Method for controlling release of active ingredients of microspheres
A technology of active ingredients and microspheres, applied in the field of controlling the release of active ingredients in microspheres, can solve the problems of changes in the dissolution of pharmaceutical active ingredients, aggravating the uptake of water in the microspheres, and reducing the pH value inside the microspheres, achieving good reproducibility, To achieve the effect of release control
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Embodiment 1
[0023] (1) Preparation of refined copolymer: Weigh 20 g of lactide-glycolide copolymer (7525) (batch number: L00020601311) (the oligomer content has been detected to be greater than 10%), add 20 ml of acetone and stir to dissolve, after the solution is clarified , slowly poured into 2L mixed solution (20% acetone: 30% methanol: 50% water), let stand, discard the supernatant, wash the precipitate with water twice, and place the precipitate in the lower layer to dry under vacuum with phosphorus pentoxide desiccant Dry in vacuum for 48 hours. That is, 7g of purified copolymer is obtained, and the content of oligomer in the purified copolymer should be controlled below 10%, and if the content of oligomer is greater than 10%, step (1) is repeated for further purification until the content of oligomer is less than 10%.
[0024] (2) Detection of oligomers in the copolymer: Accurately weigh 60.11 mg of the purified lactide-glycolide copolymer (7525) (batch number: L00020601311-01), ad...
Embodiment 2
[0042] The comparison of the release degree before and after the purification of the copolymer of Example 2:
[0043] In order to verify the feasibility of the method described in Example 1, the following verifications were carried out. The four samples listed in the following (1)-(4) were prepared in sequence:
[0044] (1) Unrefined copolymer.
[0045] (2) One-time purification of copolymer: Weigh 100 g of lactide-glycolide copolymer (7525) (batch number: L00020601312), add 20 ml of acetone and stir to dissolve, after the solution is clarified, slowly pour it into 5 L of mixed solution (20% acetone) : 30% methanol: 50% water), let stand, discard the supernatant, wash the precipitate with water twice, and place the precipitate in a vacuum desiccator with phosphorus pentoxide desiccant in the lower layer for 48 hours. That is, 60 g of purified copolymer was obtained.
[0046] (3) Secondary refined copolymer: Weigh 30 g of primary refined copolymer (7525), add 20 ml of aceton...
Embodiment 3
[0059] (1) Preparation of refined copolymer: Weigh 20 g of polylactic acid (batch number: 0002064569), add 20 ml of acetone and stir to dissolve, after the solution is clarified, slowly pour it into 2 L of mixed solution (20% acetone: 30% methanol: 50% water) ), let stand, discard the supernatant, wash the precipitate with water twice, and place the precipitate in a vacuum desiccator with a phosphorus pentoxide desiccant in the lower layer for 48 hours of vacuum drying. That is, 7g of purified copolymer is obtained, and the oligomer content in the purified copolymer should be controlled between 5% and 10%, and if it is greater than 10%, repeat step (1) for further purification, until the oligomer content is between 5% and 10%. .
[0060] (2) Detection of oligomers in the copolymer: Accurately weigh 60.24 mg of purified polylactic acid, add 2 ml of acetone to dissolve, then add 2 ml of methanol, centrifuge at 9500 rpm for 10 minutes, absorb the supernatant, add 2 ml of methanol...
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