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Fast-dissolving and high-drug-loaded, Fatty Acid-based self-emulsifying solid dispersions of diacerein.
PDA J Pharm Sci Technol. 2012 May-Jun; 66(3):201-13.PJ

Abstract

The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions (SDs) containing polyethylene glycol 6000 (PEG 6000), surfactant, and self-emulsifying excipient with high drug content. Ternary and self-emulsifying SDs containing high drug content were prepared and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based SDs, a remarkable enhancement of the dissolution rate was observed, even in SDs with high drug content. The presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the PXRD spectra and absence of drug melting peak in DSC spectra demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix. The utilization of self-emulsifying excipient and surfactant in PEG 6000-based SDs could be a useful tool to enhance the dissolution and bioavailability of diacerein by forming solubilizing and microemulsifying systems with high drug content.

LAY ABSTRACT

The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions with high drug content. These solid dispersions were prepared and characterized by powder X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based solid dispersions, a remarkable enhancement of the dissolution rate was observed, even in solid dispersions with high drug content. Moreover, the presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the powder X-ray diffraction spectra and absence of drug melting peak in the spectra obtained by differential scanning calorimetry demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix.

Authors+Show Affiliations

Rayat Institute of Pharmacy, Railmajra, Distt. Ropar, Punjab, India.No affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22634586

Citation

Aggarwal, Amit Kumar, and Samarpreet Singh. "Fast-dissolving and High-drug-loaded, Fatty Acid-based Self-emulsifying Solid Dispersions of Diacerein." PDA Journal of Pharmaceutical Science and Technology, vol. 66, no. 3, 2012, pp. 201-13.
Aggarwal AK, Singh S. Fast-dissolving and high-drug-loaded, Fatty Acid-based self-emulsifying solid dispersions of diacerein. PDA J Pharm Sci Technol. 2012;66(3):201-13.
Aggarwal, A. K., & Singh, S. (2012). Fast-dissolving and high-drug-loaded, Fatty Acid-based self-emulsifying solid dispersions of diacerein. PDA Journal of Pharmaceutical Science and Technology, 66(3), 201-13. https://doi.org/10.5731/pdajpst.2012.00857
Aggarwal AK, Singh S. Fast-dissolving and High-drug-loaded, Fatty Acid-based Self-emulsifying Solid Dispersions of Diacerein. PDA J Pharm Sci Technol. 2012 May-Jun;66(3):201-13. PubMed PMID: 22634586.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fast-dissolving and high-drug-loaded, Fatty Acid-based self-emulsifying solid dispersions of diacerein. AU - Aggarwal,Amit Kumar, AU - Singh,Samarpreet, PY - 2012/5/29/entrez PY - 2012/5/29/pubmed PY - 2016/4/23/medline SP - 201 EP - 13 JF - PDA journal of pharmaceutical science and technology JO - PDA J Pharm Sci Technol VL - 66 IS - 3 N2 - UNLABELLED: The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions (SDs) containing polyethylene glycol 6000 (PEG 6000), surfactant, and self-emulsifying excipient with high drug content. Ternary and self-emulsifying SDs containing high drug content were prepared and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based SDs, a remarkable enhancement of the dissolution rate was observed, even in SDs with high drug content. The presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the PXRD spectra and absence of drug melting peak in DSC spectra demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix. The utilization of self-emulsifying excipient and surfactant in PEG 6000-based SDs could be a useful tool to enhance the dissolution and bioavailability of diacerein by forming solubilizing and microemulsifying systems with high drug content. LAY ABSTRACT: The purpose of the present study was to enhance the solubility and dissolution of diacerein by preparing their fatty acid-based, self-emulsifying solid dispersions with high drug content. These solid dispersions were prepared and characterized by powder X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy, solubility studies, and dissolution studies. When hydrophilic and lipophilic excipients were combined and incorporated into PEG 6000-based solid dispersions, a remarkable enhancement of the dissolution rate was observed, even in solid dispersions with high drug content. Moreover, the presence of surfactant and self-emulsifying excipient did not affect the solid state characterization of the drug. The decrease in the intensity of the numerous distinctive peaks of the drug in the powder X-ray diffraction spectra and absence of drug melting peak in the spectra obtained by differential scanning calorimetry demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix. SN - 1948-2124 UR - https://www.unboundmedicine.com/medline/citation/22634586/Fast_dissolving_and_high_drug_loaded_Fatty_Acid_based_self_emulsifying_solid_dispersions_of_diacerein_ L2 - http://journal.pda.org/cgi/pmidlookup?view=long&pmid=22634586 DB - PRIME DP - Unbound Medicine ER -