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At least 451 records · Page 25Linked to original sources
PubMed1994

Biopharmaceutic approach in designing a controlled release tablet of sodium monofluoro phosphate. Characterization of absorption sites and evaluation of modified dosage form.

Based on the results from in vivo study in dogs, it was decided to characterize the absorption sites of sodium monofluoro phosphate (NaMFP). It was hypothesized that bioavailability upon p.o. administration can be improved for controlled release dosage forms if the drug release is confined to segments of gastrointestinal tract responsible for absorption. To characterize the principal sites of absorption of NaMFP, in situ segmental absorption studies were carried out in rats. It was found that NaMFP is predominantly absorbed from the small intestine. The larger surface area and presence of alkaline phosphatase enzymes, are attributed to the higher absorption from the small intestine. Based on these results the delivery time was limited to 6 h to restrict the release of the drug within the principal sites of absorption. The dose was adjusted to 160 mg of NaMFP. After studying in vitro release profiles, the drug to polymer ratio was adjusted to 1: 1.1. The modified dosage form was finally subjected to bioavailability studies in humans. An immediate release dosage form was used to compare the efficacy in a two-period crossover study. The extent of bioavailability was 99% and the dosage form was effective in reducing the fluctuations.

Absorption↗
PubMed1994

[Biopharmaceutic properties of slow-release codeine phosphate. Drug release from ion exchangers in vitro and in vivo].

The release of bound codeine (CAS 76-57-3) from a cation exchanger was examined in vitro by the flow-through method and in vivo by measuring the plasma concentrations of codeine after administration of slow-release (Codipront Retard) and standard non-retarded drops. Both sets of results show that codeine release from the ion exchanger is protracted and continuous. Relative to the standard formulation the slow-release codeine drops give a lower maximal plasma concentration (Cmax), a delayed time of maximal concentration (tmax), slower absorption (t0.5) and protracted plasma levels. The in vitro and in vivo results were in good agreement.

Adult↗