Abstract

MODIFIED SOLUTION ATOMIZATION AND CRYSTALLIZATION BY SONICATION (SAXS) METHOD ENHANCES FLOWABILITY AND SOLUBILITY OF ANTI-CANCER MEBENDAZOLE DRUG AGGLOMERATES

Dharmeshkumar M. Modi*, Akshat D. Modi, Rajesh H. Parikh and Jolly R. Parikh

ABSTRACT

Mebendazole is a widely used broad-spectrum benzimidazole class anthelmintic, useful in the treatment of ascariasis, uncinariasis, trichuriasis, and oxyuriasis. Due to its low water solubility, it has slow rate of dissolution, which leads to poor absorption form gastrointestinal tract. Moreover, its needle shaped crystals, it shows poor flowability. In this study, an attempt was made to increase the flowability and solubility of Mebendazole by imparting the spherical shape and converting it into amorphous by atomization of solution and crystallization by using ultrasonic waves. A 32 full factorial design was used to investigate the effect of the amount of Mebendazole and the amount of water as an external phase. The resulting spherical agglomerates showed improvements in flowability, compressibility, and % dissolved in 60 minutes. The treated Mebendazole spherical agglomerates showed an increase in particle size and were found to be monodisperse. The desirability function approach was used to select the best batch. Fourier Transform Infra-Red of the best batch study showed no chemical changes in the treated Mebendazole. The best batch was confirmed by Scanning Electron Micrograph in terms of sphericity and reduced crystallinity as demonstrated by X-Ray diffraction and Differential Scanning Calorimetry studies. This alternative approach can be used for drugs with similar properties to Mebendazole.

Keywords: Mebendazole; Ultrasonic waves; Spherical agglomerates, Uniformity index, Desirability function, Flowability, Compressibility, Dissolution.