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A kind of surface anesthesia drug composition, microemulsion and its preparation method and application

A technology of topical anesthesia and composition, which is applied in the direction of drug combination, anesthetic, pharmaceutical formula, etc., to achieve the effect of good transdermal effect, fast onset of anesthesia and narrow distribution

Active Publication Date: 2019-05-28
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, as far as the inventor knows, there has not been a report on how to configure a drug that contains lidocaine and can solve the above three surface anesthesia problems.

Method used

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  • A kind of surface anesthesia drug composition, microemulsion and its preparation method and application
  • A kind of surface anesthesia drug composition, microemulsion and its preparation method and application
  • A kind of surface anesthesia drug composition, microemulsion and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 1 drug preparation

[0044] 1.1 Place Zanthoxylum bungeanum, LMZ, Herba Asarum and Gurixiang respectively in 4 times the amount (weight) of 70% (volume fraction) ethanol solution, and carry out reflux extraction for 1 hour to obtain Zanthoxylum bungeanum extract, LMZ extract, saponin extract, Xin extract and Jiulixiang extract.

[0045] Each of the obtained extracts is spray-dried until the water content is below 8%, and the corresponding dry powder of the extracts is obtained.

[0046] Select the pharmaceutical composition according to Table 1.

[0047] Table 1

[0048]

[0049]

[0050] Wherein, "·" indicates that the corresponding component is contained, and no "·" indicates that the corresponding component is not contained. The addition amount of each component in each group in the table is all the same amount.

[0051] 1.2 Preparation of microemulsion

[0052] The compositions corresponding to each group in Table 1 were respectively placed in oleic acid ...

Embodiment 2

[0061] Although the results of Example 1 show that lidocaine, dezocine, scopolamine and dry powder of Liangmianzhen extract have synergistic effects, the influence of the addition ratio of each component on the experimental results was not investigated. The inventor guesses that its matching ratio may also be an important influencing factor. Therefore, according to the formula of Table 3, the inventor has carried out further experiment.

[0062] table 3

[0063]

[0064] In Table 3, each component is expressed in parts by weight, such as "0.5" means 0.5 parts.

[0065] The pharmaceutical composition in Table 3 was prepared into a microemulsion according to the preparation method of Example 1, and the drug effect was evaluated according to the same experimental method as in Example 1, and the results are shown in Table 4.

[0066] Table 4

[0067]

[0068] As shown in Table 4, the effect of groups 5-8 is obviously due to groups 1-4, which suggests that the addition rat...

Embodiment 3

[0070] On the basis of Examples 1 and 2, we further investigated the effect of the pharmaceutical composition on shivering after anesthesia.

[0071] We coated the microemulsions obtained in groups 5-8 in Example 2 on the torsos of mice as experimental groups 1-4, respectively, and group 1 in Example 1 as a control group to investigate the incidence of shivering. In this experiment, there were 30 mice in each group. The results are shown in Table 5.

[0072] table 5

[0073]

[0074] It can be seen from Table 5 that the pharmaceutical composition of the present invention can effectively avoid the occurrence of shivering after anesthesia.

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Abstract

The invention provides surface anesthesia medicine composition. The medicine composition is prepared from components in parts by weight as follows: 2-3 parts of lidocaine, 0.5-1 part of dezocine, 1-2parts of scopolamine and 0.3-0.5 parts of a radix zanthoxyli ethanol extract. The invention also provides a corresponding preparation of the medicine composition, a preparation method of the preparation as well as an application of the medicine composition in preparation of a surface anesthesia medicine. The medicine composition has the effects that the medicine composition takes anesthesia effectquickly, has long anesthesia holding time and can prevent shiver after anesthesia. The obtained microemulsion has small particle size, narrow particle size distribution and good transdermal effects.The medicine composition has good prospects in clinical application of surface anesthesia.

Description

technical field [0001] The invention belongs to the technical field of anesthetics, relates to the technical field of topical anesthetics, in particular to a topical anesthetic composition, a microemulsion and a preparation method and application thereof. Background technique [0002] Our country has a long history in the use of anesthetics. In the 2nd century AD, Hua Tuo invented "Mafeisan" and performed abdominal surgery; in 652 AD and 1596 AD, Sun Simiao and Li Shizhen recorded that datura flower had anesthetic effect; , Chuanwu and Tiannanxing, etc. composed of anesthetics. [0003] One of the developmental symbols of modern anesthetics is the use of cocaine by Carl Koller in 1884 for local anesthesia of the eye. Subsequently, N. Lofgren and B. Lundquist synthesized lidocaine, and Boaf Ekenstarn synthesized ropivacaine, opening a new chapter in the research of anesthetics. [0004] Compared with acupuncture and injection anesthesia, topical anesthesia refers to a meth...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/758A61K9/107A61P23/00A61K31/167A61K31/135A61K31/46
CPCA61K9/1075A61K31/135A61K31/167A61K31/46A61K36/758A61K47/44A61P23/00A61K2300/00
Inventor 肖红银燕李俊杨邦祥刘慧
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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