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Buserelin acetate lipid microbubble and preparation method thereof

A technology of lipid microbubbles and acetate, applied in pharmaceutical formulations, peptide/protein components, medical preparations containing active ingredients, etc., to achieve the effects of improving permeability, reducing side effects, and achieving dose-effect

Inactive Publication Date: 2015-02-18
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Although ultrasound-mediated targeted drug-loaded microbubbles have the advantages of safety, high efficiency and strong controllability, this technology has not been applied to a class of polypeptides with similar structures to buserelin acetate at home and abroad. It needs further research and improvement

Method used

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  • Buserelin acetate lipid microbubble and preparation method thereof
  • Buserelin acetate lipid microbubble and preparation method thereof
  • Buserelin acetate lipid microbubble and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Preparation of buserelin acetate lipid microbubbles and detection of drug-loaded microbubble morphology and particle size analysis

[0033] 1. Preparation of lipid microbubbles

[0034] Put 5.0mg egg yolk phospholipids and 4.0mg cholesterol into the reaction bottle of the rotary evaporator, add ether to dissolve the lecithin and cholesterol; 40°C water bath, the rotary evaporator is working, until a layer of dry film is formed at the bottom of the reaction bottle to end the reaction.

[0035] Add a degassed phosphate buffer solution with a pH value of 7.4 to a container containing a dry phospholipid film, add 150mg PEG-1500, 0.10m1Tween80, and homogenize under high pressure; stir at 500rpm at 45°C, and feed inert gas at the same time After 1 min, filter to obtain lipid microbubbles.

[0036] The lipid microbubbles were washed with PBS solution for 3 times by centrifugation, and freeze-dried to obtain the lipid microbubble freeze-dried powder.

[0037] 2. Pr...

Embodiment 2

[0045] Example 2: Preparation of Buserelin Acetate Lipid Microbubbles

[0046] 1. Preparation of lipid microbubbles

[0047] Put 6.0mg egg yolk phospholipid and 4.0mg cholesterol into the reaction bottle of the rotary evaporator, add ether to dissolve lecithin and cholesterol; 40 ℃ water bath, the rotary evaporator is working, and the bottom of the reaction bottle forms a layer of dry film to end the reaction.

[0048] Add a degassed phosphate buffer solution with a pH value of 7.4 to the container containing the dry phospholipid film, add 180mg PEG-1500, 0.1m1Tween80, and homogenize under high pressure; stir at 800rpm at 45°C, and feed inert gas at the same time After 1 min, filter to obtain lipid microbubbles.

[0049] The lipid microbubbles were washed with PBS solution for 3 times by centrifugation, and freeze-dried to obtain the lipid microbubble freeze-dried powder.

[0050] 2. Preparation of buserelin acetate lipid microbubbles

[0051] Dissolve 10mg of buserelin ace...

Embodiment 3

[0052] Example 3: Preparation of buserelin acetate lipid microbubbles and establishment of an in vitro ultrasound imaging model

[0053] 1. Preparation of lipid microbubbles

[0054] Put 8.0mg egg yolk phospholipids and 5.0mg cholesterol into the reaction bottle of the rotary evaporator, add ether to dissolve the lecithin and cholesterol; 40 ℃ water bath, the rotary evaporator is working, and the bottom of the reaction bottle forms a layer of dry film to end the reaction;

[0055] Add a degassed phosphate buffer solution with a pH value of 7.4 to the container containing the dry phospholipid film, add 200mg PEG-1500, 0.3m1Tween80, and homogenize under high pressure; stir at 1000rpm at 45°C, and at the same time pass inert gas After 1 min, filter to obtain lipid microbubbles.

[0056] The lipid microbubbles were washed with PBS solution for 3 times by centrifugation, and freeze-dried to obtain the lipid microbubble freeze-dried powder.

[0057] 2. Preparation of buserelin ace...

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Abstract

The invention belongs to the technical field of drug synthesis, and discloses a buserelin acetate lipid microbubble (BLM) and a preparation method thereof. The lipid microbubble comprises a lipid bilayer film, buserelin acetate connected with the outside of the lipid bilayer and inert gas wrapped in the lipid bilayer. Being as a drug carrier, the buserelin acetate lipid microbubble prepared by the method has good targeting property, thereby reducing drug dosage, lowering toxicity and minimizing side effects. Besides, the buserelin acetate lipid microbubble is simple in structure and convenient for preparation. Moreover, the buserelin acetate lipid microbubble can be applied in combination with ultrasonic technology and realize specified and visible release of the drug at the targeting sites; and at the same time, an ultrasonic cavitation effect produced when the buserelin acetate lipid microbubble is subjected to self-ultrasonic blasting at the targeting sites greatly increases permeability of the drug in tissues, thereby realizing maximization of dose-effect.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a lipid microbubble of buserelin acetate and a preparation method thereof. Background technique [0002] Buserelin acetate is a synthetic natural gonadotropin-releasing hormone (GnRH / LHRH) analogue secreted by the hypothalamus. It is a water-soluble polypeptide drug consisting of 10 amino acid residues. Its relative molecular mass is 1299.5, the isoelectric point is 5.4, and its amino acid sequence is shown in the following formula: [0003] H-5-oxo-Pro-His-Trp-Ser-Tyr-D-Ser(t-C 4 h 9 )-Leu-Arg-Pro-NHC 2 h 5 ·CH 3 COOH. [0004] Buserelin was found in 1984, affected by the pituitary gland, it promotes the secretion of luteinizing hormone (LH), follicle-stimulating hormone (FSH) and sex hormones in the early stage of use, and its pharmacological effect is that of LHRH. 20 to 170 times. Chronic administration of buserelin sustainably suppresses chorionic gonadotropin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/09A61K9/00A61P5/06A61P15/00A61P35/00
Inventor 颜携国陶安进马亚平袁建成
Owner HYBIO PHARMA