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Composites medicine composition and application thereof

A composition and drug technology, applied in the field of compound pharmaceutical compositions containing ursolic acid and epalrestat, can solve the problems of low bioavailability, excessive metabolism, low activity and the like, achieve strong anti-proliferative activity, reduce The effect of producing toxic side effects and inhibiting the proliferation of cancer cells

Inactive Publication Date: 2018-11-02
FOSHAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, ursolic acid has low activity in the body, little absorption, fast metabolism and low bioavailability, these characteristics greatly limit its application

Method used

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  • Composites medicine composition and application thereof
  • Composites medicine composition and application thereof
  • Composites medicine composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: Adopt K562 cell screening optimization ursolic acid UA and epalrestat EPA compound pharmaceutical composition

[0020] Take the cells in the logarithmic growth phase and inoculate 3×10 4 Cells / well were placed on a 96-well plate, and after 6 hours of growth, the supernatant was discarded by centrifugation, and then administered according to the following groups: Tumor cells were divided into no drug group and drug-added group, and the drug-added group was composed of UA and EPA single drugs Group, UA and EPA combined drug groups with different molar ratios, set 4-6 duplicate wells in each group, culture for 24 hours, discard the supernatant, add 100 μl of MTT (tetrazolium salt) serum-free culture medium containing 0.5 mg / ml for culture After 4 hours, add 100 μl of DMSO (dimethyl sulfoxide), place on a micro-oscillator to vibrate for 10 minutes, and then place on a microplate reader to detect the OD value at 570 nm. Results The inhibition rate of tumor cel...

Embodiment 2

[0027] Embodiment 2: UA and EPA joint administration effect analysis

[0028] Based on the Median-effect Principle (moderate effect principle or Chou-Talalay combined index method), the dose-response curve and the combined index curve (fa-C curve) under different effects were drawn using CombiDrug statistical software. The relationship between the effect and the combination index quantitatively evaluates whether there is a synergistic, antagonistic or additive relationship between the two drugs. Specific steps are as follows:

[0029] The drug effect is the inhibition rate (fa)=1-(the average OD570 value of the test group / the average OD570 of the tumor cell blank control group) according to the intermediate effect equation fa / fu=(D / Dm) m , take the logarithm logfa / fu=mlogD–mlogDm on both sides, set a=-mlogDm, b=m, x=logD, y=logfa / fu, and substitute into the intermediate effect equation to get y=bx–a; where fa is the drug effect , fu=1–fa, D is the drug concentration, m is th...

Embodiment 3

[0035] Embodiment 3: ursolic acid UA and epalrestat EPA compound pharmaceutical composition are made tablet according to following prescription:

[0036] The prescription is as follows:

[0037]

[0038] The preparation process is as follows:

[0039]Drug and auxiliary materials are respectively passed through 80 mesh sieves, ursolic acid is fully mixed with 48 grams of microcrystalline cellulose and 12 grams of carboxymethyl starch sodium, 10% starch slurry is used as soft material, granulated with 18 mesh sieves, and dried at 60°C , get particle 1. Epalrestat was fully mixed with 24 grams of microcrystalline cellulose, 15 grams of starch and 8 grams of sodium carboxymethyl starch, 10% starch slurry was made into a soft material, granulated with a 18-mesh sieve, and dried at 60° C. to obtain Granule 2. According to the principle of equal increase, fully mix granule 1 and granule 2, sieve the granules with 16 mesh, add magnesium stearate, mix well, and compress into table...

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Abstract

The invention belongs to the field of natural medicines and discloses a composites medicine composition and the application thereof. The composite medicine composition comprises active components, namely ursolic acid and an aldose reductase inhibitor epalrestat in a mole ratio of 1-1 to 1-8. With the combination of the two components, the composites medicine composition has good application in synergetic treatment on leukemia.

Description

technical field [0001] The invention belongs to the field of natural medicines, in particular to a compound pharmaceutical composition containing ursolic acid and epalrestat and its application. Background technique [0002] Cancer is a chronic disease that seriously endangers human health, and has become the second largest killer after cardiovascular disease. Therefore, it is of great significance to find safe, effective, and low-toxic antitumor drugs and study their mechanism of action. [0003] Ursolic acid (Ursolid Acid, referred to as UA) is 3β-hydroxy-ursolic-12-ene-28-acid (3β-hydroxy-urs-12-en-28-oic acid), which belongs to pentacyclic triterpenoids, It is a natural active compound widely distributed in nature, such as the leaves of Paulownia tomentosa of Scrophulariaceae, the fruit of Gardenia of Rubiaceae, the wet buds of Gentianae, and the leaves of Ligustrum of Oleaceae, etc. in plants. A large number of studies have shown that ursolic acid has various biologic...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K31/426A61P35/02
CPCA61K31/426A61K31/56A61P35/02A61K2300/00
Inventor 刘连刘腾彭咏波刘靖李雄崔亮刘武昆谢国健
Owner FOSHAN UNIVERSITY
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