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Strychnine-hydroxypropyl-beta-cyclodextrin liposome, preparation method and applications thereof

A technology of strychnine and hydroxypropyl, applied in the field of strychnine-hydroxypropyl-β-cyclodextrin liposome and its preparation, can solve the problem of fast metabolism, low bioavailability, blood drug concentration Low-level problems, to achieve the effect of simple preparation method, reduce hemolysis, and increase drug concentration

Inactive Publication Date: 2013-07-31
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to overcome the above-mentioned shortcomings and deficiencies of the prior art, the object of the present invention is to solve the shortcomings of strychnine in vivo metabolism, low blood concentration, low bioavailability, etc., to provide a strychnine-hydroxypropyl- β-cyclodextrin liposomes can increase the drug loading capacity, prolong the elimination half-life of strychnine, reduce the dissociation of inclusion complexes in the transfer process in vivo, improve stability, and realize the inclusion complexes in the lymphatic system. Targeting, reducing its toxic and side effects on the heart and central nervous system, reducing the hemolysis of inclusion complexes, and improving bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The formula of the strychnine-hydroxypropyl-β-cyclodextrin liposome of the present embodiment contains by weight ratio: 1.5 parts of strychnine, 2 parts of HP-β-cyclodextrin, 20 parts of soybean lecithin , Cholesterol 5 parts.

[0025] The preparation method of the strychnine-HP-β-CD inclusion complex liposome of the present embodiment comprises the following steps:

[0026] (1) Preparation of strychnine-HP-β-CD inclusion compound: Weigh 2 parts of HP-β-CD and dissolve them in distilled water to obtain solution IV; mix 1 part of strychnine with a mass ratio of 1:1 dissolved in absolute ethanol to obtain solution V; under constant stirring by a magnetic stirrer, solution V was added dropwise to solution IV, and clathration was performed in a constant temperature water bath at 60°C, and stirring was continued for 2 hours after the dropwise addition to fully clad After combining, refrigerate and pre-freeze, and freeze-dry in a freeze dryer to obtain a white powder strychn...

Embodiment 2

[0035] The formula of the strychnine-hydroxypropyl-β-cyclodextrin liposome of this embodiment contains by weight ratio: 3 parts of strychnine, 4 parts of HP-β-cyclodextrin, 80 parts of soybean lecithin , Cholesterol 10 parts.

[0036] The preparation method of the strychnine-HP-β-CD inclusion complex liposome of the present embodiment comprises the following steps:

[0037](1) Preparation of strychnine-HP-β-CD inclusion compound: Weigh 4 parts of HP-β-CD and dissolve in distilled water to obtain solution IV; 1 part of strychnine with a mass ratio of 1:1 dissolved in absolute ethanol to obtain solution V; under constant stirring by a magnetic stirrer, solution V was added dropwise to solution IV, and clathration was performed in a constant temperature water bath at 70°C, and stirring was continued for 2 hours after the dropwise addition to fully clad After combining, refrigerate and pre-freeze, and freeze-dry in a freeze dryer to obtain a white powder strychnine-HP-β-CD inclus...

Embodiment 3

[0045] The formula of the strychnine-hydroxypropyl-β-cyclodextrin liposome of the present embodiment contains by weight ratio: 4 parts of strychnine, 15 parts of HP-β-cyclodextrin, 180 parts of soybean lecithin 20 servings of cholesterol.

[0046] The preparation method of the strychnine-HP-β-CD inclusion complex liposome of the present embodiment comprises the following steps:

[0047] (1) Preparation of strychnine-HP-β-CD inclusion compound: Weigh 15 parts of HP-β-CD and dissolve them in distilled water to obtain solution IV; mix 3 parts of strychnine with a mass ratio of 1:1 dissolved in absolute ethanol to obtain solution V; under constant stirring by a magnetic stirrer, solution V was added dropwise to solution IV, and clathration was performed in a constant temperature water bath at 70°C, and stirring was continued for 2 hours after the dropwise addition to fully clad After combining, refrigerate and pre-freeze, and freeze-dry in a freeze dryer to obtain a white powder ...

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Abstract

The present invention discloses a strychnine-hydroxypropyl-beta-cyclodextrin liposome, which contains, by weight, 0.5-2 parts of strychnine, 2-20 parts of a strychnine-HP-beta-cyclodextrin inclusion compound, 20-200 parts of soybean lecithin, and 5-20 parts of cholesterol. The present invention further discloses a strychnine-hydroxypropyl-beta-cyclodextrin liposome preparation method, which comprises: carrying out inclusion on strychnine with hydroxypropyl-beta-cyclodextrin, and then preparing into the liposome. According to the present invention, drug loading capacity is improved, an elimination half-life of the strychnine is prolonged, stability is improved, lymphatic system targeting is achieved, toxic and side effects on heart and central nervous system are reduced, and bioavailability is improved.

Description

technical field [0001] The invention relates to the preparation technology of anti-inflammatory and analgesic drugs, in particular to a strychnine-hydroxypropyl-β-cyclodextrin liposome and its preparation method and application. Background technique [0002] Strychnine is the active ingredient of Strychnos nux-vomica L or SPierriana A.W.Hill, a plant of the family Strychnosaceae. It is an effective drug for the treatment of rheumatoid arthritis. Oral administration of strychnine can easily cause abdominal pain and diarrhea. Long-term use of strychnine can damage renal tubular epithelial cells, cause renal function damage, and can excite the central nervous system to produce heart and central side effects. At the same time, it metabolizes quickly in the body and has low bioavailability. The promotion of sub-alkaline in clinical application. [0003] Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a hydroxyalkyl derivative of β-cyclodextrin (β-CD). It has an excellent enveloping ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/40A61K31/475A61P29/00
Inventor 潘娅
Owner SOUTH CHINA UNIV OF TECH
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