Abstract
The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.
Highlights
Water-soluble drugs are increasingly becoming a problem in terms of obtaining the satisfactory dissolution within the gastrointestinal tract that is necessary for good bioavailability[1]
Aceclofenac is an example of BCS class II compound, its oral bioavailability is determined by dissolution rate in the gastro intestinal tract
The results indicates that that release pattern from solid dispersions formulations A10 shows the best result in comparison to A11, A12 and A13 which was 74.55% within an hour (Figure 4)
Summary
Water-soluble drugs are increasingly becoming a problem in terms of obtaining the satisfactory dissolution within the gastrointestinal tract that is necessary for good bioavailability[1]. It is existing drugs that cause problems but it is the challenge of medicinal chemists to ensure that new drugs are active pharmacologically but have enough solubility to ensure fast enough dissolution at the site of administration, often gastrointestinal tract. Aceclofenac is a new generation NSAID used in the treatment of osteoarthritis, rheumatoid arthritis and other joint diseases[3]. It is chemically designated as 2-[(2,6-diclorophenyl) amine] phenyl acetoxy acetic acid). Aceclofenac is an example of BCS class II compound (highly permeable and low Soluble), its oral bioavailability is determined by dissolution rate in the gastro intestinal tract. The improvement of Aceclofenac dissolution is an important issue for enhancing its bioavailability and therapeutic efficacy[7]
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