tragacanth was used. The absorption rate of baicalin from the coprecipitated product was raster than the from Scutellaria extract, but the absorption of berberine from CPP was slower in stomach, duodenum and jejunum of rats compared with Coptis expract. The time equired for the maximum serum concentration (Cmax) of baicalin and berberine from CPP in mice were 150 and 200 min after oral administration. respectively. The maximum serum concentration of baicalin from CPP in mice was higher than Scutellaria extract, but the concentration of berberine was lower compared with Coptis extract. The minimum inhibitory concentration of CPP was below 50 ug/ml against gram positive bacteria, and was higher than that against gram negative bacteria. The antibacterial activity of CPP was lower than the of berberine.but was more potent than Scutellaria extract. It was found that the ingibition rates of growth by CPP against S. cpidermidis, K. pneumoniae, B cereus and S. aureus were 60.1, 5.11, 45.4, and 39.9%. respectively.

Transdermal Delivery System of Triamcinolone Acetonide from a Gel Using Phonophoresis

양재헌,김대근,윤미영,김태열,신상철 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.5

Triamcinolone acetonide (TA) is a corticosteroid that is used in the systemic and topical treatment of many inflammatory diseases. In this study, a phonophoretic drug delivery system was designed to enhance the TA permeability and the influence of ultrasound was examined. In order to establish the transdermal delivery system for TA, a hydrophilic carbopol gel containing TA was prepared after adopting phonophoresis. A permeation study through mouse skin was performed at 37oC using a Franz diffusion cell, and the ultrasound treatment was carried out for 10 h. The level of TA permeation through the skin was evaluated under various ultrasound conditions including the frequency (1.0, 3.0 MHz), intensity (1.0, 2.5 W/cm2), and duty cycle (continuous, pulse mode) using a 0.5% TA gel. The highest permeation was observed under the ultrasound treatment conditions of low frequency, high intensity, and in continuous mode.

Preparation and Evaluation of Ketorolac Tromethamine Gel Containing Genipin for Periodontal Diseases

양재헌,윤미영,Dae-Keun Kim,Mi-Jeong Kim,Young-Il Kim,Tae-Youl Kim,양규호,신상철 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.7

Ketorolac tromethamine gel (KT gel) and ketorolac tromethamine gel containing genipin (KTG gel) were prepared and their therapeutic effects on periodontitis were evaluated. The skin permeation rate of ketorolac from the KT gel and KTG gel was 5.75±0.53 and 5.82 ± 0.74 µg/cm2/ h, respectively. The skin permeation rate of genipin from the KTG gel was 10.13 ± 1.47 µg/ cm2/h. The tensile strength of the KTG gel was larger than the KT gel. After 4 weeks, the periodontal pocket depth of the KTG gel group (3.22 ± 0.20 mm) significantly decreased compared with the non-treated group (4.50 ± 0.25 mm) and the KT group (3.84 ± 00.26 mm). The KTG gel did not induce separation of the stratum corneum and subcutaneous tissue, and the collagen layers of the corium were closer, more fibrous, and showed longer connections than in the other groups. The KTG gel appears to be effective against gingivitis in the periodontal pocket through its increased anti-inflammatory activity and the crosslinking of genipin with the biological tissue.

The Effects of Ketorolac Tromethamine and Baicalein on the Levels of Inflammatory Factors in Human Synoviocytes

양재헌,윤미영,이남희,김대근,김영일,노영희,김태열,윤서원,신상철 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.11

This study examined the effects of ketorolac tromethamine (KT) and baicalein (BE) on the levels of inflammatory factors in human synoviocytes. The fibroblast-like synoviocytes (FLS) cells were used to determine the possible regulatory effects of KT and BE (KTBE) on the levels of inflammatory factors in FLS cells. In addition, the levels of TNF-α, IL-6, and IL-1β mRNA expression in FLS cells induced by a TNF-α and IL-1β co-treatment were largely inhibited by a KTBE treatment. The level of FLS cells proliferation was increased by IL-1β and TNF-α, and strongly inhibited by KTBE treatment. The production of oxygen species (ROS) was inhibited by KTBE in FLS cells. KTBE appears to regulate the levels of mRNA that are important for regulating RA progression.

Anti-Hyperalgesic and Anti-Inflammatory Effects of Ketorolac Tromethamine Gel using Pulsed Ultrasound in Inflamed Rats

양재헌,김태열,Ji-Hye Lee,Se-Won Yoon,양규호,신상철 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.4

The aim of this study was to determine if a Ketorolac Tromethamine (KT) gel solution could be administered in vivo via phonophoretic transdermal delivery using pulsed ultrasound by examining its anti-hyperalgesic and anti-inflammatory effects in a rat carrageenan inflammation model. 1% carrageenan was injected into the plantar surface of the right hindpaw of a rat, and anti-hyperalgesic and anti-inflammatory effects of KT via phonophoretic transdermal delivery were examined. The changes in the mechanical and thermal hyperalgesia, nociceptive flexor reflex (NFR), as well as the swelling changes were determined. According to the anti-hyperagesia and anti-inflammation tests, which were used to determine the change in the pain threshold, NFR and swelling showed that the group given the phonophoretic transdermal delivery of KT exhibited significantly more noticeable anti-hyperalgesic and anti-inflammatory effects than those treated with the simple application of a KT gel. The transdermal application of KT gel using phonophoresis had significant anti-hyperalgesic and anti-inflammatory effects. These findings suggest that the transdermal administration of a KT gel using phonophoresis using pulsed ultrasound might be useful for treating acute inflammation and pain.

바이칼린 함유생약의 제제화 및 생체이용률 (제 1보): 황금 및 황련 공침물의 확인 및 물리화학적 성질

양재헌,김동수,박현구,이남희,Yang, Jae-Heon,Kim, Dong-Su,Park, Hyun-Goo,Lee, Nam-Hee 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.4

Precipitation was formed during the preparation of decoction from a mixture of Scutellariae Radix and Coptidis Rhizoma or Phellodendri Cortex according to the prescription of Hwang-ryean-hae-dog-tang. Baicalin and berberine were identified in coprecipitated product and these components were the active ingredients of two herbal medicine. The coprecipitated product was very slightly soluble in water and sparingly soluble in ethanol. The stoichiometric ratio of baicalin and berberine was found to be 1:1. The lipid-water partition coefficients of coprecipitated product were increased more than baicalin and berberine in chloroform, but were decreased in other organic solvents. The content of baicalin and berberine in coprecipitated product, determined by HPLC, were 23.08% and 26.75%, but the content of active ingredients in supernatant were 0.66% and 0.26%, respectively. The dissolution profile of baicalin of coprecipitated product was increased more than extract of Scutellariae Radix in artificial gastric juice, but was decreased in artificial intestinal juice. The dissolution rate of berberine of coprecipitated product was lower than extract of Coptidis Rhizoma in artificial gastric juice and intestinal juice commonly.

치자 엑스의 가수분해에 의한 피부투과 및 항염효과

양재헌,이남희 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.2

Geniposide and its related iridoid compounds have been used in traditional herbal medicine for the treatment of Jaundice hepatic diseases and various inflammatorys. For the purpose to increase trandsdermal absorption, the hydrolyzed products of Gardeniae Furcuts were identified and assayed of active ingredients and investigated trandsdermal absorption and anti-inflammatory effects. Geniposide was hydrolyzed to genipin by β-glucosidase and it was suggested that genipin was more suitableform than geniposide for transdermal absorption by its lipophilic property. Using Franz type diffusion cell and the skin of hairless mouse, the permeation rate of hydrolyzed products and their emulsion preparation were determined. Genipin have more increased absorption ratio through the skin hairless mouse than geniposide. Also, the emulsion of hydrolyzed products of extracts showed higher permeability than that of nonhydrolyzed preparations. After 9 hours 280.85 ㎍/㎠ of genipin was absorbed and 193.52 ㎍/㎠ in case of geniposide. The Js of geniposide and genipin were 26.27±4.11 ㎍/㎠/hr and 40.35±5.04 ㎍/㎠/hr respectively. After carrageenan injection, the swelling was increased rapidly to 24 hr and maintained as a plateau. But emulsion group were reached about 2.5 mL and the swelling decreased successively from 24 hr to 72 hr. The anti-inflammation effects of extracts and hydrolyzed products emulsion were increased with significant difference with control group after 24 hr, 48 hr and 72 hr. In carrageenan induced edema, inhibition of swelling was increased in case of hydrolyzed product emulsion compare with nonhydrolyzed group at 24 hr, 48 hr and 72 hr after swelling. In histological study, the anti-inflammatory effects of hydrolyzed products were remarkable at 48 hr and 72 hr compare with nonhydrolyzed. Hydrolyzed products of Gardeniae Frucuts extract containing genipin would be a suitable preparation to increase the transdermal absorption and anti-inflammatory effects.

한국산 고등균류에 관한 연구(제1보) : 능이버섯의 단백분해효소 활성

양재헌,은재순,조덕이,이태규 한국약제학회 1988 Journal of Pharmaceutical Investigation Vol.18 No.3

This study was undertaken to investigate the proteolytic enzyme from Neungee mushroom [Sarcodon aspratus (Berk) S. Ito]. The proteolytic activity of Neungee was higher than other several edible mushrooms under various pHs. The potency of proteolytic enzyme of Neungee was same as the digestive drugs containing protease. So the proteolytic activity of the enzyme was increased in neutral or weak alkaline pH, whose characteristics would be alkaline protease. The specific activity of the purified enzyme obtained by using Tris acryl CM-cellulose ion exchange increased 20 times as compared with that of the crude extract. The proteolytic enzyme was stable at room temperature, but decomposition was fast when incubated at higher temperature more than 40℃. The half life of the enzyme was longest in neutral pH and rate constant was increased in acidic or alkaline solution.

복합제제의 약물 상호작용과 개선방안

양재헌 한국약제학회 1998 의약품 복합제제의 개발전략 Vol.- No.-