Ropivacaine nano particle, preparation method thereof and optimizing experimental method of effect of the ropivacaine nano particle

A technology of ropivacaine and nanoparticles, applied in the field of ropivacaine nanoparticles and its preparation, can solve the problems of catheter infection, short half-life, discount, etc., and achieve smooth and smooth appearance, long sustained release time, and sustained release effect Good results

Active Publication Date: 2014-11-19
FUZHOU GENERAL HOSPITAL OF NANJING MILITARY COMMAND P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the injection form of ropivacaine currently used clinically has a short half-life, and generally only maintains the curative effect for 4-6 hours after a single administration, which is difficult to meet the long-term analgesic needs
If multiple administrations or catheter implantation in the body is used for continuous administration to meet long-term analgesic requirements, excessive administration times will cause drug accumulation and inhibition of respiration and circulation, causing local anesthetic poisoning; Indwelling catheters are easy to cause infection or catheter displacement and discount, so these methods are not the best way to solve long-term analgesia

Method used

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  • Ropivacaine nano particle, preparation method thereof and optimizing experimental method of effect of the ropivacaine nano particle
  • Ropivacaine nano particle, preparation method thereof and optimizing experimental method of effect of the ropivacaine nano particle
  • Ropivacaine nano particle, preparation method thereof and optimizing experimental method of effect of the ropivacaine nano particle

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Effect test

Embodiment 1

[0029] The preparation method of ropivacaine nanoparticles is as follows:

[0030] (A) dissolving ropivacaine free base and poly(lactic-co-polyglycolic acid) block copolymer in dichloromethane as organic phase, polyvinyl alcohol solution as water phase, and slowly adding organic phase into water phase Ultrasonic treatment at 0°C yielded a white emulsion, in which the mass concentration of PLGA in the organic phase was 35 mg / ml, the mass concentration of RVC was 5 mg / ml, and the oil-water volume ratio of the organic phase to the aqueous phase was 0.05.

[0031] (B) Evaporating the white emulsion at 30°C to remove the organic phase to obtain a light blue opalescent suspension;

[0032] (C) The light blue opalescent suspension was centrifuged to obtain a precipitate, and the precipitate was washed, ultrasonically dispersed, and vacuum freeze-dried to obtain ropivacaine nanoparticles RVC-PLGA-NPS.

Embodiment 2

[0034] The preparation method of ropivacaine nanoparticles is as follows:

[0035](A) dissolving ropivacaine hydrochloride in water to make a saturated aqueous solution, adding ammonia water to obtain a precipitate, washing and drying the precipitate to obtain ropivacaine free base;

[0036] (B) dissolving ropivacaine free base and polylactic acid polyglycolic acid block copolymer in dichloromethane as the organic phase, the mass percent concentration is 1% polyvinyl alcohol solution as the water phase, and the organic phase is slowly Add dropwise into the water phase and ultrasonically treat at 5°C to obtain a white emulsion, in which the mass concentration of PLGA in the organic phase is 75 mg / ml, the mass concentration of RVC is 17 mg / ml, and the oil-water volume ratio of the organic phase to the water phase is 0.1.

[0037] (C) Evaporate the white emulsion at 40°C with a rotary evaporator to remove the organic phase to obtain a light blue opalescent suspension, and the ro...

Embodiment 3

[0040] The preparation method of ropivacaine nanoparticles is as follows:

[0041] (A) Dissolve ropivacaine hydrochloride in water to make a saturated aqueous solution, add ammonia water with a mass concentration of 0.9g / ml to completely precipitate to obtain a precipitate, wash the precipitate to neutrality, and then store it at 42°C Dry to constant weight to get ropivacaine free base;

[0042] (B) dissolving ropivacaine free base and polylactic acid polyglycolic acid block copolymer in dichloromethane as organic phase, mass percent concentration is 1.5% polyvinyl alcohol solution as water phase, and organic phase slowly Add dropwise into the water phase and ultrasonically treat at 2°C to obtain a white emulsion, in which the mass concentration of PLGA in the organic phase is 65 mg / ml, the mass concentration of RVC is 15 mg / ml, and the oil-water volume ratio of the organic phase to the water phase is 0.08.

[0043] (C) Evaporate the white emulsion at 37° C. with a rotary ev...

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Abstract

The invention relates to the field of preparation of medicines and particularly relates to ropivacaine nano particles, a preparation method thereof and an optimizing experimental method of effects of the ropivacaine nano particles. The preparation method comprises following steps: (A) dissolving ropivacaine free alkali and polylactic acid-polyglycollic acid segmented copolymer in dichloromethane to form an organic phase while a polyvinyl alcohol solution is employed as an aqueous phase; (B) performing evaporation to a white emulsion at 30-40 DEG C to remove the organic phase to obtain a pale blue opalescence suspension liquid; and (C) performing centrifugal separation to the pale blue opalescence suspension liquid to obtain a precipitate, washing the precipitate, and performing ultrasonic dispersion and a vacuum freeze-drying process to obtain the ropivacaine nano particles. By means of the prepration method of the ropivacaine nano particles, an in-vitro releasing research proves that the ropivacaine nano particles has a releasing rate being about 73% in 96 h, a slow-releasing effect is quite good and a pain-relieving requirement on acute pains, such as post-operation pain and the like, can be satisfied just through one-time dosing.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a ropivacaine nanoparticle, a preparation method thereof, and an experimental method for optimizing its effect. Background technique [0002] Postoperative pain is an important issue during perioperative care. Because local anesthetics can reversibly block the nerve conduction at the injection site, causing temporary loss of sensation in a specific area of ​​the body, injection of local anesthetics is the most direct and effective analgesic method for postoperative pain. Ropivacaine is a local anesthetic commonly used in clinical practice. Compared with other local anesthetics, it has a high degree of sensory-motor nerve separation blocking properties, and is very suitable for postoperative analgesic treatment. [0003] However, the injection form of ropivacaine currently used clinically has a short half-life, and generally only maintains the curative effect for 4-6 hours aft...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/445A61K47/34A61P23/02
Inventor 王丽萍陈国忠黄爱文宋洪涛杨建藤
Owner FUZHOU GENERAL HOSPITAL OF NANJING MILITARY COMMAND P L A
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