Ciprofloxacin is a fluoroquinolone antibiotic with a broad spectrum of activity used for the treatment of various bacterial infections and is characterized by poor aqueous solubility and low permeability. The aim of this study is to formulate and characterize ciprofloxacin solid dispersions using hydrophilic and lipophilic matrices for improved product qualities and drug delivery. Ciprofloxacin hydrochloride tablets were formulated as solid dispersions by melting and solvent evaporation in tablet moulds using varying concentrations of stearic acid (10-40 %w/w), Polyethylene glycol 4000 (PEG 4000) (10-40 %w/w) and Soluplus® (10-20 %w/w as ethanolic solution) as components. The prepared tablets were evaluated for weight uniformity, friability, hardness, Fourier transform-infrared spectroscopy (FT-IR), moisture uptake, swelling index, disintegration time and dissolution rate, using standard methods and optimization techniques. The results showed uniform solid dispersion weights with friability, hardness, moisture uptake and swelling index of 0.4-0.5%, 3.0-7.5 kgf, mostly <20% and 1-71%, respectively. The formulations were chemically stable with no transformational interactions between components. Formulations without stearic acid disintegrated within 30 min whereas those containing the lipid broke up after more than 1 h. Drug release studies showed high immediate release in tablets without stearic acid but with cumulative steady state release higher in formulations with 10 %w/w Soluplus and different concentrations of stearic acid and PEG 4000. In conclusion, ciprofloxacin was presented as solid dispersion tablets with modified physicochemical attributes for improved drug delivery.
Keywords: Ciprofloxacin; solid dispersion; drug delivery
A monodisperse aerosol generator (MAGE) was used to generate calibration or monodisperse aerosols containing stearic acid and carnauba wax. Some of the factors affecting the size of aerosol particles generated with the MAGE were determined. The factors include: temperature of operation of the MAGE, type and purity of coating material used. The reproducibility of aerosol particles and stability of the aerosol generated were evaluated. The performance characteristics of the MAGE over an extended period of time of operation were also established. The calibration aerosols generated with the MAGE can be used in situ for studies of aerosol deposition measurement equipment.
A method to determine adhesion of suppository mass to intestinal tissue was developed using excised pig intestine. The method which employs the princip e of drainage unto and subsequent detachment from the mucosa, of an adherent suppository mass is simple, inexpensive and accurate. Fully optimised, it can be used to assess differences between suppository formulations, as shown by the preliminary results obtained with commercial Anusol formulations.
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