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Toad extract liposome preparation for injection and its preparing method

A technology of liposome preparation and extract, which is applied in the field of pharmaceutical preparations for injection, can solve the problems of low effective concentration and achieve good therapeutic effect and uniform particle size distribution of the product

Inactive Publication Date: 2005-08-03
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of its low effective concentration, its use is limited

Method used

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  • Toad extract liposome preparation for injection and its preparing method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] prescription:

[0038] Lecithin 5 grams, cholesterol 1 gram; bufalin 1 gram.

[0039] Preparation Process:

[0040] Take lecithin, cholesterol and bufa fat-soluble extracts such as bufalin and dissolve them in 18ml of chloroform, then remove the chloroform under reduced pressure at a temperature of 40°C, add 100ml of water for injection, treat in an ultrasonic water bath for 15 minutes, homogenize under high pressure, and filter , freeze-dried using conventional methods.

[0041] Its particle size distribution is as figure 1 , figure 1 It is the particle size distribution figure measured by the laser diffraction method, as can be seen from the figure, the average particle size is 80nm, and no particle greater than 200nm is seen.

Embodiment 2

[0043] prescription:

[0044] Lecithin 8 grams, cholesterol 1 gram, toad water-soluble extract 0.5 grams, dextran 10 grams.

[0045] Preparation Process:

[0046] After dissolving lecithin and cholesterol with 15ml ethanol, drop by drop into TongN 2 200ml of bufa lipid aqueous extract and dextran aqueous solution were dissolved with rapid stirring, filtered with 5u, 0.45u, 0.2u filter membranes, and then freeze-dried by conventional methods. The particle size distribution measured by the laser diffraction method is: the average particle size is 80nm, and no particle larger than 500nm is found.

Embodiment 3

[0048] prescription:

[0049] Part (A): 9 grams of lecithin, 2 grams of cholesterol, 1 gram of bufafolin, 0.5 gram of lipobufagenin, and 0.14 gram of cinobufagin.

[0050] Part (B): 5 grams of lecithin, 1 gram of cholesterol, 0.5 grams of toad water-soluble extract, 10 grams of dextran or 20 grams of mannitol.

[0051] Preparation Process:

[0052] (1) Dissolve all the materials in part (A) in chloroform, reduce the pressure on a water bath at 40°C, and remove the chloroform to obtain a drug-containing phospholipid film;

[0053] (2) After dissolving lecithin and cholesterol with ethanol, drop by drop into TongN 2 Rapidly stirred aqueous solution of bufa lipid aqueous extract and dextran aqueous solution or mannitol aqueous solution;

[0054] (3) Add the product of step (1) and step (2) into water, and stir under N 2 Dissolve, homogenize under high pressure, pass through a 0.45u, 0.2u filter membrane, and freeze-dry using a conventional method.

[0055] The average partic...

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Abstract

The toad extract liposome preparation for injection includes toad extract in effective amount, lecithin and cholesterol. Experiment shows that the preparation has toxicity obviously lower than available product, high treating effect, targeting treatment effect and homogeneous distribution of product grain size, and may be used in treating several kinds of tumor.

Description

technical field [0001] The invention relates to a pharmaceutical preparation containing toad extract, in particular to an injection pharmaceutical preparation containing toad extract. Background technique [0002] There are more than 250 kinds of anurans in the amphibian class, and they are widely distributed. Among them, the large number of toads and the black-orbited toad are relatively large. The extracts of its skin, skin glands and post-auricular glands are sweet, pungent and warm in nature. It has the functions of detoxification, detumescence, cardiac strengthening and pain relief. Indications of malignant sores, carbuncles, sore throat and other diseases. [0003] The main component of toad extract is cardiac glycosides, which can be hydrolyzed to obtain more than 10 kinds of bufogenins. Such as: Cinobufagin, Cinobufagin, Cinobufagin, Hydroxy-Cinobufagin, Cinobufagin. Indole derivatives: bufynine, bufamethine, 5-hydroxytryptamine, epinephrine, etc. For details, s...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K35/65A61P35/00
Inventor 贺芬侯惠民
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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