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Progestin sustained-release microsphere and nanoparticle and preparation method thereof and progestin sustained-release injection

A technology for slow-release microspheres and progesterone, which can be used in pharmaceutical formulations, microcapsules, nanocapsules, etc., and can solve problems such as pain, inconvenience of progesterone injection, and induration at the injection site.

Inactive Publication Date: 2017-09-15
CHANGCHUN GENESCIENCE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And oily progesterone has a long half-life, and it usually takes several weeks to recover
Long-term high-frequency injections will also cause other symptoms such as induration at the injection site, which is not conducive to the health of the tissue at the injection site
The patients are all pregnant women, and it is extremely inconvenient to inject progesterone every day, and the presence of oil solvent in progesterone injection can easily cause problems such as muscle hardening and pain

Method used

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  • Progestin sustained-release microsphere and nanoparticle and preparation method thereof and progestin sustained-release injection
  • Progestin sustained-release microsphere and nanoparticle and preparation method thereof and progestin sustained-release injection
  • Progestin sustained-release microsphere and nanoparticle and preparation method thereof and progestin sustained-release injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] The preparation of embodiment 1 progesterone microspheres

[0067] Weigh 150mg PLGA (50 / 50 (the molar ratio of lactic acid and glycolic acid), molecular weight 13000 Daltons, the following examples represent the same as Example 1), 75mg progesterone, and dissolve in 1.5mL methylene chloride to form an organic phase. The organic phase was quickly poured into 25 mL of 1% PVA (Kuraray Japan) solution, and the o / w emulsion was formed by high-speed shearing at 12000 rpm for 2 min. After diluting with 5 times the volume of water, distill under reduced pressure at 40°C for 15 minutes to volatilize the organic solvent to solidify the microspheres. After the solidified microspheres are washed with deionized water to excess PVA, the microspheres are collected by centrifugation and freeze-dried to obtain progesterone controlled-release microspheres for intramuscular injection.

[0068] Among them, the freeze-drying process includes: pre-freezing at -40°C for four hours, vacuuming...

Embodiment 2-4

[0072] Embodiment 2-4 Different molecular weight PLGA prepares microsphere

[0073] Weigh 150mg of PLGA (50 / 50) with molecular weights of 13,000, 25,000, and 30,000 Daltons; 75mg of progesterone were dissolved in 1.5mL of dichloromethane to form an organic phase. The organic phase was quickly poured into 25 mL of 1% PVA solution, and was sheared at 12000 rpm for 2 min to form an o / w emulsion. After diluting with 5 times the volume of water, distill under reduced pressure at 40°C for 15 minutes to volatilize the organic solvent to solidify the microspheres. After the solidified microspheres are washed with deionized water to excess PVA, the microspheres are collected by centrifugation and freeze-dried to obtain progesterone controlled-release microspheres for intramuscular injection. The prescription among the embodiment 2-4 is referring to table 2:

[0074] The prescription in the embodiment 2-4 of table 2

[0075]

Embodiment 5-7

[0076] Example 5-7 Preparation of microspheres with different theoretical drug loads

[0077] Weigh 150mg of PLGA (50 / 50; 13000), weigh 75mg, 90mg, and 100mg of progesterone, and dissolve in 1.5mL of dichloromethane to form an organic phase. The organic phase was quickly poured into 25 mL of 1% PVA solution, and was sheared at 12000 rpm for 2 min to form an o / w emulsion. After diluting with 5 times the volume of water, distill under reduced pressure at 40°C for 15 minutes to volatilize the organic solvent to solidify the microspheres. After the solidified microspheres are washed with deionized water to excess PVA, the microspheres are collected by centrifugation and freeze-dried to obtain progesterone controlled-release microspheres for intramuscular injection. See Table 3 for the theoretical drug loading of the progesterone microspheres prepared in Examples 5-7:

[0078] Theoretical drug loading of the progesterone microspheres prepared by table 3 embodiment 5-7

[0079] ...

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Abstract

The invention provides a progestin sustained-release microsphere and nanoparticle and a preparation method thereof and a progestin sustained-release injection. The preparation provided by the invention comprises progestin and biodegradable polymers PLGA, PLA, PCL and PGA; and the progestin microsphere is prepared by adopting an emulsion-solvent evaporation method and the progestin nanoparticle is prepared by adopting a nano-emulsification method in the process aspect. According to the prepared microsphere, the particle size is within a range of 10-20 microns, the drug loading capacity is 30-40% and the encapsulation efficiency is greater than 90%; and according to the nanoparticle, the particle size is within a range of 100-400nm, the drug loading capacity can reach 10-20% and the encapsulation efficiency is 80-90%. The progestin preparation requires frequent administration for multiple times; and the sustained-release injection has good correlation in vivo and vitro, the sustained-release effect of more than a week is reached, the medication compliance of a patient can be improved, and the living quality is improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a progesterone sustained-release microsphere and a preparation method thereof, a progesterone sustained-release nanoparticle and a preparation method thereof, and a progesterone sustained-release injection. Background technique [0002] Habitual abortion refers to ≥3 consecutive spontaneous abortions, the cause of which is not completely clear, which brings great psychological harm to the patient. There are many and complicated causes of recurrent miscarriage, including immune factors, genetics, and endocrine disorders, which bring certain difficulties to clinical treatment. According to relevant practice studies, the corpus luteum insufficiency in patients suffering from this disease is 24%-68%. For the occurrence of luteal phase defect, researchers mostly believe that it is due to the use of gonadotropin-releasing hormone agonist (GnRHa) for down-regulation in most IVF cycles...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/51A61K9/50A61K31/57A61K47/34A61P15/06
CPCA61K9/5153A61K9/0002A61K9/0019A61K9/5031A61K31/57
Inventor 金磊唐星张士权徐万国王世曼
Owner CHANGCHUN GENESCIENCE PHARM CO LTD
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