A method to microencapsulate water-soluble and liquid-paraffin insoluble drugs into spherical, discrete and free-flowing particles of approximately 175 microns size with excellent yield has been described taking diethylcarbamazine citrate as a model drug. In this method a gelatin-drug dispersion at 50 degrees C is sprayed, using a simple apparatus designed in our laboratory, into chilled, dry liquid paraffin present in a china dish previously coated with a layer of hard paraffin and maintained at 5 degrees C. After allowing the droplets to gel at 5 degrees C for an hour, water was removed by freeze drying. Later liquid paraffin adhering to freeze-dried microcapsules was removed by washing with chilled, dry acetone. Various factors affecting the yield, size, shape and size distribution of microcapsules were optimized.
Aim:The aim of the project was to develop cross-linked b-cyclodextrin (CL β-CD) microparticles for controlled delivery of a highly water-soluble drug.Materials and Methods:CL β-CD microparticles were prepared by emulsification phase separation technique using epichlorohydrin as a cross-linking reagent. The developed microparticles were compared with β-CD for their pharmacotechnical properties. A highly water-soluble model drug, pravastatin sodium (PS) was loaded within these hydrophobic microparticles by active drug loading method using nonionic surfactant Tween 80 as the loading facilitator.Results:Maximal drug fixation (216.8 mg/g beads) was observed in pH 4 at 20°C. In vitro release studies of PS-loaded CL β-CD microparticles in simulated gastric fluid and simulated intestinal fluid resulted in modified dissolution profiles. Modeling of release profiles confirmed controlled release (r2 = 0.9910) of PS from the cross-linked system.Conclusion:Controlled release CL β-CD microparticles PS that have the potential to enhance its therapeutic properties by offering the advantage of less frequent dosing and decreased fluctuations in the blood levels during the dosing interval were successfully developed.
Aim: This study was to develop a controlled release formulation of various proton pump inhibitor drugs to maintain constant therapeutic levels of the drug over 24 h. Settings and Design: Dexlansoprazole was selected as model drugs. Various formulations were developed with different polymers for each drug molecule. To achieve pH-independent drug release of formulations, pH modifying agents were used. Materials and Methods: The precompression blends of all formulations were subjected to various flow property tests, and all the formulations were passed the tests. Various grades of hydroxypropyl methylcellulose were employed as polymers. Statistical Analysis Used: Absence of probable chemical interactions of Fourier transform infrared between pure drug and polymers. Results: Dexlansoprazole dose was fixed as 30 mg. Total weight of the tablet was considered as 250 mg. Polymers were used in the concentration of 75 and 150 mg concentration. All the formulations were passed various physicochemical evaluation parameters and they were found to be within limits. Conclusions: Whereas from the dissolution studies it was evident that the formulation (F-2) showed better and desired drug release pattern, i.e. 98.79 ± 0.48 in 24 h. It followed zero-order release kinetics mechanism.
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