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Dilip M. Kumbhar ¹, Kailas K. Mali ¹, Remeth J. Dias ¹, Vijay D. Havaldar ¹, Vishwajeet S. Ghorpade ¹, Nitin H. Salunkhe ¹

Affiliations
1 YSPM’s, YTC, Wadhe, Satara, 415011, IN

Abstract

The main objective of present investigation was to design the colorectal microspheres of Capecitabine by using inexpensive natural polysaccharide based polymers. The pectin microspheres were prepared by single emulsification technique using calcium chloride as crosslinking agent. Pectin loaded microspheres were coated with ethyl cellulose by solvent evaporation method. The prepared microspheres were characterized by entrapment efficiency, particle size, in-vitro drug release, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and Differential scanning calorimetry (DSC). The in-vitro drug release behaviour of ethyl cellulose coated pectin microspheres done in varying pH conditions up to 12 hr. Optimized uncoated batch of pectin based capecitabine microspheres showed optimum particle size with good drug encapsulation efficiency and spherical in nature. All the formulations showed less than 20 % drug release in acidic environment. Ethyl cellulose coated microspheres mininised initial burst effect and showed drug release in the range of 85.33 to 95.55% at the end of 12h. As concentration of ethyl cellulose was increased drug release was found to be retarded well. From above results it can be concluded that capecitabine loaded ethyl cellulose coated pectin based microspheres may be the best alternative to conventional tablets to treat the colon cancer.

Keywords

Capecitabine, Ethyl Cellulose, Microsphere, Natural Polymers, Pectin.

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Dilip M. Kumbhar ¹, Vijay D. Havaldar ¹, Kailas K. Mali ¹, Remeth J. Dias ¹, Vishwajeet S. Ghorpade ¹, Rahul B. Londhe ¹

Affiliations
1 YSPM’s, YTC, Wadhe, Satara, 415011, IN

Abstract

The purpose of present investigation was to formulate the sustained release tablets of Venlafaxine HCl (VHL) by direct compression method using natural polymer, xanthan gum and semi synthetic polymers such as hydroxypropyl methylcellulose (HPMC) K4M, HPMC K15M, HPMC K100M and Carbopol alone or in combination. The drug and all the excipients were evaluated to study compatibility and flow properties. The prepared tablets were evaluated for tablet dimensions, weight variation test, friability, drug content and in vitro drug release study. The FTIR study of drug with all excipients showed that there was no any interaction between the drug and excipients. The precompression study of powder blend showed good flow properties. All the tablets showed dimensions and hardness within prescribed limit. Friability and weight variation test was found to be satisfactory. Drug content was found to be in the range of 94.24 to 101.02% and all the formulations sustained release of drug. Formulation containing equal concentrations of carbopol and xanthan gum showed 90.02% drug release in 12 h. From above results, it can be concluded that tablets of VHL prepared with carbopol and xanthan gum by direct compression method have sustained release of drug that may be useful in the treatment of depressive disorders.

Keywords

Carbopol, Natural Polymers, Sustained Release, Venlafaxine HCl, Xanthan Gum.

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