Pharmaceutical composition containing non-T cell binding peptide and lactic acid glycolic acid block copolymer, its preparation method and use
A lactic acid glycolic acid block and composition technology, applied in the field of biological preparations, can solve the problems of short half-life, poor stability, and short half-life in vivo, and achieve complete drug release, good stability, high drug loading and encapsulation efficiency Effect
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Embodiment 1
[0076] Example 1 Preparation of Microspheres by Phase Separation
[0077] Dissolve 300 mg of PLGA with a molecular weight of 9000 (wherein the mass ratio of PLA:PGA is 50:50) in 2 ml of an organic solvent (dichloromethane) to prepare an oil phase, add 10 mg of non-T cell binding peptide powder to the above oil phase, and use High-speed mixer 30000r / min to homogenize it for 60s to form S / O suspension, 4ml of silicone oil was added dropwise to the S / O suspension, and a magnetic stirrer was used to stir at low speed at 300rpm during the dropwise addition. , add 70ml of n-heptane to the emulsion, stir at a low speed of 300rpm for 30min to solidify the microspheres, and collect the microspheres.
[0078] The obtained composition has an average particle size of 60.7 μm, an encapsulation rate of 80.3%, a drug load of 4.2%, a burst release rate of 18.2%, and can be stably released in vitro for 20 days, with a total drug release amount of 85.5%.
Embodiment 2
[0079] Example 2 Preparation of Microspheres by Phase Separation
[0080] Dissolve 300mg of PLGA with a molecular weight of 13000 (wherein the mass ratio of PLA:PGA is 50:50) in 2ml of an organic solvent (the volume ratio of dichloromethane and acetone is a mixture of 75:35) to make oil phase, and take 40mg The non-T cell-binding peptide powder was added to the above oil phase, and it was homogenized for 240s with a high-speed mixer at 20000r / min to form an S / O suspension. 6ml of silicone oil was added dropwise to the S / O suspension. During the dropping process Use a magnetic stirrer to stir at a low speed of 300 rpm. After the dropwise addition is completed, add 180 ml of n-heptane to the emulsion, stir at a low speed of 300 rpm for 30 min to solidify the microspheres, and collect the microspheres.
[0081] The obtained composition has an average particle size of 69.0 μm, an encapsulation rate of 75.3%, a drug load of 3.8%, a burst release rate of 15.2%, and can be stably r...
Embodiment 3
[0083] Example 3 W / O / W double emulsification solvent evaporation method
[0084] 10mg of non-T cell binding peptide powder was dissolved in 0.2ml of 0.3M glycine-sodium hydroxide buffer (pH 10.0), and added to 2ml of PLGA with a concentration of 150mg / ml and a molecular weight of 9000 (wherein the mass of PLA:PGA was The ratio is 50:50) in the dichloromethane solution, emulsified for 120s with a high-speed mixer at a stirring rate of 24000r / min to obtain a W / O primary emulsion; the emulsion was injected into 200ml containing 2% polymer with a pipette. In the 0.02M phosphate buffer (pH7.4) of vinyl alcohol, stir at 500rpm for 1min to prepare a W / O / W emulsion, add 200ml of 0.02M phosphate buffer (pH5.8) to the emulsion, at room temperature Stir at 300 rpm for 6 h, volatilize the organic solvent, collect the microspheres by centrifugation after solidification, wash with double distilled water three times, and freeze-dry according to a conventional method to obtain a non-T cell...
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