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Cubic liquid crystal in situ gel injection of local anesthetic and preparation method thereof

A technology of local anesthetics and gel injections, applied in the field of pharmaceutical preparations, can solve the problems of complex preparation process of PLGA microspheres, short action time of local anesthetics, and restrictions on the application of PLGA microspheres, so as to facilitate stability and storage, and inhibit breeding The effect of simple and easy reproduction and preparation methods

Active Publication Date: 2020-01-21
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the complex preparation process of PLGA microspheres, low drug loading, and the degradation products lactic acid and glycolic acid will cause changes in the pH of the injection site, thereby triggering an inflammatory response
These deficiencies limit the application of PLGA microspheres in the field of local anesthetic long-acting preparations
[0006] Therefore, it is necessary to study new long-acting preparations of local anesthetics for the short-acting time of local anesthetics.

Method used

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  • Cubic liquid crystal in situ gel injection of local anesthetic and preparation method thereof
  • Cubic liquid crystal in situ gel injection of local anesthetic and preparation method thereof
  • Cubic liquid crystal in situ gel injection of local anesthetic and preparation method thereof

Examples

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Effect test

Embodiment 1

[0036] This embodiment provides a bupivacaine hydrochloride cubic liquid crystal in situ gel injection and a preparation method thereof, the preparation method comprising the following steps:

[0037] 1) Heating a certain amount of glycerol monooleate (GMO) in a water bath at 45°C to melt, adding a certain amount of absolute ethanol so that the mass ratio of GMO and absolute ethanol is 8:2, and vortexing to obtain in situ gel precursor solution;

[0038] 2) Weigh a certain mass of bupivacaine hydrochloride and add it to the in-situ gel precursor solution obtained in step 1), so that the mass concentration of bupivacaine hydrochloride is 5% (w / w), and vortex to mix , ultrasonically dispersed to obtain an in situ gel injection containing 5w / w% bupivacaine hydrochloride.

[0039] The following experiment was carried out to the bupivacaine hydrochloride cubic liquid crystal in situ gel injection of the present embodiment:

[0040] (1) In vitro gelation test: a small amount of wa...

Embodiment 2

[0045] This embodiment provides the bupivacaine hydrochloride cubic liquid crystal in situ gel injection prepared by GMO and absolute ethanol in different mass ratios, and its preparation method comprises the following steps:

[0046] 1) Heat a certain amount of glycerol monooleate (GMO) in a 45°C water bath until it melts, and add a certain amount of absolute ethanol so that the mass ratios of GMO and absolute ethanol are 6:4, 7:3, and 8, respectively. :2, vortex mixing to obtain the corresponding in situ gel precursor solution;

[0047] 2) Weigh a certain mass of bupivacaine hydrochloride and add them to the in-situ gel precursor solution obtained in step 1), so that the concentration of bupivacaine hydrochloride is 5% (w / w), and vortex to mix , and ultrasonically dispersed to obtain in situ gel injections containing 5w / w% bupivacaine hydrochloride, respectively.

[0048] Three kinds of bupivacaine hydrochloride cubic liquid crystal in situ gel injections prepared in this e...

Embodiment 3

[0056] The bupivacaine hydrochloride cubic liquid crystal in situ gel injection and its preparation method provided in this embodiment, the preparation method comprises the following steps:

[0057] 1) Heating a certain amount of glycerol monooleate (GMO) in a water bath at 45°C to melt, adding a certain amount of absolute ethanol so that the mass ratio of GMO and absolute ethanol is 8:2, and vortexing to obtain Corresponding in situ gel precursor solution A;

[0058] 2) Tocopheryl acetate was added to the in-situ gel precursor solution respectively to make the mass concentrations 10%, 20%, and 30%, respectively, to obtain in-situ gel precursor solutions B with different contents of tocopherol acetate.

[0059] 3) Weigh a certain mass of bupivacaine hydrochloride and add them to the in-situ gel precursor solution B obtained in step 2), so that the concentration of bupivacaine hydrochloride is 5% (w / w), and vortex to mix Uniform, ultrasonic dispersion, respectively to obtain b...

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Abstract

The invention relates to cubic liquid crystal in-situ gel injection of local anesthetic, and a preparation method of the injection. The injection is prepared from the local anesthetic, a liquid crystal material and an organic solvent and / or a release regulator; the local anesthetic is amide local anesthetic and the mass concentration of the local anesthetic is 0.1 to 8 w / w%; the organic solvent is an organic solvent which is mutually soluble with water, the liquid crystal material is mono-oleic acid glycerolipid, and the mass ratio of the liquid crystal material to the organic solvent is (1-9):1; and the release regulator is selected from at least one of medium chain triglyceride, oleic acid, tocopherol and tocopheryl acetate, and the mass concentration of the release regulator is 0 to 30 w / w%. The cubic liquid crystal in-situ gel injection of the local anesthetic has very good long-acting sustained release effect, low sudden release raten high compliance and small adverse effect, can reduce administration times and can avoid the peak valley phenomenon.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a cubic liquid crystal in-situ gel injection of local anesthetics and a preparation method thereof. Background technique [0002] Pain is a major health problem that plagues human beings, and the prevalence of pain in the world is as high as 80%. Postoperative pain belongs to the category of acute pain. Postoperative pain brings a series of physiological and psychological reactions to patients, leading to abnormalities in gastrointestinal function, cardiopulmonary function, blood coagulation function, endocrine metabolism, etc., and various complications, which seriously affect the postoperative recovery of patients. Postoperative pain usually lasts for 48 to 72 hours. [0003] Local anesthetics are a class of drugs that can reversibly block the occurrence and conduction of sensory nerve impulses locally. It is often used clinically to control and relieve pain. Howe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/14A61P23/02A61K47/12A61K47/22A61K31/445A61K31/167
CPCA61K9/0019A61K9/06A61K31/167A61K31/445A61K47/12A61K47/14A61K47/22
Inventor 吴传斌谢业城潘昕黄莹梅丽玲陈航平王倍李娜
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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