| In order to obtain a kind of convenient oral dosage forms of protein, which can be absorbed fully and is efficient and safe, the medicament microcapsules of thymopeptide are prepared by using several different methods and vesicle materials. Thymopeptide- polylactic acid microsphere is prepared by duplicate-latices method and polylactic acid is used as shell. Thymopeptide- gelatin microsphere is prepared by emulsification chemical-crossline method and gelatin is used as shell. Thymopeptide- ethylcellulose microcapsule is prepared by Intra-liquid desiccation method and ethylcellulose is used as shell. The form of the medicament microcapsules of thymopeptide are proved by DTA, and the thymopeptide content and package ratio of medicament microcapsules of thymopeptide and drug release in vitro are calculated by measuring particle size and size distribution, and by measuring the medicament content. And stability of the microcapsule is also measured. The influence of several factors on the surface conformation of the microcapsule and the sustained effect of the medicament are discussed synthetically. Orthogonal design is used to optimize the technology of preparation. The microcapsule which can be used to improve the bioavailability and curative effect of thymopeptide is prepared. The optimal preparation technology of the thymopeptide- polylactic acid microsphere prepared by duplicate-latices method are that concentration of polylactic acid is 5.5%(w), ratio of water phase to oil phase is 1/10, concentration of thymopeptide in the water phase is 1%(W), mix speed in the elementary latex is 950 r·min-1, concentration of emulsion is 0.8%(w), temperature in the ultrasonic emulsification is 15℃, emulsification time is 5min, volatilization time is 5h, and concentration of gelatin in the external water phase is 0.5%(w). Thymopeptide- polylactic acid microsphere is ecru, the average arithmetic granularity diameter is 13.82μm, and package ratio of thymopeptide- polylactic acid microsphere is 80.67%. Relation between the prophase average cumulate release quantity and the square root of time is linear. The drug release in vitro can be described by model of Higuchi equation, Q=2.47277+20.34687 t1/2(r=0.996,n=10,P<0.0001),with the T1/2 in vitro is 295min.The optimal preparation technology of the thymopeptide- gelatin microsphere prepared by emulsification chemical-crossline method are that concentration of gelatin solution is 12.5%(w), ultrasonic emulsification time is 4 min, mix speed is 800 r·min-1, quantity of emulsion is 0.5g, and quantity of water used to dissolve 0.1g thymopeptide is 5ml. Thymopeptide- gelatin microsphere is flaxen, the average arithmetic granularity diameter is 14.66μm, and package ratio of thymopeptide- gelatin microsphere is 80.44%. Relation between the prophase average cumulate release quantity and the square root of time is linear. The drug release in vitro can be described by model of Higuchi equation, Q=1.52591+30.0096 t1/2(r=0.993,n=11,P<0.0001),with the T1/2 in vitro is 130 min. The anaphase release speed becomes slower, and terminal eroding phenomena is present with the complete eroding of the microsphere framework.The optimal preparation technology of the thymopeptide- ethylcellulose microcapsule prepared by Intra-liquid desiccation method are that concentration of ethylcellulose solution is 2.55% (w), mix speed is 950 r·min-1, volatilization temperature is 35℃, mass ratio of ethylcellulose to thymopeptide medicament is 2/1, and concentration of dispersant is 1.5 %(w). Thymopeptide- ethylcellulose microcapsule is ecru, and the average arithmetic granularity diameter is 52.95μm, and package ratio of thymopeptide- gelatin microsphere is 79.83%. Relation between the prophase average cumulate release quantity and the square root of time is linear. The drug release in vitro can be described by model of Higuchi equation, Q=6.8859+34.8291 t1/2 (r=0.994,n=10,P<0.0001), with the T1/2 in vitro is 80 min. The anaphase release speed becomes slower, and terminal eroding phenomena is present w...
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