Quantitative Control On Preparation Of Microcapsules By Fluidized Bed

Microencapsulation was an development direction in the important field ofmedicine preparation in recent years, the microencapsules has incomparablesuperiority than other dosage forms. Fluidized bed for preparing the microcapsulesin taste-masking, reducing gastrointestinal irritation, increasing the stability ofmedicine has been successfully applied, but the research is not enough deep, notenough system.In order to provide the basis for industrialized production, improvingthe levels of pharmaceutical production, in this paper, the parameters of technicprocess and formulation for the preparation of three different types of medicinemicrocapsule with three capsule material by fluidized bed were systematicallyinvestigated and quantified.Study of the formulation and technology of water insoluble medicinemicrocapsules, the acyclovir was chosen as the model drugs of poorly soluble inwater.First of all, the phenomenon of electrostatic adherence for the preparation ofthe powder was solved by fluidized bed,0.8%mass fraction silica powder wereadded for preparation the core material with good antistatic effect, this laid thefoundation for later experiment; secondly Eudragit S100was used as capsule wallmaterials to investigate the single factor of parameters of technic process andformulation of acyclovir microcapsules, general range of technic factors andprescription factors of influence of the microcapsule quality were studied bysingle-factor test, and the optimal condition were definited by orthogonalexperiment.The optimal parameters were as followed: Eudragit S100dosage was8%, the elasticizer of sebacic acid two butyl dosage was30%,;the antitack agent oftalc powder dosage was%; feeding rate ml/min, spray pressure was0.6bar,temperature was30±1℃; finally Eudragit NE30D was used as capsule wallmaterials to investigate the single factor of parameters of technic process andformulation of acyclovir microcapsules, general range of technic factors andprescription factors of influence of the microcapsule quality were studied bysingle-factor test, and the optimal condition were definited by orthogonal experiment.The optimal parameters were as followed: Eudragit NE30D dosage was%,;the antitack agent of talc powder dosage was15%, feeding rate0.8ml/min, spraypressure was bar, inlet pressure was bar, temperaturewas28±1℃. This part ofthe experiment obtained in particle size and encapsulation efficiency in terms ofgood performance, and it was suitabled for industrialized production, reached theintended purpose. The experiment has guiding significance in different solventcapsule material conditions preparation of water insoluble drug microcapsules byfluidized bed, and the future experiments foundation was laid in the prescriptionprocess,further optimizing and quantifying for control.Study of the formulation and technology of water soluble drug microcapsules,the propranolol was chosen as the model drugs of water soluble, referencing on thepart of the experimental results, the central composite design and response surfacemethod was used to optimized further, and Eudragit RSPO was used as capsule wallmaterials to optimized the prescription and technology condition of preparation ofpropranolol under conditions of alcohol solvent: The optimal parameters were asfollowed: Eudragit RSPO dosage was%, the elasticizer of sebacic acid two butyldosage was%, the antitack agent of talc powder dosage was18%, the capsulematerial flow rate was2.55ml/min, spray pressure was bar, temperature was30±1℃; and Eudragit NE30D was used as capsule wall materials to optimized theprescription and technology condition of preparation of propranolol under conditionsof alcohol solvent: The optimal parameters were as followed: Eudragit NE30Ddosage was%, the capsule material flow rate was1.05ml/min, spray pressure wasbar, temperature was28±1℃. This part of the experiment by central compositedesign-response surface method to optimized the prescription and technologycondition of preparation of microencapsules, the parameter of quantification controlwas provided by different size, different content, different encapsulation rate ofmicrocapsules,and the basis was provided in the realization of industrializedproduction.The preparation of microcapsule needed to deal with the common problems bythe fluidized bed in the last chapter, as well as further validation of the prescription processparameters of the second chapter and the third chapter, the tilmicosin was used as modeldrug in this chapter, Tilmicosin has the problem of preparation microcapsule needed todeal with the common problems by fluidized bed, and the conclusion of prescriptionand technological parameters were used in previous chapters, using to preparation of tilmicosin microcapsules, to study its release, the anterior prescription and thetechnological parameters were quantified further and verified. In order to achievesustained release purposes, Eudragit RSPO was choosed as capsule material,according to the different particle size of core material, different kinds of materialwere studied, in order to release as indexes by central composite design-responsesurface method has good slow release effect of the optimal prescription andtechnology condition: the core of the capsule was μm, the quantity of core wasthe g, the capsular material was g, the elasticizer of sebacic acid two butyldosage was%, the antitack agent of talc powder dosage was%, feeding rateml/min, spray pressure was bar, temperature was30±1℃.The study shows that the microcapsules of different size, differentencapsulation rate, different release can be prepared by fluidized bed, the quality ofproduct was stable, the formulation and process parameters prescription process wascontrollable, and it was favorable for industrialized production.