Interest in HME as a pharmaceutical process continues to grow and the potential of automation and reduction of capital investment and labor costs has earned this technique a necessary consideration as a drug delivery solution.
The objective of this study was to enhance the solubility as well as to mask the intensely bitter taste of the poorly soluble drug, Mefenamic acid (MA). The taste masking and solubility of the drug was improved by using Eudragit® E PO in different ratios via hot melt extrusion (HME), solid dispersion technology. Differential scanning calorimetry (DSC) studies demonstrated that MA and E PO were completely miscible up to 40% drug loads. Powder X-ray diffraction analysis indicated that MA was converted to its amorphous phase in all of the formulations. Additionally, FT-IR analysis indicated hydrogen bonding between the drug and the carrier up to 25% of drug loading. SEM images indicated aggregation of MA at over 30% of drug loading. Based on the FT-IR, SEM and dissolution results for the extrudates, two optimized formulations (20% and 25% drug loads) were selected to formulate the orally disintegrating tablets (ODTs). ODTs were successfully prepared with excellent friability and rapid disintegration time in addition to having the desired taste-masking effect. All of the extruded formulations and the ODTs were found to be physically and chemically stable over a period of 6 months at 40°C/75% RH and 12 months at 25°C/60% RH, respectively.
This article focuses on preparation and evaluation of a once a day ophthalmic delivery system for ciprofloxacin hydrochloride based on the concept of pH-triggered in situ gelation. The in situ gelling system involves the use of polyacrylic acid (Carbopol ® 980NF) as a phase transition polymer, hydroxypropyl methylcellulose (Methocel ® K100LV) as a release retardant, and ion exchange resin as a complexing agent. Ciprofloxacin hydrochloride was complexed with ion exchange resin to avoid incompatibility between drug and polyacrylic acid. The developed formulation was stable, and nonirritant to rabbit eyes and in vitro drug release was found to be around 98% over a period of 24 hours.Keywords pH-triggered in situ gel; ciprofloxacin hydrochloride; Carbopol ® ; hydroxypropyl methylcellulose; once a day ocular delivery system
INTRODUCTIONToday, topical ophthalmic application is considered the preferred way to achieve therapeutic levels of active medicament used to treat ocular diseases. Solutions, suspensions, and semisolids like ointments and gels are conventionally available as ophthalmic delivery systems. From a biopharmaceutical standpoint, their use has met some criticism over their efficiency as drug delivery systems. Bioavailability, particularly for ocular solutions, ranges from 1% to 10% of the total administered dose. This could be due to the rapid precorneal kinetics resulting from reflex tearing and blinking. The basic disadvantage associated with the use of ocular formulation is rapid loss of both solutions and suspended solid. Ophthalmic ointments give blurred vision, leading to poor patient acceptance (Olejnic, 1993).
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