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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 non-active ingredients, medical preparations containing active ingredients, and drug delivery. Problems such as low concentration and ineffective curative effect

Inactive Publication Date: 2011-11-23
SHANGHAI INST OF PHARMA IND CO LTD +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 present invention provides a method for preparing the sustained-release microspheres, which comprises the steps of: (a) mixing and dissolving nomegestrol acetate or its analog, 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 present invention adopts the alloy skeleton method to prepare the above-mentioned sustained-release microspheres. "Polymer-alloys Method" refers to a technique in which one polymer phase is dispersed in a solid mixture of another polymer phase. Under certain conditions, the two polymers can be automatically separated into two solutions in organic solvents. Taking polylactic acid (PLA) and polylactic-glycolic acid...

Embodiment 1

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

Embodiment 2

[0103] 800 mg of polyDL-lactide-glycolide (PLCG75 / 25, ester-terminated, 10 kD, purchased from Shandong Institute of Medical Devices) was dissolved in 2.5 ml of acetonitrile, and 200 mg of nomegestrol acetate was added. Stir to dissolve. as the internal oil phase (O 1 phase); in 30ml liquid paraffin, add 1.5% Span80, and mix it as the outer oil phase (O 2 Mutually). At 3000rpm, turn O 1 drop O 2 , make it O 1 / O 2 Emulsion. The temperature of the system was controlled, and the organic solvent in the dispersed phase was gradually evaporated to dryness in a constant temperature water bath at 30°C. The suspension was centrifuged, and the supernatant was removed. The microspheres were washed several times with hexane and dried under reduced pressure at room temperature. That's it.

[0104] The obtained microspheres are observed under a microscope, the spherical shape is round, the particle size is between 20-150 μm, and the average particle size is about 100 μm. The drug c...

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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 for treating endometriosis and / or contraception or its analogs, and preparation methods and uses thereof . Background technique [0002] Nomegestrol acetate is a synthetic 17α-hydroxy-19-nor-progesterone derivative, which is a second-generation progestin contraceptive. The chemical name is 17α-acetoxy-6-methyl-19-norpregna-4,6-dien-3,20-dione, as shown in formula I. It is also clinically suitable for the treatment of diseases caused by luteal insufficiency, such as menstrual disorders, dysmenorrhea, endometriosis, premenstrual syndrome, breast pain, menopausal syndrome, etc., with definite curative effect. [0003] [0004] Nomegestrol can specifically bind to progesterone receptors, which can reduce the occurrence of side effects; and Nomegestrol has no estrogenic activit...

Claims

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Application Information

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Patent Type & Authority Patents(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 CO LTD
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