Local anesthesia pain relieving and slow-release medicine delivery system as well as preparation method and application thereof

A local anesthesia and drug delivery system technology, applied in the field of medicine, can solve the problems of osmotic pressure reduction, interference, etc., and achieve the effects of uniform particle size, good sustained release effect, high encapsulation efficiency and drug loading capacity

Inactive Publication Date: 2018-08-03
XIAN LIBANG BIOMEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is similar to the ordinary liposome pH gradient method or ion gradient drug loading. Since the multivesicular liposome is a structure in which most small capsules exist in a large capsule, when using this technology to load drugs, the outer layer must be small. Drugs are preferentially loaded into the vesicles, and after the drug is loaded in the outer vesicles, the osmotic pressure of the drug loaded into the vesicles in the inner layer of the large vesicles will decrease, so there must be some small vesicles in the large vesicles of multivesicular liposomes that are inactive. Drug filling, in addition, the

Method used

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  • Local anesthesia pain relieving and slow-release medicine delivery system as well as preparation method and application thereof
  • Local anesthesia pain relieving and slow-release medicine delivery system as well as preparation method and application thereof
  • Local anesthesia pain relieving and slow-release medicine delivery system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Prescription composition:

[0039]

[0040]

[0041] The preparation method of multivesicular liposome is as follows:

[0042] (1) Preparation of the inner aqueous phase

[0043]Weigh a certain amount of levobupivacaine hydrochloride, dissolve it in water, add 1M sodium hydroxide, and when no more insoluble matter appears, filter and collect the solid, wash with water for injection until neutral, dry at 60°C, and add to the solid Add other substances in the inner water phase to the powder, add 3ml of 1M phosphoric acid, dissolve and add water to 5ml to obtain the water phase.

[0044] (2) Preparation of the external aqueous phase

[0045] Weigh niacin and sodium citrate in the outer aqueous phase in the above table, add 80ml of water to dissolve, adjust the pH to 7.4 with arginine, add water to 100ml, and obtain the outer aqueous phase.

[0046] (3) Preparation of oil phase

[0047] Weigh the substances in the oil phase in the above table, and dissolve them in...

Embodiment 2

[0053] Prescription composition:

[0054]

[0055] The preparation method of multivesicular liposome is as follows:

[0056] (1) Preparation of the inner aqueous phase

[0057] Weigh 200 mg of bupivacaine, add other substances in the inner water phase, add 2.5 ml of 1M nitric acid, dissolve and add water to 5 ml to obtain an aqueous phase.

[0058] (2) Preparation of the external aqueous phase

[0059] Weigh glucuronic acid, sucrose and sodium citrate from the outer aqueous phase in the above table, add 80ml of water to dissolve, adjust the pH to 8.0 with arginine, add water to 100ml, and obtain the outer aqueous phase.

[0060] (3) Preparation of oil phase

[0061] Weigh the substances in the oil phase in the above table, and dissolve them in a mixed solution of 5 ml of chloroform and ether (volume ratio 4:1) to obtain the oil phase.

[0062] (4) Preparation of colostrum

[0063] The prepared internal water phase was added to the oil phase, and sheared at 16000 rpm fo...

Embodiment 3

[0067] Prescription composition:

[0068]

[0069] The preparation method of multivesicular liposome is as follows:

[0070] (1) Preparation of the inner aqueous phase

[0071] Weigh 250 mg of ropivacaine, add other substances in the inner water phase, add 3.5 ml of 1M phosphoric acid, dissolve and add water to 5 ml to obtain the water phase.

[0072] (2) Preparation of the external aqueous phase

[0073] Weigh vitamin C, sucrose and sodium tartrate from the outer water phase in the above table, add 80ml of water to dissolve, adjust the pH to 8.5 with lysine, add water to 100ml, and obtain the outer water phase.

[0074] (3) Preparation of oil phase

[0075] Weigh each substance of the oil phase in the above table and dissolve it with 5ml of chloroform to obtain the oil phase.

[0076] (4) Preparation of colostrum

[0077] The prepared internal water phase was added to the oil phase, and sheared for 10 min at 13000 rpm to obtain colostrum.

[0078] (5) Preparation of ...

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PUM

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Abstract

The invention discloses a novel local anesthesia pain relieving and slow-release medicine delivery system, which comprises an inner water phase, an outer water phase, an oil phase, an organic solvent,an isotonic regulator and a pH regulator, wherein the inner phase comprises a pain relieving agent, a medicine solvent and a medicine solubilizing agent; the pain relieving agent is selected from onekind of materials from bupivacaine, levobupivacaine, ropivacaine, lidocaine, bupivacaine or mepivacaine; the pain relieving agent is in a free alkali form or acid salt form; the medicine solvent is selected from N or P containing inorganic acid; the medicine solubilizing agent is selected from one or several kinds of materials from sugar or annular organic acid. The prepared muhivescular liposomes have high encapsulation rate, high medicine carrying capacity, uniform particle diameter and good slow release effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a local anesthesia analgesic slow-release drug delivery system and its preparation method and application. Background technique [0002] At present, clinical local anesthetic drugs mainly include esters and amides, and the action time of these drugs is generally less than 3 hours. If long-term analgesia is required, continuous administration is required to maintain an appropriate blood drug concentration. If such drugs are prepared into preparations with sustained release function, such as microspheres and multivesicular liposomes, the analgesic effect can last for a long time, and the tolerance of patients can also be improved. The Chinese patent whose patent number is CN102274183B proposes two kinds of multivesicular liposome preparation methods, the first method is to dissolve the active ingredient of the drug and the osmotic pressure regulator in water to make the inner wate...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/12A61K47/14A61K31/445A61K31/167A61K31/4458A61P23/02
CPCA61K47/12A61K47/14A61P23/02A61K9/127A61K31/167A61K31/445A61K31/4458A61K9/1277
Inventor 马玉樊陈涛孔丹凤刘倩
Owner XIAN LIBANG BIOMEDICAL TECH CO LTD
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