The quality of 8 commercially available pantethine products of powders, fine granules or granules was evaluated by several tests on pharmaceutical properties such as stability. 50% dissolution time (T₅₀) of each product was less than 5 min and no difference in T₅₀ was observed among the products. Content of 6 products was lower than the labeled amount, and most of these products showed some impurities detected on TLC. 6 products were unstable under severe conditions of high temperature and humidity. 7 products showed adhesive property, uhile 2 products showed a large content segregation of different-size fractions.
It was found that the products containing same ingredient show qualitative difference due to the difference in production technique.

抄録全体を表示

The quality of 10 kinds of ubidecarenone tablets commercially available from 6 pharmaceutical companies was evaluated on dissolution, weight variation, disintegration and content uniformity. Ubidecarenone is insoluble in hydrophilic solutions such as the 1st fluid specified in J. P. X, which are commonly used as dissolution media, and easily soluble in alcoholic solutions.
The authors developed a method of a new dissolution test consisting of the following two steps: 1) Disintegration step: 70 ml of the 1st fluid was placed in the vessel (U. S. P. XIX). The paddle (J. P. X) was assembled so that there is a distance of O.5 cm between the paddle and the bottom of the vessel. One tablet was placed in the vessel and the paddle was rotated at 100 rpm for 10 min (plain tablet) and 60 min (sugar coated tablet). 2) Dissolution step: Immediately after 830 ml of 99.5% ethanol was added, 10 ml each of specimens was withdrawn at certain intervals and the contents of ubidecarenone dissolved was determined by photometry. 50% dissolution time (T₅₀) and dissolution rate at T₅₀ were obtained from each dissolution curve plotted using the mean values (n= 6).
The variations in dissolution rates (more than 90 to 3%/ min) and T₅₀ (0.5 to 10 min) were observed among the samples. Disintegration times of the plain tablets and of the sugar coated tablets varied from 0.2 to 14.2 min and from 7.4 to 20.9 min, respectively. No significant difference in weight variation (0.5 to 4.6%) and content (96 to 106%) was observed among the samples.

抄録全体を表示

In the previous paper (Jap. J. Hosp. Pharm., 9 (1), 14, 1983) it was reported that the commercially available ubidecarenone tablets showed various dissolution rates in the newly devised dissolution test, though they met the disintegration and content uniformity tests in J. P. X. In order to investigate the relationship between the results of such dissolution test and bioavailability of the tablets, 3 kinds of 10 mg ubidecarenone tablets, A-10-T₁, A-10-T₂, and B-10-SCT₁ of which dissolution rates (min for T₅₀) were high (0.5), medium (1.0) and low (10), respectively, were administered to healthy male subjects in dose of 2 tablets 3 times daily after meals for 8 to 14 days. Bioavailability of the tablets was evaluated on the basis of plasma levels of ubidecarenone (Ubiquinone-10, CoQ₁₀).
When compared by a cross-over experiment using 14 subjects, A-10-T₁ and B-10-SCT₁ increased plasma levels of CoQ₁₀ to 1.87 and 1.13 times after 4 days, and to 2.20 and 1.20 times after 8 days as high as the control level. On the other hand, when A-10-T₂ was administered to 9 subjects, plasma levels of CoQ₁₀ were 1.44 times after 4 days, 1.70 times after 7 days, and 1.61 times after 14 days higher than those of the control. Thus, the increase of plasma levels of CoQ₁₀ by these three tablets corresponded with their dissolution rates. Consequently, it was suggested that the dissolution test described in the previous report is useful for estimation of bioavailability as well as quality control of ubidecarenone tablets.

抄録全体を表示

Compatibility and residual activity of β-galactosidase were studied by organoleptic test and onitrophenyl-β-D-galactopyranoside (ONPG) method, respectively. 22 drugs were mixed with β-galactosidase. 4 preparations of β-galactosidase (Organase powder, Organase granule, Galantase powder, and Lactyme powder) were mixed with each of the 22 drugs and allowed to stand for 14 days under severe conditions, at 30° and RH 92%, The order of the stability of the preparations was as follows: Organase powder>Organase granule>Lactyme powder>Galantase powder. Optimal pH of the 4 preparations ranged from 4.0-4.5; they were stable between pH 4.0 and 7.5. The preparations were stable at 30° and 40° and unstable at 65°.
The data on change in compatibility with time were analyzed statistically by scoring, in addition to the classification with the marks of-, ±, + and++. The amount of compatibility was also studied with time series analysis.

抄録全体を表示

Although there have been a number of clinical reports on preoperative hand disinfection, a very few evaluation tests for efficacy of general hand washing in hospital have been made, hence resulting in few reports on this subject. Comparative test of sterilizing ability were carried out with Hibiscrub, a preoperative hand disinfectant, and Osvan and Phisohex, diluted disinfectants in basin. The method. used for these tests is Price's continuous basin method which is most reliable. in measuring the reappearing number of resident bacteria on hands. Efficacy duration test was also studied for Hibiscrub. Hence, it was shown that Hibiscrub, compared with the other two disinfectants, has satisfactory efficacy for general hand washing in wards or examination rooms in short time (30 sec) and in small amount (20 ml).

抄録全体を表示

High pressure liquid chromatographic determination of clorprenaline hydrochloride, isoproterenol hydrochloride, orciprenaline sulfate, salbutamol sulfate and trimetoquinol hydrochloride in inhalant preparations was made using a Zorbax ODS reverse phase column and acetonitrile-phosphate buffer (pH 2.3) as mobile phase. The peaks of the additives and decomposition products in the solutions on chromatograms did not interfere with those of the bronchodilators. The coefficients of variation for analytical values, calculated from 2 different concentrations of the bronchodilators, ranged from 0.3 to 2.9%. Moreover, good recoveries (95.5-101.9%) were obtained from Alevaire or Bisolvon Solution.
Thus, the methods can be applied to the evaluation of these inhalant preparations.

抄録全体を表示

Compatibility and stability of sympathomimetic bronchodilators, clorprenaline hydrochloride (CP), isoproterenol hydrochloride (IP), orciprenaline sulfate (OP), salbutamol sulfate (SM) and trimetoquinol hydrochloride (TQ) with physiological salme, Bisolvon Solution or Alevaire were studied using a high pressure liquid chromatography. NQ visual change was observed when each solution of bronchodilator was mixed with physiological saline or Bisolvon Solution. And all of the bronchodilators maintained more than 96% of the initial amount in the mixed solution for 2 weeks at room temperature. When mixed with Alevaire, however, most of the bronchodilators except CP showed a decrease in content developing a brown color, and TQ and IP showed a marked decrease. It was considered that this observation was due to oxidative degradation of bronchodilators in Alevaire. It can be concluded that TQ, IP, OP and SM are incompatible with alkaline solutions.

抄録全体を表示

L-Keflex is a sustained-release preparation of cephalexin (CEX). It is composed of non-enteric coated granules and enteric coated ones at the potency ratio of 3 to 7. The effect of food on the prolonged activity of L-Keflex was investigated in six volunteers by a cross-over method. 1000 mg of L-Keflex was orally administered to the volunteers after usual meal or light meal. The followings are the results of the study: In both groups of usual and light meals, L-Keflex level of more than 3.13μg/ml in serum lasted for about 8 hours. However, the serum level pattern in the light meal group was apparently different from that in the usual meal group. The former group showed 2 peaks of serum levels, whereas the latter one gave only a single peak.

抄録全体を表示

Stability of ergocalciferol (EC) in absorption ointment, hydrophilic ointment and seven kinds of ointment constituents were examined; in addition, antioxidative activities of gallic acid derivatives for EC in hydrophilic ointment were studied. Samples were exposed to air at 40°C and their oxidation stability was measured with high performance liquid chromatography (HPLC). Several kinds-of EC decomposition products were detected by HPLC. It was confirmed by the use of dual UV-wavelength that peaks corresponding to EC and other substances did not overlap each other.
The results are as follows: 1) The amount of EC in hydrophilic ointment decreased ; however, that in absorption ointment did not change. 2) The amount of EC decreased markedly in lauromacrogol and sorbitan sesquioleate. 3) The amount of EC decreased as the proportion of stearyl alcohol in ointment increased, while cetanol showed reversible behavior. 4) The antioxidative activities of gallic acid derivatives for EC in hydrophilic ointment were as followes in the order of strength: lauryl gallate, isoamyl gallate, n-propyl gallate, ethyl gallate, gallic acid. The results of the experiment suggested that higher alcohol concentration is an important factor in the stabilization of EC in ointment.

抄録全体を表示

With recent advances in electric technology, about 300 million micro-batteries are manufactured annually in Japan, being widely used for children's electric toys as well as for cameras, watches, calculators, and hearing aids. The accidents of ingestion of the batteries by small children have often been reported in the past one year. These batteries consist of an outer nickel-plated container (cathode) and a cap (anode) which are jointed by a plastic seal. They usually contain highly concentrated potassium hydroxide, mercury salts, zinc and some others depending on the type.
This paper describes the process of corrosion and leakage of the batteries in several kinds of solutions. It also analyzes the 11 cases of inadvertent ingestion of the batteries which our poison informatiqn services accepted in the last half year.

抄録全体を表示