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Sufentanil pharmaceutical composition for transdermal administration as well as preparation method and application of composition

A technology for transdermal drug delivery and composition, which is applied in the field of sufentanil transdermal drug drug composition and its preparation, and can solve the problems of inconvenient drug use and poor compliance of patients

Active Publication Date: 2020-07-17
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it needs to be used under the guidance of professional doctors in clinical practice, and it is often accompanied by injection pain during injection, which is inconvenient for patients to use and has poor compliance.

Method used

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  • Sufentanil pharmaceutical composition for transdermal administration as well as preparation method and application of composition
  • Sufentanil pharmaceutical composition for transdermal administration as well as preparation method and application of composition
  • Sufentanil pharmaceutical composition for transdermal administration as well as preparation method and application of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The transdermal patch preparation of embodiment 1 sufentanil citrate

[0068] (1) Sufentanil citrate 5g, Soluplus 2g, and magnesium stearate 0.1g are micronized, mixed uniformly to obtain a physical mixture, and polyethylene glycol (molecular weight 2000) 2.9g is added;

[0069] (2) Set the extrusion temperature of the twin-screw extruder to 120°C, start the screw after rising to the set temperature, add the physical mixture in step (1) to the extruder, heat-melt and extrude, It is extruded in the form of spherical particles to obtain amorphous particles, which are then micronized, and the particle size is controlled at about 100-150nm.

[0070] (3) Weighing 0.5 g of micronized amorphous particles prepared in step (2), 0.2 g of soybean lecithin, 0.03 g of cholesterol, 3 g of absolute ethanol, and 6.27 g of water;

[0071] (4) Dissolving soybean lecithin, cholesterol, and sufentanil citrate particles in absolute ethanol, heating to 30-45°C to dissolve them to obtain a m...

Embodiment 2

[0075] The transdermal patch preparation of embodiment 2 sufentanil hydrochloride

[0076] (1) Micronize sufentanil hydrochloride 3g, povidone (PVP-S630) 1.5g, and talcum powder 0.2g, mix uniformly to obtain a physical mixture, add polyethylene glycol (molecular weight 3000) 5.3g;

[0077] (2) Set the extrusion temperature of the twin-screw extruder to 100°C, start the screw after rising to the set temperature, add the physical mixture in step (1) to the extruder, heat-melt and extrude, It is extruded in the form of spherical particles to obtain amorphous particles, which are then micronized, and the particle size is controlled at about 150-200nm.

[0078] (3) Weigh 0.3 g of micronized amorphous particles prepared in step (2), 0.2 g of phosphatidylcholine, 0.08 g of cholesterol, 3 g of propylene glycol, and 6.42 g of water;

[0079](4) Dissolving phosphatidylcholine, cholesterol, and sufentanil hydrochloride microparticles in propylene glycol, and heating to 30-45° C. to diss...

Embodiment 3

[0083] The transdermal patch preparation of embodiment 3 sufentanil tosylate

[0084] (1) Micronize sufentanil tosylate 0.5g, povidone (PVP-VA64) 4g, and magnesium stearate 0.3g, mix uniformly to obtain a physical mixture, add polyethylene glycol (molecular weight 4000) 5.2g;

[0085] (2) Set the extrusion temperature of the twin-screw extruder to 140°C, start the screw after rising to the set temperature, add the physical mixture in step (1) to the extruder, heat-melt and extrude, It is extruded in the form of spherical particles to obtain amorphous particles, which are then micronized, and the particle size is controlled at about 250-300nm.

[0086] (3) Weighing 0.5 g of micronized amorphous particles prepared in step (2), 2 g of dipalmitoylphosphatidylcholine, 0.3 g of cholesterol, 30 g of absolute ethanol, and 60.7 g of water;

[0087] (4) dissolving dipalmitoylphosphatidylcholine, cholesterol, and sufentanil tosylate microparticles in absolute ethanol, and heating to 30...

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Abstract

The invention discloses a pharmaceutical composition for transdermal administration. The pharmaceutical composition comprises sufentanil or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a hot-melt protective agent and an optional solubilizer. The pharmaceutical composition for transdermal administration is obtained by the following steps: mixing the sufentanilor the pharmaceutically acceptable salt thereof, the polymer dispersion carrier material, the hot-melt protective agent and the optional solubilizer, performing hot-melt extrusion and micronization toobtain microparticles of the sufentanil or the pharmaceutically acceptable salt of the sufentanil. In addition, the invention provides a preparation method and application of the above pharmaceuticalcomposition. According to the pharmaceutical composition for transdermal administration, the sufentanil can be quickly absorbed, the purpose of treating postoperative pain without affecting breathingcan be achieved, and adverse psychological effects of intramuscular injection or intravenous injection acupuncture on patients can be avoided; and at the same time, the pharmaceutical composition canbe used to prevent and / or treat postherpetic neuralgia.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, more specifically to a pharmaceutical composition for transdermal administration of sufentanil, a preparation method and application thereof. Background technique [0002] Sufentanil is a powerful narcotic analgesic, which has the characteristics of stable cardiovascular system function, no histamine release, and a large safety range. It has obvious effects at low concentrations and is often used for postoperative analgesia. Postoperative analgesia can effectively suppress the discomfort caused by the patient's stress response and coughing, reduce postoperative complications and promote functional recovery. Maintaining an appropriate blood concentration of sufentanil is the key to postoperative analgesia. If the blood concentration is too low, the purpose of analgesia cannot be achieved, and if it is too high, adverse reactions such as excessive sedation and respiratory depression may occu...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K9/127A61K47/32A61K47/34A61K47/10A61K47/02A61K47/12A61K31/4535A61P31/22A61P25/00
CPCA61K9/7023A61K9/1271A61K47/32A61K47/34A61K47/10A61K47/02A61K47/12A61K31/4535A61P31/22A61P25/00
Inventor 刘敏汪淼张丽娜杨玉萍袁靖郭建锋田峦鸢曲龙妹吕金良朱圣姬李莉娥李仕群杜文涛金芬熊俊
Owner YICHANG HUMANWELL PHARMA
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