Amylase isozymes in commercial multiple digestive enzyme preparations were detected by a discontinuous buffer system in which Tris-Borate buffer was used for supporting medium and Veronal buffer for electrophoretic chamber. The supporting medium was first immersed in Tris-Borate buffer, then electrophoresis was performed with Veronal buffer. Oxoid membrane of cellulose acetate was used, and Dy Amyl (warner-Lambert) and Blue Starch (Pharmacia) were employed as substrates. In this procedure, the isozyme bands were well separated. Quality index of 11 enzyme preparations was made up on the basis of total amylase activity determined after incubation for 2 hours at 37° or 56°. The quality index corresponded to isozyme pattern.

View full abstract

Compatibility of Clonazepam granule with other agents was studied on the basis of weight change and UV spectroscopy. Thirteen mixtures of Clonazepam granule and different agents, wrapped in white paraffine paper, were left to stand for a long time at three grades of constant temperature and constant relative humidity (30°, 92%; 25°, 75%; 5°, 52%). Change with time in stability of respective mixtures was examined. Three of the 13 mixtures melted partially in 3 days at 30° but that was not caused by Clonazepam granule. It is especially interesting that the weight of the mixture of Clonazepam granule with Mino-Aleviatin (30°, 92%; 25°, 75%) decreased gradually with time. That was attributable to the sublimation of Mino-Aleviatin.

View full abstract

The enzyme activity may be affected by various factors in manufacturing process. The interaction of antiphlogistic enzymes contained in three commercial products was examined by Kunitz method, viscometry and polarimetry, with casein as substrate. Also, disintegration test and weight variation test were carried out. The activity of enzyme at optimal pH does not always correspond to its stability. The result of the tests was in conformity with the standard of J. P.IX.

View full abstract

Commercial cephalexin capsules were compared in terms of their in vivo absorption in humans, as well as of weight variations, disintegration and dissolution rates. No significant difference was found in dissolution rates among five of the six brands examined, but in the remaining one brands maximum plasma concentration was lower and the time for the concentration to reach the maximum level was varied between capsulles. That may be attributed to slow dispersion of the granule taken out from the capsules. Bioavailability of cephalexin, a readily absorbable substance, may largely depend on lubricants or granulation methods.

View full abstract

The relation between dry and moist states of potato starch and change in physical properties of the powder (agglomeration, dispersibility, apparent specific volume and angle of repose) by the addition of various lubricants (talc, magnesium stearate, calcium stearate, synthetic aluminum silicate and hydrous silicic acid) were studied. Following results were obtained: 1) Effect of hydrous silicic acid and synthetic aluminum silicate added to dried potato starch was most potent, and that of magnesium stearate was weakest. 2) When added to moist starch, hydrous silicic acid and synthetic aluminum silicate were most effective, but it was notable that calcium stearate, which was not so effective when added to dried starch, proved effective in moist starch. Almost all of the lubricants proved more effective in moist starch than in dried starch. 3) The effect of hydrous silicic acid added to dried starch was not changed even after the starch was moistened. All other lubricants reduced their effect after moistening. Especially, the lubricant effect of talc and magnesium stearate was lost when the water content of starch exceeded about 13%.

View full abstract

A method to determine the drug releasing characteristics of suppository bases with technetium-99m as tracer was developed. Each suppository contained 1.3g of base, 50μCi of Na^99mTcO₄ and 150mg od sulpyrine. Two water-soluble bases, 3 emulsified bases and 11 oleaginous bases were tested. The rate of release of ^99mTcO₄^- from a suppository throgh a cellulose film was higher in water-soluble bases, oilw type emulsified base, and Witepsol H-15 and 11-5 type bases as oleaginous bases. The release of ^99mTc0₄^- in oleagi nous bases and emulsified bases was markedly inhibited by the addition of a small amount of bees wax.

View full abstract

Commercial tranexamic acid preparations (of 4 manufacturers) and alclofenac preparations (2 manufacturers) were evaluated by disintegration test (J. P. VIII), weight variation test (J. P. VIII) and measurement of content. In the quantitative test, gas chromatography was employed for tranexamic acid preparations, and spectrophotometry for alclofenac preparations. Content of tranexamic acid was within the range of J. P. standard, with the difference of about 6% between the products. In the weight variation test, standard deviation between the products ranged from 2.22%(min.) to 10.89%(max.). All preparations tested showed similar disintegration times within the range of 3-4 minutes. There were some products containing cis form. Of alclofenac preparations, samples and products in the market were compared as for their content, disintegration times and weight variation. The test results came up to the J. P. standard in both groups. But weight variation of samples was 13.1%, standing far above 6.2% for the products in the market.

View full abstract

A study was made on the number of oral drugs by dosage form and by specialty, drugs commonly used in specialties, frequency of prescribing and the number of drugs prescribed, comparison of the frequency, and other matters. The oral drugs were selected from prescriptions for inpatients staying in the hospital for 5 months. Five lists of date of prescription, names of specialties, names of drugs, quantity of drugs and period of administration (days) were made up by use of computers (TOSBAC-40 and TOSBAC-5400). Some significant findings were obtained in the study. But the subsequent study should be made in improved method and effective use of computers.

View full abstract

Preparations of lithium carbonate, owing to the strong alkalinity of the agent, must be manufactured in enteric coated tablet. The composition and conditions of the manufacture of enteric coated tablet of lithium carbonate was studied. A tablet compounded by direct compression of lithium carbonte, Avicel, Perfiller and CMC-Ca in the ratio of 100: 20: 20: 1 proved most excellent in respect of disintegration time, dissolution rate, tablet hardness and standard deviation. A tablet coated with EC101 over the core covered with FC101 in equal weight to that of the tablet was freely disintegrated in alkaline test solution but not in acid test solution. Caution should be taken against humidity effect, since the disintegration of moistened tablet is hindered in alkaline test solution.

View full abstract