CN113876710B - Compound lidocaine spray - Google Patents
Compound lidocaine spray Download PDFInfo
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- CN113876710B CN113876710B CN202111145678.5A CN202111145678A CN113876710B CN 113876710 B CN113876710 B CN 113876710B CN 202111145678 A CN202111145678 A CN 202111145678A CN 113876710 B CN113876710 B CN 113876710B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
- A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Abstract
The invention relates to a compound lidocaine spraying agent, which is prepared from the following components in percentage by weight: 2-6% of lidocaine hydrochloride, 2-6% of oxybuprocaine hydrochloride, 1-5% of natural percutaneous absorption enhancer, 40-60% of cosolvent, 0.5-1% of stabilizer and the balance of water. The compound lidocaine spraying agent has stable quality, good treatment effect, simple process and small side effect.
Description
Technical Field
The invention relates to the field of medicines, and in particular relates to a medicinal spray.
Background
Local anesthetics are drugs that act locally around the nerve trunk or nerve endings, temporarily, completely, and reversibly blocking the generation and conduction of nerve impulses, thereby temporarily eliminating the local pain sensation. The local anesthetic has the action mechanism as follows: the generation and conduction of nerve impulses depend on the depolarization of cell membranes generated by inward flow, and the local anesthetic inhibits the inward flow of the nerve cell membranes so as to prevent the generation of nerve action potentials and the conduction of impulses and further generate local anesthesia. Local anesthetics are characterized by a temporary disappearance of local pain sensation with conscious awareness to allow minor surgery to be performed smoothly. The local anesthesia methods mainly include superficial anesthesia, infiltration anesthesia, and block anesthesia. In recent years, local anesthetics play an indispensable role in clinical anesthesia and treatment of various acute and chronic pains, and play an increasingly important role.
Lidocaine is a local anesthetic commonly used in medical clinic, has the effects of relieving pain and itching, and is also reported to be used for treating certain diseases on the skin. The lidocaine spray has the advantages of painlessness, no damage, convenient administration and the like, can replace local infiltration anesthesia administration, and is particularly suitable for treatment unsuitable for local infiltration anesthesia.
Oxybuprocaine is a lipid local anesthetic, has a structure similar to procaine, and can be combined with a receptor on the inner side of a sodium channel of a nerve cell membrane to block sodium ion inflow, so that a local anesthetic effect is generated. The oxybuprocaine hydrochloride is mainly used for surface anesthesia, and has the advantages of quick response, strong analgesic effect, small irritation, no cross infection and the like.
At present, a product sold in the market does not have a compound lidocaine spray combining two local anesthetics, so that the development of a compound lidocaine preparation with good storage stability and high percutaneous absorption speed is urgently needed.
Disclosure of Invention
The invention aims to provide a compound lidocaine spraying agent with stable quality and good treatment effect, which has simple preparation process and small side effect.
In order to achieve the purpose, the invention provides a compound lidocaine spraying agent in a first aspect, wherein the spraying agent is prepared from the following components in percentage by weight: 2-6% of lidocaine hydrochloride, 2-6% of oxybuprocaine hydrochloride, 1-5% of natural percutaneous absorption enhancer, 40-60% of cosolvent, 0.5-1% of stabilizer and the balance of water.
Preferably, the natural transdermal absorption enhancer is selected from alpha-cyperone, beta-caryophyllene or a mixture of the two. More preferably, the natural transdermal absorption enhancer is a mixture of alpha-cyperone and beta-caryophyllene. More preferably, the natural transdermal absorption enhancer is a mixture of alpha-cyperone and beta-caryophyllene with the weight ratio of 1:1. Most preferably, the natural transdermal absorption enhancer is a mixture of 2% by weight of alpha-cyperone and 2% by weight of beta-caryophyllene.
Preferably, the cosolvent is absolute ethyl alcohol, propylene glycol or a mixture thereof. More preferably, the cosolvent is absolute ethyl alcohol. More preferably, the cosolvent is 45-55% by weight of absolute ethyl alcohol. Most preferably, the cosolvent is 50% by weight of absolute ethanol.
Preferably, the stabilizer is selected from sodium thiosulfate, sodium sulfite or a mixture of the two. More preferably, the stabilizer is a mixture of sodium thiosulfate and sodium sulfite. More preferably, the stabilizer is a mixture of sodium thiosulfate and sodium sulfite in a weight ratio of 1:1. Most preferably, the stabilizer is a mixture of 0.4 weight percent sodium thiosulfate and 0.4 weight percent sodium sulfite.
Preferably, the spray is prepared from the following components in percentage by weight: 3-5% of lidocaine hydrochloride, 3-5% of oxybuprocaine hydrochloride, 2-4% of natural percutaneous absorption enhancer, 45-55% of cosolvent, 0.6-0.8% of stabilizer and the balance of water.
More preferably, the spray is prepared from the following components in percentage by weight: 4% of lidocaine hydrochloride, 4% of oxybuprocaine hydrochloride, 4% of natural percutaneous absorption enhancer, 50% of cosolvent, 0.8% of stabilizer and the balance of water.
More preferably, the spray is prepared from the following components in percentage by weight: 4% of lidocaine hydrochloride, 4% of oxybuprocaine hydrochloride, 2% of alpha-cyperone, 2% of beta-caryophyllene, 50% of cosolvent, 0.8% of stabilizer and the balance of water.
More preferably, the spray is prepared from the following components in percentage by weight: 4% lidocaine hydrochloride, 4% oxybuprocaine hydrochloride, 2% alpha-cyperone, 2% beta-caryophyllene, 50% absolute ethyl alcohol, 0.8% stabilizer and the balance of water.
Most preferably, the spray is prepared from the following components in percentage by weight: 4% lidocaine hydrochloride, 4% oxybuprocaine hydrochloride, 2% alpha-cyperone, 2% beta-caryophyllene, 50% absolute ethyl alcohol, 0.4% sodium thiosulfate, 0.4% sodium sulfite and the balance of water.
The second aspect of the invention provides a preparation method of the compound lidocaine spray, which comprises the following steps: weighing lidocaine hydrochloride and oxybuprocaine hydrochloride according to prescription amount, adding into cosolvent for dissolving completely, sequentially adding natural percutaneous absorption enhancer and stabilizer, stirring completely, adding water to the prescription amount, and bottling.
The third aspect of the invention provides application of the compound lidocaine spraying agent in preparing a medicine for treating pain.
The fourth aspect of the invention provides the application of a natural percutaneous absorption enhancer in preparing a medicament for improving the pain treatment effect of the compound lidocaine spray, wherein the natural percutaneous absorption enhancer is selected from alpha-cyperone, beta-caryophyllene or a mixture of the alpha-cyperone and the beta-caryophyllene.
Preferably, the natural transdermal absorption enhancer is a mixture of alpha-cyperone and beta-caryophyllene.
More preferably, the natural transdermal absorption enhancer is a mixture of alpha-cyperone and beta-caryophyllene with the weight ratio of 1:1.
Most preferably, the natural skin penetration enhancer is a mixture of 2% by weight of alpha-cyperone and 2% by weight of beta-caryophyllene.
In a fifth aspect, the present invention provides the use of a stabilizer selected from sodium thiosulfate, sodium sulfite or a mixture of the two, for improving the storage stability of the compound lidocaine spray.
Preferably, the stabilizer is a mixture of sodium thiosulfate and sodium sulfite.
More preferably, the stabilizer is a mixture of sodium thiosulfate and sodium sulfite in a weight ratio of 1:1.
Most preferably, the stabilizer is a mixture of 0.4 weight percent sodium thiosulfate and 0.4 weight percent sodium sulfite.
Preferably, the improvement of the storage stability is the inhibition of the generation of impurities of lidocaine hydrochloride and/or oxybuprocaine hydrochloride.
The invention has the positive and beneficial effects that:
the inventor of the present invention has unexpectedly found in experiments that the analgesic effect of lidocaine and oxybuprocaine when used in combination has a synergistic effect. In order to improve the analgesic effect of the compound lidocaine spraying agent, the invention selects a specific natural transdermal absorption enhancer (alpha-cyperone and/or beta-caryophyllene), obviously improves the in vivo absorption of the lidocaine hydrochloride and the oxybuprocaine hydrochloride spraying agent, and improves the clinical use curative effect of the spraying agent. In addition, by selecting a specific stabilizer (sodium thiosulfate and/or sodium sulfite), the generation of impurities of lidocaine hydrochloride and/or oxybuprocaine hydrochloride in the spray is effectively inhibited, and the stability of the spray in the storage process is improved.
Detailed Description
The present invention will be further described with reference to the following examples, but the embodiments of the present invention are not limited thereto. The experimental procedures used in the following examples are all conventional procedures unless otherwise specified.
Example 1 Compound lidocaine spray S1 according to the invention
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray S1.
Example 2 Compound lidocaine spray S2 of the invention
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.4g of alpha-cyperone, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray S2.
Example 3 Compound lidocaine spray S3 of the invention
0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride are weighed and added into 5ml of absolute ethyl alcohol for full dissolution, then 0.4g of beta-caryophyllene, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite are sequentially added, the mixture is fully and uniformly stirred, water is added to 10ml, and filling is carried out, thus obtaining the compound lidocaine spray S3.
Example 4 Compound lidocaine spray S4 of the invention
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.1g of alpha-cyperone, 0.3g of beta-caryophyllene, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray S4.
EXAMPLE 5 Compound lidocaine spray S5 according to the invention
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene and 0.08g of sodium thiosulfate, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray S5.
Example 6 Compound lidocaine spray S6 of the invention
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene and 0.08g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray S6.
Example 7 Compound Lidocaine spray S7 of the invention
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene, 0.02g of sodium thiosulfate and 0.06g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray S7.
Comparative example 1 lidocaine spray C1
Weighing 0.8g of lidocaine hydrochloride, adding the lidocaine hydrochloride into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the lidocaine spray C1.
Comparative example 2 oxybuprocaine spray C2
Weighing 0.8g of oxybuprocaine hydrochloride, adding the oxybuprocaine hydrochloride into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the oxybuprocaine spray C2.
Comparative example 3 Compound Lidocaine spray C3
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.4g of azone, 0.04g of sodium thiosulfate and 0.04g of sodium sulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray C3.
Comparative example 4 Compound Lidocaine spray C4
Weighing 0.4g of lidocaine hydrochloride and 0.4g of oxybuprocaine hydrochloride, adding the weighed materials into 5ml of absolute ethyl alcohol for full dissolution, then sequentially adding 0.2g of alpha-cyperone, 0.2g of beta-caryophyllene and 0.08g of sodium metabisulfite, fully and uniformly stirring, adding water to 10ml, and filling to obtain the compound lidocaine spray C4.
Experimental example 1 study on analgesic effect of Compound Lidocaine spray of the present invention
1. Test method
Taking 90 Kunming mice with half male and female and 18-22g of body weight, and randomly dividing the Kunming mice into 9 groups according to 10 groups: the spray (S1 to S4) of examples 1 to 4 was topically administered, the spray (C1 to C3) of comparative examples 1 to 3 was administered in the same manner as in the drug control group 1 to 4, the distilled water of the same volume was administered in the same manner as in the blank control group, and the 50% absolute ethanol solution of the same volume was administered in the same manner as in the solvent control group. Before the test, the abdomen of the mouse is unhaired, the unhaired part is coated with the medicine, the administration volume is 5ml/kg, the medicine is administered for 1 time every day, and the medicine is continuously administered for 3 days. 30 minutes after the last administration, each mouse was injected with 0.6% acetic acid 0.2ml to induce pain, and the number of writhing reactions (abdominal concavity, trunk and hind leg stretch, hip elevation) occurred in each mouse was observed within 15min, and the percentage of inhibition was calculated according to the following formula:
inhibition (%) = (number of writhing in blank control group-number of writhing in drug group)/number of writhing in blank control group × 100%.
2. Test results
The number of writhing times observed in the mice and the calculated pain inhibition percentage for each test group are shown in table 1 below.
TABLE 1 analgesic action of the compound lidocaine spray of the present invention on mice
| Test group | Number of times of body twisting | Inhibition ratio (%) |
| Blank control group | 23.40±5.79 | — |
| Solvent control group | 22.10±5.14 | 5.56％ |
| Inventive drug group 1 (S1) | 10.90±3.21 | 53.4％ |
| Inventive drug group 2 (S2) | 13.80±3.95 | 41.0％ |
| Inventive drug group 3 (S3) | 14.00±3.98 | 40.2％ |
| Inventive drug group 4 (S4) | 12.80±3.74 | 45.3％ |
| Control drug group 1 (C1) | 16.40±4.11 | 29.9％ |
| Control drug group 2 (C2) | 15.90±3.88 | 32.0％ |
| Control drug group 3 (C3) | 15.20±3.27 | 35.0％ |
As can be seen from the analgesic data in the above table, compared with the single spray of comparative example 1-2 (drug control group 1-2), the compound spray of examples 1-4 (drug group 1-4) of the present invention containing the same weight percentage of active ingredients has a more significant percentage of pain inhibition, which confirms that the two active ingredients in the compound spray of the present invention have a synergistic effect, and the combined application effect of the two active ingredients is better. In addition, compared with the comparative example 3 (drug control group 3) in which azone is used as a transdermal absorption enhancer, the natural transdermal absorption enhancers (alpha-cyperone and/or beta-caryophyllene) used in the embodiments 1 to 4 of the invention have better analgesic effects, and the natural transdermal absorption enhancers selected by the invention have excellent effects of promoting the absorption of lidocaine hydrochloride and oxybuprocaine hydrochloride, which indicates that the compound spray of the invention has good local analgesic effects.
Experimental example 2 study on storage stability of Compound Lidocaine spray of the present invention
1. Test method
In this test, 5 test groups were set, wherein test groups 1 to 4 used the compound lidocaine sprays S1 and S5 to 7 of the present invention prepared in examples 1 and 5 to 7, respectively, and test group 5 used the compound lidocaine spray C4 prepared in comparative example 4. The sprays from the 5 test groups were placed in spray bottles and 3 replicates per test group were used. The spray bottles containing the sprays for each test group were placed in a glass desiccator, which was maintained at 60% relative humidity, and the desiccator was stored in a 60 ℃ incubator for 6 months. Samples were taken at 0, 1, 3 and 6 months during the whole test, and the average of the lidocaine hydrochloride and oxybuproca hydrochloride content at each sampling point was calculated.
2. Test results
The contents of lidocaine hydrochloride and oxybuprocaine hydrochloride in the accelerated stability test in each test group are shown in tables 2 and 3 below.
TABLE 2 accelerated stability test results of lidocaine hydrochloride in the compound spray of the invention
TABLE 3 accelerated stability test results for oxybuprocaine hydrochloride in the compound spray of the present invention
As can be seen from the acceleration stability data in the table above, compared with the case that the spray of comparative example 4 (test group 5) uses sodium metabisulfite as the stabilizer, the spray of examples 1 and 5-7 (test groups 1-4) of the present invention using sodium sulfite and/or sodium thiosulfate has no significant decrease in the content of lidocaine hydrochloride and oxybuprocaine hydrochloride after being stored under high temperature and high humidity conditions, and the total impurity content of the two active ingredients is effectively controlled, which proves that the stabilizer of the present invention can effectively inhibit the generation of various impurities of lidocaine hydrochloride and oxybuprocaine hydrochloride at the same time, and indicates that the compound spray of the present invention has good stability during storage and meets the quality requirement of long-term storage.
Claims (12)
1. The compound lidocaine spray is characterized by being prepared from the following components in percentage by weight: 2-6% of lidocaine hydrochloride, 2-6% of oxybuprocaine hydrochloride, 1-5% of natural transdermal absorption enhancer, 40-60% of cosolvent, 0.5-1% of stabilizer and the balance of water, wherein the natural transdermal absorption enhancer is a mixture of alpha-cyperone and beta-caryophyllene with the weight ratio of 1:1, and the stabilizer is a mixture of sodium thiosulfate and sodium sulfite with the weight ratio of 1:1.
2. The spray according to claim 1, wherein the natural transdermal absorption enhancer is a mixture of 2% by weight of α -cyperone and 2% by weight of β -caryophyllene.
3. The spray according to claim 1, wherein the cosolvent is absolute ethanol, propylene glycol or a mixture thereof.
4. The spray according to claim 3, wherein the cosolvent is absolute ethanol.
5. The spray according to claim 4, wherein the cosolvent is 50% by weight of absolute ethanol.
6. The spray according to claim 1, wherein the stabilizer is a mixture of 0.4% by weight of sodium thiosulfate and 0.4% by weight of sodium sulfite.
7. The spray according to claim 1, which is prepared from the following components in percentage by weight: 3-5% of lidocaine hydrochloride, 3-5% of oxybuprocaine hydrochloride, 2-4% of natural percutaneous absorption enhancer, 45-55% of cosolvent, 0.6-0.8% of stabilizer and the balance of water.
8. The spray according to claim 7, which is prepared from the following components in percentage by weight: 4% of lidocaine hydrochloride, 4% of oxybuprocaine hydrochloride, 4% of natural percutaneous absorption enhancer, 50% of cosolvent, 0.8% of stabilizer and the balance of water.
9. The spray according to claim 8, is prepared from the following components in percentage by weight: 4% lidocaine hydrochloride, 4% oxybuprocaine hydrochloride, 2% alpha-cyperone, 2% beta-caryophyllene, 50% absolute ethyl alcohol, 0.8% stabilizer and the balance of water.
10. The spray according to claim 9, which is prepared from the following components in percentage by weight: 4% lidocaine hydrochloride, 4% oxybuprocaine hydrochloride, 2% alpha-cyperone, 2% beta-caryophyllene, 50% absolute ethyl alcohol, 0.4% sodium thiosulfate, 0.4% sodium sulfite and the balance of water.
11. A method for preparing a compound lidocaine spray according to any one of claims 1-10, comprising the steps of: weighing lidocaine hydrochloride and oxybuprocaine hydrochloride according to the prescription amount, adding into cosolvent for full dissolution, sequentially adding natural percutaneous absorption enhancer and stabilizer, stirring well, adding water to the prescription amount, and bottling.
12. Use of a compound lidocaine spray according to any of claims 1-10 for the preparation of a medicament for the treatment of pain.
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| Title |
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| 奥布卡因临床应用的研究进展;李佳瑛等;《神经药理学报》;20201031;第10卷(第5期);第24-27页 * |
| 月桂氮卓酮对利多卡因喷雾剂中利多卡因透皮吸收的影响;张峰等;《医药导报》;20100131;第29卷(第1期);第31-33页 * |
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