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Incorporation Efficiency (incorporation + efficiency)
Selected AbstractsInfluence of chitosan crosslinking on bitterness of mefloquine hydrochloride microparticles using central composite designJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 2 2009Punit P. Shah Abstract The present work examines the influence of various process and product parameters on mefloquine hydrochloride (MFL) entrapped in crosslinked chitosan microparticles for masking the bitterness. A central composite design (CCD) was employed to investigate the effect of three process and product variables, namely amount of MFL, chitosan and sodium hydroxide (crosslinking agent) on the incorporation efficiency, particle size, drug release at pH 6.8 and bitterness score. The microparticles were prepared by ionotropic gelation method, with a hardening time of 60 min. The optimum condition for process and product variables was evaluated using desirability function. The model is further cross validated for bias. The optimized microparticles were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. Bitterness score was evaluated by human gustatory sensation test. Multiple linear regression analysis revealed that the crosslinking of chitosan significantly affects incorporation efficiency, particle size, drug release and bitterness score. The bitterness score was decreased to zero compared to 3+ of pure MFL. It can be inferred that the proposed methodology can be used to prepare MFL microparticles for bitter taste masking. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:690,703, 2009 [source] Effect of chitosan crosslinking on bitterness of artemether using response surface methodologyJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 4 2008Punit P. Shah This work examines the influence of various process parameters on artemether entrapped in crosslinked chitosan microparticles for masking bitterness. A central composite design was used to optimize the experimental conditions for bitterness masking. Critical parameters such as the amounts of artemether, chitosan and crosslinking agent have been studied to evaluate how they affect responses such as incorporation efficiency, particle size and drug release at pH 6.8. The desirability function approach has been used to find the best compromise between the experimental results. The optimized microparticles were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. Bitterness score was evaluated by human gustatory sensation test. Multiple linear regression analysis revealed that the crosslinking of chitosan significantly affects incorporation efficiency, particle size and drug release at pH 6.8. The bitterness score of microparticles was decreased to 0, compared with 3+ for pure artemether. The proposed method completed masked the bitter taste of artemether. [source] Sustained Release of 5-Fluorouracil from Polymeric NanoparticlesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 12 2000PAUL A. McCARRON The use of biodegradable nanoparticles loaded with 5-fluorouracil was investigated as a potential means to sustain the release of this drug. Nanoparticles prepared from four biodegradable polymers were loaded with 5-fluorouracil using three loading concentrations of drug and three different concentrations of added polymer. Washing particles using a centrifugation/re-suspension with ultrasound protocol was found to dislodge the majority of drug, resulting in an over-estimation of incorporation efficiency and low levels of strongly entrapped drug. Increasing the initial 5-fluorouracil concentration before polymer/monomer addition increased the drug loading in both washed and unwashed particles. Increasing the amount of polymer used to make nanoparticles did not increase loadings, but did produce increased amounts of unusable polymer waste. Drug release from nanoparticles was evaluated using a Franz cell diffusion apparatus, which showed an initial burst effect followed by a slower release phase over 24 h. Indeed, nanoparticles prepared from poly(lactide-co-glycolide) released 66% of their 5-fluorouracil payload over this period. It was concluded that 5-fluorouracil-loaded nanoparticles could be readily included into a hydrogel-based delivery system to provide sustained drug release for trans-epithelial drug-delivery applications. [source] Solid-phase incorporation of gaseous carbon dioxide into oxirane-containing copolymersJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 15 2004Bungo Ochiai Abstract Carbon dioxide was incorporated into poly(glycidyl methacrylate- co -methyl methacrylate) by a solid-phase reaction, which transformed the pendent oxirane moieties into cyclic carbonate moieties, with quaternary ammonium halide catalysts. The incorporation of carbon dioxide into the copolymer led to soluble carbonate-containing polymers, whereas the incorporation of carbon dioxide into the glycidyl methacrylate homopolymer produced an insoluble product. The copolymer composition, reaction temperature, and catalyst amount affected the incorporation efficiency and the side reaction that caused crosslinking. Effective incorporation was achieved under the following reaction conditions: the glycidyl methacrylate content was less than approximately 50%, the temperature was greater than the glass-transition temperature, and the catalyst concentration was 1.5,6 mol %. © 2004 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 42: 3812,3817, 2004 [source] Reactivity of ethyl acetate and its derivatives toward ammonolysis: ramifications for ammonolysis-based microencapsulation processPOLYMERS FOR ADVANCED TECHNOLOGIES, Issue 10 2009Younglim Chung Abstract The reactivity of three ester organic solvents toward ammonolysis was examined in relation to the development of an ammonolysis-based microencapsulation process. Ethyl acetate, ethyl chloroacetate, and ethyl fluoroacetate were chosen as ester organic solvents. Progesterone was considered as a model drug to be encapsulated into poly- D, L -lactide- co -glycolide microspheres. A polymeric dispersed phase was emulsified in an aqueous phase, to which ammonia was added to initiate ammonolysis. The polarization status of a carbonyl group in the backbone of the ester was found to decide the magnitude of the ester reactivity. In fact, the simple ester ethyl acetate hardly reacted with ammonia, while ethyl chloroacetate and ethyl fluoroacetate showed greater reactivity toward ammonolysis. The rapid completion of ammonolysis led to the conversion of the water-immiscible solvents into water-soluble solvents, thereby providing an efficient tool for microsphere solidification. Among microencapsulation parameters, the type of dispersed solvent, the molar ratio of ammonia to a dispersed solvent, and the percentage of the progesterone payload decisively influenced the characteristics of the microspheres. Subsequently, variations in such parameters accompanied considerable influence on microsphere morphology, incorporation efficiency, thermal behavior, the degree of residual solvents, and the physical status of progesterone. Optimization of the process parameters would not only contribute to improving the ammonolysis-based microencapsulation process, but would also permit the tailoring of microsphere properties to specific demands. Copyright © 2008 John Wiley & Sons, Ltd. [source] | ||||||||||