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

A technology for transdermal drug delivery and composition, which is applied in the field of alfentanil transdermal drug drug composition and its preparation, which can solve the problems of poor compliance and inconvenient medication for patients, and achieve the effect of improving transdermal permeability

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The transdermal patch preparation of embodiment 1 alfentanil hydrochloride

[0068] (1) 3 g of alfentanil hydrochloride, 2 g of povidone (PVP-S630) and 0.15 g of magnesium stearate are micronized, mixed uniformly to obtain a physical mixture, and 4.85 g of polyethylene glycol (molecular weight 2000) 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 alfentanil hydrochloride particles in absolute ethanol, hea...

Embodiment 2

[0075] The transdermal patch preparation of embodiment 2 alfentanil hydrobromide

[0076] (1) Micronize 3 g of alfentanil hydrobromide, 1.5 g of povidone (PVP-S630), and 0.1 g of talcum powder, mix well to obtain a physical mixture, and add 5.4 g of polyethylene glycol (molecular weight 3000) ;

[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 alfentanyl hydrobromide microparticles in propylene glycol, and heating to 30...

Embodiment 3

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

[0084] (1) Micronize 0.5 g of alfentanil tosylate, 4 g of povidone (PVP-VA64), and 0.1 g of magnesium stearate, mix well to obtain a physical mixture, add polyethylene glycol (molecular weight 4000) 5.4g;

[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) Weigh 6 g of micronized amorphous particles prepared in step (2), 2 g of dipalmitoylphosphatidylcholine, 0.3 g of cholesterol, 24 g of absolute ethanol, and 67.7 g of water;

[0087] (4) Dissolving dipalmitoylphosphatidylcholine, cholesterol, and alfentanyl tosylate microparticles in absolute ethanol, and heating to ...

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Abstract

The invention provides an alfentanil pharmaceutical composition for transdermal administration as well as a preparation method and application of the pharmaceutical composition. The pharmaceutical composition for transdermal administration disclosed by the invention comprises alfentanil or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a hot-melt protective agent and an optional solubilizer, the pharmaceutical composition is obtained by the steps of mixing the alfentanil or the pharmaceutically acceptable salt thereof, the polymer dispersion carrier material, the hot-melt protective agent and the optional solubilizer, and performing hot-melt extrusion and micronization to obtain microparticles of the alfentanil or the pharmaceutically acceptable salt ofthe alfentanil. In addition, the invention provides the preparation method and application of the above pharmaceutical composition. According to the pharmaceutical composition for transdermal administration, the alfentanil or the pharmaceutically acceptable salt thereof can be quickly absorbed to achieve the purpose of pain anesthesia in treating without affecting breathing, and avoids the adversepsychological effects brought to patients by intramuscular injection or intravenous injection; and at the same time, the pharmaceutical composition can also be used to prevent and / or treat skin itching.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, more specifically to a pharmaceutical composition for transdermal administration of alfentanil, a preparation method and application thereof. Background technique [0002] Alfentanil hydrochloride is a fentanyl analgesic, English name: Alfentanil Hydrochloride, chemical name: N-[1-[2-(4-ethyl-4,5-dihydro-5-oxo-1H -tetrazol-1-yl) ethyl]-4-(methoxymethyl)-4-piperidinyl]-N-phenylpropanamide hydrochloride monohydrate, the structural chemical formula is as follows: [0003] [0004] Alfentanil hydrochloride, a patented product of Belgian Janssen, has been widely used in Europe and the United States, and was first listed in the Netherlands in 1983; it is a fast-acting strong narcotic analgesic for intravenous injection, and is used in cardiovascular surgery such as coronary artery bypass grafting. Intravenous general anesthetic. It acts very quickly and has a short duration of action. The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K9/127A61K47/32A61K47/34A61K47/12A61K47/02A61K47/10A61K31/454A61P17/04
CPCA61K9/7023A61K9/1271A61K47/32A61K47/34A61K47/12A61K47/02A61K47/10A61K31/454A61P17/04
Inventor 杨玉萍刘敏袁靖熊俊田峦鸢汪淼陈轶苗吕金良曲龙妹朱圣姬郭建锋李莉娥李仕群杜文涛金芬
Owner YICHANG HUMANWELL PHARMA
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