Progesterone slow-release nanoparticles, preparation method of progesterone slow-release nanoparticles and progesterone slow-release injection

A technology of progesterone and nanoparticles, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Oily progesterone has long half-life and other problems, and achieves the effect of maintaining effective blood drug concentration, good patient compliance, high drug loading and encapsulation efficiency

Active Publication Date: 2017-12-08
CHANGCHUN GENESCIENCE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
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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
[0008] In traditional sustained-release preparations, microspheres have always been the most commonly used dosage form, because traditional nanoparticles, due to their small particle size, can easily attract phagocytic cells after intramuscular injection, thereby engulfing them, although compared with microspheres The bioavailability of nanoparticles is higher, but for this reason it is difficult for nanoparticles to achieve long-term effects

Method used

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  • Progesterone slow-release nanoparticles, preparation method of progesterone slow-release nanoparticles and progesterone slow-release injection
  • Progesterone slow-release nanoparticles, preparation method of progesterone slow-release nanoparticles and progesterone slow-release injection
  • Progesterone slow-release nanoparticles, preparation method of progesterone slow-release nanoparticles and progesterone slow-release injection

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preparation example Construction

[0047] The present invention also provides a preparation method of progesterone sustained-release nanoparticles, comprising the following steps:

[0048] 1) dissolving the progesterone and the polymer in an organic solvent to form an organic phase;

[0049] 2) Pour the organic phase obtained in step 1) into an aqueous solution containing an emulsifier, and undergo high-speed (6000rpm-10000rpm) shear emulsification to obtain an oil-in-water primary emulsion; subject the oil-in-water primary emulsion to high pressure ( 600bar~800bar) homogenize to obtain the final emulsion;

[0050] 3) After diluting the final emulsion obtained in step 2) with water, solidify at low temperature (0-5° C.) to obtain a suspension of particles;

[0051] 4) After the microparticle suspension obtained in step 3) is removed by tangential flow to remove the organic solvent and free drug, the progesterone sustained-release nanoparticles are obtained.

[0052] In order to achieve the above purpose, the ...

Embodiment 13

[0098] The pharmacokinetic analysis of embodiment 13 progesterone long-acting preparation of the present invention

[0099] The progesterone nanoparticles of 2.08mg (calculated as progesterone) prepared according to the method of Example 2 are intramuscularly injected into the hind leg biceps femoris of SD rats (about 200g of body weight), and commercially available oil solution and The common progesterone nanoparticles prepared in Comparative Example 1 were used as a control test. The solvent for injection in the sustained-release preparation of the present invention is the nanoparticle reconstitution agent for injection, and its composition is 0.9% sodium chloride water for injection.

[0100] Blood was collected from the venous plexus behind the eyes of the rats regularly, and the drug concentration of progesterone in plasma was determined by establishing an LC-MS method. See the blood concentration of administration 0-196h figure 1 , figure 1 It is the concentration cur...

Embodiment 14

[0116] Embodiment 14 progesterone long-acting preparation characteristic test

[0117] external assessment. The progesterone nanoparticles prepared in the above-mentioned comparative example 1 and embodiment 2 were observed under a transmission electron microscope, and the results can be found in Figure 5 and Figure 6 . Figure 5 The transmission electron microscope image (TEM) of the PEG-modified progesterone nanoparticles prepared for the embodiments of the present invention, Figure 6 Transmission electron micrograph (TEM) of traditional progesterone nanoparticles prepared for Comparative Example 1 of the present invention. It can be seen from the above results that the nanoparticles prepared in Example 2 of the present invention and Comparative Example 1 are regular and circular, and the particle diameters are equivalent.

[0118] Drug loading: Precisely measure 10 mg of the nanoparticles prepared in the above examples, put them in a 25 mL volumetric flask, add 1 mL ...

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Abstract

The invention provides progesterone slow-release nanoparticles modified by PEG, a preparation method of the progesterone slow-release nanoparticles and a progesterone slow-release injection. A preparation provided by the invention comprises progesterone and biodegradable polymers PLGA, PLA, PCL, PGA and the like; in the process aspect, a nanoemulsion method is adopted to prepare the progesterone nanoparticles. According to the nanoparticles prepared by the preparation method disclosed by the invention, a particle size is in a range of 100 to 400nm, a drug-loading rate can reach 1% to 10%, and encapsulation efficiency is 80% to 100%. A progesterone listed preparation needs to be repeatedly and frequently administrated, but the progesterone slow-release injection provided by the invention has a higher biological utilization degree than market preparations and conventional progesterone nanoparticles, and reaches not less than one week of slow-release effect; compliance of medicine use of a patient can be improved; life quality is improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to progesterone sustained-release nanoparticles, a preparation method thereof and 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, and GnRha causes pituitary suppression, which makes the recovery of pituitary functi...

Claims

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Application Information

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