Gefarnate is geranyl farnesylacetate which is easily oxidizable and is prone to hydrolysis owing to the presence of 5 double bonds in the molecule. Therefore, highly advanced technique is required to prepare the product. Some qualitative differences may occur among the products depending on manufacturing techniques.
The quality of the products on the market of 9 manufacturers was compared in terms of dissolution rate, content uniformity, peroxide value and hydrolysis rate. Two products showed excellent results, but there were a few products which were very questionable in view of their dissolution rate, content uniformity and peroxide value.

View full abstract

Statistical study on weight, disintegration time and hardness was carried out on 170 kinds of commercial tablets (uncoated, sugar-and film-coated) and capsules. 1. Significant differences in the distribution of weight, disintegration time and hardness were observed among the dosage forms. 2. The coefficients of weight variation was extremely small but those of disintegration time and hardness varied widely. 3. The coefficients of determination (r²) on the correlation of hardness-disintegration time, weight-hardness and weight-disintegration time were all smaller than 0.5 and, therefore, it was considered that there is no correlation among the above three variations.

View full abstract

The number and amount of external liquid preparations made in Shinshu University Hospital were studied by time series analysis. Time was represented by t (eg, t=1 stands for April 1974) and the analysis was made by the following equation model: Y (t) =T (t) +S (t) +I (t)[Y: original data, S (t): trend variation, I (t): residual variation]. It was found that 9 and 12 month periodicity was observed by the correlogram of the number of external liquid preparations, and 12 month periodicity by that of the amount. The switching point was estimated by Quandt's method. The regression polygonal lines were proved useful since the residuals were assured at random by Durbin-Watson ratio. The number and amount of external liquid preparations decreased in January and increased in the Summer months and in December. Inconsistent coefficient by Theil was 0.03 when seasonal variation was modified.

View full abstract

Serum level of phenytoin (DPH) in 204 patients receiving an oral anticonvulsant was determined by EMIT AED method. DPH level was significantly higher (P<0.05) in patients given DPH and 2 or more other drugs than in those on DPH only or on DPH and one other agent. In 127 patients given DPH and 2 or more other drugs, influence of phenobarbital, primidone, carbamazepine and acetazolamide on serum DPH level was studied. The influence in the group was not significantly different from the group given phenytoin only. The DPH level was lowered significantly (P<0.05) in the group subjected to the combination therapy of DPH with clonazepam. Then, serum level of DPH bulk powder marketed from manufacturer A was compared with that of bulk powder of manufacturer B, both products given to the same patients in the same dosage. The serum level of DPH-B, as a result, was 3 times (P<0.01) as high as that of DPH-A.

View full abstract

High-pressure liquid chromatography (HLC) was evaluated in determination of hexestrol in ointment. Sample ointments were mixed with ethanol and isooctane. Hexestrol in the Hexron ointment was extracted into ethanol layer. Butyl p-hydroxybenozate was used as the internal standard. HLC was performed under the following conditions: model, Shimadzu LC-2F; detector, UV visible spectrophotomer Shimadzu SPD-1; wave length, 280nm; column, Permaphase ODS (2.1φ×0.5m); mobile phase, gradient elution system, 10% to 40% MeOH in H₂O at 3% min; flow rate, 1 ml/min (at room temperature). The calibration curve was traced by plotting the ratio of the peak weight against the amount of each hexestrol. Satisfactory linearity was observed in the range of 0.125 to 1μg and quantitative determination was found to be possible. Other components in the Hexron ointment did not interfere in determination of hexestrol in this method. Hexestrol in the Hexron ointment was recovered at the rate 94% on an average by ethanol extraction. The quantitative determination of hexestrol in an ointment by HLC was carried out simply and rapidly.

View full abstract

Single dose (10mg) of metoclopramide injection, syrup and tablet was given in crossover design to 3 healthy male volunteers in the fasting state. Excretion of metoclopramide into urine was determined by spectrophotometry. Urinary excretion of metoclopramide 24 hours after administration of syrup was 77.7% and that of tablet 91.0%, as against the excretion after intravenous infusion as 100%. Urinary excretion of N⁴-glucuronide was larger by oral administration than by intravenous infusion, and unchanged metoclopramide was excreted more by intravenous infusion.

View full abstract

At present radioimmunoassay is the most popular method to determine digoxin in human serum. The method of quantitative determination by enzyme immunoassay was examined with use of peroxidase-labeled digoxin, and the results were compared with those in Emit method. It was found that such factors as temperature and reaction stopper produce great influence in digoxin determination. Radioimmunoassay proved to be fairly correlated to Emit method.

View full abstract

Stability and moisture content of ascorbyl monopalmitate (AsA-MP), ascorbic acid (AsA) and their diluted powders were investigated after storage for 2 weeks at 37° in various relative humidities (20, 50, 70, 100%). Diluted powders were prepared by mixing AsA-MP and AsA with phenacetin and lactose, all in the same quantity (100mg). The residual rate of AsA-MP and its diluted powders was determined by selenium dioxide method. The data obtained indicated that the decomposition of the two compounds and their diluted powders was accelerated in parallel with the increase in moisture content. AsA-MP was more stable than AsA in every degree of relative humidity. The moisture content of AsA-MP in various relative humidities was lower than that of AsA.Diluted powders of the two compounds showed corresponding tendency both in stability and in moisture content. Further, the logarithm of residual rate of AsA-MP in various relative humidities changed in direct proportion to the moisture content, but AsA did not.

View full abstract

Change in appearance, potency and weight increase of ascorbic acid granules (Hicee) in the presence of 74 adjuvant drugs was investigated. When combined with adjuvant drugs containing metal, potency of ascorbic acid was lowered. It was suggested in the study on weight increase that moisture content is closely related with potency. In the test by thinlayer chromatography it was found that 4-methylaminoantipyrine was detected when ascorbic acid was combined with sulpyrin.

View full abstract

Dust particles in hospital pharmacy were reduced to 1/10 to 1/50 by an electric vacuum cleaner placed near the source of dust. The dust removal rate in the area away from the cleaner was lower: 1/3 to 1/15. Dust particles produced in drug dispensing consisted of relatively large ones (1.0-5.0μm in diameter), and most of those due to other factors such as smoking and working personnel were smaller (0.3-0.5μm). Consequently, the ratio of large dust particles of 1.0-5.0μm was higher in pharmacy than in other places, and the ratio of small ones of 0.3-0.5 μm was not so higher. When the vacuum cleaner was placed near the source of dust, most of the large particles over 1.0-5.0μm were removed. Consequently, the particles of this size were reduced in any part of pharmacy. However, smaller particles of 0.3-0.5μm were not efficiently removed in the area distant from the cleaner: particles left unremoved in such area were 3 to 6 folds as many as in the place around the cleaner.

View full abstract

Apparent compatibility of sulfamethoxazole-trimethoprim granules (ST) with 41 drugs was tested under medium (20°, RH 75%) and the worst condition (30°, RH 92%). There was no change in appearance of ST wrapped by itself in chartula under medium condition. But, under the worst condition, ST wrapped mechanically in laminated glassine was moistened in 10 days. Of the mixtures of ST and 41 drugs wrapped in laminated glassine, 7 mixtures showed a moistening tendency in 14 days under medium condition. Mixtures with 25 other drugs showed the same tendency under the worst condition, but mixing did not cause increase in moistening tendency. In conclusion, ST remains stable in the climate of Japan even if it is combined with many other drugs.

View full abstract