One of the most important task of the pharmaceutical technology is to reach a possible high gastrointestinal absorbtion of the active ingredient. Therefore, it is necessary to have a good solubility in the gastric/intestinal medium. In this way the applied drug quantity and unwanted side effects can be reduced with solubility increasing. The water-insoluble drug's solubility and bioavailability can be increased by the alteration of their physicochemical properties. Nifluminic acid is a frequently used anti-inflammatory drug with low aqueous solubility. Inclusion complexation with cyclodextrins is an efficacious method to improve the solubility, stability and bioavailability. Ternary systems were prepared and investigated to use nifluminic acid, hydoxypropyl-beta-cyclodextrin and polyvidone. The aims of the study were to investigate the solubility rate, the in vitro diffusion ability, to determine the n-octanol/water partition coefficient, and to study the thermoanalitycal properties of products. The results suggested that complexation with cyclodextrin and the use of polyvidone is better method than to prepare binary systems. Inclusion complexation was presumed in the event of the ternary composition to improve the bioavailability of nifluminic acid.
Download full-text PDF |
Source |
---|
Acta Pharm Hung
September 2005
Szegedi Tudományegyetem, Gyógyszerésztudományi Kar, Gyógyszertechnológiai Intézet, Szeged, Eötvös.
One of the most important task of the pharmaceutical technology is to reach a possible high gastrointestinal absorbtion of the active ingredient. Therefore, it is necessary to have a good solubility in the gastric/intestinal medium. In this way the applied drug quantity and unwanted side effects can be reduced with solubility increasing.
View Article and Find Full Text PDFActa Physiol Hung
April 1991
Institute of Pharmacodynamics, Albert Szent-Györgyi Medical University, Szeged, Hungary.
Mouse ear oedema induced with dithranol in mice of the CFLP strain was decreased significantly, in a dose-dependent manner, by the oral administration of the following non-steroids 60 minutes before induction of the oedema: piroxicam, proquazone, azapropazone, nifluminic acid and phenylbutazone. An approximately 50% inhibitory effect could be attained with the following doses: 3.3 mg/kg piroxicam, 5 mg/kg proquazone, 5 mg/kg azapropazone, and 1 mg/kg nifluminic acid.
View Article and Find Full Text PDFArch Int Pharmacodyn Ther
October 1989
Department of Pharmacodynamics, Albert Szent-Györgyi Medical University, Szeged, Hungary.
The oedema disk technique was used to study the effects of orally administered nonsteroidal antiphlogistics (piroxicam, phenylbutazone, proquazone, azapropazone and nifluminic acid) on the inflammation induced with croton oil in the mouse ear. This method was demonstrated to be suitable for the detection of an antiphlogistic effect. The substances examined exerted a statistically significant extent of inhibition in a dose-dependent manner.
View Article and Find Full Text PDFSince for various reasons the Lansbury Index appeared inadequate to define the therapeutic efficacy of antirheumatic compounds, we chose to investigate in our trials the prednisolone saving effect in patients with rheumatoid arthritis. Our investigations with the new antirheumatic substance d-2-(6'-methoxy-2'-naphthyl)-propionic acid (naproxen) in most cases showed a prednisolone saving effect of 5 mg/day with a naproxen dose of 750 mg daily. In cases where a daily dose of 10 mg of prednisolone was necessary, a saving of 7.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!