Composition and microsphere for controlled-release of exendin, and method of preparing the same
一种组合物、微球的技术,应用在药物组合、非有效成分的医用配制品、含有效成分的医用配制品等方向,能够解决生物利用度变低、生物利用度不足、不能被应用等问题
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Embodiment 1
[0221] Preparation of microspheres containing Exenatide-4 by spray drying
[0222] 4.850 g of biodegradable polymer RG502H (Lot No. 1009848, IV=0.19 dL / g) and 0.150 g of Exenatide-4 (Polypeptide Laboratories, USA) were uniformly dissolved in 97 mL of glacial acetic acid. The solution prepared using a piston pump at a flow rate of 1.5 mL / min was charged into a spray dryer (SODEVA, France) with an ultrasonic nozzle (Sono-tek, 120 kHz) while supplying dry air at 180 °C to prepare Microspheres. The prepared microspheres were suspended in 0.5M lysine aqueous solution (preparation 1-1), suspended in 0.01M lysine aqueous solution (preparation 1-2), suspended in 0.1M histidine aqueous solution (preparation 1-3) and suspended in 0.5M arginine aqueous solution (preparation 1-4), wherein the solution contains 1% (W / V) polyvinyl alcohol (polyvinyl alcohol , Gohsenol, EG-50) as a protective colloid, collected after stirring for 3 hours, washed with distilled water and then lyophilized. ...
Embodiment 2
[0223] depends on the effect of the composition of different polymers
[0224] Exenatide-4-containing microspheres were prepared according to the same method as described in Example 1, the only difference being that the polymers used as biodegradable polymers were: RG503H (Lot No.1006370, IV=0.38 dL / g, formulations 2, 2-1 and 2-2), equal amounts of RG502H and RG503H (Lot No.1009848: Lot No.1006370=1:1, IV=0.29dL / g, formulations 3 and 3-1) Mixture, RG504H (Lot No. 1016605, IV = 0.51 dL / g, formulations 4 and 4-1), 5050DL2A (Lot No. LP-207, IV = 0.18 dL / g, formulations 5 and 5-1) and 5050DL 4A (Lot No. LP-206, IV=0.46 dL / g, formulations 6 and 6-1).
experiment Embodiment 1-1
[0225] Test the effect of microsphere coating layer
[0226] The content of Exenatide in the microspheres prepared in Examples 1 and 2 was quantitatively measured using the following method. Exenatide-4 (Polypeptide Laboratories, USA) was dissolved in DMSO (dimethyl sulfoxide), and diluted with DMSO to a concentration of 2, 5, and 10 μg / mL, respectively, the solution was used as a standard solution, and used A fluorescence photometer (Cary Eclipse, Varian, USA) was used for fluorescence measurement at Ex 280nm and Em 350nm to obtain a measurement curve. The prepared microspheres were dissolved in DMSO to a concentration of 150 μg / mL, and then the fluorescence measurement was also performed, and the exenatide content in the microspheres was measured by extrapolation from the above measurement curve.
[0227] The content of the coating material used in the composition of the present invention, specifically, the content of lysine, arginine, histidine, etc. contained on the surf...
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