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Kusnezoff monkshood root esculin microemulsion and its preparation

A technology of aconitin and microemulsion, which is applied in the direction of anti-inflammatory agent, emulsion delivery, non-central analgesic, etc., and can solve the problems that nasal spray is not suitable for long-term storage at room temperature, etc.

Inactive Publication Date: 2008-04-02
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when stored in this environment for a long time, aconitin is easily degraded and cannot meet the requirements of long-term storage at room temperature.
[0010] Although nasal cavity or skin administration is beneficial to improve the drug compliance and safety of aconitin, it is not suitable to be directly made into nasal spray or transdermal drug release patch (pressure-sensitive adhesive matrix water-insoluble patch) due to the influence of physicochemical properties. tablets or cataplasm matrix water-based patch)

Method used

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  • Kusnezoff monkshood root esculin microemulsion and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: preparation method of drug-containing microemulsion (1)

[0029] [Prescription Composition] Ingredients Dosage

[0030] Aconitin 0.5g

[0031] Oleic acid 4.0g

[0032] Cremophor RH40 20g

[0033] Labrosol 20g

[0034] Double distilled water 55.4g

[0035]

[0036] Made a total of 100g

[0037] [Preparation process] Heat oleic acid in a water bath at 40°C to dissolve, add aconitin; another take Cremophor RH40 to heat and dissolve, mix with Labrosol, add to the oil phase, and mix well; take double distilled water, slowly add to the oil phase and mix In the solution, stir while adding to obtain a transparent (slightly cloudy) microemulsion.

Embodiment 2

[0038] Embodiment 2: preparation method of drug-containing microemulsion (2)

[0039] [Prescription Composition] Ingredients Dosage

[0040] Aconitin 0.5g

[0041] Oleic acid 4.0g

[0042] Cremophor RH40 20g

[0043] Absolute ethanol 20g

[0044] Double distilled water 55.4g

[0045]

[0046] Made a total of 100g

[0047] [Preparation process] Labrosol is replaced by absolute ethanol, and the others are the same as in Example 1.

Embodiment 3

[0048] Embodiment 3: preparation method of drug-containing microemulsion (3)

[0049] [Prescription Composition] Ingredients Dosage

[0050] Aconitin 0.5g

[0051] Oleic acid 4.0g

[0052] Transcutol 20g

[0053] Labroso l 20g

[0054] Double distilled water 55.4g

[0055]

[0056] Made a total of 100g

[0057] [Preparation process] with embodiment 1.

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Abstract

The present invention discloses a Bulleyaconitine A microemulsion and the preparing method. The Bulleyaconitine A is dissolved in oil phase. Emulsifier, assistant emulsifier and other additives are added. A microemulsion which is transparent or is with slightly turbid light and is with a particle size of less than 100 nm is prepared. Compared with material drug of Bulleyaconitine A, the chemical stability and mucosa permeance capability of the drug-containing microemulsion are significantly improved. The Bulleyaconitine A microemulsion is used as releasing vector and is combined with an excipient which is acceptable on pharmacy. An appropriate preparing method is used to prepare a nasal cavity preparation which is high in biological absorption degree, safe, stable and convenient and various paper release formulation preparation. The present invention is used for the treatment of various pains.

Description

technical field [0001] The invention relates to the preparation technology of aconitin microemulsion and its preparation. Dissolve aconitin in the oil phase, add emulsifier, co-emulsifier and other additives to prepare transparent or slightly hazy, particle size in [0002] Microemulsions below 100nm can improve the long-term storage stability and mucosal penetration of drugs, and improve the bioavailability of nasal cavity or transdermal drug delivery preparations. Background technique [0003] Chronic pain is characterized by recurrent attacks, long duration, and varying degrees of mildness and severity. Therefore, clinical drugs need to have long-lasting anti-inflammatory and analgesic effects and good safety. At present, according to the characteristics of chronic pain, the principles of clinical medication can be summarized as (1) administering drugs on time to maintain the concentration of the drug in the blood and control the pain stimulation below the pain range; (2...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/439A61K9/72A61K9/70A61P29/00
Inventor 刘玉玲吴晓辉夏学军王洪亮周圆汪仁芸金笃佳
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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