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Medicinal emulsion adapted for difficultly soluble medicine and method for preparing the same

A kind of active drug, water-insoluble technology, applied in the direction of emulsion delivery, etc., can solve the problems of poor uniformity, large side effects, complex active ingredients and so on

Inactive Publication Date: 2006-01-18
JC (WUXI) CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The "Chinese herbal medicine movement" in the 1970s brought Chinese medicine injections into a period of rapid development. The total number of related materials and reports reached 700 to 1,400. Left in the cold, left a bad impression on doctors and patients, now there are very few left
As for the compound Chinese medicine, because its active ingredients are very complex, so its emulsion varieties are very few.
In addition, most of the existing emulsions have large particle size and poor uniformity, so the side effects are relatively large and the curative effect is still unsatisfactory

Method used

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  • Medicinal emulsion adapted for difficultly soluble medicine and method for preparing the same
  • Medicinal emulsion adapted for difficultly soluble medicine and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0124] The preparation of embodiment 1 Mailuoning prescription medicinal material extract

[0125] Take 500 grams of honeysuckle honeysuckle, 500 grams of Dendrobium officinalis, 500 grams of Zhejiang Scrophulariaceae and 500 grams of Achyranthes bidentata, mix them thoroughly according to the process method of Chinese invention patent 92107848. filter. The secondary supernatants were combined, placed in an R501B Xinghai rotary evaporator (Wuxi Xinghaiwang Biochemical Equipment Co., Ltd.), and concentrated under reduced pressure at 70-80°C until semi-solid. Add ethanol for precipitation, let it stand overnight, take out the ethanol by pouring, and still use the R501B Xinghai rotary evaporator to recover the ethanol under reduced pressure at 45-55°C. After the residual alcohol is exhausted, it is extracted with ethyl acetate for 7 to 10 times, the extracts are combined, recovered in a water bath and the ethyl acetate is removed to obtain the medicinal material extract.

[012...

Embodiment 14

[0205] Example 14 Rabbit Ear Vascular Perfusion Test

[0206] Preparation of contrast Mailuoning injection: get the Mailuoning extract obtained by extracting in Example 1 (equivalent to 500 grams of raw medicinal material) and add 200 ml of fresh distilled water, heat and stir, cool, and filter. Add 4ml of Tween-80, stir, adjust the pH value to 8.8-9.2 with 20% NaOH solution, add fresh distilled water to 500ml to obtain the control Mailuoning injection.

[0207] Test method: Take a healthy rabbit (New Zealand white rabbit), anesthetize it with intravenous injection of Dongmianling (15mg / kg), fix it on its side, take a vascular clamp to clamp the root of the rabbit's ear to block the blood flow. Drip the Lok's solution from the central artery of the rabbit's ear, cut the peripheral vein, and flush out the blood in the blood vessel. Give Lok liquid. Record the number of Roxy droplets per minute for 5 minutes. Give the test samples respectively, record the outflow drops per mi...

Embodiment 17-24

[0222] The preparation of embodiment 17-24 emulsion 15-22

[0223] Prepare emulsions 15, 16, 17, 18, 19, 20, 21, and 22 according to the same method as in Example 10, except that 1 gram of Danshen extract, compound Danshen extract, Shengmai extract, and Shenmai extract are used , Bupleurum extract, Houttuynia cordata extract, winter plum extract or Xinnaojing extract to replace 1 gram of Mailuoning extract respectively.

[0224] Measure the particle diameter with the same method, and the average particle diameter of the measurement result is between 20-60nm. After being placed at 60°C for 10 days, the variation range of the average particle size is less than 10%.

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Abstract

The invention discloses an oil-in-water medicinal emulsion suitable for water-indissoluble medicaments which comprises, (1) 0.5-50 weight parts of active medicament, which contains water-indissoluble substance with a dissolvability of 0.001-10000mg / l of water at 25 deg. C, (2) 5-300 weight parts of emulsifying agent, (3) 0.5-200 weight parts of fatty oil, (4) 500-1500 weight parts of water. The disclosed medicinal emulsion has little side effect, and is especially suitable for extracts of traditional Chinese medicines.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an emulsion suitable for poorly water-soluble pharmaceutical ingredients, a preparation method and a use method thereof. Background technique [0002] Parenteral administration, especially intravenous administration, is one of the important ways for drugs to enter the body. Parenteral administration of poorly water-soluble drugs (including fat-soluble biomacromolecules) has always been one of the challenging topics for pharmacists. Insoluble drugs such as paclitaxel, cyclosporine, cortisone, griseofulvin, ibuprofen, diazepam, interleukin-2, etoposide and other direct injections have great side effects, which may lead to hemolysis, phlebitis, Hypersensitivity, organ failure and even death. Making emulsions can eliminate or alleviate these side effects, and can significantly increase the solubility of poorly water-soluble drugs and fat-soluble drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107
Inventor 程景才袁生良
Owner JC (WUXI) CO INC
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