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Oral mesalazine colon-specific adhesive pellet

The technology of mesalazine and pellets is applied in the field of colon positioning adhering pellets containing mesalazine and the preparation thereof, and can solve the problem of no location-release coating, no targeted release of the pellets, and no loading of the pellets. Problems such as low doses, to reduce the inconvenience of taking drugs, avoid overheating, and improve tolerance

Inactive Publication Date: 2013-07-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The micropills obtained by the method described in the above-mentioned patents have adhesion, but the invention still has the following disadvantages: 1. The drug loading of the micropills is low, and the main drug is less than 5g per 100g preparation, which is not suitable for taking large doses of medicines. Preparation, and mesalamine is a large dose of medicine, a single dose of 500mg, the maximum daily dose of 4g, the above method is obviously not suitable for the preparation of preparations; It has the effect of targeted release, especially for locally acting drugs such as mesalazine, which needs further processing to make it targeted; Operation, cumbersome process, low production efficiency

Method used

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  • Oral mesalazine colon-specific adhesive pellet
  • Oral mesalazine colon-specific adhesive pellet
  • Oral mesalazine colon-specific adhesive pellet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Drug-containing core prescription

[0030] Mesalamine 70%

[0031] Microcrystalline Cellulose 20%

[0032] Carbomer 10%

[0033] Appropriate amount of distilled water

[0034] Made into 1000g

[0035] Preparation process of drug-containing pill core: respectively pulverize mesalazine, microcrystalline cellulose, and carbomer, pass through an 80-mesh sieve, and mix evenly. The output frequency is 30Hz, the extrusion temperature does not exceed 30°C, spheronize in the spheronizing equipment, the spheronizing frequency is 25Hz, the spheronizing time is 8min, the wet pellets are dried at 30°C for 2h, and the 20-30 mesh pellets are sieved to obtain the pills core.

[0036] Coating Solution Prescription

[0037] Eudragit L100 154g

[0038] Triethyl citrate 16g

[0039] Talc powder 31g

[0040] Distilled water 1809g

[0041]Coating process: use bottom spray fluidized bed for coating, place the core containing pills in the fluidized bed, preheat the bed with 40°C hot ...

Embodiment 2

[0043] Pill Core Prescription

[0044] Mesalamine 60%

[0045] Starch 25%

[0046] Polycarbophil 15%

[0047] 25% ethanol-water appropriate amount

[0048] Made into 1000g

[0049] Preparation process of drug-containing pill core: Grind mesalamine, starch, and polycarbophil separately, pass through an 80-mesh sieve, and mix evenly. 30Hz, the extrusion temperature does not exceed 30°C, spheronize in the spheronization equipment, the spheronization frequency is 25Hz, the spheronization time is 8min, the wet pellets are dried at 30°C for 2h, and the 20-30 mesh pellets are sieved to obtain the drug-containing pellet core.

[0050] Coating Solution Prescription

[0051] Eudragit L100 62g

[0052] Eudragit S100 15g

[0053] Dibutyl phthalate 8g

[0054] Talc powder 16g

[0055] 95% ethanol 1021g

[0056] Coating process: use bottom spray fluidized bed for coating, place the core containing pills in the fluidized bed, preheat the bed with 40°C hot air for 10 minutes before ...

Embodiment 3

[0058] Pill Core Prescription

[0059] Mesalamine 80%

[0060] Microcrystalline Cellulose 11%

[0061] Carbomer 3%

[0062] Hypromellose K4M 3%

[0063] Polyvinylpyrrolidone 3%

[0064] Appropriate amount of distilled water

[0065] Made into 1000g

[0066] Preparation process of drug-containing pill core: respectively pulverize mesalazine, microcrystalline cellulose, carbomer, hypromellose K4M, and polyvinylpyrrolidone, pass through an 80-mesh sieve, and mix evenly; The material is extruded in a low-temperature extruder, the extrusion frequency is 30Hz, and the extrusion temperature does not exceed 30°C. It is spheronized in a spheronizing device with a spheronization frequency of 25Hz and a spheronization time of 8 minutes. The wet pellets are dried at 30°C for 2 hours, and sieved to take 20-30 mesh micropills to get the drug-containing pill core.

[0067] Coating Solution Prescription

[0068] Eudragit S100 63g

[0069] Triethyl citrate 31g

[0070] Glyceryl monos...

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Abstract

The invention discloses an oral mesalazine colon-specific adhesive preparation with a high drug-loading rate, which can be used for effectively treating ulcerative colitis and segmental ileitis, as well as a preparation method of the oral mesalazine colon-specific adhesive preparation. The preparation is composed of a pill-containing core and an enteric coating layer, wherein the pill-containing core consists of mesalazine, excipient, adhesive and boning agent. Compared with the other oral preparations, the oral mesalazine colon-specific adhesive pellet has the effects of improving the curative effect and lowering adverse reactions when the dosage is the same. Compared with enema and suppository, the pellet has better tolerance. The preparation method can be used for effectively controlling the temperature in the production process and avoiding an overheating phenomenon in the preparation process, and is simple in preparation process and high in drug-loading rate. Besides, the oral mesalazine colon-specific adhesive pellet is applicable to the large-dose dosing characteristic of mesalazine, thereby reducing the medicine taking inconvenience of a patient and improving the dependence of the patient.

Description

[0001] technical field [0002] The invention belongs to the field of pharmaceutical preparations, and relates to a colon-positioned adhesion pellet containing mesalazine and a preparation method thereof. More precisely, it is a pharmaceutical preparation that can release mesalamine at the ileocecal site and the colon site, and can prolong the residence time at the ileocecal site and the colon site, and a preparation method thereof. Background technique [0003] Mesalamine, also known as 5-aminosalicylic acid, is the active ingredient of sulfasalazine and is an effective drug for treating mild to moderate active ulcerative colitis and Crohn's disease. Mesalamine can inhibit the synthesis of prostaglandins that cause inflammation and the formation of inflammatory mediator leukotrienes, remove active oxygen and other damage factors, and inhibit the movement of intestinal macrophages to leukotrienes, so that macrophages move to the inflammatory area Migration is reduced so tha...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/32A61K31/606A61P1/00A61P1/04
Inventor 程刚张啸
Owner SHENYANG PHARMA UNIVERSITY
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