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Microemulsion containing matrine

A technology of matrine and microemulsion, which is applied in the field of medicine, can solve the problems of low drug concentration in target organs, low drug skin penetration rate, and short half-life of oral preparations, so as to prolong circulation time, promote drug absorption, and facilitate industrial production Effect

Inactive Publication Date: 2007-07-18
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, injections have problems such as poor targeting and low drug concentration in target organs; oral preparations have short half-life, high gastrointestinal side effects, and significant first-pass effects; conventional transdermal preparations also have short action time and frequent administration. Disadvantages such as frequent and low drug skin penetration rate

Method used

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  • Microemulsion containing matrine
  • Microemulsion containing matrine
  • Microemulsion containing matrine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1 prepares matrine microemulsion

[0022] Formula and ratio:

[0023] Matrine 1g Isopropyl myristate 6g

[0024] Tween 805g Deionized water 34g

[0025] Phospholipid 4g prepared drug-containing microemulsion 50g

[0026] The preparation method is:

[0027] 1. High-pressure homogenization method, mixing deionized water and Tween 80 as (I) phase, mixing isopropyl myristate and phospholipids as (II) phase, dissolving matrine into (II) phase as phase (II) For the internal phase of the drug, mix the internal phase containing the drug with the phase (I) under continuous stirring, and homogenize the mixture for 3-5 times under the homogeneous condition of the primary valve pressure of 60-70 bar and the secondary valve pressure of 600-700 bar , to obtain drug-containing microemulsion, the drug-containing particle size distribution of Sophora flavescens microemulsion is detected by dynamic light scattering method, the results are shown in Figure 1, the microemulsi...

Embodiment 2

[0029] Embodiment 2 prepares matrine microemulsion

[0030] Formula and ratio:

[0031] Matrine 2g Oleic Acid 12g

[0032] Tween 206g Deionized water 50g

[0033] Caprylic acid / capric acid macrogol glyceride 10g prepared drug-containing microemulsion 80g

[0034] The preparation method is:

[0035] 1. Manual drop method, mix deionized water and Tween 20 as (I) phase, mix caprylic / capric macrogol glyceride and oleic acid as (II) phase, dissolve matrine into (II) In the phase, it is the drug-containing internal phase, and the drug-containing internal phase is added dropwise at a speed of 1ml / min under continuous stirring at 40°C to form a clear drug-containing microemulsion. The particle size distribution is detected by the dynamic light scattering method, and the results are shown in Figure 3. The particle size range of the microemulsion is about 100nm (90-110nm), the particle size is uniform, and the appearance is clear.

[0036] 2. Ultrasonic emulsification method, mixin...

Embodiment 3

[0037] Embodiment 3 prepares matrine microemulsion

[0038] Formula and ratio:

[0039] Matrine 4g ethyl acetate 15g

[0040] Tween 8010g deionized water 55g

[0041] 6g of phospholipids prepared 100g of drug-containing microemulsion

[0042] The preparation method is:

[0043] 1. Ultrasonic emulsion method, mixing deionized water and Tween 80 as (I) phase, miscible ethyl acetate and phospholipids as (II) phase, dissolving matrine into (II) phase as drug-containing phase, under continuous stirring, the drug-containing internal phase and (I) phase are miscible, and the mixture is ultrasonically emulsified for 30 min under a power of 250w to obtain a drug-containing microemulsion. The drug-containing particle size distribution of the Sophora flavescens microemulsion is dynamically The light scattering method is used for detection, and the results are shown in Figure 5. The particle size range of the microemulsion is about 100nm (90-110nm), the particle size is uniform, and t...

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Abstract

A microemulsion of matrine with high biologic utilization rate and stability is proportionally prepared from matrine, emulsifier, emulsifying aid, oil phase and water phase. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to the technical field of medicine, and is a new dosage form of matrine - microemulsion and a preparation method thereof. Background technique [0002] Matrine is a quinolizidine alkaloid extracted from traditional Chinese medicine Sophora flavescens, Sophora flavescens, and Sophora flavescens. regulation of biological responses. Matrine has injections, tablets, capsules, liposomes, gels and other dosage forms. Matrine injections are often used to treat diseases such as hepatitis B, viral hepatitis, and tumors; matrine oral preparations have the ability to enhance the body's anti-cancer ability, reduce chemotherapy toxicity and other effects; transdermal administration of matrine can treat skin allergic diseases, improve skin scar tissue hyperplasia, etc. However, injections have problems such as poor targeting and low drug concentration in target organs; oral preparations have short half-life, high gastrointestinal side effects...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61K9/107A61K47/44A61K47/34A61K47/24A61K47/14A61P1/16A61P7/10A61P9/06A61P31/04A61P31/14A61P31/20A61P29/00A61P35/00A61P37/02A61P37/08A61K47/26
Inventor 胡晋红赵永哲刘继勇李凤前
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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