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[Prospects of using hard dispersions in development of dosage forms for therapeutic and prophylactic use].

Thermoanalytical, chromatographic, and microscopic methods of analysis were used for identification of hard dispersions (HD) and their differences from physical mixtures (PM) by benzene PEG-4000 model systems. A complex of physiocochemical methods showed that benzonal and PEG-4000 are not thermally destroyed during simultaneous melting at 140 degrees C. Differences in thermoanalytical characteristics of PM and HD, expressed in suppression of phase transition temperatures, changes in the type of melting peaks and heats, and in the absence of drug melting peak and heats in HD vs. PM confirm the formation of new physiochemical systems differing from PM. The resultant quantitative relationships between temperature depression and melting heats for HD and PM of different composition correlate with chromatographic findings.

Chemistry, Pharmaceutical↗

[Didanosine as a capsule. A reliable drug in a new dosage form].

Ten years ago, the first clinical trial on the tolerability and efficacy of didanosine (ddl) was initiated in German therapeutic centers. At that time, AIDS patients in an advanced stage of the disease who failed to respond to monotherapy with AZT, were treated with ddl. However, the form of presentation of ddl, namely buffered powder, was poorly tolerated. In the meantime, galenical improvements have been made. Today, treatment with ddl is possible at a daily dose of one EC (enteric-coated) capsule. Given this in this form, the substance is highly effective, and the absorption of indinavir, ciprofloxacin, and ketoconazole is in no way impaired.

Anti-HIV Agents↗

Bioequivalence of isoniazid in a two drug fixed dose combination and in a single drug dosage form.

To increase the patient compliance and reduce the risk of drug resistant strains, WHO and IUATLD recommend the use of Fixed Dose Combination (FDC) tablets as a routine therapeutic regimen in Directly Observed Treatment Shortcourse (DOTS). But the main issue in the use of FDC is the quality of the formulation. At present WHO and IUATLD suggest the bioequivalence assessment of only rifampicin from FDC compared to separate formulations. For the therapeutic effectiveness all the components of the FDCs should be bioavailable at tissue site. Also, the primary and acquired resistance rate of isoniazid is much higher compared to other anti-tubercular drugs. Hence, a comparative bioavailability study of isoniazid from a two drugs FDC compared to a separate formulation was carried out on a group of 12 healthy volunteers. When evaluated by normal or log transformed confidence interval, Two Way ANOVA and Hauschke analysis, the bioequivalence limits for AUC0-8 and AUC0-24 were within 0.8-1.25. For Cmax and Tmax, these limits were within 0.7-1.43. Hence, isoniazid from a FDC formulation was found to be bioequivalent to a separate formulation at same dose levels.

Adolescent↗

Equivalence of microbiological and hydroxylamine methods of analysis for ampicillin dosage forms.

Ampicillin formulations were assayed by microbiological and hydroxylamine methods to determine whether thehydroxylamine analytical method is a suitable substitute for the microbiological method. Paired assay results by the 2 analytical methods were obtained on different strengths of tablet, capsule, and suspension, formulations containing ampicillin and ampicillin degradation compounds. Several statistical tests were used to assess the equivalence of the paired assay results. The data analyses indicate that the hydroxylamine method is a suitable substitute for the microbiological method for potency assays and stability studies of ampicillin formulations. The hydroxylamine method yielded slightly higher assay results than the microbiological method for severely degraded formulations.

Ampicillin↗

[Acute biochemical effects of calcium: comparison of two dosage forms of calcium carbonate (powder and effervescent tablets) and milk in healthy women].

BACKGROUND: The aim of this study was to assess acute biochemical changes after the administration of two different pharmaceutical forms of calcium carbonate or milk. METHODS AND RESULTS: The group of 12 young (aged 20-27 years) and 12 older women (aged 63-71 years). After overnight fasting, each of the volunteers received a 1 g of elemental calcium in either form of the tested preparation: powder form of calcium carbonate--Vitacalcin pulvis (Slovakofarma, SR) or effervescent tablet--Calcium 500 mg Pharmavit (Pharmavit, MR) or in 250 ml of milk enriched with the milk calcium complex. Between each test the interval of 1-2 weeks was held. Samples of blood and urine were taken in the fasting state before and during 5.5 h following ingestion of the calcium load. Both calcium carbonate and milk induced a significant increase in the serum ionised calcium (iCa) and a significant decrease in plasma parathormone level (PTH) in comparison with the baseline levels in both groups of women. Comparison between individual preparations and between preparations and milk did not reveal any significant differences in suppression of PTH. Comparison of the effects between young and elderly women did not show any statistically significant difference in any measured parameter. CONCLUSIONS: Our results confirmed the good bioavailability of calcium from milk and from both calcium preparations in both age groups of women. Significantly more frequent hypercalcemia in the young women (p < 0.05) and also the slightly higher hypercalciuria occurred after the application of calcium in the pharmaceutical form of effervescent tablet than after the application of calcium in the form of powder or after the application of milk.

Adult↗

[Antiherpetic activity of l-lysine-alpha-oxidase in different dosage forms].

The antiviral effect of different medicinal forms on base of L-lysin-alpha-oxidase (LO) in treatment of experimental keratits and skin diseases induced by herpes simplex virus type 1 (HSV-1) at the rabbits was examined. Treatment with gel form of LO was more effective in comparison with water solution form of LO. This effect was tested by morphological, histological and immunoblotting methods in dynamics of viral disease.

Administration, Topical↗

Determination of sodium cromoglycate in pharmaceutical dosage forms using TLC-densitometry.

A TLC-UV densitometric method for the determination of sodium cromoglycate (SCG) in ophthalmic solutions, gels and capsules has been developed. After TLC separation of active substance on silica gel GF254 using methanol-water-ethylacetate (15:45:40 v/v/v) as the mobile phase, densitometric measurements were performed with HPTLC scanner at 254 nm. The proposed method is rapid and simple, free from interference by adjuvants and can be suggested for the routine analysis of sodium cromoglycate.

Capsules↗