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Sirolimus sustained-release microsphere for injection and preparation method of sirolimus sustained-release microsphere

A technology of slow-release microspheres and sirolimus, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve the problem of low encapsulation efficiency and failure to meet the requirements of the Pharmacopoeia, etc. Problems, to achieve the effect of suitable particle size, avoiding adverse drug reactions, and improving drug bioavailability

Pending Publication Date: 2021-05-14
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is reported in the literature that polyhydroxypentylbutyrate (PHBV) was used as a carrier to prepare sirolimus-PHBV microspheres with a particle size of 186.73 (±12.62) nm and an in vitro drug release period of 7 days, which has a certain effect on lymphocyte proliferation. Inhibitory effect, but the encapsulation rate is only 73%, which does not meet the requirements of the Pharmacopoeia (Liu Wei et al., Preparation of sirolimus sustained-release microspheres and research on its inhibitory effect on lymphocyte proliferation, Chinese Journal of Clinical Pharmacology, 2017, Issue 10, pp. 933-935)

Method used

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  • Sirolimus sustained-release microsphere for injection and preparation method of sirolimus sustained-release microsphere
  • Sirolimus sustained-release microsphere for injection and preparation method of sirolimus sustained-release microsphere
  • Sirolimus sustained-release microsphere for injection and preparation method of sirolimus sustained-release microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] prescription:

[0051]

[0052] Preparation steps:

[0053] 1) Weigh the prescribed amount of sirolimus and PLGA, add to the mixed solvent system (8ml) of propylene carbonate and ethyl acetate, stir and dissolve, and prepare solution 1;

[0054]2) Weigh the prescribed amount of PVA into 500ml of water for injection (100°C), stir until dissolved, cool the PVA solution to 25°C, add water for injection to 800ml, and make a 3mg / mL PVA solution;

[0055] 3) Slowly add solution 1 to 3mg / mL PVA solution, homogeneously emulsify at 1500rpm for 1min;

[0056] 4) After the emulsification is over, turn on the mechanical stirring to evaporate the solvent, and stop stirring after 3 hours;

[0057] 5) Filter the obtained microsphere suspension through a 120-mesh sieve to collect the microspheres, rinse the microspheres with water for injection 3 times, transfer to a petri dish, and freeze-dry in a freeze dryer;

[0058] 6) The freeze-dried product is sieved through a 120-mesh si...

Embodiment 2

[0064] prescription:

[0065]

[0066]

[0067] Preparation steps:

[0068] 1) Weigh the prescribed amount of sirolimus and PLGA, add to the mixed solvent system (8ml) of isopropanol and dichloromethane, stir and dissolve, and prepare solution 1;

[0069] 2) Weigh the prescribed amount of PVA into 500ml of water for injection (100°C), stir until dissolved, cool the PVA solution to 25°C, add water for injection to 800ml, and make a 30mg / mL PVA solution;

[0070] 3) Slowly add solution 1 to 30mg / mL PVA solution, homogeneously emulsify at 1500rpm for 1min;

[0071] 4) After the emulsification is over, turn on the mechanical stirring to evaporate the solvent, and stop stirring after 3 hours;

[0072] 5) Filter the obtained microsphere suspension through a 120-mesh sieve to collect the microspheres, rinse the microspheres with water for injection 3 times, transfer to a petri dish, and freeze-dry in a freeze dryer;

[0073] 6) The freeze-dried product is sieved through a 12...

Embodiment 3

[0079] prescription:

[0080]

[0081] Preparation steps:

[0082] 1) Weigh the prescribed amount of sirolimus and PLGA, add to the mixed solvent system (8ml) of benzyl alcohol and dichloromethane, stir and dissolve, and prepare solution 1;

[0083] 2) Weigh the prescribed amount of PVA and add it to 500ml water for injection (100°C), stir until dissolved, cool the PVA solution to 25°C, add water for injection to 800ml, and make 8mg / mL PVA solution;

[0084] 3) Slowly add solution 1 to 8mg / mL PVA solution, homogeneously emulsify at 1500rpm for 1min;

[0085] 4) After the emulsification is over, turn on the mechanical stirring to evaporate the solvent, and stop stirring after 3 hours;

[0086] 5) Filter the obtained microsphere suspension through a 120-mesh sieve to collect the microspheres, rinse the microspheres with water for injection 3 times, transfer to a petri dish, and freeze-dry in a freeze dryer;

[0087] 6) The freeze-dried product is sieved through a 120-mesh ...

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Abstract

The invention belongs to the technical field of drug sustained-release preparations, and particularly discloses sirolimus sustained-release microspheres for injection and a preparation method of the sirolimus sustained-release microspheres. The sirolimus sustained release microsphere for injection is prepared from the following components in percentage by weight: 5 to 50 percent of sirolimus and 50 to 95 percent of lactide-glycolide copolymer. In the invention, the microspheres are prepared by adopting a mixed solvent system intervened O / W single emulsification-solvent volatilization method. Compared with the prior art, the invention has the following advantages: (1) the drug release period of the drug is prolonged, and the drug administration frequency of the drug is obviously reduced; (2) the release of the medicine is effectively promoted, the accumulative release amount is up to 95%, the bioavailability of the medicine is greatly improved, and the administration dosage of the medicine is reduced; and (3) the method has the advantage of process amplification, industrial production process parameters are not obviously changed, and industrial reproducibility is easy to realize.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and in particular relates to a sirolimus sustained-release microsphere for injection and a preparation method thereof. Background technique [0002] As a potent immunosuppressant, sirolimus is clinically used to prevent rejection after organ transplantation and to treat autoimmune diseases. Inside the cell, sirolimus binds to immunophilins (FK-binding protein-12, FKBP-12), generating an immunosuppressive complex. This complex has no effect on calcineurin activity, but binds to and inhibits the mammalian target of sirolimus (mTOR, a key regulatory kinase); this inhibition represses the The progression from G1 phase to S phase inhibits the activation of T lymphocytes and proliferation of T cells stimulated by antigens and cytokines (interleukin [IL]-2, IL-4, and IL-15). [0003] Sirolimus is a class of macrolide antibiotics, molecular formula: C 51 h 79 NO 13 , rela...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/34A61K31/436A61P37/06
CPCA61K9/5031A61K9/5089A61K9/0019A61K31/436A61P37/06
Inventor 张贵民杜丽平周苗苗
Owner LUNAN PHARMA GROUP CORPORATION
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