The concentrations of diphenylhydantoin (DPH) and phenobarbital (PB) in the plasma obtained from the outpatients with epilepsy were determined by the enzyme multiplied immunoassay technique (EMIT), and the results were recorded on a data sheet which was named “Monitoring Chart” of the respective patients.
These data were retained and possible correlations were analyzed, and the plasma concentrations of DPH were found to be higher when DPH was administered in the dosage form of tablet than when administered in the form of powder. It was also suggested that the concentrations of DPH were decreased when the other antiepileptics such as PB and valproic acid (VPA) were used in combination. However, PB in the blood was increased when it was combined with VPA or DPH.

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Theophylline concentration in plasma collected from asthmatic patients was determined by Substrate-Labeled Fluorescent Immunoassay (SLFIA, AMES TDA). The results of this method were compared with those of Homogeneous Enzyme Immunoassay (EMIT). High correlation was found between SLFIA and EMIT, showing the correlation coefficient 0.970 (n=47). The variation coefficient of replicate analysis on a spiked sample by the SLFIA method was below 5%. The modified SLFIA method was applied to the theophylline plasma level of a small sample for immature infants. The values of the modified SLFIA correlated well to those determined by SLFIA and EMIT. The correlation coefficients were 0.989 (n=15) between modified SLFIA and SLFIA, and was 0.964 (n=15) between the modified SLFIA and EMIT, respectively. The variation coefficient of the replicate analysis on a spiked sample by the modified SLFIA was below 8%. In view of application to pediatric patients, the procedure of the modified SLFIA has considerable advantages over hitherto available method which requires only 10μl of plasma for a single determination thanks to the elimination of the deproteinization and extraction steps.

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Five lactase preparations in powder (G-TT, O-ON, L-WM, L-NK, ORG) were compared in terms of sensory test, weight deviation, potency deviation and residual rate. Further, the changes in appearance and potencies were examined for the maximum of 26 weeks in three conditions: A (5°±1°, RH 40-50%), B (23°±1°, RH 75-80%) and C (40°±1°, RH 90-92%). Consequently G-TT showed the poorest result in the sensory test, while O-ON recorded a high residual rate and it was found that the actual dose of this agent was smaller than that was expected.
L-WM was recognized as the best product in the test of change with time, but about 10% of L-WM was deteriorated at the part of cutting. ORG showed faster change in appearance than any other product due to poor moistureproofing. L-NK proved not inferior in any test.

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Five β-galactosidase preparations (A, B, C, D and E) from different manufacturers were studied comparatively. Their pH stability, optimum pH of the enzyme preparations with 3 substrates (ONPG, lactose and milk) and change on standing were tested by ONPG (o-nitrophenyl-β-galactopyranoside) method and blood sugar GOD perid test. Protease activity and impurities were determined by Casein-Folin method and gel-filtration chromatography, respectively. While preparations B, C, D and E showed almost similar results of stability test, .preparation A was most unstable and apt to undergo change in appearance. Further, preparation A showed protease activity 50-60 times higher than that of the others, and contained impurities. Based on these results, it was concluded that preparations B, C, D and E are better products than preparation A.

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Comparisons of enzymatic activities of five commercial lactase preparations were made in terms of the sensory tests of such properties as appearance, smell and taste.β-Galactosidase activities were different among preparations, and the activity was found to be higher or lower than the labelled activity of the respective preparations. Stability of the enzyme activity at various temperatures and pH was also different among preparations. Marcked characteristics of other enzymes contained were also shown in the potency test and sensory test.

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The quality of five different brands of lysozyme chloride granules (A to E) was evaluated by the dissolution test (U. S. P. XIX) and several in vitro tests. The activity of lysozyme chloride was proportional to its content, whereas the activity of product B was slightly weaker than that of the other products. All the products met the requirements for the disintegration test of J. P. IX. The dissolution rates of the products A and B reached 100% within 60 minutes in the 1st and 2nd fluids (J. P. IX), and water, but those of the products C and E remained below 70% even after 120 minutes in any solution. The dissolution rate of product D was considerably influenced by the dissolution solutions used.

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Drugs in fine granules are characterized by the minimum loss of components caused by dusting in dispensing, easy and uniform mixing with powdered drugs, and comparable bioavailability to powdered drugs. In this regard, 4 brands of γ-oryzanol preparation were tested for their physicochemical properties, mixing efficiency of γ-oryzanol with lactose, and dissolution rate. As a result, all the brands complied with the Particle Size Distribution Test of J. P. and the proposed test on flow behavior in terms of angle of repose, whereas the dispersibility was as high as 31% with one brand. The test on the uniform distribution by mixing test materials also showed a significant variation including CV value as high as 8% in one brand. The high CV value is a factor affecting the uniform distribution of γ-oryzanol due to the aggregation of this active component. The 4 brands were also tested for 50% dissolution time with three different test solutions. The values obtained were compared by a two-way analysis of covariance at.a significant level of 5%. Significant differences were observed among the brands, but not among the test solutions.

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The quality control of drugs was evaluated from the direction of microbial contamination which was determined by sterility test, total aerobic microbial counts and the detection of coliform bacteria. 19 pharmaceutical products showing serious microbial contamination in our previous tests and 41 additional pharmaceutical products newly developed from natural substances (chinese medicines) were selected for the present study.
The total aerobic microbial counts exceeding 10³/g were observed in 5 of the 19 products, which showed the same incidence as that in the previous test. The results of the sterility test and microbial counts were correlated well. Coliform bacteria were detected in 3 products, compared with 2 products in the previous test. In case of the newly tested 41 products, the total aerobic microbial counts over 10³/g were observed in 6 products, whereas coliform bacteria were detected in 1. Although the microbial contamination at high degrees was still observed especially in products consisting of natural substances, it is concluded that the recent microbial quality control of the pharmaceutical products has generally been improved.

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A number of papers have been reported on the quality of tablets and capsules containing the same ingredient. However, a little attention has been paid to the quality of injections. In this study, we used six kinds of aprotinin injections. Aprotinin is a kind of proteolytic enzyme inhibitors extracted from bovine lung. The quality of such preparations of extracts from organs may be influenced by the method of extraction and purification as well as by preparation technique. The quality was evaluated by general pharmaceutical tests of infections, electrophoresis and measurement of particle size.
The quantity of all the six products in containers was compatible with J. P. IX. The aprotinin and protein contents were 94.9-111.9% and 0.15-0.26μg/KIE (KIE: Kallidonogenase inactivator units), respectively. In the electrophoretic test, one of the preparations showed a different band from that of others.

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Eight types of the commercial FAD injection were studied from the pharmaceutical viewpoint with high-performance liquid chromatography (HPLC). lt was found that most of the commercial FAD injections had lower content of FAD than their labelled amount. FAD was detected from the HPLC peaks whether it is manufactured by synthetic method or fermentation method.

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Various types of machines have been used for dividing and packing of powders and/or granules at most pharmacies. It is essential that powders and/or granules be divided accurately by a machine. Comparative studies of 4 machines were carried out on the variation of weight after the division. The machines tested were Konishi KC-747-K12 type (B) equipped with a belt conveyor to feed powders and/or granules into the division holes by alternating motion, Konishi KC-787-K15 type (L-1) and its modified type (L-2) equipped with a linear vibrator in place of a belt conveyor of type B, and Towa VS-42 type (R). Enteronon-R Powder, Popon-S Fine Granule and Berizym Granule were selected as the samples for the studies. 15g of each sample were divided into 15 parts by each of these machines, and the process of dividing was repeated 10 times.
As a result, the machine L-2 showed smaller variations of weight after the division than any other machine tested. When Enteronon-R, Popon-S and Berizym were divided by this machine, the coefficients of the variation of the weight after the division were 2.2-4.4%, 2.7-4.7% and 2.6-5.1%, respectively.

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Recently, we have reported that theophylline concentrations in plasma as determined by substratelabeled fluorescent immunoassay (SLFIA) well correlated (r= 0.96) with the concentrations by high-pressure liquid chromatography, and that SLFIA procedure had considerable advantages over hitherto available method. Methods for measurin.g theophylline in saliva previously reported were spectrophotometry, gas-liquid and high-pressure liquid chromatographies. Here, we used the SLFIA for the determination of theophylline concentrations in saliva. It was possible to determine salivary theophylline in low concentrations by using salivary altered first dilution rates with SLFIA method. The concentrations of theophylline in the plasma and saliva in 7 normal adults and 3 asthmatic patients who were administered aminophylline were determined by SLFIA method. In normal adults, the time-course of plasma and salivary theophylline levels showed a parallel relationship, and theophylline concentrations in the saliva as determined 2 and 4 hours after administration were about 44% lower than those in the plasma. In asthmatic patients, theophylline concentrations in saliva 2, 4, 6 and 8 hours after administration were also 32% lower than those in the plasma. These results suggested that monitoring patients by means of salivary theophylline level is effective way to predict plasma levels and to help patients avoid pain of bloodletting.

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The therapeutic effects of D-penicillamine were evaluated statistically in 44 patients with rheumatoid arthritis, and the adverse reactions were investigated in 47 patients including 3 patients with progressive systemic sclerosis.
Statistically, significant improvement was observed especially in the number of painful joints, erythrocyte sedimentation rate and grip strength of hands. D-penicillamine, like gold salts, was proved to be undoubtedly an effective anti-rheumatoid drug. The adverse reactions were observed in 55.3% of the patients, including 4 patients in which major of fatal reactions were seen. Therefore, D-penicillamine should be used carefully and the therapy should be started with the lowest dose.

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