Tags

Type your tag names separated by a space and hit enter

Preparation and characterization of domperidone solid dispersions.
Pak J Pharm Sci. 2012 Oct; 25(4):783-91.PJ

Abstract

Domperidone is a highly water insoluble drug exhibiting poor dissolution pattern. The purpose of this work was to increase the dissolution rate of Domperidone by formation of solid dispersion with different water soluble carriers. Binary systems of Domperidone were prepared with polyvinyl pyrrolidone k-30 (PVP), poloxamer 188 (P188) and polyethylene glycol 6000 (PEG 6000) at different weight ratios using the solvent evaporation method, physical mixtures of the same systems were also used. The effect of the method of preparation was also investigated by preparing some selected formulations using melting method. As P188 is known to inhibit CYP3A4 enzyme which is responsible for hepatic metabolism of many drugs including Domperidone, the effect of incorporation of PVP or PEG 6000 as ternary component to P188 solid dispersion on dissolution rate was also investigated. Formulations were characterized by Fourier transform infrared (FTIR) and Differential scanning calorimetry (DSC). Drug content uniformity and dissolution rate were studied. Solid dispersions showed a better dissolution compared to the pure drug and physical mixtures, with PVP showing the highest dissolution efficiency. As indicated from DSC data, Domperidone was in the amorphous form, which confirmed the better dissolution rate of solid dispersions. Some ternary P188 combinations showed a better enhancement in drug dissolution compared to the optimized P188 binary system. This would present a potential of increasing oral bioavailability of Domperidone by increasing its dissolution rate and by inhibiting its pre-systemic metabolism by the presence of P188.

Authors+Show Affiliations

Department of Pharmaceutics, Umm Al Qura University, Saudi Arabia. eaessa@uqu.edu.saNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

23009995

Citation

Essa, Ebtessam Ahmed, and Gehan Fathy Balata. "Preparation and Characterization of Domperidone Solid Dispersions." Pakistan Journal of Pharmaceutical Sciences, vol. 25, no. 4, 2012, pp. 783-91.
Essa EA, Balata GF. Preparation and characterization of domperidone solid dispersions. Pak J Pharm Sci. 2012;25(4):783-91.
Essa, E. A., & Balata, G. F. (2012). Preparation and characterization of domperidone solid dispersions. Pakistan Journal of Pharmaceutical Sciences, 25(4), 783-91.
Essa EA, Balata GF. Preparation and Characterization of Domperidone Solid Dispersions. Pak J Pharm Sci. 2012;25(4):783-91. PubMed PMID: 23009995.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and characterization of domperidone solid dispersions. AU - Essa,Ebtessam Ahmed, AU - Balata,Gehan Fathy, PY - 2012/9/27/entrez PY - 2012/9/27/pubmed PY - 2012/12/12/medline SP - 783 EP - 91 JF - Pakistan journal of pharmaceutical sciences JO - Pak J Pharm Sci VL - 25 IS - 4 N2 - Domperidone is a highly water insoluble drug exhibiting poor dissolution pattern. The purpose of this work was to increase the dissolution rate of Domperidone by formation of solid dispersion with different water soluble carriers. Binary systems of Domperidone were prepared with polyvinyl pyrrolidone k-30 (PVP), poloxamer 188 (P188) and polyethylene glycol 6000 (PEG 6000) at different weight ratios using the solvent evaporation method, physical mixtures of the same systems were also used. The effect of the method of preparation was also investigated by preparing some selected formulations using melting method. As P188 is known to inhibit CYP3A4 enzyme which is responsible for hepatic metabolism of many drugs including Domperidone, the effect of incorporation of PVP or PEG 6000 as ternary component to P188 solid dispersion on dissolution rate was also investigated. Formulations were characterized by Fourier transform infrared (FTIR) and Differential scanning calorimetry (DSC). Drug content uniformity and dissolution rate were studied. Solid dispersions showed a better dissolution compared to the pure drug and physical mixtures, with PVP showing the highest dissolution efficiency. As indicated from DSC data, Domperidone was in the amorphous form, which confirmed the better dissolution rate of solid dispersions. Some ternary P188 combinations showed a better enhancement in drug dissolution compared to the optimized P188 binary system. This would present a potential of increasing oral bioavailability of Domperidone by increasing its dissolution rate and by inhibiting its pre-systemic metabolism by the presence of P188. SN - 1011-601X UR - https://www.unboundmedicine.com/medline/citation/23009995/Preparation_and_characterization_of_domperidone_solid_dispersions_ DB - PRIME DP - Unbound Medicine ER -