In order to examine whether 50 mg mucopolysaccharide polysulfuric acid esters (MPS) is the optimal dose for osteoarthrosis of the knee, a . double blind comparative study was carried out. A total of 101 patients were divided into three groups ; 32 patients treated with 25mg MPS, 34 patients with 50 mg, 35 patients with 100 mg. Intra-articular injections were given five to ten times at about weekly intervals. No statistical difference between the three groups was noted in the degree and the incidence of side effects. The rates of usefulness were 53.1% in the 25 mg group, 67.6% in the 50 mg and 54.3% in the 100 mg, while there was no statistically significant difference among the three. An improvement of score is superior in the order of concentration. The effect of ten-times injection was superior to that of five. In conclusion, 50 mg MPS seems to be an appropriate therapeutic dose, and ten-times injection is recommended for osteoarthrosis of the knee.

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This study was designed to compare the sedative effects of alprazolam and diazepam in healthy subjects using the choice reaction time test (CRTT) and the visual analogue self-rating scales. The subjects were 22 male volunteers, 19 to 23yr old. Eleven subjects had high neuroticism (HN) levels determined by Maudsley Personality Inventory, and 11 had lower neuroticism (LN) levels. Subjects took a single 0.8 mg dose of alprazolam or a single 5 mg dose of diazepam in a-cross-over design using a double-blind method. Subjects were allowed to practice the CRTT to reach a plateau level of learning curve before entering the experimental sessions. The absorption rate of alprazolam was suggested to be delayed by food intake. The 0.8 mg alprazolam produced almost equivalent sedative effects to 5 mg diazepam in the CRTT performance of HN subjects. Alprazolam produced relatively marked subjective sedative effects such as “drowsiness” and “mentally slow” in LN subjects as compared to diazepam. With both drugs, the subjective sedative' effects and the decrease in blood pressure and pulse rate were found in LN subjects.

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The effect of captopril, an inhibitor of angiotensin converting enzyme, on cardiovascular hemodynamics was studied in 7 patients with chronic congestive heart failure. After single oral administration of 25 mg, systemic blood pressure, pulmonary arterial pressure, pulmonary capillary wedge pressure, cardiac output, heart rate, plasma renin activity (PRA) and plasma aldosterone concentration (PAC) were measured for 4 hours.
Systemic blood pressure was measured by a sphygmomanometer, pulmonary arterial and capillary wedge pressure by an electromanometer, and cardiac output by thermodilution method.
Captopril produced a significant decrease in systemic blood pressure, pulmonary arterial and capillary wedge pressure. Cardiac output did not change significantly. PRA showed a significant increase throughout the observation. PAC showed a significant decrease from 2 hours after administration.
These results suggest that captopril has a potency of ameliorating congestive heart failure through the reduction of left ventricular afterload and preload and the suppression of renin-angiotensin-aldosterone axis.

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In order to investigate the effects of mecobalamin on experimental carcinomatous neuropathy, hepatoma-bearing rats were produced by chronic feeding of 3'-methyl 4-dimethylaminoazobenzene (3'-Me-DAB), and neuropathy was quantitatively evaluated by the motor nerve conduction velocity (MCV) of the dorsal nerve trunks.
The rats were kept feeding on Oriiental Solid Food containing 0.06% 3'-Me-DAB until 12 weeks after the start of the experiment when hepatoma was confirmed to develop and 500μg of mecobalamin injection was initiated twice a week. At 17 and 23 weeks with an interval of 2 weeks after the last injection, MCV and serum B₁₂ level were measured. The MCV's of vitamin B₁₂-treated hepatoma rats were not reduced at 17 weeks as compared with untreated hepatoma-bearing rats although in the later stage the difference between the two groups was not remarkable. It was quite reasonable that the serum vitamin B₁₂ levels were low in the control hepatoma rats while those of vitamin B₁₂-treated hepatoma rats were high. However, interesting enough, a positive correlation was observed between MCV and serum vitamin B₁₂ level in the control hepatoma rats.
From the above results, it was suggested that vitamin B₁₂ deficiency may at least one of the causes of neuropathy in hepatoma-bearing rats, and vitamin B₁₂ administration could prevent carcinomatous neuropathy.

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The effects of fenoterol and salbutamol on the allergen-induced histamine release from leukocytes were compared. Leukocytes used in this study were obtained from 24 children with bronchial asthma who were judged by questioning and skin test to have the offending allergen. For measurement of histamine, Pruzansky and Patterson's method, a modification of Shore and Anton's technique, was applied.
Fenoterol was superior to salbutamol in the rate of inhibition of the histamine release, no matter what stage in the process of histamine release the drug was added. Especially, the inhibitory rate of fenoterol was significantly higher than that of salbutamol in case where the drugs were added at the first stage.
The inhibition rates of the two drugs on histamine release were compared in the range from 10^-3M to 10^-7M. The result was that the inhibitory rate of fenoterol was higher than that of salbutamol in any concentration, significant difference being observed in 10^-4M and 10^-5M.
The findings as referred to above suggest that fenoterol, a bronchodilator, having such a strong action on the inhibition of release of chemical mediators, could be of great value in treating prolonged asthmatic attacks as it could be used for prophylaxis of asthmatic attacks.

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Clinical effects of disopyramide phosphate injectable (DP) 100 mg were examinedby comparing with intravenous injection of procainamide (PA) 500 mg, using“adequate well -controlled study”, which means that the drugs were allocated atrandom to the patients and physicians know the used drug but the effect wasevaluated by the evaluation committee without information about the drug. Theregular double blind method was not employed, because intravenous antiarrhythmicdrugs, in general, are used in the emergency situation and severe risk can notbe avoided. In 126 cases of tachycardic arrhythmias (paroxismal atrial and ventriculartachycardia, and transient atrial fibrillation and flutter), DP was moreeffective (60.9%) than PA (46.8%) with a statistically significant difference, althoughno difference was observed in the effectiveness in 90 cases of extrasystolesbetween both drugs (95.6% and 88.9%). The incidence of side effects was 12.8%with DP and 12.1% with PA, showing no significant difference. These resultsindicate the usefulness of DP.

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In vivo distribution and the activation of HCFU were studied by using rabbitsand mice bearing Sarcoma 180 following oral administration, and the phamacokineticbehaviours were compared with other masked type derivatives of 5-FU.
HCFU was absorbed gradually from gastrointestinal tracts, and HCFU and theoxidation products (CPEFU, CPRFU, etc.), (HCFU fraction) persisted for severalhours in the tissues and they were successively converted to 5-FU.
HCFU fraction and 5-FU distributed highly in the stomach, kidney and urinebladderand slightly in the brain and spleen. A relative high concentration of 5-FUwas detected in the tumor tissues and lung, lip, rectum, skin, etc.
5-FU level in the tumors was elevated by co-administration of HCFU withthymine, thymidine or uracil. Among them, thymine had the strongest effects toincrease 5-FU level and anticancer activities to Sarcoma 180.
The production of 5-FU from HCFU was not influenced by pre-treatments ofphenobarbital and glutathione, or CCl₄. This indicates that the activation of HCFU is not mainly depend to the liver.

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