In the preparation of 0.1% atropine sulfate powder, the effect of the method of preparation on mixing degree, distribution of particle size and component in different particle size was studied by three different methods using tartrazin as a model. Solution mixing method (SMM) as compared with powder dilution method (PDM) and combined method of SMM and PDM, though the component in different particle size was different, gave a good mixing degree which showed small variance at various sampling weight. Distribution of the component in SMM was affected by material or volume of bindet. All the particles in granules which passed through 42-mesh sieve and remained on 200-mesh sieve maintained the 90-110% content when 10% water was used as binder in SMM. Furthermore, packaging procedure had little effect on content uniformity of the powder prepared by SMM and PDM. SMM, if the component in the different size fraction was checked, proved to be a very good method in the preparation of the powders with very low content of active ingredient in hospital pharmacy. Thus 0.1% atropine sulfate powder with good content uniformity was obtained by SMM.

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The enteric coated granules contained in 10 kinds of commercial digestive enzyme capsules were examined for change with time of resistance in pH 5.0 test solution and dissolution in pH 7.0 solution. Changes of resistivity with time were recognized in nine samples. Furthermore, the enteric coated films of two samples were weakened with ime and were liable to rapid dissolution, whereas those of two other samples were hardened and interfered with enzyme dissolution. Consequently, it was suggested that one must be more careful about the change of the enteric coated films of digestive enzyme preparations with time than that of their activity.

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Compatibility of lactase preparations (G-TT, O-ON, L-WM, L-NK, ORG) with 20 other drugs was studied. The samples mixed with the drugs were wrapped with polyethylene-glassine and observed for the change in appearance and activities for 28 days under 3 different conditions: 5±1°, RH 40-50%; 25±1°, RH 75%; 30±1°, RH 90-92%. Then, compatibility of the lactase preparations was compared with each other.
In the above study, the samples mixed with G-TT indicated the fastest change, while those mixed with L-NK, ORG, O-ON and L-WM showed evidently different compatibility from that of the others. In spite of the preparations of the same component, a significant difference was recognized between them. Most of them corresponded with each other in the change of appearance and decrease of activities. It is also important that one must be carefull with a case resulting only in decrease of activities when lactase is mixed with acid or alkaline agents.

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Buformin tablets of 5 Japanese brands (A, B, C, D, E) were tested for their pharmaceutical properties. Brand E had higher dissolution rate and shorter disintegration time than those of the other brands.
Urinary excretion measurement of brand A was made in 31 diabetic patients and 4 healthy males after oral administration. In all the healthy males and most of diabetic patients, about 80% of the dose administered was excreted in urine within 24 hours, as compared with about 30% in 2 diabetic patients.
The correlation was investigated between urinary excretion of buformin and several clinical laboratory findings, and the following results were obtained: 1) A good correlation was observed between urinary excretion of buformin and creatinine clearance. 2) Quantity of biogenic amines after oral administration of buformin was decreased in comparison with that before the administration.

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The quality of two kinds of commercial pindolol tablets, uncoated A and sugar-coated B, was evaluated by 3 tests: dissolution, weight variation, and content uniformity. The dissolution test was made with Sartorius Solubility Simulator. The weight variation test was made according to the method prescribed in J. P. X. In the content uniformity test, both tablets A and B were dissolved in 0.1 N HCL solution. Pindolol was determined spectrophotometrically.
Following results were obtained: 1) In the dissolution test, 50% dissolution time of the two kinds of tablets was almost the same. However, the dissolution ratio at 5 min of the tablet A was significantly higher than that of the tablet B. 2) In the weight variation test, the tablet A met the criteria of J. P. X, and the weight variation of the tablet B was also very small. 3) In the content uniformity test, the mean contents of the two tablets were about 100%.

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The dissolution pattern of 5 kinds of commercial indomethacin capsules were measured with the U. S.P. dissolution tester in pH shift test solution adding 0.25% Tween 80 in consideration of the acidity in the gastrointestinal tract. Sample A was not coated capsules containing 25mg of indomethacin, whereas samples B and C were prolonged activity capsules containing 25mg, and samples D and E were prolonged activity capsules containing 37.5mg. pH of the medium was designed to rise gradually from 2.3 to 3.7 in the first 150 min, rapidly from 3.7 to 6.2 in the subsequent 30 min, and gradually up to 6.9 after 300 min.
The following results were obtained: 1) Sample A: The time required for 100% dissolution was about 30 min. 2) Samples B and C: The dissolution pattern of B was apparently different from that of sample C. About 100% of sample B was dissolved after 300 min, compared with about 75% of sample C. 3) Samples D and E: The dissolution pattern of sample D was apparently different from that of sample C. About 100% of sample D was dissolved after 300 min, as against about 80% of sample E.

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A competitive binding enzyme immunoassay (MARKIT) procedure for determination of the concentration of antiepileptic drugs was assessed and compared with gas-liquid chromatographic (GLC) procedures. Furthermore the Possibility of antiepileptic drugs determination in serum ultrafiltrate and mixed saliva was investigated with MARKIT. The two methods of MARKIT and GLC gave essentially the same results in determination of the serum levels of phenobarbital. The correlation coefficient of MARKIT between GLC was as high as 0.922. The recovery of the phenytoin in serum, serum ultrafiltrate and saliva were 98.1±1.9, 97.5±2.9 and 72.5±3.6%, respectively. The correlation coefficients between serum and serum ultrafiltrate and serum and saliva were 0.926 and 0.654, respectively. These data suggest that MARKIT is a reliable method for the determination of the concentration of antiepileptic drugs in serum, serum ultrafiltrate and saliva.

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Therapeutic drug monitoring procedures after high-dose methotrexate (MTX) therapy were studied with enzyme homogeneous immunoassay technique (EMIT). MTX levels in serum of osteosarcoma patients administered intravenously 200-300 mg/kg dropped below 10μM in 24 hours after the initiation of the therapy.
Ultrafree filtration method was used for the separation of the drug in free form from the protein-bound form in serum. The ratios of free to total MTX levels were approximately 0.60 in 0.1-650μM of total MTX levels. MTX monitored with EMIT is clinically useful to prevent or reduce its toxicity. MTX in infusion solution was susceptible to photodecomposition with the addition of vitamin B₂.

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Environmental sanitation in the dispensary is discussed in view of the probable microbial contamination of pharmacists to be caused in contact with prescriptions brought by patients. Following results were obtained:
1) In the pharmacists who prepared powder drugs, the number of microorganisms on their fingers recorded after 2-hour service preceded by handwashing was larger than that checked upon their arrival at the dispensary in the morning. In the positions of the dispensary where powder products were not handled, the bacterial contamination after 2-hour service was on almost the same degree as that immediately after pharmacists arrived at the dispensary. The total number after service was somewhat larger.
2) The number of microorganisms detected in the prescriptions was largest in those issued from the department of dermatology, followed by that from internal medicine and from ophthalmology, in that order. More microorganisms were detected in the fingers of pharmacists who touched highly contaminated prescriptions from the dermatologic department.

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The microbial contamination of commercial purified water (J. P.) was studied. All of 8 samples examined were contaminated, especially with non-fermentative gram-negative rods and gave the bacterial counts of 50 to 100, 000/ ml. Organisms isolated from the purified water were highly susceptible to tetracyclines and aminoglycosides, but most of the isolates showed a resistance to β-lactam antibiotics and polymyxin B. The resistance of the isolates against heat and ultraviolet light was comparatively lower. These results reaffirmed that storage at 80° and ultraviolet radiation are very useful in controlling the bacterial contamination of purified water.

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Recently there has been remarkable increase in the amount of antibiotics used for various infections. Various problems concerning drug-resistance or microbisme selectionné et substitué were studied in terms of frequency of use or combination of the antibiotics. The following results were obtained from the prescriptions written during June 1 to 30 of 1978, 1979 and 1980 at Miyazaki Medical College Hospital: 1) The ratio of antibiotic prescriptions to the total prescriptions was approximately 20-24%. 2) The descending order of the frequency of use by group of antibiotics was: cephalosporins, penicillins, aminoglycosides, tetracyclines, maclorides, others. The same tendency was seen in each of the three years. 3) Aminoglycosides were the most frequently combined antibiotics. 4) Among the departments, the department of surgery recorded the largest number of antibiotics (single and combined use), while the internal medicine had the largest number of prescriptions written.

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In this study, based on the prescriptions written during June 1 to 30 of 1978, 1979 and 1980 at Miyazaki Medical College Hospital, quantitative studies were carried out on various antibiotics used orally or intravenously at different medical departments. The following results were obtained:
1) Cephalosporins and penicillins were the most frequently used antibiotics accounting for 90% of the total amount of antibiotics used. 2) The amount of use of cephalosporins and penicillins was large in surgery as well as in internal medicine, while aminoglycosides were used remarkably in surgery. However, macrolides and tetracyclines were scarcely used in surgery. 3) Injections were more frequently used than oral dosage forms in case of cephalosporins, penicillins and aminoglycosides. But macrolides and tetracyclines in oral forms were used more often than in injections. 4) Sulbenicillin, cephalexin, kanamycin, erythromycin and minocycline were used most frequently among penicillins, cephalosporins, aminoglycosides, maclorides and tetracyclines, respectively.

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