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Injection sustained-release preparation of LHRH (luteinizing hormone releasing hormone) antagonist substance and preparation thereof

A technology for sustained-release preparations and injections, which can be applied to non-active ingredients medical preparations, medical preparations containing active ingredients, and drug combinations, etc. question

Inactive Publication Date: 2012-07-04
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its short half-life, the bioavailability of common preparations in the blood is very low and the side effects are increased; in addition, conventional solutions need to be administered every day, and the course of treatment is long, which brings pain and inconvenience to patients

Method used

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  • Injection sustained-release preparation of LHRH (luteinizing hormone releasing hormone) antagonist substance and preparation thereof
  • Injection sustained-release preparation of LHRH (luteinizing hormone releasing hormone) antagonist substance and preparation thereof
  • Injection sustained-release preparation of LHRH (luteinizing hormone releasing hormone) antagonist substance and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0066] Preparation method of sustained-release preparation for injection

[0067] In another aspect, the preparation method of the sustained-release preparation for injection of the present invention is provided, the method comprising the following steps:

[0068] (a) dispersing a compound of formula (I) or a pharmaceutically acceptable salt thereof in an aqueous solvent to obtain an aqueous dispersion;

[0069] (b) dispersing acidic phospholipids or pharmaceutically acceptable salts thereof and neutral phospholipids in an aqueous solvent to obtain an aqueous dispersion;

[0070] (c) uniformly mixing the aqueous dispersion obtained in step (a) with the aqueous dispersion obtained in step (b);

[0071] (d) drying the mixed solution obtained in step (c) into a solid; and

[0072] (e) dispersing the solid obtained in step (d) in an oily solvent.

[0073] As used herein, the term "dispersion" refers to the distribution of one or more substances (ie, dispersoid) in another sub...

Embodiment 1

[0092] Embodiment 1: Preparation of sustained-release preparation for injection

[0093] Materials and Reagents

[0094] active pharmaceutical ingredient

[0095] LXT101: Synthesized by the inventor's laboratory according to the method of Chinese patent ZL 90108955.9.

[0096] oily solvent

[0097] Medium-chain oil for injection and soybean oil for injection: both were purchased from China Tieling Beiya Pharmaceutical Oil Co., Ltd.

[0098] other reagents

[0099] Vitamin E (VE): purchased from Zhejiang NHU Co., Ltd.;

[0100] Dipalmitoylphosphatidylcholine (DPPG), distearoylphosphatidylcholine (DSPG) and egg yolk lecithin (EPC): were purchased from China Shanghai Dongshang Industrial Co., Ltd.;

[0101] Oleic acid: purchased from Shanghai Dongshang Industrial Co., Ltd.

[0102] pure distilled water

[0103] method

[0104] The preparation method comprises the following steps:

[0105] (a) Disperse LXT101 in pure distilled water;

[0106] (b) DPPG or DSPG a...

Embodiment 2

[0114] Example 2: Results of pharmacodynamic studies in rats

[0115] Six sustained-release preparations for LXT101 injection prepared in Example 1 were injected intramuscularly (i.m) into rats. Testosterone content (ng / ml) was measured at different times (days) after administration to indirectly measure the sustained-release effect of the LXT101 preparation in vivo. The entire determination process was completed using a BECKMAN COULTER Access Immunoassay System chemiluminescence instrument. The results fit in Table 2 below.

[0116] As mentioned above, the sustained-release effect of the LXT-101 preparation was evaluated by measuring the testosterone level in rats. As shown in Table 2, when the dose is 3.5 mg / kg, preparation 1 can continuously suppress testosterone to castrate level for 5 to 7 days; when the dose is 3.5 mg / kg, preparation 2 can continuously suppress testosterone to castrate level The time of castration level is 7 to 9 days; when the dose is 3.5mg / kg, the...

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Abstract

The invention provides an injection sustained-release preparation containing an LHRH (luteinizing hormone releasing hormone) antagonist substance or a pharmaceutically acceptable salt thereof and a preparation method thereof.

Description

technical field [0001] The invention relates to an injectable sustained-release preparation containing LHRH antagonist substances or pharmaceutically acceptable salts thereof and a preparation method thereof. Background technique [0002] Luteinizing hormone-releasing hormone (LHRH) is a decapeptide neurohormone secreted by the hypothalamus. Its main function is to promote the synthesis of pituitary gland and release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which stimulate pubertal development and regulate fertility. and sex hormone-related processes. Chemical modification and transformation of the molecular structure of LHRH, substitution or deletion of certain amino acid residues may produce new active analogs. Divided by function, these analogs can be divided into two categories: LHRH agonists and LHRH antagonists. LHRH analogs can not only be used to regulate endocrine, but also can be used to treat hormone-dependent malignant tumors, such as pr...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K38/09A61K47/24A61P5/00A61P35/00
Inventor 刘克良全东琴周文霞周宁郄建坤程军平迟哓丽梁远军张永祥
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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