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Title: The influence of meglumine on the pharmaceutical availability of drugs from pellets

Abstract:

The aim of this study was application of meglumine as a carrier in solid dispersions pellets containing poorly water soluble drugs. Three drugs were selected as a model: ketoprofen, piroxicam, indomethacin. The melting method and spray-drying method were used to prepare solid dispersions. The properties of meglumine solid dispersions were depended on the method of preparation, the drug/meglumine ratio and properties of the drug. It was found, that melting method was appropriate to obtain solid dispersions of good quality for all drugs. The spray–drying method was suitable for preparation piroxicam and indomethacin meglumine solid dispersions. The best results were obtained for ketoprofen solid dispersions: (1+0.5), (1+1) prepared by melting method and for spray-dried indomethacin solid dispersions (1+0.5), (1+0.25). Three kinds of pellets were prepared by extrusion/spheronisation: containing the drug alone, solid dispersion or physical mixture. The pellets formulation was based on the results of rheological behaviour of wet powder mass which was assessed by using the compresso-rheometer. The present work has demonstrated the improvement of rheological properties of mass for extrusion in the presence of meglumine. Formulations composed of microcrystalline cellulose-lactose-meglumine in the ratio (7+3+0.4) and (7+3+0.5) showed the best rheological properties. Pellets prepared from different kinds of excipients were characterised in terms of shape, porosity, size distribution and dissolution behaviour. Dissolution studies of solid dispersion pellets showed enhancement in the dissolution rate of drugs. The increase in the amount of released drug from solid dispersions pellets was greater than from the pellets containing drug alone. After 20 minutes almost total amount of ketoprofen and indomethacin was dissolved from pellets. In the case of piroxicam the best results were obtained by using the layering method in pellets formulation. The amount of piroxicam dissolved from these pellets was two times greater than from pellets obtained by extrusion spheronisation. The dissolution profiles of drugs from pellets were unchanged after one year storage.

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmakologia

Degree grantor:

Wydział Lekarski

Promoter:

Renata Jachowicz

Date issued:

2006

Format:

application/pdf

Identifier:

oai:dl.cm-uj.krakow.pl:1118

Call number:

ZB-105403

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Access rights:

tylko w bibliotece

Location of original object:

Biblioteka Medyczna Uniwersytetu Jagiellońskiego - Collegium Medicum

Object collections:

Last modified:

Jun 24, 2019

In our library since:

Nov 21, 2012

Number of object content hits:

9

Number of object content views in PDF format

7

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/1118

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ZB-105403 Jun 24, 2019
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