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Sustained release preparation for injection of LHRH antagonist substances and preparation thereof

A technology for sustained-release preparations and injections, applied in the field of sustained-release preparations for injection of LXT101 and its preparation, which can solve the problems of short half-life, long course of treatment, pain of patients and inconvenience of medication

Inactive Publication Date: 2010-02-17
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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  • Sustained release preparation for injection of LHRH antagonist substances and preparation thereof
  • Sustained release preparation for injection of LHRH antagonist substances and preparation thereof
  • Sustained release preparation for injection of LHRH antagonist substances and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: Preparation of formulation

[0048] The preparation of the present invention is prepared according to the following general method: Grind or pulverize LXT101 and pass it through a 100-mesh sieve, add it to the mixture of other ingredients, stir or grind, and use a high-pressure homogenizer to disperse, so that the particle size in the LXT101 suspension is different. If it exceeds 15μm, the preparation can be obtained by dispensing.

[0049] Different formulations as shown in Table 1 were prepared.

[0050] Table 1. Different formulations prepared by the present invention

[0051]

Embodiment 2

[0052] Example 2: Determination of cumulative release in vitro

[0053] Take the active ingredient reference substance and add water to prepare standard active ingredient solutions with concentrations of 10μg / mL, 20μg / mL, 30μg / mL, 50μg / mL, 100μg / mL, 200μg / mL, and measure the absorbance A by the Folin method. Absorbance A is used to regress the concentration, and a standard curve regression equation is established.

[0054] Take an appropriate amount of the prepared LXT101 sustained-release preparation and place it in a 50 mL conical flask with a stopper, and add 10 mL of a pH 7.2 PBS buffer solution to it. Place the Erlenmeyer flask in a constant temperature shaker at 37±1°C and oscillate at a frequency of 70r / m. At different time points, 200 μL of the liquid was quantitatively taken, and 200 μL of pH 7.2 PBS buffer solution was added at the same time. Centrifuge at 12,000r / m for 10 minutes, and take the supernatant as a sample solution. Measure the absorbance of the sample solu...

Embodiment 3

[0059] Example 3: Results of pharmacodynamic research in rats

[0060] Rats were given intramuscular injection (im) of the different LXT-101 preparations (including different doses) prepared in Example 1 according to Table 3 below, and the testosterone content (ng / ml) in the serum was determined at different times (days) after administration to Indirectly measure the release effect of LXT101 oily sustained-release preparation in vivo. The entire determination process is automatically completed by the BECKMAN COULTER Access Immunoassay System chemiluminescence instrument according to a predetermined program. The results are shown in Table 3 below.

[0061] The sustained release effect of the LXT-101 preparation was evaluated by measuring the testosterone level in the rat serum. From the results in Table 3, it can be seen that the preparation 1 can significantly inhibit the serum testosterone level for 5 to 7 days when the dose is 3.5 mg / kg; 2 When the dose is 3.5 mg / kg, it can sig...

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Abstract

The invention relates to a sustained release preparation for injection of LHRH antagonist substances and a preparation method thereof. The sustained release preparation comprises a therapeutic effective dose of an active component in a structure of a formula (I) or pharmaceutically acceptable salts or prodrugs thereof, and oily solvent.

Description

Technical field [0001] The invention relates to a sustained-release preparation for injection of LHRH antagonist substances and a preparation method thereof, and in particular to a sustained-release preparation of LXT101 for injection 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 the pituitary gland and release luteinizing hormone (LH) and follicle stimulating hormone (FSH) to 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. According to their functions, these analogues can be divided into two categories: LHRH agonists and LHRH antagonists. LHRH analogs can be used not only to regulate endocrine, but also t...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/107A61K38/09A61P35/00A61P5/00
CPCA61K9/0019A61K38/09A61K9/10A61P5/00A61P35/00
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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