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At least 1,261 records · Page 70Linked to original sources

Food intake and dosage level, but not tablet vs solution dosage form, affect the absorption of metformin HCl in man.

The pharmacokinetics of four single-dose treatments of the metformin administered orally (as the HCl salt) were compared in 24 healthy subjects: 500 mg and 850 mg tablets and 850 mg solution fasting and 850 mg tablet with food. Solution and tablet formulations are bioequivalent. Bioavailability of a 500 mg tablet is 14% greater than that of an 850 mg tablet. Compared with the fasting state, bioavailability is 24% lower, and the peak concentration delayed about 37 min when an 850 mg tablet is administered with food.

Adult↗

Comparative in vitro evaluation of six commercial vincamine prolonged-release dosage forms.

This study consisted of a comparison of the release rates of six commercial brands of prolonged-release vincamine. The pH of the dissolution medium was found to be highly significant. Due to the low solubility of vincamine in media close to the neutral point, all of the preparations tested, with the exception of one, showed highly variable release curves under the three pH conditions chosen.

Delayed-Action Preparations↗

New sustained release dosage form of chlorhexidine for dental use: use for plaque control in partial denture wearers.

The aim of this work was to test the effectiveness of a local sustained release application of chlorhexidine in prevention of plaque formation in a group of five partial denture wearers when oral hygiene procedures were withdrawn. The clinical study demonstrates that coating of the partial dentures with ethyl cellulose polymer containing the drug, prevents accumulation of plaque during a period of 12 days. No typical side effects of chlorhexidine such as tooth staining and unpleasant taste were observed during the study.

Aged↗

Pharmacokinetic comparison of tablet and suspension dosage forms of carbamazepine.

The bioavailability of two preparations of carbamazepine--the tablet and a new syrup-was studied in 9 adult male volunteers by measuring saliva and serum levels. Peak time was significantly earlier and peak level significantly higher in serum for syrup as compared to tablet. Levels remained higher for syrup for 12 hr. Saliva was contaminated for up to 2 hr by syrup ingestion, possibly for a half hour by the tablet. Beyond that, saliva/serum ratios remained stable. Saliva level variation was too large for pharmacokinetic studies but acceptable for clinical purposes if sampling was long enough after the last dose.

Adult↗

Cornea preparation for in vitro bio-pharmaceutical evaluation of ophthalmic dosage forms.

A system has been developed for a specific biopharmaceutical purpose: testing for ophthalmic preparations, the influence of formulation on drug transport through the cornea. The apparatus is a lucite cell, divided in two compartments by a clamped rabbit cornea. Physiological conditions are ensured by a supply of oxygenated perfusion medium. They are monitored by electrical conductivity and corneal thickness measurements. Reliability of the system was tested in a set of experiments.

Animals↗

Sustained-release dosage forms of microencapsulated isoniazid.

The preparation and release characteristics of microcapsules of isoniazid have been studied. The differing techniques of microencapsulation are assessed and the dissolution of drug from suspended and tableted microcapsules prepared using the chosen technique has been monitored for in vitro release.

Capsules↗

Specification of limits for particulate contamination in pharmaceutical dosage forms.

Limits for the control of particulate contamination in large volume parenteral solutions and metered-dose aerosols are discussed. It is suggested that is would be desirable to use limits based on measurement of both mean and the standard deviation of the particle counts obtained for each of the containers tested. Use of the statistic ST, assuming a target value of zero, is considered to be an appropriate means of measuring the container to container variation in particulate contamination.

Aerosols↗

Design and in-vitro evaluation of a modified-release oral dosage form of nifedipine by hybridization of hydroxypropyl-beta-cyclodextrin and hydroxypropylcellulose.

To modify the release rate of nifedipine, a potent calcium channel antagonist, a double-layer tablet was designed, anticipating a more balanced oral bioavailability and a prolonged efficacy than the simple plain tablet. Amorphous nifedipine powders prepared by spray-drying with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) and nonionic surfactant HCO-60 were employed as a fast-release portion to attain an initial rapid dissolution of nifedipine. Hydroxypropylcelluloses (HPCs) with different viscosity grades (type L, M, and H) were used for a slow-release portion to provide an appropriate sustained-release. Taking into account the physiological conditions of the gastrointestinal tract (pH and motility), an optimal formulation of the double-layer tablet was obtained by changing the mixing ratios of each component. For example, the tablet consisting of HP-beta-CyD with 3% HCO-60/(HPC-L:HPC-M) in the weight ratio 1/2(1:1) provided a sufficient slow release of the drug over a wide pH region following an initial rapid dissolution. The release of nifedipine from the double-layer tablets was little affected by pH of the medium and rotation speed of paddle after accelerated storage conditions (60 degrees C, 75% r.h.). The present results suggest that a combination of HP-beta-CyD, HCO-60 and HPCs can serve as a modified-release carrier for poorly water-soluble nifedipine.

2-Hydroxypropyl-beta-cyclodextrin↗

In-vivo and in-vitro evaluations of a modified-release oral dosage form of nifedipine by hybridization of hydroxypropyl-beta-cyclodextrin and hydroxypropylcelluloses in dogs.

To maintain a suitable blood level of nifedipine for a long period of time, double-layer tablets consisting of 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) and 3% nonionic surfactant (HCO-60) as a fast-release portion and hydroxypropylcelluloses (HPCs) with different viscosity grades (low, medium and high) as a slow-release portion were prepared, and their in-vitro and in-vivo release behaviours were investigated. Among the seven formulations, the tablet having the mean dissolution time of 0.8-1.3 h gave prolonged plasma nifedipine levels without decrease of AUC after oral administration to dogs. Consequently, the double-layer tablet consisting of HP-beta-CyD with 3% HCO-60/(HPC-low:HPC-medium) in a weight ratio 1/(1.5:1.5) was selected as an appropriate modified-release formulation because it elicited almost comparable retarding effects with superior oral bioavailability compared with those of a commercially available slow-release nifedipine product.

2-Hydroxypropyl-beta-cyclodextrin↗

Etoposide microcrystals suspended in oil: a new dosage form to peritoneal carcinomatosis in mice.

Etoposide microcrystals suspended in oil (ETOP-OIL) were examined for their therapeutic effects on peritoneal carcinomatosis in mice. Two days after intraperitoneal inoculation with 10(5) P388 leukemia cells/mouse to CDF1 male mice, etoposide at 10-80 mg/kg was administered intraperitoneally in bolus in the form of ETOP-OIL or in the aqueous solution form. In every dose, the survival curve of the mice given ETOP-OIL was statistically significantly improved in spite of its small lethal toxicity, as compared with those given the identical dose of etoposide aqueous solution.

Animals↗