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Pharmaceutical composition for transdermal administration and preparation method of pharmaceutical composition

A technology for transdermal drug delivery and composition, which is applied in the field of transdermal drug drug composition and its preparation, and can solve problems such as poor compliance, adverse psychological effects of patients, and inconvenient medication for patients

Active Publication Date: 2020-06-30
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, at present, injections are mainly used in the market, and they need to be used under the guidance of professional doctors in clinical practice, and the injections are often accompanied by injection pain, which is inconvenient for patients and poor in compliance, which often brings adverse effects to patients. Psychological effects, especially when administered to young children, which are more likely

Method used

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  • Pharmaceutical composition for transdermal administration and preparation method of pharmaceutical composition
  • Pharmaceutical composition for transdermal administration and preparation method of pharmaceutical composition
  • Pharmaceutical composition for transdermal administration and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Preparation of hydrochloride transdermal patch of compound shown in embodiment 1 formula (I)

[0065] (1) 3g of hydrochloride of the compound shown in formula (I) and povidone (PVP-S630) 3.35g, magnesium stearate 0.15g are micronized, add polyethylene glycol (molecular weight 2000) 3.5g, mix homogeneous, resulting in a physical mixture;

[0066] (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, Extrude in the form of spherical particles to obtain amorphous particles, and then micronize them to obtain micronized amorphous particles with a particle size of about 100-150nm;

[0067] (3) Weighing 0.4 g of micronized amorphous particles prepared in step (2), 2 g of soybean lecithin, 0.3 g of cholesterol, 30 g of absolute ethanol, and 67.3 g of water;

[0068] (4) dissolving soybean lecithin, cholesterol, and micronized amorp...

Embodiment 2

[0072] The transdermal patch preparation of the compound shown in embodiment 2 formula (I)

[0073] (1) 0.2g of compound shown in formula (I) and povidone (PVP-VA64) 4g, talcum powder 0.25g are micronized, add polyethylene glycol (molecular weight 3000) 5.55g, mix well, make physical mixture ;

[0074] (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, Extrude in the form of spherical particles to obtain amorphous particles, and then micronize them to obtain micronized amorphous particles with a particle size of about 150-200nm.

[0075](3) Weigh 0.4 g of micronized amorphous particles prepared in step (2), 2 g of phosphatidylcholine, 0.8 g of cholesterol, 30 g of propylene glycol, and 66.8 g of water;

[0076] (4) dissolving phosphatidylcholine, cholesterol, and micronized amorphous particles of the compound represented by for...

Embodiment 3

[0080] Preparation of the mesylate transdermal patch of the compound shown in embodiment 3 formula (I)

[0081] (1) 0.5g of methanesulfonate of the compound shown in formula (I) and povidone (PVP-VA64) 3.5g, magnesium stearate 0.2g are micronized, add polyethylene glycol (molecular weight 4000) 5.8g , mixed evenly to obtain a physical mixture;

[0082] (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 to obtain micronized amorphous particles, and the particle size is controlled at about 250-300nm.

[0083] (3) Weighing 0.4 g of micronized amorphous particles prepared in step (2), 2 g of dipalmitoylphosphatidylcholine, 0.3 g of cholesterol, 30 g of absolute ethanol, and 67.3 g of water;

[0084] (4) dissolving dipalmitoylp...

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Abstract

The invention relates to a pharmaceutical composition for transdermal administration. The pharmaceutical composition contains a compound represented by a formula (I) shown in the specification or a pharmaceutically acceptable salt thereof, a polymer dispersion carrier material, a hot-melt protective agent, and an optional solubilizer. A preparation method of the pharmaceutical composition for thepercutaneous administration includes the following steps: micronizing the compound represented by the formula (I), the polymer dispersion carrier material and the hot-melt protective agent, optionallyadding the solubilizer, performing uniform mixing, performing hot-melt extrusion, and performing micronization to obtain the microparticles of the compound represented by the formula (I) or the pharmaceutically acceptable salt thereof. The pharmaceutical composition for the transdermal administration can make the compound represented by the formula (I) rapidly absorbed, and achieve the purpose ofsedation before anesthesia without affecting breathing, thereby avoiding the adverse psychological effects of intramuscular injection or intravenous injection acupuncture on children.

Description

technical field [0001] The present invention relates to pharmaceutical preparation technology, more specifically to a pharmaceutical composition for transdermal administration of a compound represented by formula (I) and a preparation method thereof. Background technique [0002] The compound represented by formula (I) is an effective and highly selective α2 receptor agonist, which has the effects of sedation, analgesia, anxiolysis, sympathetic nerve block, and opioid thrift, and provides a unique type of sedation That is "sedation with preserved consciousness", the patient seems to be in a sleep state, but is easily awakened, and can communicate and cooperate with the examiner; it has strong analgesic, sedative and anti-anxiety effects in the process of clinical use, and can also suppress The activity of sympathetic nerves is an essential drug for the anesthesia of surgical patients. Compared with common opioid analgesics, the compound shown in formula (I) can effectively i...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K9/127A61K47/32A61K47/34A61K47/10A61K47/02A61K31/4174A61P25/04A61P25/20A61P25/22
CPCA61K9/7023A61K9/1271A61K47/32A61K47/34A61K47/10A61K47/02A61K31/4174A61P25/04A61P25/20A61P25/22
Inventor 李莉娥田峦鸢曲龙妹吕金良吴有斌汪淼金芬郭建锋张丽娜符义刚李仕群李杰杜文涛
Owner YICHANG HUMANWELL PHARMA
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