Power for intravenous injection with liver-protecting action, and its preparation and quality control method

A powder injection and action technology, which is used in the field of intravenous injection powder injection with liver-protecting effect and its preparation and quality control, can solve the problems of unsatisfactory release and bioavailability discovery results, extreme shortage of drugs, and influence on release.

Inactive Publication Date: 2005-12-21
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These preparations are mainly silymarin extracts or free silybin, and the results of their release and bioavailability tests were found to be unsatisfactory
Some preparations cannot be effectively disintegrated at all, affecting release
There are literature records: silymarin water-soluble derivatives such as silibinin. Meglucoside salt, silibinin · phthalic acid monosodium salt injection; silymarin solubility in non-aqueous solvents and composite solvents. : Polyethylene glycol-ethanol-water (5:2:3) can dissolve 16mg / ml in a mixed solvent, which can be used as a solvent for injections; however, when the prepared injection is diluted with water until the water content accounts for more than 75%, it will appear turbid , so it can only be used for intramuscular injection, not intravenous injection
Chinese patent 02125823 discloses silymarin injection containing cyclodextrin or its derivatives. Although it has fast drug absorption and high bioavailability, due to the poor solubility and stability of silybin meglumine salt in water, clinical The application is very limited, and there is no injection of milk thistle available on the market
[0005] At present, there are many liver injury diseases in China, and the market for therapeutic drugs is large, especially for injections, where drugs are in short supply. Glycyrrhizic acid injections are mainly used in a large number of clinical applications, but their curative effect is limited.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 produces.

[0032] Experimental animals Wistar rats were provided by the Medical Experimental Animal Center of Shandong Medical University.

[0033] Test Method and Results

[0034] 60 male common-grade Wistar rats, with a body weight of 201 ± 10g, were randomly divided into 6 groups, 10 in each group: control group, model group, positive drug group (silymarin injection), large dose group of the present invention, and the present invention. dosage group and the small dosage group of the present invention. Establishment of liver fibrosis model: Rats were subcutaneously injected with 40% carbon tetrachloride peanut oil solution 0.5ml / 100g for the first time in the hind legs, and then changed to 0.3ml / 100g, twice a week for a total of 6 weeks. The animals were fed a high-fat diet (79.5% rice flour + 20% lard + 0.5% cholesterol) for the first two weeks, and pure cornmeal (mixed with 0.5% cholesterol) for the next 4 weeks. Animals were administered by intrape...

Embodiment 2

[0166] Silibinin Meglumine 50g

[0167] Mannitol 50g

[0168] Weigh the prescribed amount of mannitol, add an appropriate amount of water for injection and stir to dissolve, put the amount of silibinin meglumine into 10 times the amount of water for injection, stir, dissolve, and centrifuge to obtain a supernatant, which is mixed with mannitol solution Merge, mix, pre-filter, the filtrate is then passed through an ultrafiltration column with a molecular weight of 5000-10000, ultrafiltration, ultrafiltrate filling, freeze-drying to obtain about 100g of freeze-dried powder, capping, quality inspection, packaging, that is, powder needle.

[0169] The quality control method is:

[0170] (1) Identification of silybin meglumine

[0171]Take 500 mg of this product, dissolve it with methanol sonication, concentrate the solution to 10 ml, centrifuge, and take the supernatant as the test solution; take an appropriate amount of silibinin reference substance, add methanol to make a sol...

Embodiment 3

[0177] Silybin Meglumine 30g

[0178] Mannitol 70g

[0179] Weigh the prescribed amount of mannitol, add an appropriate amount of water for injection and stir to dissolve, put the amount of silibinin meglumine into 30 times the amount of water for injection, stir, dissolve, and centrifuge to obtain a supernatant, which is mixed with the mannitol solution Merge, mix, pre-filter, the filtrate is then passed through an ultrafiltration column with a molecular weight of 5000-10000, ultrafiltration, ultrafiltrate filling, freeze-drying to obtain about 100g of freeze-dried powder, capping, quality inspection, packaging, that is, powder needle.

[0180] The quality control method is:

[0181] (1) Identification of silybin meglumine

[0182] Take 100mg of this product, dissolve it with methanol sonication, concentrate the solution to 5ml, centrifuge, take the supernatant as the test solution; take an appropriate amount of silibinin reference substance, add methanol to make a solutio...

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Abstract

The present invention discloses a powder injection for intravenous injection for curing several diseases of liver damage with obvious therapeutic effect. Said powder injection has the action of protecting liver, its main component is silibinin-N-methylglucamine whose content is 20-500 mg/g.

Description

technical field [0001] The invention relates to a powder for injection with hepatoprotective effect for treating various liver damage diseases, a preparation method and a quality control method thereof. In particular, it relates to a silibinin meglumine salt powder injection for treating various liver injuries. Background technique [0002] The liver is an important metabolic organ of the human body, with complex structures and functions, and is susceptible to various pathogens, toxins and immunopathology. Viruses, chemicals, drugs, alcohol, and autoimmunity can all cause liver damage. Viral hepatitis, in particular, is distributed all over the world. Because it is difficult to cure and has a wide range of harm, it is also called "the three chronic diseases of the century" together with cancer and AIDS; 130 million. With the rapid development of the pharmaceutical industry, drug-induced hepatitis has increasingly become a major worldwide problem. Long-term medication or h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357
Inventor 赵志全
Owner LUNAN PHARMA GROUP CORPORATION
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