| The traditional drug dosage forems were changed by microcapsule,the relesse of capsule drug was extended and controlled,lightening the pill burden,improving the storage stability of the drug,achieving controlled release and targeted drugs.In this research,the sodium alginate/chitosan microcapsule and the pH responsed complex microcapsule with sodium alginate/polyacrylic resin?were proposed by the microcapsule technology,the tinidazole as model drug.The characteristics and release efficiency were studied.Improving the stability of the drug and the slow controlled release by microcapsule technology,the utilization of tindazole was increased and the toxicity of drug was reduced.The chitosan thermosensitive hydrogel encapsulating complex microcapsule was prepared,and the performance was tested,using mesh structure of the hydrogel to avoid drug liquid,the drug sustained release slowly to realize.This topic research is divided into three chapters:1.The preparation and performance of sodium alginate/chitosan/tinidazole microcapsule: microcapsule was preparation using the method of orifice extrusion.The preparation conditions were optimized using single factor experiment.Firstly,the microcapsules of different conditions(the concentration of sodium alginate,the concentration of chitosan,the concentration of anhydrous calcium chloride and curing temperature)were prepared and the characterization such as the encapsulation efficiency and drug-loading rate were studied to evaluate the influence of different preparing factors.Then the microcapsule preparation conditions were further optimized through the response surface design.The results showed that the optimal to prepare microcapsule were that the SA concentration was 1.5%(w/v),the CS concentration was 1.0%(w/v),the CaCl2 concentration was 2.0%(w/v),the curing temperature was 55 ? and the microcapsule has good surface morphology,the microcapsule of entrapment efficiency was 68.89% and drug-loading rate was 7.67%,the cumulative drug release rated was fast at beginning and then released slowly,the cumulative drug release rate was 83.9% in 24 h.2.The preparation and performance of pH response of complex microcapsule with sodium alginate/polyacrylic resin ? was preparation using the method of emulsification-solvent volatilization.The influence of preparation conditions,such as the concentration of sodium alginate,the concentration of polyacrylic resin?,the concentration of tinidazole and curing temperature and emulsifying time were optimized using single factor experiment.The characterization of the complex microcapsule,the encapsulation efficiency and drug-loading rate were investigated.Furthermore,the complex microcapsule preparation conditions were further optimized by the by the method of response surface design and the drug release properties and its performance were tested.The results showed that the optimal parameters to prepare complex microcapsule were that the SA concentration was 2.0%(w/v),the polyacrylic resin?concentration was 3.0%(w/v),the tinidazole concentration was 0.05 g/ml(w/v),the curing temperature was 25 ?,the complex microcapsule has good surface morphology,the complex microcapsule of drug-loading rate was 8.78%.It could be seen that the tinidazole from the complex microcapsule had almost no release in dilute hydrochloric acid solution(pH 1.2)and released in PBS(pH 6.8),the cumulative drug release rate was 82.7% in 24 h,it has been achieved the pH response.3.The preparation and performance of the chitosan thermosensitive hydrogel encapsulating complex microcapsule: the hydrogel was preparation using physical crosslinking method.The preparation conditions were optimized using single factor experiment.The influence of concentration of chitosan,concentration of ??-glycerol and the diameter size of microcapsule were evaluated and the characterization of the hydrogel was investigated to screen the best parameters.Then the hrdrogel film was preparation using the optimal formulas.The results showed that the optimal formulas to prepare hydrogel film were that the CS concentration was 5.0%(w/v),the ??-glycerol concentration was 0.15% and the microcapsule size was 250 ?m.The phase change time of the chitosan hydrogel encapsulating complex microcapsule was 10 s.the swelling rate was 51.3%,130.1% and 79.4% within pH 1.2,pH 6.8 and pH 7.4,The moisture absorption of membranes was 53%,42% and 33% in different relative humidity 80 ± 2%,50 ± 2% and 30 ± 2% at 25 ± 1?.Comparing the different cumulative drug release rate the hydrogel was 75.2% in 24 h,lower than other cumnlative release rate.It has been seen that the sudden release of drugs to improve,and the mobility of microcapsule was decrease to achieve local drug delivery. |
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