Abstract
Objective: The purpose of the present study was to enhance solubility and dissolution characteristics of indomethacin by preparing inclusion complexes with hydroxypropyl β-cyclodextrin (HP β-CD) and solid dispersions with PEG 6000 to enhance its in vitro drug release and to further formulate it as a tabletMethods: Solid dispersions (SDs) and inclusion complexes (ICs) of Indomethacin with PEG 6000 and HP β-CD respectively were prepared to enhance the dissolution rate of this poorly water-soluble drug belonging to BCS class II. A comparison was made between two systems: solid dispersions with PEG 6000 obtained using melting and solvent evaporation technique, inclusion complexes with HP β-CD prepared by kneading technique. SDs were prepared in 1:1, 1:2, 1:3 and ICs in 1:0.25, 1:0.5, 1:1 w/w ratios of drug: polymer. Both the systems were characterized by FTIR, SEM, DSC, X-RD.Results: The dissolution of indomethacin increased with the increase in the concentration of the polymers. F4 and F9 formulations showed complete drug release in less than 30 min. Dissolution studies indicated that cyclodextrin complexes showed a better enhancement of dissolution rate when compared to solid dispersions. CDs were found to be more effective than PEGs at lower concentrations. These formulations were further compressed as tablets.Conclusion: The FTIR and DSC studies showed that no interactions existed between the drug and the polymer.
Highlights
On the basis of two parameters: aqueous solubility and membrane permeability, the Biopharmaceutical Classification System (BCS) categorizes the drugs into four classes
Indomethacin, Polyethylene glycols (PEGs) 6000 were obtained from Yarrow Chem Products, hydroxypropyl β-cyclodextrin (HP β-CD), Sodium hydroxide were obtained from Finar Chemicals, ethanol and potassium di-hydrogen phosphate from Thermo Fisher Scientific India Pvt, Ltd (Mumbai, India)
All the SDs and the inclusion complexes (ICs) exhibited higher dissolution rate when compared to pure indomethacin drug
Summary
On the basis of two parameters: aqueous solubility and membrane permeability, the Biopharmaceutical Classification System (BCS) categorizes the drugs into four classes. Drugs belonging to BCS class II show low solubility and high permeability, requiring larger doses on oral administration to obtain therapeutic plasma concentration. At the site of absorption, as a drug requires being available in solution form, dissolution becomes a rate-limiting step. Improving solubility and oral bioavailability of such drugs by formulation design approaches prove to be promising [1]. It relieves pain related to inflammation or tissue injury. It inhibits prostaglandin synthesis and suppresses motility of neutrophils. The poor aqueous solubility of this drug limits its absorption and rate of dissolution which further decreases its bioavailability [3]
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