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THE PHARMA REVIEW (APRIL - MAY, 2008)

Impact of Sucrose Esters on Dissolution Rate of Itraconazole

Murthy Dwibhashyam V.S.N., Keerthi P., Rohini P., Padmaja T., Bhanu Teja B., Vijaya Ratna J.

Abstract: Itraconazole is a potent antifungal drug belonging to the triazole group. It suffers from poor aqueous solubility and a correspondingly poor dissolution profile. Various approaches have been tried out to enhance the solubility and hence dissolution of itraconazole. In the present investigation, various sucrose esters viz., sucrose stearate (S-970, S-1670), sucrose palmitate (P-1670), sucrose myristate (M-1695), and sucrose oleate (O-1570) were used to enhance the itraconazole solubility. The investigated formulations contain drug and sucrose ester in 1:1 ratio. No significant increase in itraconazole solubility was observed with the investigated sucrose esters. A maximum of about two-fold increase in drug dissolution was observed with sucrose palmitate of HLB 16. The order of dissolution enhancement effect of the investigated sucrose esters for the 2 hr period was of the following order: sucrose palmitate sucrose stearate of HLB 16 sucrose stearate of HLB 9 and sucrose oleate sucrose myristate. Dissolution enhancement effect of the sucrose esters could not be correlated with their HLB values and the sucrose esters were found to be poor solubilizers for itraconazole.

Introduction

Itraconazole is a potent antifungal drug having broad spectrum of activity against dermatophytes, yeasts, dimorphic and diatomaceous fungi and some moulds such as Aspergillus. It belongs to the triazole group and is structurally related to ketoconazole. It has very low aqueous solubility ( 1g/ml) and a correspondingly poor dissolution profile and high permeability (Peff 3.8 x 10-6 cm/s). Different approaches have been tried out to enhance the solubility of itraconazole out of which solid dispersion technique is the most researched technique.

Surfactants are known to enhance the solubility of poorly water-soluble drugs. Sucrose fatty acid esters are non-ionic type surfactants having a sugar substituent, sucrose, as the polar head group and fatty acids as non-polar groups. Sucrose fatty acid esters contain different fatty acids in various ratios. Their HLB value ranges from 1 to 16, which is wider as compared to that of Tweens and Spans. These compounds show many advantages such as biodegradability and lack of toxicity. The primary aim of the present investigation was to check the impact of various sucrose acid esters on the dissolution rate of itraconazole.

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