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Compound lidocaine aerosol and preparation method thereof

A technology of lidocaine and aerosol, which is applied in the direction of aerosol delivery, anti-inflammatory agent, pharmaceutical formula, etc., to achieve the effect of maintaining resistance, less irritation, and convenient use

Active Publication Date: 2021-01-29
北京中泰邦医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a compound lidocaine aerosol and preparation method thereof, to solve the technical problems of how to make it easy to carry and use, improve curative effect, shorten onset time, reduce dosage, and reduce adverse reactions; and how to Prepare the aerosol

Method used

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  • Compound lidocaine aerosol and preparation method thereof
  • Compound lidocaine aerosol and preparation method thereof
  • Compound lidocaine aerosol and preparation method thereof

Examples

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Effect test

Embodiment 1

[0041] This embodiment relates to a compound lidocaine aerosol and a preparation method thereof, which consists of the following components in parts by weight: 0.2 parts of lidocaine, 0.2 parts of prilocaine, 1 part of 0.1M sodium hydroxide, 2 parts of propane, 1 part of polyvinyl alcohol with a degree of alcoholysis of 68%, and 0.1 part of sodium rutin.

[0042] A preparation method of compound lidocaine aerosol, the specific steps are as follows.

[0043] a. Add deionized water to polyvinyl alcohol, heat to 78°C, stir until completely dissolved, and cool to room temperature for later use.

[0044] b, the preparation of rutin derivatives:

[0045] b1 Add 9 times the amount of 68% ethanol aqueous solution of Sophora japonica rice to Sophora japonica rice, extract in a water bath with an ultrasonic frequency of 10KHZ for 30 minutes, and separate solid-liquid to obtain the first crude extract;

[0046] b2, adding the filter residue in b1 to 68% ethanol aqueous solution, after ...

Embodiment 2

[0051] This embodiment relates to a compound lidocaine aerosol and a preparation method thereof, which consists of the following components in parts by weight: 3.5 parts of lidocaine, 3.5 parts of prilocaine, 3.5 parts of 0.1M sodium hydroxide, 15 parts of 1,1,1,2-tetrafluoroethane, 11 parts of propane, 17.6 parts of polyvinyl alcohol with an alcoholysis degree of 75%, and 1.75 parts of sodium rutin.

[0052] A preparation method of compound lidocaine aerosol, the specific steps are as follows.

[0053] a. Add deionized water to polyvinyl alcohol, heat to 85°C, stir until completely dissolved, and cool to room temperature for later use.

[0054] b, the preparation of rutin derivatives:

[0055] b1 Add 9 times the amount of 72% ethanol aqueous solution of Sophora japonica rice to Sophora japonica rice, extract in a water bath with an ultrasonic frequency of 30KHZ for 40 minutes, and separate solid-liquid to obtain the first crude extract;

[0056] b2, adding the filter residu...

Embodiment 3

[0061] This embodiment relates to a compound lidocaine aerosol and a preparation method thereof, which consists of the following components in parts by weight: 2 parts of lidocaine, 2 parts of prilocaine, 2 parts of 0.1M sodium hydroxide, 10 parts of 1,1,1,2,3,3,3-heptafluoropropane, 8 parts of propane, 9.5 parts of polyvinyl alcohol with an alcoholysis degree of 75%, and 1 part of sodium rutin.

[0062] A preparation method of compound lidocaine aerosol, the specific steps are as follows.

[0063] a. Add deionized water to polyvinyl alcohol, heat to 85°C, stir until completely dissolved, and cool to room temperature for later use.

[0064] b, the preparation of rutin derivatives:

[0065] b1 Adding 9.5 times the amount of 72% ethanol aqueous solution of Sophora japonica rice to Sophora japonica rice, leaching in a water bath with an ultrasonic frequency of 25KHZ for 36 minutes, and then separating the solid and liquid to obtain the first crude extract;

[0066] b2, adding t...

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Abstract

The invention discloses a compound lidocaine aerosol and a preparation method thereof. The compound lidocaine aerosol comprises the following components in parts by weight: 0.2-3.5 parts of lidocaine,0.2-3.5 parts of propylamine caine, 1-3.5 parts of 0.1 M sodium hydroxide, 2-35 parts of propellant, 1-17.6 parts of polyvinyl alcohol and 0.1-1.75 parts of rutin derivative. Under the condition of not containing penetrant and surfactant components, lidocaine and propylamine caine in a basic group form are released to the subcutaneous layer, and polyvinyl alcohol is used for forming a film on thesurface of the skin, so that the dosage of lidocaine and propylamine caine is reduced, and the safety of clinical use is enhanced; the treatment of male premature ejaculation is mainly used for inhibiting the expansion of the minor artery and capillary anterior sphincter of the cavernous body of the penis, so that the smooth muscle is relaxed, and the blood flow volume is increased; the rutin derivative is added, the elasticity and permeability of the drug are improved by improving the capillary function, and adverse reactions such as vascular bleeding caused by long-term use of traditional lidocaine drugs are avoided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a compound lidocaine aerosol and a preparation method thereof. Background technique [0002] At present, the most widely used dosage form of compound lidocaine is cream or patch, which is mainly used as a local topical anesthetic, to treat premature ejaculation in men, and to reduce the stinging sensation caused by mosquito bites. [0003] Male premature ejaculation is mainly caused by the excessive sensitivity of local nerves and the low threshold of tolerance to sexual stimulation; the current oral treatment drug for male premature ejaculation at home and abroad is dapoxetine, which is mainly an antidepressant and occasionally used for male premature ejaculation; There are also sildenafil and apomorphine hydrochloride buccal tablets for treatment. These two drugs have obvious side effects, such as headache, even syncope, indigestion, etc.; Penile swelling and pain, t...

Claims

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Application Information

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IPC IPC(8): A61K31/167A61K31/7048A61K9/12A61K47/32A61K47/02A61P15/08A61P9/14A61P17/02A61P29/00
CPCA61K9/124A61K31/167A61K31/7048A61K47/02A61K47/32A61P9/14A61P15/08A61P17/02A61P29/00A61K2300/00
Inventor 鲍亚华
Owner 北京中泰邦医药科技有限公司
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