Abstract
Objective: Oral drug delivery is the most desired route for drug administration for its well-known features. Therefore, many attempts were implemented to improve the poor solubility of many active ingredients in order to enhance their dissolution and absorption via the oral route. From these, the liquisolid system is a very promising technology for enhancing solubility and bioavailability of poorly soluble drugs.Methods: In this research, oral capsules of cefixime were prepared by liquisolid technique after mixing different concentrations of the drug with propylene glycol (non-volatile solvent), followed by their addition to different proportions of microcrystalline cellulose and aerosil i.e. different carrier: coating (R-value). The liquisolid capsules were evaluated for In vitro disintegration and dissolution in addition to content uniformity and weight variations. Furthermore, solubility studies, scanning electron microscope (SEM) were performed to the optimum formula. Finally, the release profile of the optimum formula was compared with the marketed cefixime capsules.Results: Liquisolid formula (F3) with 70% cefixime and R-value equals 10 was selected as the optimum formula having higher % release in 45 min (99.5%±0.53) compared to other formulas with faster release rate in the first 20 min than marketed capsules. It had an acceptable disintegration time (25 min±0.76), content uniformity (197.6±0.92) and weight variation (698.04±0.16). Results of solubility study, SEM assured enhancement in solubility and dispersibility of the drug.Conclusion: This research proved that liquisolid system is a promising technology in improving the solubility and dissolution of cefixime from its capsules and hence it may improve its absorption and oral bioavailability.
Highlights
Despite of plenty of different routes for administrating a drug, yet oral route solely remains the preferred one, because of its convenience, optimum patient compliance as well as low costs of production
According to the USP the results clearly demonstrate that all cefixime liquisolid powder had an acceptable flowability
The results clearly show that disintegration time for all formulas was less than 30 min with no significant differences between formulas
Summary
Despite of plenty of different routes for administrating a drug, yet oral route solely remains the preferred one, because of its convenience, optimum patient compliance as well as low costs of production. For a scientist to formulate a drug into, any oral dosage form, a drug must possess sufficient water solubility, it is quite challenging to formulate any drug in oral dosage form since nearly half of the active substances being identified are either insoluble or poorly soluble in water. The poor dissolution rates of water-insoluble or poorly soluble drugs are significant problem confronting the pharmaceutical industry as it is considered the rate limiting step for absorption and for bioavailability
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