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

A sustained-release preparation, the technology of dezocine, applied in the field of medicine, achieves the effect of relieving pain and stabilizing drug release speed

Active Publication Date: 2020-04-10
TIANJIN CITY THIRD CENT HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Clinically, when dezocine injection is used for analgesia, in order to achieve longer drug action time, dezocine injection with higher concentration and larger amount of non-aqueous solvent has to be used to prolong the drug effect, thus giving patients bring more pain

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] 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 high The shear dispersing emulsifier is dispersed in ethanol and configured as an organic phase solution. The stirring speed of the high-speed shearing machine is 5000rpm, and the stirring time is 30min;

[0068] Step b. Weighing 0.1g sodium chloride as the osmotic pressure regulator and 0.1g wetting agent are dissolved in the water for injection of 100mL to form the inner aqueous phase solution and the outer aqueous phase solution respectively;

[0069] Step c. using a buffer solution of sodium dihydrogen phosphate / sodium hydrogen phosphate to adjust the pH value of the inner aqueous phase solution obtained in step b to 2-7;

[0070] Step d. At room temperature, mix the organic phase solution obtained in the above step a and the 20mL internal aqueous phase solution obtaine...

Embodiment 7

[0079] Example 7 Study on the Analgesic Effect of Dezocine Sustained-release Preparation Take 30 male SD rats, weighing (180±20) g, and place them in the experimental environment for 3 days.

[0080] Place the mouse on a metal plate with a temperature of 60°C, and stimulate the foot of the mouse to produce a pain response. When the mouse licks the foot, it will produce pain. Choose the mouse that licks the foot for less than 20 seconds after touching the hot plate. Mice were used in the experiment, and the ones longer than 20s were eliminated, and the average value was taken for three times, and 9 mice with the average value less than 20s were randomly selected for the experiment, and were divided into 3 groups on average, with 3 mice in each group.

[0081] Administration method:

[0082] Test group: administration injection dezocine injection 0.2 μg / 0.2mL physiological saline of embodiment 1 of the present invention;

[0083] Control group: 0.2 mL of Dezocine Injection (Yan...

Embodiment 8

[0089] Example 8 Pharmacokinetic evaluation of dezocine sustained-release preparation in rats Take 30 male SD rats with a body weight of (180±20) g, and place them in the experimental environment to raise them for 3 days. Fasting for 12 hours before the experiment, the dezocine preparation prepared by the method described in Example 1 of the present invention and the administration injection control sample dezocine injection (Yangzijiang Pharmaceutical Group Co., Ltd. Company, batch number: 12030121 Specification: 1 mL: 5 mg) 0.2 mL. After 30 minutes, 1, 2, 3, 4, 5, 6, 7, and 8 hours, take about 0.2 mL of blood from the ear vein, put it in a pre-heparinized 1.5 mL centrifuge tube, centrifuge at 5000 rpm for 5 minutes, and draw The upper layer of plasma was stored frozen at -80°C.

[0090] At room temperature, accurately draw 100 μL of plasma sample into a 5 mL centrifuge tube, add 100 μL of saturated sodium bicarbonate, mix well, add 2 mL of ethyl acetate, continue vortex mix...

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Abstract

The invention provides a dizocine-containing medicine sustained-release preparation and a preparation method thereof. The dizocine-containing medicine sustained-release preparation is prepared from, by weight, 1-10 parts of dezocine, 1-10 parts of a polylactic acid-hydroxyacetic acid block copolymer, 1-10 parts of a dissolution aiding additive, 1-10 parts of an osmotic pressure regulator, 0.1-0.5part 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 withan existing dezocine injection reagent, the dezocine is encapsulated in a biocompatible high-molecular polymer, the medicine can be released slowly, the release speed of the medicine is stable, the stable blood concentration can be maintained for 8h or more after single-time administration, the pain of a patient can be effectively relieved, and the dezocine injection reagent can be used for relieving the pain of the patient after the operation.

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 drug sustained-release preparation containing dezocine and a preparation method thereof. Background technique [0002] Dezocine is a mixed agonist-antagonist of opioid receptors, which is a small-molecule highly fat-soluble drug that fully agonizes κ receptors and partially agonizes and partially antagonizes μ receptors. When the blood concentration of dazocine reaches 5-9 μg / L, it will produce analgesic effect, and the analgesic effect is strong, and its analgesic effect is 5-9 times that of pethidine, which is equivalent to morphine. Studies have shown that the spinal cord κ receptor is an important target for dezocine to produce analgesic effect. Dezocine absorbs quickly in the body, distributes rapidly, and has a long half-life, so its analgesic effect has ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/10A61K31/135A61P25/04
CPCA61K31/135A61K47/10A61K47/34A61P25/04
Inventor 王海云孙熠赵茗姝华伟
Owner TIANJIN CITY THIRD CENT HOSPITAL
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