Kinds Of Tablets Research Articles

市販プレドニゾロン錠の品質試験

The quality of 3 kinds of commercial prednisolone intact tablets was evaluated by weight variation, content uniformity and dissolution, and that of tablet halves, prepared by manual division of tablets along the score, by weight variation and dissolution. These tests were made according to the method prescribed in JP X. Following results were obtained: 1) All of the 3 kinds of intact tablets met the quality standard prescribed in JP X. 2) In each of the 3 kinds of tablets, no difference was found in dissolution patterns between intact tablets and tablet halves. 3) In each of the 3 kinds, percentage range of weight variation was wider in tablet halves than in intact tablets.

Influence of Light on the Quality of Commercial Nifedipine Preparations

In oredr to investigate the influence of light on the quality of commercial nifedipine preparations, the light of fluorescent lamp (FL-1.5 SW-G, Hitachi, 860 lux) was irradiated to 3 kinds of tablets and 3 kinds of capsules at a distance of 30 cm from the beam source and then the content of nifedipine was determined every week over 4 weeks by high performance liquid chromatography under the light of infrared lamp. This irradiation was also carried out to pure and fine crystal of nifedipine in a test tube and then the light-degradation product was identified with infrared spectrophotometer.The results were as follows: 1) In the case of irradiation to the preparations with PTP package, the contents of nifedipine of all the preparations tested remained unchanged after 2 weeks, but those of preparation C (tablet) and E (capsule) decreased after 4 weeks. 2) In the caseof irradiation to the preparations without PTP package, a decrease in the content of nifedipine was observed in preparations C and E after a week and in all the preparations tested after 3weeks, although the decrease varied. 3) In the case of irradiation to the pure and fine crystals, the content of nifedipine [4-(2'-nitropheny1)-2, 6-dimethy1-3, 5-dimethoxycarbonyl-1, 4-dihydro-pyridine] decreased gradually with time and changed completely into 4-(2'-nitrosophenyl)-2, 6-dimethyl-3, 5-dimethoxycarbonyl-pyridine upon exposure to the light for 7 days.

Quality Test of Commercial Nifedipine Preparations

The quality of 3 kinds of tablets and capsules of commercial nifedipine preparations was evaluated in 5 tests: content uniformity, weight variation, disintegration, hardness and dissolution.Following results were obtained; 1) In the weight variation test and the disintegration test, all the preparations tested met the criteria of J. P. X. 2) There was no correlation between hardness and disintegration time. 3) In the content uniformity test, the mean contents of all preparations tested were almost equal to the indicated content; however, in one preparation p-hydroxybenzoic acid derivatives added to the capsule were dissolved in the contents ana interfered with the determination of nifedipine under the analytical condition applied to the others. Consequantly, it was necessary to find another analytical condition for this preparation. 4) The dissolution ratios of 5 kinds of preparations were good, but that of one tablet showed low tendency compared with those of the others at every measurement.

Quality Test of Commercial Pindolol Tablets

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%.

Evaluation of Acid-resistance of Enteric-coated Films of Multiple Digestive Enzyme Preparations

The acid-resistance of 2 kinds of tablets (A and B) and 3 kinds of capsules (C, D and E) containing enteric-coated granules was compared. Alkaline protease activity dissolved from samples was measured in different test solutions:(a) pH 5.0, 6.5 and 7.5 test solutions, (b) lst fluid and 2nd fluid in disintegration test (J. P. IX), and (c) pH shift test solution in consideration of pH values of gastrointestinal tract. The following results were obtained:(1) At pH 5.0, 4 of the 5 samples (except C) did not disintegrated after 120 min, and at pH 6.5 only sample B scarcely disintegrated. At pH 7.5, the disintegration times of tablets tested were 2-3 times longer than those of the enteric-coated granules.(2) Entericcoated granules in sample C met disintegration test (J. P. IX), butthe enzyme activity in 2nd fluid was 30% weaker than that at the optimal pH.(3) For the pH shift test solution, enzyme activities of samples A, B and E rapidly increased 180 min after start of the test, when pH of dissolution medium exceeded 6.0. Maximum activities of these three samples were slightly weaker than those at the optimal pH, and the activityof sample C decreased 70%. Digestive potential of the samples estimated from the area under activity curve according to Berndt method was compared with each other. The acid-resistance of samples A, B and E was better than C, indicating that digestive potentials of the three preparations were higher. The digestive potential was very useful for evaluationof the acid-resistance of enteric-coated film.

Dissolution and Stability of Enzymes Contained in Anti-inflammatory Enzyme Preparations

Pharmaceutical properties of 2 kinds of tablets and 3 kinds of capsules of anti-inflammatory enzyme preparations were compared. All preparations tested passed weight variation test and disintegration test (J. P. IX). In order to test the stability of enzyme in the, solutions of different pH, alkaline protease activity of each preparation was measured at 3 different pH values; 6.2, 7.2 and 8.0. In all preparations tested, the enzyme was more stable at pH 7.2 than at any other pH's. Acid resistance of films of 4 kinds (A, B, C and D) of enteric-coated tablets and granules was tested in accordance with disintegration test (J. P. IX). The enteric-coated films of 3 (A, B, C) of the 4 samples kept satisfactory acid resistance in the 1st fluid (J. P. IX), because maximum activity of enzyme dissolved from each preparation in the 2nd fluid (J. P. IX) was equal to the activity of optimal pH range of the enzyme. In consideration of the pH value in gastrointestinal tract, a pH shift test solution was prepared, and the activities of enzyme dissolved from each preparation into this solution were observed. The result was that the activity curves showed different pattern from each other and especially maximum activity of sample D decreased to the 40% level of that in optimal pH range. Enteric-coated enzyme preparations should, therefore, be perfectly coated with enteric-soluble materials and the pH shift test method in this test must be effective in a quality test of the preparations of such type.

Relationship between quality and serum level after the oral administration of commercial erythromycin tablets in man (author's transl)

Disintegration of erythromycin tablets was compared by the disintegration test method in Japanese Pharmacopoeiae VIII and by the Erweka Disintegration Tester, using commercial erythromycin tablets (200 mg/tablet) manufactured by 16 firms and marketed in Japan during June to September, 1975. From the result of these tests, four kinds of tablets that required the longest time for disintegration and a kind of standard tablet that required the shortest time were selected. These tablets were alloted to 20 female subjects at a time (making a total of 100 test subjects) by the Latin square design method. The subjects took the tablets before breakfast and serum level of erythromycin was measured by the bioassay method 2, 4, 6, 9, and 12 hr later to examine bioavailability in humans. According to its result, two of these five products were bioinequivalent and, especially, one of them showed a maximum serum level and AUC of only 4% and 3.8%, respectively, of the values obtained from the product giving the highest values. In order to find the reason for such bioinequivalence and to detect such a product, dissolution rate of these tablets was examined by four methods ; J.P. VIII, U.S. Pharmacopoeia XIX, Sartorius SS, and Erweka Tester. It was thereby found that one of the bioinequivalent products did not undergo disintegation or dissolution in a solution of below pH 6.5, and this was thought to be the reason for its poor absorption from the digestive tract. In the other product, dissolution at pH 5.0-5.5 seemed to be related to the serum level of the ingredient but this point requires further examinations.

Effect of Humidity on Hardness and Disintegration Time of Tablets

Effect of humidity on hardness and disintegration time was examined on 25 kinds of uncoated tablets. Depending on the humidity in storage, hardness of the tablets changed in the following three patterns:(1) Larger in relative humidity (RH) of 30-50% than in drier state, but smaller in RH more than 75%.(2) No marked change in dry state and in RH up to 30-50%, but smaller in RH more than 75%.(3) Largest in dry state, and smaller as humidity increases.Tablets were prevented from being moistened in low humidity, but not in high humidity. The effect of humidity on disintegration which occurred within one minute was, not noted, since the disintegration time was too short. The disintegration time was reduced in 1 of 5 kinds of tablets which disintegrated in 1-2 min, 1 of 4 in 2-3 min, all of 4 in 3-5 min, and 1 of 2 in 9-11 min.

Lipase Activity of Digestive Enzyme Preparations

Lipase activity was measured of various digestive enzyme preparations in the gastric and intestinal juice in terms of the pH values. As compared with the lipase activity of pancreatin (J. P. VIII) as control, the tested preparations might showed a similar activity at pH 3-8 in the gastric juice, and a high activity at pH 7-8 in the intestinal juice. In a comparative study of the lipase activity of the preparations in different lot numbers, it can be said that the activity of newer preparations was not always higher (though only 2 kinds of tablets were compared with pancreatin). Before drawing conclusion on the matter, the storage condition of the preparations must be taken into consideration.

Pharmaceutical Study on Oxazepam Tablets

A pharmaceutical study was carried out on three kinds of tablets on the market (A, B and C) containing, respectively, 10 mg of oxazepam. The variation of the average weight was widest in tablet B, followed by C and A, in that order. Disintegration took place rapidly in all of the three tablets, but dissolution slowly. The dissolution rate in the primary solution in 60 minutes was 95% with tablet C, 90% with A, and 75% with B. Oxazepam content was not less than 96% in each tablet. In the test with rabbits, no significant difference in blood concentration of oxazepam was observed between the tablets.

Griseofulvin tablets

Last year we drew attention to the confusion caused by the co-existence of coarse and fine particle preparations of griseofulvin for the treatment of fungus infections.1 The coarse particle tablets offer no advantage and cost twice as much as the official fine particle preparation, and we concluded that they should be withdrawn. We are pleased to note that one manufacturer, ICI, has now stopped making coarse particle tablets, and is supplying only the fine particle preparation. The other manufacturer, Glaxo, will continue to supply both kinds of tablets, at least in Britain, and has introduced new labelling designed to avoid confusion between the two preparations.