Oxymatrine nano preparations for liver cell targeting injection and preparation thereof

A technology of nano-preparation and matrine, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, antiviral agents, etc., can solve the problems of increased adverse drug reactions, decreased therapeutic effect, and high dosage problem, achieve the effect of increasing residence time, improving curative effect and slowing release

Inactive Publication Date: 2008-09-17
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Matrine injection has the problems of short half-life and low distribution in the target organ (liver): the drug is eliminated quickly after entering the body, and the T1 / 2β of healthy people is only 130.4min; the prototype drug and its metabolites are mainly distributed in the kidney, enters the liver in very small amounts
In order to ensure the curative effect, the clinical dosage is higher, which will increase the adverse reactions of the drug
Oral preparations are easy to use, but about 86.8% of matrine will be metabolized into matrine with relatively low efficacy and large side effects under the action of intestinal flora, which will reduce the therapeutic effect

Method used

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  • Oxymatrine nano preparations for liver cell targeting injection and preparation thereof
  • Oxymatrine nano preparations for liver cell targeting injection and preparation thereof
  • Oxymatrine nano preparations for liver cell targeting injection and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A. Matrine 1g

[0028] B. Lecithin 3.6g

[0029] C. Stearic acid 0.4g

[0030] D. Mannitol 4g

[0031] Stirring speed: 1000rpm

[0032] Stirring temperature: 60°C

[0033] Dropping speed: 0.1ml / min

[0034] Dispersion liquid temperature: 0~4℃

[0035] Weigh matrine, lecithin, stearic acid, add 10ml of ethanol, heat to dissolve, slowly drop into heated water with stirring, stir to evaporate the solvent, form a colloidal solution, disperse with ice water to form a SLN suspension, 0.22 Filter through a microporous membrane, add mannitol to mix, dilute to 100ml, sonicate, freeze-dry and store.

[0036] After adding water to the obtained matrine nano freeze-dried powder, the particle size distribution range is 104±34nm, the surface potential is -32.6mV, and the encapsulation rate is 81%. The in vitro release study was carried out by dialysis, and the release time was as long as 12 hours, and about 80% was released in 8 hours.

[0037] After administration of 100 mg / k...

Embodiment 2

[0045] Embodiment 2 (No. 2-18)

[0046] Preparation method of matrine nano-preparation for liver cell targeting injection (see Table 3).

[0047] Table 3 Preparation method of matrine nano-preparation for liver cell targeting injection

[0048]

[0049] Specific steps are as follows:

[0050] Weigh matrine, lecithin, stearic acid, add 10ml of ethanol, heat to dissolve, slowly drop into heated water with stirring, stir to evaporate the solvent, form a colloidal solution, disperse with ice water to form a SLN suspension, 0.22 Filter through a microporous membrane, add mannitol to mix, dilute to 100ml, sonicate, freeze-dry and store.

[0051] The particle size of the prepared matrine nano-preparation for liver cell targeting injection (see Table 4).

[0052] The particle size of matrine nano-preparation for liver cell targeting injection prepared in table 4

[0053]

Embodiment 3

[0054] Embodiment 3 (No. 19-25)

[0055] Preparation method of matrine nano-preparation for liver cell targeting injection (see Table 5).

[0056]Table 5 Preparation method of matrine nano-preparation for liver cell targeting injection

[0057]

[0058] Weigh A, B, C, add 10ml of ethanol, heat to dissolve, slowly drop into the heated water containing E under stirring, stir and evaporate the solvent to form a colloidal solution, disperse with ice water to form a SLN suspension, 0.22μ micro Filter through a pore filter, add D to mix, dilute to 100ml, sonicate, freeze-dry and store.

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Abstract

The invention relates to medicine preparation field in particular to hepatocyte targeting oxymatrine nanometer powder injection and the preparation method for the treatment of hepatitis b, severe hepatitis and severe jaundice hepatitis. The invention is characterized in that the oxymatrine nanometer powder injection comprises oxymatrine, stearic acid, lecithin for injection, glycyrrhetinic acid, surfacetant and frozen dried adjunct. After dissolution and heating, the organic phase is formed; the solvent is agitated and evaporated in the heating condition to get the colloidal solution; then after agitating and filtering, the even nanometer grade dispersion; after the frozen dried adjunct is added, the mixing ultrasounding and frozen storage is made; according to the preparation course method, the discharging of medicine is reduced; the time that the oxymatrine stay in the body is prolonged; the medicine tends to and is centralized to the liver; therefore, the therapeutic effect is improved. The invention has the advantages that the preparation is simple; the sustained release effect is obvious; the time that the medicine staying in the body is raised; the liver forward effect is excellent; the therapeutic effect is outstanding.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to matrine nanopowder injection for liver cell-targeted injection for treating hepatitis B, severe hepatitis and severe icteric hepatitis and a preparation method thereof. Background technique [0002] Matrine is the main active ingredient of traditional Chinese medicine Sophora flavescens, mountain bean root and bitter bean. Studies have confirmed that it has a significant effect in the treatment of chronic hepatitis B, can directly inhibit the replication of hepatitis B virus, and can effectively inhibit abnormal apoptosis of liver cells. Block and reduce the degree of liver fibrosis, and have a certain effect on severe hepatitis and severe icteric hepatitis. The main indicators are better than or equal to alpha interferon, but the price is much lower than interferon. [0003] The existing dosage forms of matrine mainly include injections (powder injection, water inject...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K31/56A61K9/14A61K47/24A61P1/16A61P31/12
Inventor 孙洁胤周芝芳刘放郑晓亮
Owner ZHEJIANG ACAD OF MEDICAL SCI
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