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Controlled clinical trial of a new dosage form of metaproterenol.

In a double-blind, crossover study of single doses an inhalant solution of metaproterenol was compared with an 0.5% solution of isoproterenol and placebo in nine patients with bronchial asthma and 13 patients with chronic obstructive pulmonary disease. The solutions were administered by IPPB in 15-minute treatment sessions. The mean duration of effect of metaproterenol, in terms of FEV1, and the magnitude of the FEV1 response to metaproterenol exceeded the isoproterenol data to a statistically significant degree, as did global ratings of response. FEF 25-75% and airway resistance showed similar patterns of response. Adverse experiences were minimal after both drugs.

Adult↗

Influence of dosage form and administration route on the pharmacokinetic parameters of cefadroxil.

A cross-over study was utilized to compare the pharmacokinetics of 500 mg cefadroxil administered intravenously and orally in solution, suspension, and in capsule form, and to calculate its bioavailability. The antibiotic was administered to four healthy volunteers on whom four experiments were carried out. Cefadroxil was determined in serum and in urine using a microbiologic plate diffusion method. Administered intravenously the antibiotic follows a two-compartment open kinetic model, whereas orally administered, its mode is that of a single-compartment model. There are no statistically significant differences between the parameters defining the elimination of the antibiotic in the four groups studied.

Administration, Oral↗

Simultaneous determination of vitamins A and D in a dosage forms by high pressure liquid chromatography.

Vitamins A and D were determined simultaneously in oily solutions, ointments, and elixirs, but only vitamin A could be determined in capsules. Samples were saponified with KOH in isopropanol-water, using hydroquinone as antioxidant, and extracted with ether-petroleum ether (1 + 1). After evaporation of solvent, residues were dissolved in isopropanol. Vitamins in these solutions were determined by reverse phase high pressure liquid chromatography, using methanol-water as mobile phase and detection at 254 nm. The reproducibility, using external standards, was 1.6-2.5% and 1.2-3.8% for vitamins A and D, respectively.

Capsules↗

Bioavailability of allopurinol oral and rectal dosage forms.

The bioavailability of allopurinol from orally administered tablets and rectally administered suppositories is reported. Two types of rectal suppositories (cocoa butter and polyethylene glycol) were compounded and contained 300 mg allopurinol (from oral tablets). Five healthy volunteers received 300 mg allopurinol orally from tablets or rectally from suppositories in a randomized, three-way crossover design. Serial blood samples were drawn for 72 hours following administration and were analyzed by high-pressure liquid chromatography for allopurinol and its metabolite, oxipurinol. The interaction between allopurinol and PEG was studied in vitro using a dialysis method. Serum allopurinol levels following oral administration of tablets peaked at 1.5 +/- 0.23 microgram/ml at 5.20 +/- 0.65 hours. Allopurinol was not detectable after administration of cocoa butter/allopurinol suppositories; oxipurinol peaked at 0.34 +/- 0.14 microgram/ml at 13 +/- 11 hours. The bioavailability of allopurinol from the cocoa butter suppository, relative to the tablet, was 5.77 +/- 2.5%. Neither allopurinol nor oxipurinol was detectable (less than 0.1 microgram/ml) in the sera of persons following administration of PEG suppositories. Dialysis studies showed decreased loss of allopurinol from the dialysis sac as PEG concentration increased. The rectal suppositories of allopurinol used in this study did not appear to be an efficient means of administering this drug.

Administration, Oral↗

The construction and uses of factorial designs in the preparation of solid dosage forms. Part 2: Granulation in a fluidized bed.

With the help of a factorial design of experiments, the optimum conditions for preparing aminophenazone granules in a fluidized bed were established by which high quality tablets were obtained with a minimum energy expenditure. Granules with given technological properties could be prepared by controlling the regime of the granulation process. By varying the experimental conditions, a reproducible correlation was found between the parameters of optimization (mean granule diameter and work of compression) and the factors controlling the granulation process (pressure of compressed air, velocity and temperature of fluidizing air and binder concentration). The effect of the granule quality on tablet physical properties was discussed. Recommendations were given for the exploitation of fluidized bed units in the practice of granulation and tableting.

Aminopyrine↗