Akiko Tomino

Studies on the syntheses of heterocyclic compounds. Part 855. Cycloaddition reaction of bis(trimethylsilyl) allenedicarboxylate with homocyclic dienes

Halogenolactonisation of the Diels–Alder adduct (4a) derived from bis(trimethylsilyl) allenedicarboxylate (3) and furan, followed by treatment of the products (5) and (8) with diazomethane, afforded the corresponding αβ-unsaturated methyl esters (6) and (9) respectively. Catalytic hydrogenation of both compounds provided the desired methyl esters (7) and (10) which were identical to the compounds derived by Arndt–Eistert reaction of the halogenolactonic acids (11) and (13) respectively.

Practical Analysis on the Trial Drugs under the Previous GCP.

The practical management regarding trial drugs according to the previous GCP system was analyzed between 1992 and 1996 to provide important information regarding the developmental status of new drugs or preparations under a newly revised revised system in our hospital. These findings helped to clarify the present status regarding the management of trial drugs especially regarding each specific drug.

Comparison of Enzyme Immunoassay with Gas-liquid Chromatography in Phenytoin Determination

The serum phenytoin level determined by enzyme immunoassy (EMIT) was compared with that by gas-liquid chromatography (GLC). There was a close correlation between EMIT and GLC, and EMIT gave better result than GLC. EMIT was carried out simply using a small quantity of untreated serum. The hemolysis of serum sample in this test was found to have no effect on EMIT. The mean phenytoin level was widely distributed, 2.33±3.54 μg/ml, and that was lower than the optimum range.

Pharmaceutical study on Commercial Medazepam Tablets and Capsules

A pharmaceutical study was conduced on commercially available tablets and capsules containing, respectively, 5 or 10 mg of medazepam. The variation of the average weight was less in tablets than in capsules. The disintegration time was shorter and its variation smaller in capsules than in tablets. In the quantative test, capsuels showed medazepam content which was 4-6% higher than that of tablets. The dissolution rate reached the maximum at the time of disintegration: to about 100% in 5 minutes with capsules, and about 95% in 20 minutes with tablets.

Pharmaceutical Study on Oxazepam Tablets

A pharmaceutical study was carried out on three kinds of tablets on the market (A, B and C) containing, respectively, 10 mg of oxazepam. The variation of the average weight was widest in tablet B, followed by C and A, in that order. Disintegration took place rapidly in all of the three tablets, but dissolution slowly. The dissolution rate in the primary solution in 60 minutes was 95% with tablet C, 90% with A, and 75% with B. Oxazepam content was not less than 96% in each tablet. In the test with rabbits, no significant difference in blood concentration of oxazepam was observed between the tablets.