Dissolution Enhancement of Diacerein Using Water Soluble Carrier by Solid Dispersion Technology

Abstract

Diacerein is generally used in the treatment of Osteoarthritis , this drug comes under the class anthraquinone. The drug is practically insoluble in water and exhibits exceptionally slow and intrinsic dissolution rate with poor bioavailability. In the present study, diacerein and β-cyclodextrin (β-CD) solid dispersions were prepared with a view to study the effect and influence of β-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of diacerein was significantly increased in the presence of β-CD and indicating the possible 1:1 stoichiometric inclusion complex with a stability constant of 339.66 M-1. Effect of variable such as drug: Carrier ratios were studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and X-ray diffraction studies (XRD). These studies revealed that a distinct loss of drug crystallinity in the solid dispersion is ostensibly accounting for enhancement of dissolution rate in distilled water containing 0.1% Tween 80. The scanning electron microscopy (SEM) study revealed that all the binary systems appeared as agglomerates and exhibiting the presence of a homogenous solid phase which could also be responsible for the enhanced dissolution rate in comparison with the pure drug. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersion of diacerein showed a 7.66 times fold increase in dissolution rate over the pure drug.

Solid Dispersions of Anthelmintics and Plant Protection Preparations

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Solid Dispersions of Biologically Active Substances

“…Usually SD are widely used in medicine [6][7][8][9][10], because these systems can provide many additional advantages: 1. to increase the solubility of poorly soluble drugs, thereby increasing the rate of dissolution, absorption and bioavailability. 2. to improve the drug output of ointments creams and gels.…”

Solid Dispersion and Inclusion Complex for Solubility Enhancement of Rifabutine: A Comparative Study

“…Hence, they can be utilised broadly in the pharmaceutical industry. (Patel et al, 2010;Nagasamy et al, 2017) The l -cyclodextrin, a -cyclodextrin and ß -cyclodextrin, are the most common natural CDs which are formed by six, seven, and eight glucose units respectively along with hydrophobic cavity and hydrophilic external area. Inclusion complex improves bioavailability, solubility rate, dissolution pro ile and stability.…”