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Sustained-release microsphere of nomegestrol acetate of analogs thereof and preparation method and application thereof

A technology of nomegestrol acetate and sustained-release microspheres, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, and drug delivery, and can solve drug side effects, unreasonable drug release modes, low blood drug concentration

Inactive Publication Date: 2009-12-30
SHANGHAI INST OF PHARMA IND +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The microspheres prepared by this method can slowly release the drug for one month. Although the drug encapsulation rate is good, the release mode is not reasonable: (1) The microspheres have a large burst release effect on the first day, and the blood drug concentration Higher (up to 27-35ng / ml), leading to side effects of the drug on the body, (2) followed by a long period of time (about 6 days) of approximate drug release stagnation, during which the blood drug concentration is relatively high Low (approximately 6-10ng / ml), which may cause the problem of ineffective efficacy

Method used

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  • Sustained-release microsphere of nomegestrol acetate of analogs thereof and preparation method and application thereof
  • Sustained-release microsphere of nomegestrol acetate of analogs thereof and preparation method and application thereof
  • Sustained-release microsphere of nomegestrol acetate of analogs thereof and preparation method and application thereof

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preparation example Construction

[0081] The invention provides a preparation method of the sustained-release microspheres, the method comprising the steps of: (a) mixing and dissolving nomegestrol acetate or its analogues, a biodegradable polymer and an organic solvent to prepare a dispersed phase; (b) adding the dispersed phase obtained in step (a) to the continuous phase, mixing and stirring to obtain an emulsion; and (c) heating and evaporating to remove the organic solvent in the emulsion obtained in step (b) to obtain the emulsion of the present invention Slow-release microspheres.

[0082] The invention adopts the alloy skeleton method to prepare the above-mentioned slow-release microspheres. "Polymer-alloys Method" refers to a technique in which one polymer phase is dispersed in another polymer phase as a solid mixture. Under certain conditions, the two polymers can automatically separate into two solutions in an organic solvent. Taking polylactic acid (PLA) and polylactic-glycolic acid (PLGA) as exa...

Embodiment 1

[0100] Dissolve 160mg of polylactic-glycolic acid (PLGA75 / 25, carboxyl-terminated, 14kD, purchased from Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences) in 0.5ml of ethyl acetate, add 40mg of nomegestone acetate, and stir to form a clear solution. Add 5ml of 1% PVPk-30 aqueous solution saturated with ethyl acetate, homogenize with 4000rpm, the gained emulsion is transferred to a flat-bottomed beaker with a stirring paddle containing a large amount of distilled water, keep constant temperature (30°C), and stir for 4 hours with 200rpm rotating speed, The organic solvent in the o / w emulsion was gradually evaporated to dryness. Sampling and microscopic inspection were carried out continuously during the whole process to observe the formation process of microspheres at each stage. The above solution is centrifuged, the supernatant is poured off, the microspheres are collected under reduced pressure on a filter membrane, washed with a small amount of distilled wa...

Embodiment 2

[0103] Dissolve 800 mg of poly DL lactide-glycolide (PLCG75 / 25, ester-terminated, 10 kD, purchased from Shandong Institute of Medical Devices) in 2.5 ml of acetonitrile, and add 200 mg of nomegestone acetate. Stir to dissolve. As the internal oil phase (O 1 phase); in 30ml liquid paraffin, add 1.5% Span80, after mixing as the outer oil phase (O 2 Mutually). At 3000rpm, the O 1 drop into O 2 In, make O 1 / O 2 emulsion. Control the temperature of the system, and gradually evaporate the organic solvent in the dispersed phase to dryness in a constant temperature water bath at 30°C. The suspension is centrifuged, and the supernatant is removed. The microspheres are washed with a small amount of hexane several times, and dried at room temperature under reduced pressure. Instantly.

[0104] Obtained microspheres are observed under a microscope, the spherical shape is round, the particle diameter is between 20-150 μm, and the average particle diameter is about 100 μm. The dru...

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Abstract

The invention discloses a sustained-release microsphere to achieve the aims of contraception and long-term treatment of endometriosis uterine, which comprises the following components: (1) nomegestrol acetate or analogs thereof, and (2) a biodegradable polymer, wherein the weight ratio of an ester-terminated polymer to a carboxyl-terminated polymer is between 1:0.01-1:1; the ester-terminated polymer is selected from polylactide-glycolide, polylactide, poly-beta-hydroxybutyrate, poly ortho ester, polycaprolactone, poly-phosphate, polyanhydride, or poly-cyanoacrylate; the carboxyl-terminated polymer is selected from polyglycolic acid and polylactic acid-glycolic acid; and the weight of the nomegestrol acetate or the analogs thereof accounts for 5 to 80 percent of the total weight of the microsphere. The invention also discloses a preparation method and application of the sustained-release microsphere.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to injectable sustained-release long-acting microspheres containing nomegestrol acetate or its analogs for treating endometriosis and / or contraception, and their preparation methods and uses . Background technique [0002] Nomegestrol acetate is a synthetic 17α-hydroxy-19-nor-progesterone derivative, which is the second-generation progestin contraceptive. The chemical name is 17α-acetoxy-6-methyl-19-norpregna-4,6-diene-3,20-dione, as shown in formula I. Clinically, it is also suitable for the treatment of diseases caused by insufficient corpus luteum function, such as menstrual disorders, dysmenorrhea, endometriosis, premenstrual syndrome, breast pain, menopausal syndrome, etc., with definite curative effect. [0003] [0004] Nomegestone can specifically bind to progesterone receptors, which can reduce the occurrence of side effects; and nomegestone has no es...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/14A61K31/57A61K47/30A61P15/00
Inventor 肖莉莉陈庆华马骊曹霖包泳初朱焰潘峰赵炎龙李坤
Owner SHANGHAI INST OF PHARMA IND
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