Application of andrographolide in the preparation of a pharmaceutical for treatment of inflammatory bowel disease, andrographolide enteric targeting micropellet, and method for preparation thereof

Abstract

The present invention relates to an andrographolide enteric targeting micropellet and method for preparation thereof; furthermore, the present invention also relates to uses of andrographolide and andrographolide enteric targeting micropellets in the preparation of a pharmaceutical for treatment of inflammatory bowel disease.

What is claimed is: 
     
         1 . A method of preparing medicine for treating inflammatory bowel disease comprising:
 utilizing an andrographolide enteric targeting micropellet which is composed of a blank pellet, a drug layer and an enteric coating layer, wherein said drug layer contains andrographolide, a polymer A that dissolves under a condition of pH≧7.0, and an excipient; where said ratio of the andrographolide and polymer A is 1:2˜1:0.2 by weight; and wherein the weight gain of the drug layer is 20 wt %˜100 wt %, said enteric coating layer containing a polymer B that dissolves under a condition of pH≧5.5 and an excipient; and wherein the weight gain of the enteric coating layer is 5 wt %˜30 wt %.   
     
     
         2 . The method of  claim 1 , wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease. 
     
     
         3 . The method of  claim 1  wherein treating inflammatory bowel disease includes improving colon adhesion, intestinal wall red swelling and thickening and decreased elasticity. 
     
     
         4 . The method of  claim 1  wherein treating inflammatory bowel disease includes reducing colon ulcer surface, hemorrhagic spot and perforation. 
     
     
         5 . The method of  claim 1 , wherein the enteric targeting micropellet is prepared into a granule or capsule. 
     
     
         6 . The method of  claim 1 , wherein the excipient of the drug layer is selected from the group consisting of plasticizer, anti-sticking agent, pigment, hydrophilic polymer and surfactant; and wherein the excipient of the enteric coating layer is at least one selected from the group consisting of plasticizer and anti-sticking agent. 
     
     
         7 . The method of  claim 1 , wherein the polymer A is a copolymer of methacrylic acid and methyl methacrylate and polymer B is a copolymer of methacrylic acid and ethyl acrylate. 
     
     
         8 . The method of  claim 1 , wherein the polymer A is a copolymer of methacrylic acid and methyl methacrylate in a ratio of 1:2 and/or the polymer B is a copolymer of methacrylic acid and ethyl acrylate in a ratio of 1:1. 
     
     
         9 . The method of  claim 6 , wherein the excipients of the drug layer are plasticizer and antisticking agent, wherein the plasticizer is at least one selected from the group consisting of triethyl citrate, dibutyl sebacate, propanediol and polyethylene glycol, and wherein the plasticizer is 10˜70 wt % of the polymer A of the drug layer; and wherein said anti-sticking agent is talc, and is 25˜100 wt % of the polymer A of the drug layer; or where said anti-sticking agent is glyceryl monostearate, which is 2˜20 wt % of the polymer A of the drug layer. 
     
     
         10 . The method of  claim 6 , wherein said ingredients are present in proportion by weight parts:blank micropellet:andrographolide:polymer A:plasticizer:anti-sticking agent:surfactant=200:(10-100):(10-100):(1-15):(1-30):(0-3). 
     
     
         11 . The method of  claim 6  wherein the ingredients are present in proportion by weight parts:blank micropellet:andrographolide:polymer A:plasticizer:antisticking agent:surfactant=200:(15-66):(13-74):(2-13.5):(3-27):(0-1.32). 
     
     
         12 . The method of  claim 6  wherein the ingredients are present in proportion by weight parts:blank micropellet:andrographolide:polymer A:plasticizer:antisticking agent:surfactant=200:(20-50):(30-60):(5-10):(5-20):(0.5-1.2). 
     
     
         13 . The method of  claim 1 , wherein the diameter of the blank pellet is 200˜600 μm, and wherein the blank pellet is 10˜70 wt % of the weight of the micropellet. 
     
     
         14 . The method of  claim 1  wherein the ratio of the andrographolide and polymer A is 1:2.5˜1:0.5 by weight. 
     
     
         15 . A method of preparing medicine for treating inflammatory bowel disease comprising:
 utilizing an andrographolide enteric targeting micropellet prepared into a granule or capsule which is composed of a blank pellet, a drug layer and an enteric coating layer, wherein said drug layer contains andrographolide, a polymer A that dissolves under a condition of pH≧7.0, and an excipient; where said ratio of the andrographolide and polymer A is 1:2.5˜1:0.5 by weight; and wherein the weight gain of the drug layer is 20 wt %˜100 wt %, said enteric coating layer containing a polymer B that dissolves under a condition of pH≧5.5 and an excipient; and wherein the weight gain of the enteric coating layer is 5 wt %˜30 wt %.   
     
     
         16 . The method of  claim 15  wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease. 
     
     
         17 . The method of  claim 15  wherein treating inflammatory bowel disease includes improving colon adhesion, intestinal wall red swelling and thickening and decreased elasticity. 
     
     
         18 . The method of  claim 15  wherein treating inflammatory bowel disease includes reducing colon ulcer surface, hemorrhagic spot and perforation. 
     
     
         19 . The method of  claim 15  wherein the ingredients are present in proportion by weight parts:blank micropellet:andrographolide:polymer A:plasticizer antisticking agent:surfactant=200:(15-66):(13-74):(2-13.5):(3-27):(0-1.32). 
     
     
         20 . The method of  claim 15  wherein the ingredients are present in proportion by weight parts:blank micropellet:andrographolide:polymer A:plasticizer antisticking agent:surfactant=200:(20-50):(30-60):(5-10):(5-20):(0.5-1.2).