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Combination of ligusticum lactone, preparation method and application

A technology of ligustilide and its composition, which is applied in the field of ligustilide composition and its preparation, can solve the problems of instability of ligustilide, difficulty in preparation and inability to learn from it, and reduce microvascular leakage, reduce Mortality rate, effect of shortening ear-eye cycle time

Inactive Publication Date: 2005-11-16
北京九龙制药厂
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] The above method for protecting ligustilide, except the 3 method is unknown, the remaining two methods are difficult to use in the production of industrialized preparations, and the 3 method cannot be used for reference because there is no prescription
[0020] Difficulty in preparing stable ligustilide preparations due to instability of ligustilide
At present, there is no ligustilide preparation available for clinical application

Method used

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  • Combination of ligusticum lactone, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 295g of ligustilide was dissolved in 2680g of soybean oil, and conventional soft capsule preparation techniques were used to prepare soft capsules with a loading capacity of 250 mg. After being placed at room temperature for one and a half years, it was shown that the contents were basically stable. The results are shown in Table 3.

[0042] placement conditions

Embodiment 2

[0044] Add 5kg of soybean oil (by vacuum pumping) into the batching tank, heat up to 80°C, add 0.6kg of lecithin, stir for 5-8 minutes, add 250g of ligustilide after the lecithin is completely dispersed, and turn on the circulation pump. Mix the oil and glycerin in the batching tank in proportion, and start high-speed stirring. Add sodium hydroxide solution (1moL / L) to adjust the pH to 6.0-7. Stop stirring, add filtered water for injection to the full amount of 50000ml, stir evenly, it is primary emulsion, measure glycerin content, pH value (glycerol content 95%-105%, pH value: 6.0-7.0). Cool the colostrum to 55-60°C, start the low-pressure homogenizer, let the colostrum circulate and homogenize in the machine, start the high-pressure homogenizer, let the emulsion enter the machine, circulate and homogenize, repeat homogenization 10 times. After the first 9 times of homogenization, the emulsion is cooled to about 50-55°C through a heat exchanger. After the 10th time of homoge...

Embodiment 3

[0047] 60g of ligustilide is dissolved in 3000g of soybean oil, and the technology is used to prepare soft capsules with a filling capacity of 250mg. After being placed at room temperature for one and a half years, it was shown that the contents were basically stable. The results are shown in Table 5.

[0048] placement conditions

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Abstract

A ligustilide composition is prepared from ligustilide and medicinal plant oil through proportionally mixing, stirring, wrapping by lecithin microspheres or softgel, and preparing emulsion or capsule. Its medical application is also disclosed.

Description

technical field [0001] The invention relates to a ligustilide composition and a preparation method and application thereof, in particular to a ligustilide emulsion and a soft capsule and a preparation method and application thereof. Background technique [0002] The structure and physical properties of ligustilide: [0003] Structural formula: [0004] [0005] Molecular formula and molecular weight: C 12 h 14 o 2 190 with 6 unsaturation. [0006] Chemical name: 3-butylene-4,5-dihydrophthalide [0007] English chemical name: 3-butylidene-4, 5-dihydrophthalide [0008] English name: ligustilide [0009] Property description: yellowish oily substance with fragrance, boiling point 168~169℃ / 6mmHg. Soluble in n-hexane, cyclohexane, petroleum ether, ether, ethyl acetate, methanol, etc. [0010] The chemical structure of ligustilide is phthalide, and there is a lively butenyl group connected to the 3-position, which are all chemically unstable factors. Under the condit...

Claims

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Application Information

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IPC IPC(8): A61K31/365
Inventor 刘俊魏玉平
Owner 北京九龙制药厂
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