今井 一洋

Enantiomeric Separation and Spectrofluorometric Detection of of the Racemic drugs, (±)-1-(2, 6-Dimethylphenoxy)-2-Propamine (mexiletine) and (3RS)-4-Amino-3-hydroxybutanoic Acid (GABOB), Derivatized With 4-Fluoro-7-nitro-2, 1, 3-benzoxadiazole on a Phenycarbomylated cyclodextrin Bonded Stationary Phase.

K.Imai, H.Matsunaga, T.Fukushima, T.Santa, H.Homma K.Nakashima and S.Akiyama : A Novel Method for thr Amino Acid Sequence/Configuration Determination of Peptides Containing D/L-Amino Acids Utilizing a Fluorogenic Edman Reagent, 7-N,N-Dimethylaminosulphonyl-4-(2,1,3-benzoxadiazolyl) isothiocyanate(DBD-NCS).

Enantiomeric Separation and Spectrofluorometric Detection of of the Racemic drugs, (±)-1-(2, 6-Dimethylphenoxy)-2-Propamine (mexiletine) and (3RS)-4-Amino-3-hydroxybutanoic Acid (GABOB), Derivatized With 4-Fluoro-7-nitro-2, 1, 3-benzoxadiazole on a Phenycarbomylated cyclodextrin Bonded Stationary Phase.

For the topical treatment of rheumatalgia arthritis, four kinds of 2% aspirin washable ointments using crotamiton (formula 1), crotamiton with 2% anhydrous sodium sulfate (formula 3), crotamiton with 5% anhydrous sodium sulfate (formula 4) and isopropanol (formula 2) as solubilizers, respectively, were prepared. Stability of aspirin in aspirin ointments (4 kinds) was examined by HPLC with UV detection. Aspirin in any ointments was stable for 21 days at 5℃, but unstable at 20℃ and 30℃. Among 4 formulas, formula 1 gave the best results on the sensory tests. Five patients with rheumatalgia arthritis were treated with the 2% aspirin ointment (formula 1). The pain of the patients was relieved moderately or markedly. The pain started to fade within 5-15 minutes and the pain relief usually lasted for 1-8 hours after treatment. With respect to the pain relief, the ointment (formula 1) was the most effective as compared with the indometacin ointment and cataplasm (cold type). From these results, 2% aspirin ointment (formula 1) appeared to be an effective analgesic for the pain associated with rheumatalgia arthritis.

A simple method was newly designed and compared with a conventional method for the measurement of percutaneous absorption of drugs into human skin from ointments. The ointment was put on the gauze (8×17mm) of a sticky plaster, the rear side of which was covered with a selophan tape, and applied to the human skins. At intervals, the residual drug in the ointment was extracted and measured. The percutaneous absorption of the drug was calculated on the residual drug concentration. The absorption of aspirin from 2% aspirin ointment, which was effective for the cure of postherpetic neuralgia, was investigated by the proposed methods using isopropanol extraction and HPLC determination of the residual aspirin in the ointment. There was no great difference between the absorption of aspirin into the arm and that into the backskin of a normal subject. About 35% of the aspirin was absorbed for 7 hours. A similar absorption pattern was observed in the two patients of postherpetic neuralgia. Thus, the proposed method might be useful for measuring absorption of many other drugs and investigating the effect of bases and accelerators on the absorption into the human skins.