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Triptorelin microspheres and preparing method and application thereof

A technology of triptorelin acetate and microspheres, which is applied in the field of pharmaceutical preparations, can solve the problems of short drug effect time and low drug loading, and achieve the effects of prolonging drug effect time, increasing drug loading, and safe clinical use

Inactive Publication Date: 2015-04-22
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

[0005] For this reason, the technical problem to be solved by the present invention lies in the problems of short drug effect time and low drug loading capacity of triptorelin preparations in the prior art, thereby proposing a kind of triptorelin microspheres for injection, and further disclosing its preparation Method and use for preparing triptorelin injection

Method used

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  • Triptorelin microspheres and preparing method and application thereof
  • Triptorelin microspheres and preparing method and application thereof
  • Triptorelin microspheres and preparing method and application thereof

Examples

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Effect test

Embodiment 1

[0188] The triptorelin microspheres described in the present embodiment are made up of the following components in parts by weight: 3.75 g of triptorelin acetate, 75 g of glycolide-lactide copolymer (molecular weight is 25000), sodium carboxymethyl cellulose 30g, mannitol 85g, polysorbate 802g.

[0189] A kind of troprelin microspheres of the present embodiment is prepared by the following method:

[0190] (1) Solution preparation

[0191] The triptorelin acetate that takes prescription quantity is dissolved in water, and the solution that makes mass concentration is 20.0%, standby; 25.0% solution, spare;

[0192] Get the mannitol of recipe quantity, sodium carboxymethylcellulose, polysorbate 80 and mix, add water to dissolve and make mass concentration be 8.5% mannitol solution, mass concentration be 3.0% sodium carboxymethylcellulose solution, mass concentration A polysorbate 80 solution with a concentration of 0.2% was prepared at 85°C for 2 hours and set aside;

[0193...

Embodiment 2

[0208] A kind of triptorelin microsphere of the present embodiment, is made up of the component of following parts by weight: triptorelin acetate 3.75g, glycolide-lactide copolymer (molecular weight is 45000) 170g, carboxymethyl cellulose Sodium 30g, mannitol 85g, polysorbate 802g.

[0209] A kind of troprelin microspheres of the present embodiment is prepared by the following method:

[0210] (1) Solution preparation

[0211] The triptorelin acetate that takes prescription quantity is dissolved in water, and the solution that makes mass concentration is 16.7%, for subsequent use;

[0212] Take by weighing the glycolic acid lactide copolymer of recipe quantity, be dissolved in dichloromethane and be mixed with the solution that mass concentration is 25.0%, standby;

[0213] Get the mannitol of recipe quantity, sodium carboxymethylcellulose, polysorbate 80 and mix, add water to dissolve and make mass concentration be 8.5% mannitol solution, mass concentration be 3.0% sodium c...

Embodiment 3

[0229] A kind of triptorelin microsphere of the present embodiment is made up of the following components in parts by weight: triptorelin acetate 3.75g, glycolide-lactide copolymer (molecular weight is 25000) 60g, sodium carboxymethylcellulose 40g, mannitol 70g, polysorbate 804g.

[0230] A kind of troprelin microspheres of the present embodiment is prepared by the following method:

[0231] (1) Solution preparation

[0232] The triptorelin acetate that takes prescription quantity is dissolved in water, makes the solution that mass concentration is 20.0%, for subsequent use;

[0233] Take the glycolic acid lactide copolymer of recipe quantity, be dissolved in methylene chloride and be mixed with the solution that mass concentration is 20.0%, standby;

[0234] Get the mannitol of recipe quantity, sodium carboxymethylcellulose, polysorbate 80 and mix, add water to dissolve and make mass concentration be 7.0% mannitol solution, mass concentration be 4.0% sodium carboxymethylcel...

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Abstract

The invention belongs to the field of pharmaceutic preparations, and particularly relates to triptorelin microspheres, a preparing method of the triptorelin microspheres and the application of the triptorelin microspheres to preparation of injections. Each triptorelin microsphere comprises, by weight, 3.75 parts of triptorelin acetate, 60-170 parts of glycolide-lactide copolymers, 20-40 parts of sodium carboxymethylcellulose, 70-100 parts of mannitol and 1-4 parts of polysorbate 80. By means of determination of an experiment for the release degree in vitro, an experiment for activity in vivo, a pharmacokinetics experiment, an accelerated stability experiment, a long-term stability experiment and the like, it is indicated that the triptorelin microspheres prolong the pesticide effect time, improve the drug loading capacity, meet officinal requirements and are safe and reliable to use clinically, the quality is stable and safe, and the formulation and the technology are reasonable.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to triptorelin microspheres, a preparation method thereof and an application for preparing injections. Background technique [0002] Triptorelin is a synthetic decapeptide, which uses D-trp to replace Gly on the sixth position of the LHRH peptide chain on the basis of natural luteinizing hormone-releasing hormone (LHRH), resulting in stronger biological activity The LHRH analogue (LHRHa). Triptorelin is mainly used clinically to treat uterine fibroids, central precocious puberty in children, endometriosis, infertility and male prostate cancer, etc., and its clinical application is closely related to its hormone physiological effects. The hormonal efficacy of triptorelin is embodied as positive promotion and negative inhibition due to different administration methods and doses. It is administered in physiological pulses, which has an excitatory effect on the go...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/09A61P35/00A61P15/00A61P15/08
Inventor 黄似焕庞桂才岑振宁郭光明冯前进
Owner 北京博恩特药业有限公司
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