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Drug sustained-release composition and preparation method

A sustained-release composition and drug technology, which is applied in drug combinations, pharmaceutical formulations, antineoplastic drugs, etc., can solve the problems of poor uniformity of microspheres and drug loading, low drug loading and encapsulation efficiency, and reduce economic burden , Stable physical and chemical properties, good stability effect

Active Publication Date: 2021-12-07
北京博恩特药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the microspheres prepared by the prior art can realize the sustained release of polypeptide drugs, the uniformity of the microspheres and drug loading is poor, and the drug loading and encapsulation efficiency are low

Method used

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  • Drug sustained-release composition and preparation method
  • Drug sustained-release composition and preparation method
  • Drug sustained-release composition and preparation method

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preparation example Construction

[0050] The second aspect of the present invention provides a preparation method of the drug sustained-release composition, sometimes referred to herein as "the preparation method of the present invention", which is a method using foaming and jet milling techniques. Specifically, the preparation method of the present invention at least includes the following steps:

[0051] (1) disperse triptorelin acetate dry powder in the solution of fat-soluble polymer to obtain dispersion liquid, wherein the concentration of solvent in the solution is 50% by weight-90% by weight;

[0052] (2) reducing the concentration of the solvent in the dispersion to 5% by weight to 25% by weight to obtain a concentrated solution;

[0053] (3) Foaming the concentrated solution to remove the solvent under negative pressure to obtain a foamed coagulation;

[0054] (4) Preliminary crushing of the foamed coagulum to obtain a coarse powder, and then secondary crushing by jet milling to form a fine powder; a...

Embodiment 1

[0068] Weigh 50 mg (1.5%) of triptorelin acetate into a 30 ml vial, add 2 ml of purified water to fully dissolve, rapidly cool and freeze in liquid nitrogen, and freeze dry in a lyophilizer. Add high molecular polymer (PLGA / PLA) 2g (65.5%) in vial (high molecular polymer (PLGA / PLA) model sees Table 1, and different models represent the mass ratio of different lactic acid and glycolic acid, the same below The greater the number followed by the letter under the ratio, the greater the molecular weight and the greater the viscosity of the polymer), 5ml of dichloromethane, sealed with a sealing plug, and mixed at a high speed for 20 minutes on the suspension instrument at a speed of 2500rpm, cooled for 30 minutes, and repeated mixing for 3 times Shake overnight at 25°C.

[0069] Use an ultrasonic cell pulverizer to pulverize the suspension, with a power of 200 watts, ultrasonic for 20s, intermittent for 20s, and work for 10 minutes. Use an ice-water mixture to cool down the bottle ...

Embodiment 2-13

[0071] The pharmaceutical composition was prepared in a similar manner to Example 1 except that the composition of each component was changed as shown in Table 1.

[0072] Table 1 Compositions prepared by different types of high molecular polymers

[0073]

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Abstract

The invention discloses a medicine slow-release composition and a preparation method. The drug sustained-release composition of the present invention is a granular composition obtained by foaming and jet milling techniques, which comprises 60-80 parts by weight of a fat-soluble polymer, 1-10 parts by weight of a hydrophilic polypeptide drug and 25-35 parts by weight. parts by weight of mannitol. Wherein, the fat-soluble high molecular polymer is a porous solid particle, the hydrophilic polypeptide drug is embedded in the inside of the fat-soluble high molecular polymer, and the mannitol is in powder form and mixed with the fat-soluble high molecular polymer to form a composition.

Description

technical field [0001] The invention relates to the field of drug sustained release, in particular to a hydrophilic drug, especially a sustained release composition of triptorelin acetate and a preparation method thereof. Background technique [0002] Triptorelin is a synthetic gonadotropin-releasing hormone analog, which can be effectively used for prostate cancer, endometriosis, precocious puberty and other diseases. Conventional triptorelin preparations have short biological half-life, poor preparation stability, difficulty in absorption after oral administration, and severe side effects after taking the medicine. [0003] Microspheres refer to tiny spherical entities formed by dissolving or dispersing drugs in the matrix of polymer materials. The common particle size is generally between 1-500 μm, which belongs to matrix-type skeleton particles. The research on its use as a drug carrier began in the mid-1970s. After the drug was made into microspheres, it has become a n...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/26A61K47/34A61K38/09A61P15/08A61P15/00A61P35/00
CPCA61K9/19A61K38/09A61K47/26A61K47/34A61P15/00A61P15/08A61P35/00
Inventor 郭光明王玉霞李志刚
Owner 北京博恩特药业有限公司
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