Correlation of Dissolution, Disintegration, and Bioavailability of Aminosalicylic acid Tablets

Schirmer, Roger E.; Kleber, John W.; Black, Henry R.

doi:10.1002/jps.2600620807

Cited by 8 publications

(2 citation statements)

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“…The dissolution and disintegration of various uncoated and enteric-coated tablets have been studied by Schirmer et al (1973) and found to be correlated with bioavailability. Others have studied the bioavailability of free para-aminosalicylic acid when given as its sodium, calcium and potassium salts (Wan et aI., 1974).…”

Section: Para-aminosalicylic Acidmentioning

confidence: 99%

Clinical Pharmacokinetics of the Antituberculosis Drugs

Holdiness

1984

Clinical Pharmacokinetics

189

106

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The quantitative aspects of the disposition in man of 12 antituberculosis drugs [isoniazid, rifampicin, (rifampin), ethambutol, para-aminosalicylic acid, pyrazinamide, streptomycin, kanamycin, ethionamide, cycloserine, capreomycin, viomycin and thiacetazone] are reviewed. Isoniazid appears to be the only agent for which plasma concentrations and clearance are related to hereditary differences in acetylator status and for which there is an appreciable 'first-pass' effect. Recent data cast doubt on the suggestion that isoniazid may be more hepatotoxic for rapid as opposed to slow acetylators. Continuous administration of rifampicin leads to induction of enzymes in the liver with a concomitant decrease in maximum plasma concentrations, the time required to achieve this level, elimination half-life, and area under the plasma concentration-time curve (AUC). Coadministration of para-aminosalicylic acid leads to increases in the serum concentrations and elimination half-life of isoniazid. With a few exceptions, the metabolites of the antituberculosis drugs are devoid of antimicrobial activity; the exceptions are 25-desacetylrifampicin which accounts for approximately 80% of the drug's antimicrobial activity in human bile, the acetylated and glycylated metabolites of para-aminosalicylic acid, and the sulphoxide metabolites of ethionamide. The effect of renal impairment is relatively unimportant for the excretion of isoniazid, rifampicin and para-aminosalicylic acid, but the elimination half-life of streptomycin increases to 100 hours when the blood urea nitrogen level is greater than 100mg/100ml, and ototoxicity is strikingly more frequent. In states of malnutrition, such as kwashiorkor, the protein binding of para-aminosalicylic acid decreases from 15% to essentially zero and in the case of ethionamide and streptomycin binding decreases by 6% and 16% respectively. Of the data concerning age-related effects, most notable are the prolonged elimination half-life of isoniazid in neonates (up to 19.8 hours), and the lower peak serum concentrations of rifampicin in children of one-third to one-tenth those of adults following a similar dose on a weight basis. For kanamycin, the maximum plasma concentration varies inversely with age but is not influenced by birthweight; however, the clearance is directly dependent upon birthweight and postnatal age. For the elderly, age is an insignificant factor for the elimination of isoniazid when compared with young adults of similar acetylator status, and the metabolism of rifampicin may be considered globally unaltered in this age group.(ABSTRACT TRUNCATED AT 400 WORDS)

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Section: Para-aminosalicylic Acidmentioning

confidence: 99%

Clinical Pharmacokinetics of the Antituberculosis Drugs

Holdiness

1984

Clinical Pharmacokinetics

189

106

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“…This test has been shown to agree with USP disintegration tests in 87% to 93% of cases [11]. The bioavailability of tablet formulations is affected by various factors, including its disintegration, dissolution, hardness, and moisture content [12][13][14]. Use of various starches as disintegrating agents in calcium tablet formulation has also been reported [15][16][17].…”

Section: Introductionmentioning

confidence: 61%

Evaluation of quick disintegrating calcium carbonate tablets

2000

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The purpose of this investigation was to develop a rapidly disintegrating calcium carbonate (CC) tablet by direct compression and compare it with commercially available calcium tablets. CC tablets were formulated on a Carver press using 3 different forms of CC direct compressed granules (Cal-Carb 4450, Cal-Carb 4457, and Cal-Carb 4462). The breaking strength was measured using a Stokes-Monsanto hardness tester. The disintegration and dissolution properties of the tablets were studied using USP methodology. The calcium concentration was determined by an atomic absorption spectrophotometer. Scanning electron microscopy was used to evaluate the surface topography of the granules and tablets. Breaking strength of Cal-Carb 4450, Cal-Carb 4457, and Cal-Carb 4462 tablets was in the range of 7.2 to 7.7 kg, as compared with a hardness of 6.2 kg and 10 kg for the commercially available calcium tablets Citracal and Tums, respectively. The disintegration time for the tablets presented in the order earlier was 4.1, 2.1, 1.9, 2.9, and 9.7 minutes, respectively. The dissolution studies showed that all formulations released 100% of the elemental calcium in simulated gastric fluid in less than 20 minutes. In summary, this study clearly demonstrated that quick disintegrating CC tablets can be formulated without expensive effervescence technology.

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