The Influence of Hydro-Alcoholic Media on Drug Release - Pharmaceutical Technology

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The Influence of Hydro-Alcoholic Media on Drug Release
The authors investigate the influence of hydro-alcoholic media on hydration and drug release from polyethylene oxide extended-release matrices.


Pharmaceutical Technology
Volume 35, Issue 7, pp. 50-58

Conclusion

Extended-release PEO tablets of the practically water insoluble drug gliclazide (30 mg) and freely soluble metformin HCl (500 mg) retained their hydrated structural integrity when exposed to 5% and 40% w/v ethanol solutions for up to 12 h. The matrices did not fail in hydro-alcoholic media. Small differences in drug release profiles were explained in terms of drug solubility in various media. The results of this study identified trends similar to those in previously published data for HPMC ER matrix systems.

Exposure of compacts of three different viscosity grades of PEO (Polyox 1105, 301, and Coagulant) to water or hydro-alcoholic solutions had shown gradual swelling and gelation without any disruption to the tablet integrity. The compact wet weight appeared to be only slightly lower in hydro-alcoholic solutions compared to water. The extent of their relative swelling was found to increase with increasing molecular weight of PEO from 900,000 Da to 5,000,000 Da. No significant difference in compact relative swelling was observed when MW increased further from 4,000,000 Da (Polyox 301) to 5,000,000 Da (Polyox Coagulant).

This study clearly indicates that PEO matrices produces consistent drug release in water and in hydro-alcoholic media with no signs of a potential dose dumping.

Marina Levina, PhD,* is senior manager, product development at Colorcon Limited,
, +44 (1) 322-627321. Dasha Palmer is product development scientist, Thomas P. Farrell, PhD, is director, product development, and Ali R. Rajabi-Siahboomi, PhD, is director of scientific affairs, all at Colorcon in Dartford, England.

*To whom all correspondence should be addressed.

Submitted: Feb. 17, 2011. Accepted: Apr. 5, 2011.

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