Solid Dispersion: Improvement of Aqueous Solubility of Poorly Soluble Drug

The intention of the current study was to boost the solubility of Fenofibrate by solid dispersion technique which is an efficient technique in improving the solubility and hence the dissolution rate of poorly soluble drugs in the form of eutectic mixtures by producing fine dispersion when in contact with gastrointestinal fluid and also the technique offers the choices of carriers to be combined with drug conveniently to improve the solubility to a considerable extent. Fenofibrate a BCS class II Antihyperlipidemic drug belongs to fibrate class and it is a lipid-lowering drug used in the treatment of hyperlipidemia. Fenofibrate is insoluble in water and hence shows poor dissolution in gastric fluid with reduced absorption characteristics. In order to improve the solubility, dissolution rate, gastrointestinal absorption and oral bioavailability, it was decided to prepare fenofibrate solid dispersion and evaluated. They were prepared using poly ethylene glycol 4000, 6000, 8000 and β-cyclodextrin by fusion technique and optimized solid dispersion was also lyophilized. Physical characterization of solid inclusion complex of fenofibrate was studied and showed that there were no drug excipients interactions. Dissolution studies showed a momentous rise in a dissolution of Fenofibrate when dispersed in polymers. Inturn aqueous solubility was enlarged linearly as a function of the concentration of β- Cyclodextrin.

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Cyclodextrin Inclusion Complexes: Novel Techniques to Improve Solubility of Poorly Soluble Drugs: A Review

Global Pharmaceutical Sciences Review ◽

10.31703/gpsr.2016(i-i).04 ◽

2016 ◽

Vol I (I) ◽

pp. 29-34

Author(s):

Sobia Noreen ◽

Irsah Maqbool ◽

Muhammad Ijaz ◽

Sairah Tanveer

Keyword(s):

Inclusion Complexes ◽

Aqueous Solubility ◽

Complexing Agents ◽

Dissolution Profile ◽

Drug Candidates ◽

Insoluble Drugs ◽

Poorly Soluble ◽

Poorly Soluble Drug ◽

Technological Strategies ◽

Crucial Test

For a formulation scientist, the dilemma of solubility is a crucial test during the product development phase that can be resolved by opting various technological strategies. Some of the strategies that are usually applied for enhancing solubility of drugs with low aqueous solubility include micronization, solvent deposition and solid dispersion. With these approaches, some advantages as well as drawbacks, are affiliated. The strategy of complexation amid all techniques, has been applied more accurately for the improvement of dissolution profile, aqueous solubility, and bioavailability of poorly soluble drug candidates. Cyclodextrin are unique cyclic carbohydrates that have been exploited as successful complexing agents having capability of forming inclusion complexes with insoluble drugs. Numerous strategies have been considered to analyze the methods for preparation of inclusion complexes. In this review, we have pursued the discussion on different complexation techniques and in a nutshell, emphasized the applications and economical/technical limitations related to these techniques.

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