Lurasidone brain-targeted lipidosome injection and preparation method thereof

A technology targeting liposomes and injections, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve problems such as low bioavailability, non-targeting, and poor patient compliance. To achieve the effects of prolonging cycle time, reducing dosage and improving product quality

Active Publication Date: 2017-11-21
HUAQIAO UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] For psychiatric patients, drugs in the form of tablets have the disadvantage of difficulty in swallowing, resulting in poor patient compliance and even life-threatening possibilities such as coughing or choking, while injection dosage forms do not have this disadvantage
Ordinary lurasidone injections have poor physical and chemical stability, and the quality of the drug decreases after long-term storage, and the stability fails to meet the requirements of injections; and the half-life in the body is short, the bioavailability is low, and it is more likely to produce toxic side effects on the human body. Leaving hidden dangers for clinical use
[0004] Liposomes can fuse with the brain vascular endothelial cell membrane through passive transport or transport drugs to the brain parenchyma through endocytosis, but ordinary liposomes are quickly phagocytosed by the reticuloendothelial system of liver, spleen, bone marrow and other tissues in vivo unable to reach the target
The sterically stabilized liposomes formed by modifying polyethylene glycol (PEG) chains on the liposome surface can avoid being recognized by phagocytes, thereby prolonging the blood circulation time of liposomes, but due to the existence of the blood-brain barrier (BBB) , brain drug delivery is difficult, simply using PEG-modified liposomes cannot pass through the BBB
Therefore, existing lurasidone hydrochloride dosage forms have defects such as difficulty in swallowing, poor compliance, short half-life and no targeting

Method used

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  • Lurasidone brain-targeted lipidosome injection and preparation method thereof
  • Lurasidone brain-targeted lipidosome injection and preparation method thereof
  • Lurasidone brain-targeted lipidosome injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 1. Prescription ratio (100ml capacity)

[0044]

[0045]

[0046] 2. Preparation method

[0047] (1) Take (2,3-dioleoxypropyl)trimethylammonium chloride, cholesterol, (-)-epicatechin gallate and glucose-glycine-polyethylene glycol 1000 in the prescribed amount, Dissolve in 30ml of chloroform-methanol (2:1 by volume) mixed solvent, place in a constant temperature magnetic stirrer and stir until completely dissolved, then dissolve the prescribed amount of lurasidone in 0.05mol / L sodium glycinate solution, dropwise into the above-mentioned chloroform-methanol mixed solvent, after the dropwise addition, homogenize 3 times under 60MPa, homogenize 3 times under 160MPa to form a W / O type emulsion;

[0048] (2) Transfer the obtained W / O emulsion to a 300ml round-bottomed flask, and place it in a water bath temperature of 50°C for 55r·min -1 Rotary evaporation under reduced pressure to remove the organic solvent until a uniform phospholipid film is formed on the bottle wa...

Embodiment 2

[0054] 1. Prescription ratio (100ml capacity)

[0055]

[0056] 2. Preparation method

[0057] (1) Take (2,3-dioleoxypropyl)trimethylammonium chloride, cholesterol, (-)-epicatechin gallate and glucose-glycine-polyethylene glycol 1000 in the prescribed amount, Dissolve in 30ml of chloroform-methanol (2:1 by volume) mixed solvent, place in a constant temperature magnetic stirrer and stir until completely dissolved, then dissolve the prescribed amount of lurasidone in 0.05mol / L sodium glycinate solution, dropwise into the above-mentioned chloroform-methanol mixed solvent, after the dropwise addition, homogenize 3 times under 60MPa, homogenize 3 times under 160MPa to form a W / O type emulsion;

[0058] (2) Transfer the obtained W / O emulsion to a 300ml round-bottomed flask, and place it in a water bath temperature of 50°C for 55r·min -1 Rotary evaporation under reduced pressure to remove the organic solvent until a uniform phospholipid film is formed on the bottle wall of the ...

Embodiment 3

[0064] 1. Prescription ratio (100ml capacity)

[0065]

[0066] 2. Preparation method

[0067] (1) Take (2,3-dioleoxypropyl)trimethylammonium chloride, cholesterol, (-)-epicatechin gallate and glucose-glycine-polyethylene glycol 1000 in the prescribed amount, Dissolve in 30ml of chloroform-methanol (2:1 by volume) mixed solvent, place in a constant temperature magnetic stirrer and stir until completely dissolved, then dissolve the prescribed amount of lurasidone in 0.05mol / L sodium glycinate solution, dropwise into the above-mentioned chloroform-methanol mixed solvent, after the dropwise addition, homogenize 3 times under 60MPa, homogenize 3 times under 160MPa to form a W / O type emulsion;

[0068] (2) Transfer the obtained W / O emulsion to a 300ml round-bottomed flask, and place it in a water bath temperature of 50°C for 55r·min -1 Rotary evaporation under reduced pressure to remove the organic solvent until a uniform phospholipid film is formed on the bottle wall of the ...

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Abstract

The invention discloses a lurasidone brain-targeted lipidosome injection which comprises lurasidone, lipidosome carrier, antioxidant and freeze-drying protecting agent according to a mass consumption ratio of 1:10-100:0.5-5:30-100. The lipidosome carrier comprises phospholipid, cholesterol and brain-targeted auxiliary material according to 40-100:10-50:5-10, phospholipid is selected from 1-palmityl-2-linoleoyl phosphatidyl choline or (2, 3-dioxy propyl) trimethyl ammonium chloride, and the brain-targeted auxiliary material is glucose-glycine-polyethylene glycol conjugate. The lurasidone brain-targeted lipidosome injection has the advantages of high stability, long in-vivo circulating time, high targeting performance and little toxic and side effect. The invention further discloses a preparation method of the lurasidone brain-targeted lipidosome injection. The preparation method is simple, practical and suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a lurasidone brain-targeting liposome injection and a preparation method thereof. Background technique [0002] Lurasidone hydrochloride is an atypical antipsychotic drug developed by Japan's Sumitomo Pharmaceutical Company. It is suitable for the treatment of patients with schizophrenia. It was approved for marketing in the United States in 2010 and sold in the market in the form of tablets. At present, it has been listed in the domestic market, but there is no relevant report about its liposome injection formulation. [0003] For mentally ill patients, drugs in the form of tablets have the disadvantage of difficulty in swallowing, resulting in poor patient compliance, and even life-threatening possibilities such as coughing or choking, while injection dosage forms do not have this disadvantage. Ordinary lurasidone injections have poor physical and chemical stability....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/496A61K47/34A61P25/18
CPCA61K9/0019A61K9/1272A61K9/1277A61K31/496A61K47/34
Inventor 王立强周玥莹
Owner HUAQIAO UNIVERSITY
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