Abstract
Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier
Highlights
The recent advent of high throughput screening of potential therapeutic agents has given rise to number of poorly soluble drug candidates
Evaluation of solid dispersions Drug content estimation The percentage drug content of all solid dispersions of leflunomide was between 95.52% and 99.86% (Table 1)
Enhancement in solubility and dissolution of solid dispersions is in the following order, Poloxamer 188>Poloxamer 407>polyethylene glycol (PEG) 6000>PEG 4000
Summary
The recent advent of high throughput screening of potential therapeutic agents has given rise to number of poorly soluble drug candidates. The formulation of poorly soluble compounds in oral delivery presents one of the most frequent and greatest challenges to formulation scientists in the pharmaceutical industry. Drugs with low aqueous solubility have low dissolution rates and suffer from oral bioavailability problems. Many methods such as solubilization in surfactant systems, formation of water soluble complexes, use of prodrug, and salt formation approach have been reported for increasing solubility, dissolution, and, in turn, bioavailability of drugs. Leflunomide is a nonsteroidal anti-inflammatory drug, which is poorly water soluble
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