Transdermal and transmucosal local narcotic analgesic and preparation method of gel formulation thereof

A technique for local anesthesia and analgesics, applied in anesthetics, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as insufficient depth, and achieve fast onset, few side effects, and long-lasting effects

Inactive Publication Date: 2009-02-04
珠海市横琴灵敏科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But this medicine has many disadvantages: the maximum depth of anesthesia on normal skin is 5mm, the depth is not enough
[0004] Announced on January 21, 2004, the announcement number is CN 1135104C, and the Chinese invention patent titled "local anesthetic for external use" was published on July 25, 2007, the publication number is CN101002759A, and the title is "Lidoca hydrochloride The Chinese invention patent application for the transdermal patch of Yin and menthol, because lidocaine hydrochloride is used as the main drug, there are similar defects to Enna cream
[0008] No one has used bupivacaine compounds in combination with menthol, azone compounds and other related substances to make other dosage forms of transdermal and transadhesive preparations for related purposes

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1, preparation: get levobupivacaine hydrochloride 2 grams, menthol 1 gram and azone 2 grams and be made into 100ml water solvent. The water solvent can be used for local spraying, coating and dressing.

[0028] Using the aqueous solution obtained in Example 1, perform the following preoperative anesthesia.

[0029] 1. Anesthesia for five people before circumcision by wrapping method: among them:

[0030] Two people took effect after 20 minutes, one person maintained the effect for five hours, and the other person maintained the effect for 5.5 hours;

[0031] Two people took effect after 22 minutes, one person's drug effect lasted for six hours, and the other person's drug effect lasted for seven hours;

[0032] One person took effect after 24 minutes, and the drug effect lasted for five hours.

[0033] 2. Anesthesia for four people before the operation of condyloma acuminata on the mucosa of the urethral opening by applying the liquid medicine method, amon...

Embodiment 2

[0037] Embodiment 2, preparation of gel transdermal transmucosal local anesthesia analgesic,

[0038] Include the following steps:

[0039] 1. Dissolve 3 grams of levobupivacaine hydrochloride into 15-20ml of water to obtain A solution;

[0040] 2. Add 1.5g of carbomer to 50ml of water, stir and dissolve to obtain B solution;

[0041] 3. Mix and shake the above liquids A and B, and add 5ml of ethanol and 20ml of propylene glycol to obtain solution C;

[0042] 4. Add 1g of menthol and 2g of azone to solution C, and shake well to obtain solution D;

[0043] 5. Neutralize solution D with 18% NaOH aqueous solution to pH=7, add water to 100ml, and stir evenly.

[0044] Use the gel transdermal and transmucosal local anesthesia analgesic agent obtained in Example 2 to perform preoperative anesthesia for five penile prepuce patients, one for smearing anesthesia, once for five minutes, three times for smearing, and it will take effect after 35 minutes , maintain the effect for thre...

Embodiment 3

[0045] Example 3: Take 5 grams of levobupivacaine hydrochloride, 2 grams of azone and 1 gram of menthol, add appropriate amount of ethanol and ethylene glycol, and finally add water to form a 100ml water solvent. (those skilled in the art can determine the consumption of ethanol and ethylene glycol as required, such as the weight concentration of both can be controlled at about 20%).

[0046] Replace levobupivacaine hydrochloride with bupivacaine hydrochloride, ropivacaine or other bupivacaine compounds and derivatives respectively, and use laurocapram, azone or other azone compounds and derivatives respectively Instead of azone, the prepared transdermal and transmucosal local anesthetic analgesics have the same advantages and characteristics. The details are omitted!

[0047] In the process of using the transdermal and transmucosal local anesthetic analgesic, the inventor has also used various other local anesthetics including Enna cream. It takes at least half an hour for ...

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PUM

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Abstract

The invention relates to a transdermal transparent mucosa local anesthesia and analgesics and the preparation method of gelatinous formulation thereof. The technical problem to be solved by the invention is that how to provide the transdermal transparent mucosa local anesthesia and analgesics which takes effect quickly, has long drug action and can be used without injection as well as the preparation method of gelatinous formulation thereof. The transdermal transparent mucosa local anesthesia and analgesics comprises bupivacaine type compounds, azone type compounds and menthol. The bupivacaine type compounds contain Bupivacaine HCL, Levobupivacaine HCL, Ropivacaine and ramification thereof. The azone type compound contains azone, Laurocapram and ramification thereof. The transdermal transparent mucosa local anesthesia and analgesics has the advantages of rapid drug effect, strong action, maintenance for long time, fewer side effects, and so on. The transdermal transparent mucosa local anesthesia and analgesics is suitable for anesthesia and reliving pain during the surgery of human skin, mucosa and when in examination by apparatus, and also can be applied to symptomatic treatment of all kinds of chronic and acute pain of skin affection and mucosa affection.

Description

technical field [0001] The invention relates to a local anesthetic analgesic, in particular to a transdermal and transmucosal local anesthetic analgesic containing bupivacaine compounds, azone compounds and menthol and a preparation method thereof. Background technique [0002] The topical anesthetic EMLA cream (EMLA cream) invented by Astila Company in Sweden is an oil-in-water preparation: 1 g of EMLA cream contains 25 mg of lidocaine hydrochloride (Lidocaine Hydrochloride) and 25 mg of prilocaine (Prilocaine HCL). This drug can penetrate the complete skin, and there is no need for injection when administering the drug, which eliminates the pain of acupuncture when administering the drug. Compared with the previous injection of local anesthetics, it has made great progress. In the past 20 years, it has been widely used all over the world, and Chinese pharmaceutical companies are still imitating it. [0003] But this medicine has many disadvantages: the maximum depth of an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/445A61K31/55A61K31/133A61P23/02
Inventor 谭国梁谭晓雯
Owner 珠海市横琴灵敏科技有限公司
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