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A compound drug sustained-release preparation containing dezocine and lidoine and its preparation method

A sustained-release preparation, the technology of dezocine, applied in the field of medicine, can solve the problems of reducing the frequency of dosing, poor bioavailability of lidocaine, etc., and achieve the effect of relieving pain and stabilizing the drug release rate

Active Publication Date: 2020-05-15
TIANJIN CITY THIRD CENT HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the problems and deficiencies in the prior art, the object of the present invention is to provide a compound drug sustained-release preparation of dezocine and lidocine for injection and a preparation method thereof. The form can effectively reduce the frequency of administration, overcome the hydrophobicity of dezocine and the poor bioavailability of lidocine, and achieve the effect of sustained and controllable drug release

Method used

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  • A compound drug sustained-release preparation containing dezocine and lidoine and its preparation method
  • A compound drug sustained-release preparation containing dezocine and lidoine and its preparation method
  • A compound drug sustained-release preparation containing dezocine and lidoine and its preparation method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Step a. At room temperature, weigh 120 mg of dezocine and 0.1 g polylactic acid-glycolic acid block copolymer (molecular weight is 100 KDa, intrinsic viscosity is 0.3 dl / g) and 0.1 g poloxamer 188 by The high-shear dispersing emulsifier is dispersed in ethanol and configured as an organic phase solution. The stirring rate of the high-speed shearing machine is 5000rpm, and the stirring time is 30min;

[0072] Step b. the lidocaine that takes 120mg is dissolved in 100mL water for injection, forms inner water phase, adopts the buffer solution of sodium dihydrogen phosphate / sodium hydrogen phosphate that the pH value of inner water phase solution is adjusted to 2-7;

[0073] Step c. Weighing 0.1g sodium chloride as an osmotic pressure regulator and 0.1g wetting agent are dissolved in 100mL of water for injection to form an external aqueous phase solution;

[0074] Step d. At room temperature, mix the organic phase solution obtained in step a above with the internal aqueous ...

Embodiment 2

[0078] Step a. At room temperature, weigh 150 mg of dezocine and 0.2 g polylactic acid-glycolic acid block copolymer (molecular weight is 100 KDa, intrinsic viscosity is 0.3 dl / g) and 0.1 g poloxamer 188 by The high-shear dispersing emulsifier is dispersed in ethanol and configured as an organic phase solution. The stirring rate of the high-speed shearing machine is 5000rpm, and the stirring time is 30min;

[0079] Step b. the lidocaine that takes 150mg is dissolved in 100mL water for injection, forms inner water phase, adopts the buffer solution of sodium dihydrogen phosphate / sodium hydrogen phosphate that the pH value of inner water phase solution is adjusted to 2-7;

[0080] Step c. Weighing 0.1g sodium chloride as an osmotic pressure regulator and 0.1g wetting agent are dissolved in 100mL of water for injection to form an external aqueous phase solution;

[0081] Step d. At room temperature, mix the organic phase solution obtained in step a above with the internal aqueous ...

Embodiment 3

[0085] Step a. At room temperature, weigh 120 mg of dezocine and 0.1 g polylactic acid-glycolic acid block copolymer (molecular weight is 100 KDa, intrinsic viscosity is 0.3 dl / g) and 0.15 g poloxamer 188 by The high-shear dispersing emulsifier is dispersed in ethanol and configured as an organic phase solution. The stirring rate of the high-speed shearing machine is 5000rpm, and the stirring time is 30min;

[0086] Step b. the lidocaine that takes 120mg is dissolved in 100mL water for injection, forms inner water phase, adopts the buffer solution of sodium dihydrogen phosphate / sodium hydrogen phosphate that the pH value of inner water phase solution is adjusted to 2-7;

[0087] Step c. Weighing 0.1g sodium chloride as an osmotic pressure regulator and 0.1g wetting agent are dissolved in 100mL of water for injection to form an external aqueous phase solution;

[0088] Step d. At room temperature, mix the organic phase solution obtained in step a above with the internal aqueous...

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Abstract

The invention provides a compound medicine sustained-release preparation containing dezocine and lidocaine and a preparation method thereof. The compound medicine sustained-release preparation is prepared from, by weight, 1-10 parts of dezocine, 1-10 parts of lidocaine, 1-10 parts of a polylactic acid-hydroxyacetic acid block copolymer, 1-10 parts of a dissolution aiding additive, 1-10 parts of anosmotic pressure regulator, 0.1-0.5 part of a pH value stabilizer, 1-5 parts of a wetting agent, 1-10 parts of a freeze-dried powder protectant, 10-50 parts of an organic solvent and 100-1000 parts of water for injection. Compared with an existing injection reagent, the compound drug sustained-release preparation containing dezocine and lidocaine is encapsulated in a biocompatible high-molecularpolymer to form an oil-in-water-in-oil structure, a medicine sustained-release effect can be obtained, the medicine release speed is stable, the stable blood concentration can be maintained for 8h ormore after single-time administration, the pain of a patient can be effectively relieved, and the compound drug sustained-release preparation can be used for analgesia of the patient after surgery.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical composition for anesthesia and analgesic injection and a preparation method thereof, in particular to a compound drug slow-release preparation containing dezocine and lidocaine and a preparation method thereof. Background technique [0002] Lidocaine (English name lidocaine) is an amide local anesthetic mainly used for infiltration anesthesia, epidural anesthesia, topical anesthesia (including mucosal anesthesia during thoracoscopic examination or abdominal surgery) and nerve conduction block . Because oral absorption is good, but the first-pass effect of the liver can make 70% of the drug be metabolized, and the blood concentration is low, so it is not suitable for oral administration. After the drug is injected intravenously, the tissue distribution is fast and wide, and the blood-brain barrier can be passed through, and the blood drug concentration drops rapid...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/113A61K9/19A61K31/135A61K31/167A61K47/34A61P25/04
CPCA61K9/0019A61K9/113A61K9/19A61K31/135A61K31/167A61K47/34A61P25/04A61K2300/00
Inventor 孙熠王海云赵茗姝华伟
Owner TIANJIN CITY THIRD CENT HOSPITAL
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