Ten commercial digestive enzyme capsule preparations (Aczym, Berizym, Excellase, Feltase, Holmilase, Panatose, Politose, 7E, Stomilase and Toughmac-E) were examined for difference in activity between new and old lots and change in activity with time in the storage for 0-65 months at 25-28°, RH 50%, in press-through pack. As a result, difference between lots was recognized in 7E and Toughmac-E, and the apparent inactivation of protease in Feltase, Panatose and Toughmac-E, amylase in Feltase and Panatose, and lipase in Berizym, Excellase, Stomilase and Toughmac-E. Though all preparations showed a reduction, to some extent, of the activity before the expiration date, that seemed not significant in clinical use.

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In order to evaluate the influence of the volume of water in oral administration upon the absorption of orally administered antibiotics, comparative evaluation was made with AMPC which was found in the previous study to have good absorbability and ABPC having poor absorbability when orally administered. The two antibiotics were given to 4 healthy male volunteers in dose of 500mg. Water was orally given with the antibiotics in two different volumes, 30 and 150ml, in fasting and non-fasting (less than 5-minute postprandial) states, and the blood levels of the antibiotics and their excretion rates in urine were determined by cross-over method. It was suggested that AMPC, particularly when administered in fasting, would give smaller individual difference in absorbability if the volume of water was increased. In contrast, no specific effect of the amount of water was exerted upon the absorbability of ABPC given in any state of fasting and non-fasting. When given postprandially, the time required for reaching the peak blood level of both antibiotics was delayed irrespective of the volume of water.

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It has been widely known that bile acids increase lipase activity, and the lipase activity of various digestive enzyme preparations has been reported. Clinically, bile acids have often been administered in combination with digestive enzyme preparations. In this study, effects of three bile salts (sodium ursodesoxycholate, sodium chenodesoxycholate and sodium dehydrocholate) on the lipase activity of digestive enzyme preparations were examined. When soybean oil emulsified by polyvinyl alcohol was used as a substrate, these bile salts increased their lipase activity. In the presence of sodium chenodesoxycholate, sodium ursodesoxycholate and sodium dehydrocholate, digestive enzyme preparations increased their lipase activity by 2.2, 1.5 and 1.3 times, respectively, stronger than that in the absence of these bile salts. When soybean oil was used as a substrate, only sodium chenodesoxycholate increased the lipase activity.

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A new immuno precipitation inhibition technique (i-PiT method) was successfully applied to the determination of phenobarbital (PB) and phenytoin (PHT) in plasma. Each coefficient of variation for the 3 levels of PB or PHT was less than 10% within-run and between-run. 82 plasma specimens of epileptic patients were examined by the i-PiT method and absorptiometry. There was good agreement between the i-PiT and absorptiometry results, and the coefficients of correlation were 0.990 for PB and 0.995 for PHT.
Neither primidone and carbamazepine, nor the metabolite of PB or PHT, p-hydroxyphenobarbital or p-hydroxyphenylphenylhydantoin, interfered the i-PiT method under therapeutic conditions. Therefore, the i-PiT method will be useful for the plasma level monitoring to patients undergoing PB and PHT therapy.

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Serum of 43 patients under digoxin therapy and 6 ampules of high concentration digoxinspiked serum were analyzed by homogeneous enzyme immunoassay (EMIT) and ¹²⁵ I-radioimmunoassay (¹²⁵ 1-RIA). The correlation coefficient was 0.923 and the regression line was Y= 1.235 X-0.195 (Y: EMIT, X: ¹²⁵ 1-RIA). Hourly change in the EMIT digoxin assay was determined by 2 specimens of control serum containing 1.0 and 3.0ng/ml of digoxin, and 3 specimens of mixed serum of patients. The coefficient of variation (CV) was less than 5.1%. Daily change in the assay was determined by 5 calibrators for 7 months and a control serum containing 1.0ng/ml of digoxin for 5 weeks. The CV was less than 7.1%. EMIT digoxin assay was thus recognized as a good substitute for RIA method especially it is recommended in hospital laboratories.

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The stability of vitamin B₂ (riboflavin phosphate sodium) in infusion solution was studied in consideration of the practical condition in hospitals. When mixed in infusion solution, vitamin B₂ (10mg) was photodecomposed, showing the residual rate 80% at 2000 lux for 3 hours. This decomposition was inhibited by the addition of ascorbic acid and in infusion solutions of amino acids. Flavineadenine dinucleotide was more stable than vitamin B₂. As a main degradation product of vitamin B₂ in infusion solution, lumichrome was identified by high-speed liquid chromatography. Vitamin B₂ of multivitamin injection for intravenous hyperalimentation (IVH) was stable in IVH solutions.

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Rectal suppositories of digoxin were made with cacao butter containing 5% of polysorbate 60, SFAE-11, SFAE-15, SML, GMS, and PGMS. Physical properties, melting point, dissolution time, and hardness of these suppositories were measured. Blood levels of digoxin in rabbits after rectal administration (0.3mg/kg) were determined by a radioimmunoassay method. Bioavailability was estimated by measuring the relative area under the concentration-time curve for digoxin suppositories. Plasma digoxin concentrations of suppositories containing SML, GMS, and PGMS were poor. The relative AUC for digoxin suppositories containing SFAE-15, SFAE-11, SML, GMS, and PGMS were 0.90, 1.02, 0.23, 0.27, and 0.23 respectively when a suppository containing polysorbate 60 was used as the standard. The ratio between 1.5-hour value and 0.5-hour value of plasma digoxin concentration after rectal administration for suppositories containing SFAE-15, and SFAE-11 were 0.56 and 0.65. The highest plasma digoxin concentration was obtained with suppository containing SFAE-15 and plasma digoxin level was kept for a long time with suppository containing SFAE-11.

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The number of drugs used per patient per day was studied at 51 hospitals in Akita Prefecture. The survey was made of 8, 182 inpatients in July 1978 and 9, 455 in February 1979. Patients took 7.4 kinds of drugs on the average in the first survey, as compared with 7.7 kinds in the second survey. In both surveys, the number of patients given only internal medicine or injection was larger at smaller hospitals. The number of patients treated with internal medicine and injection and those on internal medicine, injection and external medicine was larger at larger hospitals. The frequency of use of any of external medicine, injection and external medicine was higher at larger hospitals. The average number of internal medicines per patient was smiler at larger hospitals, whereas the number of injections was larger at smaller hospitals. In older patients, the ratio of patients treated with internal and/ or external medicines was higher and the average number of drugs larger. That tendency was not observed in patients on injections.

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L-Keflex granule is a sustained release preparation of cefalexin in rapid release granules (30%) and enteric coated granules (70%). The acid-resistance and the dissolution pattern of this preparation were measured with the U. S. P. dissolution tester in the following test solutions:(a) pH shift test solution in consideration of pH levels of gastrointestinal tract: 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.(b) Test solutions at pH 1. 2, 4. 5, 6.0 and 6.5. The following results were obtained: 1) In the pH shift test solution, the calculative dissolution rate rapidly increased to 30% in the first 20 min, unchanged in the subsequent 200 min, and again rapidly rose to 100% after 280 min. 2) At pH 1.2 and 4. 5, the calculative dissolution rapidly increased to 30% within 20 min, but the granules were not dissolved thereafter. At pH 6.0, the time required for 100% dissolution was about 140 min, and at pH 6.5, about 30 min. Thus, the dissolution of the rapid, release granules and the acidresistance and the dissolution of enteric coated granules were satisfactory, and the pH shift test method used above must be effective in a qualitative evaluation of granule preparations of such type.

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The method for determining the blood level of ethosuximide was first described by Hansen in 1963. Referring to his method, we determined the plasma level of ethosuximide by the method for measuring phenytoin and phenobarbital proposed by Saitoh and others. This method proved to be much reproducible. In the test, 2ml of phosphoric acid buffer and 11 ml of dichloroethane were added to 0.5ml of plasma. The solution was well shaken and centrifuged at 2500 rpm. After 3ml of 1N-NaOH was added to 9ml of dichloroethane layer, the mixed solution was well shaken and centrifuged at 2500 rpm. The 1N-NaOH layer was transferred to a microcell and its absorbancy at 218 nm was measured.
The standard curve showed a straight line passing through the origin of the coordinate axes. The average recovery rate was 97.8±1.4%. Thus, by the method of Saitoh and others it became possible to measure at the same time the levels of phenytoin, phenobarbital and ethosuximide.

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Compatibilty of Bricef Dry Syrup (cefatrizine oral suspension) with mixed solutions which were often pre scribed in our hospital was investigated in terms of changes in external appearance pH and residual potency of cefatrizine (CFT). These changes were checked immediately after and 1, 3, 5, 7 and 14 days after mixing. The results showed lowering, to some extent, of CFT potency in relatively high pH region. Especially, when dry syrup was mxed with an alkaline solution, CFT potency reduced significantly within 24 hours at room temperature. These results suggest that careful attention should be paid to the above combination since a risk of incompatibility may be involved.
Color of suspensions of a few preparations changed during the storage. The change in color should be avoided to prevent anxiety in patients, though its correlation with stability of CFT is not clear. In combiantions with other solutions, the change in appearance, pH and potency of CFT was small, suggesting that such combinations be clinically recommendable.

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