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Lornoxicam liposome for injection

A technology of lornoxicam fat and lornoxicam, which is applied in the field of lornoxicam liposome for injection, can solve the problems of poor compliance and high pH of lornoxicam powder injection, and achieve mild pH value and stability And the effect of good reproducibility and long-term sustained release

Pending Publication Date: 2022-07-12
MAXENMED GUANGZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pH of lornoxicam powder injection prepared under alkaline conditions is relatively high, and the compliance in clinical use is poor, and because the half-life of lornoxicam injection is only 3 to 4 hours, patients still need it every day in clinical use. multiple doses

Method used

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  • Lornoxicam liposome for injection
  • Lornoxicam liposome for injection
  • Lornoxicam liposome for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] This embodiment provides a lornoxicam liposome for injection, the components of the lornoxicam liposome for injection include 5 parts by weight of lornoxicam, 8 parts of hydrogenated soybean phosphatidylcholine parts, cholesterol 2 parts, PEG400 3 parts, phosphate buffer 5 parts, trehalose 3 parts.

[0045] Its preparation method is:

[0046] (1) Dissolving lornoxicam, hydrogenated soybean phosphatidylcholine, cholesterol, and PEG400 in chloroform at 50° C. according to the formula to obtain an oil phase solution.

[0047] (2) According to the formula, the phosphate buffer and water are mixed and dissolved at 50° C. to obtain an aqueous phase solution.

[0048] (3) The oil phase solution in step (1) is placed in a vacuum evaporator to remove chloroform.

[0049] (4) mixing the aqueous phase solution in step (2) with the oil phase in step (3), and placing it under a high-speed shearing machine for emulsification.

[0050] (5) placing the emulsified sample in step (4) ...

Embodiment 2

[0053] This embodiment provides a lornoxicam liposome for injection. The components of the lornoxicam liposome for injection include, in parts by weight, 1 part of lornoxicam, 5 parts of refined egg yolk lecithin, 1 part cholesterol, 3 parts poloxamer, 5 parts phosphate buffer, 5 parts mannitol.

[0054] Its preparation method is:

[0055] (1) Dissolving lornoxicam, refined egg yolk lecithin, cholesterol, and poloxamer in a chloroform / ethanol mixed solvent at 70° C. to obtain an oil phase solution according to the formula.

[0056] (2) According to the formula, the buffer and water are mixed and dissolved at 70° C. to obtain an aqueous phase solution.

[0057] (3) The oil phase solution in step (1) is placed in a rotary evaporator to remove the chloroform / ethanol mixed solvent.

[0058] (4) Mix the aqueous phase solution in step (2) with the oil phase in step (3), and place it under ultrasonic to emulsify.

[0059] (5) Place the emulsified sample in step (4) in a high press...

Embodiment 3

[0062] This embodiment provides a lornoxicam liposome for injection, the components of the lornoxicam liposome include 2 parts by weight of lornoxicam and 10 parts of dipalmitate phosphatidylcholine , 2 parts cholesterol, 1 part poloxamer, 5 parts phosphate buffer, and 5 parts sucrose.

[0063] Its preparation method is:

[0064] (1) Dissolving lornoxicam, dipalmitate phosphatidylcholine, cholesterol, and poloxamer in chloroform at 50° C. according to the formula to obtain an oil phase solution.

[0065] (2) According to the formula, the buffer and water are mixed and dissolved at 50° C. to obtain an aqueous phase solution.

[0066] (3) The oil phase solution in step (1) is placed in a vacuum evaporator to remove chloroform.

[0067] (4) mixing the aqueous phase solution in step (2) with the oil phase in step (3), and placing it under a high-speed shearing machine for emulsification.

[0068] (5) Place the emulsified sample in step (4) in a nitrogen extruder to homogenize t...

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Abstract

The invention belongs to the technical field of chemical and biological medicines, and particularly relates to lornoxicam liposome for injection. The lornoxicam liposome for injection is prepared from the following components in parts by weight: 1 to 10 parts of lornoxicam, 2 to 20 parts of phospholipid, 1 to 8 parts of cholesterol, 0.1 to 5 parts of a surfactant, 1 to 10 parts of a buffering agent, 1 to 10 parts of a freeze-drying excipient and 1 to 10 parts of a freeze-drying protective additive. According to the lornoxicam lipidosome for injection disclosed by the invention, various components such as specific lornoxicam, phospholipid, cholesterol, a surfactant, a buffer agent, freeze-drying auxiliary materials (a protective agent and an excipient) and the like are matched with one another, so that the product has a milder pH value, a slow release property and a longer half-life period. When the lornoxicam is used, the administration frequency of the lornoxicam can be reduced, and the analgesic effect of the lornoxicam can be quickly and continuously exerted.

Description

technical field [0001] The invention belongs to the technical fields of chemistry and biomedicine, and in particular relates to a lornoxicam liposome for injection. Background technique [0002] Lornoxicam, chemical name is 6-chloro-4-hydroxy-2-methyl-N-pyridin-2-yl-2H-thieno[2,3-E][1,2]thiazine-3- Formamide 1,1-dioxide has the formula C 13 H 10 ClN 3 O 4 S 2 , the molecular weight is 371.82, and the structural formula is: [0003] [0004] Lornoxicam is a non-steroidal anti-inflammatory analgesic, which is a thiazide derivative with strong anti-inflammatory and analgesic effects. Its mechanism of action mainly includes: (1) By inhibiting cyclooxygenase (COX) (2) activate the opioid neuropeptide system to exert a central analgesic effect. It can be used to treat acute and chronic pain caused by inflammation, such as postoperative pain, arthritis, rheumatism, soft tissue injury, etc., and is suitable for the treatment of acute and moderate postoperative pain, as wel...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/542A61K47/28A61P29/00
CPCA61K9/127A61K9/0019A61K31/542A61K47/28A61P29/00
Inventor 郭淑儿覃志君
Owner MAXENMED GUANGZHOU
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