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Ketamine transdermal patch and preparation method thereof

A transdermal patch, ketamine technology, applied in anesthetics, anti-inflammatory agents, pharmaceutical formulations, etc., can solve the problem of difficulty in controlling the amount of skin penetration enhancers and crystallization inhibitors, difficulty in completely avoiding ketamine crystallization, and low transdermal penetration rate and other problems, to achieve the effects of easy preparation and use, increased percutaneous penetration rate, and reduced risk of addiction

Inactive Publication Date: 2019-07-05
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the amount of skin penetration enhancer and crystallization inhibitor used in this technical solution is extremely difficult to control. When the skin penetration enhancer is excessive or too small, it is easy to diffuse through the stratum corneum, and the percutaneous penetration rate is extremely low; and ketamine is extremely easy to crystallize. It is necessary to add a considerable amount of crystallization inhibitors, resulting in thickening of the transdermal patch, and it is difficult to completely avoid the crystallization of ketamine, which limits the use of transdermal absorption

Method used

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  • Ketamine transdermal patch and preparation method thereof
  • Ketamine transdermal patch and preparation method thereof
  • Ketamine transdermal patch and preparation method thereof

Examples

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Embodiment 1

[0037] A preparation method of ketamine transdermal patch, comprising the following preparation steps:

[0038] (1) Decrystallization of ketamine to obtain decrystallization powder, including:

[0039] (1.1) Dissolve 10g of ketamine in 20g of hot ethanol;

[0040] (1.2) Add organic amine (diethanolamine) 30g and soybean lecithin 5g in proportion;

[0041] (1.3) After stirring uniformly at room temperature for 3 hours, spray dry to get it; spray drying conditions: spray dryer; nitrogen flow pressure: 600L / h; air inlet temperature: 90°C; air outlet temperature: 43°C; feed amount: 5mL / min; Needle pass frequency: 15 seconds / time;

[0042] (2) Disperse the decrystallized powder of step (1) in cholesterol and fatty acid to form dispersed microspheres of multiple microreservoirs; including: 77 mg of stearic acid mixed with 7 mL of heptane, 40 mg of cholesterol Heat to 60°C until a clear solution is obtained. and allow to cool to room temperature. Next, a decrystallized powder co...

Embodiment 2

[0046] A preparation method of ketamine transdermal patch, comprising the following preparation steps:

[0047] (1) Decrystallization of ketamine to obtain decrystallization powder, including:

[0048] (1.1) Dissolve 10g of ketamine in 30g of hot ethanol;

[0049] (1.2) Add organic amine (diethanolamine) 20g and soybean lecithin 5g in proportion;

[0050] (1.3) After stirring uniformly at room temperature for 4 hours, spray dry to get it; spray drying conditions: spray dryer; nitrogen flow pressure: 600L / h; air inlet temperature: 90°C; air outlet temperature: 43°C; feed amount: 5mL / min; Needle pass frequency: 15 seconds / time;

[0051] (2) Disperse the decrystallized powder of step (1) in cholesterol and fatty acid to form dispersed microspheres of multiple micro-reservoirs; including: 40 mg of stearic acid mixed with 7 mL of heptane, 40 mg of cholesterol Heat to 60°C until a clear solution is obtained. and allow to cool to room temperature. Next, a decrystallized powder c...

Embodiment 3

[0055] A preparation method of ketamine transdermal patch, comprising the following preparation steps:

[0056] (1) Decrystallization of ketamine to obtain decrystallization powder, including:

[0057] (1.1) Dissolve 10g of ketamine in 20g of hot ethanol;

[0058] (1.2) Add organic amine (triethanolamine) 30g and soybean lecithin 5g in proportion;

[0059] (1.3) After stirring uniformly at room temperature for 3 hours, spray dry to get it; spray drying conditions: spray dryer; nitrogen flow pressure: 600L / h; air inlet temperature: 90°C; air outlet temperature: 43°C; feed amount: 5mL / min; Needle pass frequency: 15 seconds / time;

[0060] (2) Disperse the decrystallized powder of step (1) in cholesterol and fatty acid to form dispersed microspheres of multiple microreservoirs; including: 77 mg of stearic acid mixed with 7 mL of heptane, 40 mg of cholesterol Heat to 60°C until a clear solution is obtained. and allow to cool to room temperature. Next, a decrystallized powder con...

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Abstract

The invention belongs to the technical field of medical preparations, particularly relates to a ketamine transdermal patch and a preparation method thereof. The preparation method includes the steps:performing decrystallization on ketamine to obtain decrystallization powder; dispersing the decrystallization powder into cholesterol and fatty acid to form dispersion micro-spheres of a micro-storagewarehouse; coating a high-molecular pressure sensitive adhesive with the micro-spheres to obtain the transdermal patch. According to the transdermal patch, a crystallization inhibitor is omitted, ketamine can be effectively quantified, addiction risks are reduced, the transdermal patch is conveniently prepared and used and does not easily diffuse to penetrate cuticles, percutaneous penetration rate is obviously increased, and major depressive disorder (MDD) and / or pain treatment effects are ensured.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a ketamine transdermal patch and a preparation method thereof. Background technique [0002] Ketamine, English name Ketamine, CAS No.: 6740-88-1, is a white crystalline powder, odorless, easily soluble in water. Its chemical structural formula is as follows: [0003] [0004] Ketamine is used as an anesthetic, and the clinically used ketamine is a racemate of D- and L-ketamine. The anesthetic potency of D-ketamine was 4 times that of L-ketamine, but the psychomotor response was less in the awakening period. Commercially available ketamine is hydrochloride, pH 3.5-5.5, PKa 7.5. [0005] The advantage of the transdermal patch is that it eliminates the first-pass clearance effect of the liver, avoids the stimulation of the gastrointestinal tract by the chemical and biological effects of the drug, reduces or avoids the occurrence of side effects, and because...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/135A61K47/12A61K47/28A61P23/02A61P25/00A61P25/24A61P29/00
CPCA61K9/7084A61K31/135A61K47/12A61K47/28A61P23/02A61P25/00A61P25/24A61P29/00
Inventor 张晗贾文强李翰
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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