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A kind of mesalamine microparticle preparation with time-dependent release mechanism and preparation method thereof

A time-dependent, mesalamine technology, applied in the preparation of mesalamine microparticle preparations, in the field of mesalamine microparticle preparations, can solve the problems of poor process reproducibility and poor quality stability, and achieve good reproducibility and process stability Good results

Active Publication Date: 2019-06-07
PIVOT PHARMA TECH SHANGHAI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation has the characteristics of sustained, stable and complete drug release, and overcomes the defects of poor process reproducibility and poor quality stability of existing preparations

Method used

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  • A kind of mesalamine microparticle preparation with time-dependent release mechanism and preparation method thereof
  • A kind of mesalamine microparticle preparation with time-dependent release mechanism and preparation method thereof
  • A kind of mesalamine microparticle preparation with time-dependent release mechanism and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Prescription with pill core:

[0035]

[0036]Preparation method of ball core: take the above components 1, 2 and 3 and mix them well, divide them into two parts evenly, one part is wetted with appropriate amount of water in a high-speed wet granulator and sieved through a 30-mesh sieve, and the other part is used as For powder. Put the raw material in the centrifugal granulator, control the centrifugal speed at 300-500rpm, the material temperature at 40-50°C, the blast flow rate at 12-15L / min, the jet pressure at 1.2-1.6bar, and the fan frequency at 25-30HZ. The liquid flow rate is 5-8g / min, the powder supply speed is 4-6g / min, and the aqueous solution of 4 is sprayed while supplying the powder to gradually enlarge and granulate, and the particle size of the pellets is controlled to be about 600-1000μm, and the core of the pellets containing the drug is obtained after drying.

[0037] Coating prescription:

[0038]

[0039] Preparation of coating solution: firs...

Embodiment 2

[0042] Prescription with pill core:

[0043]

[0044] Preparation method of ball core: Mix the above components 1, 2, 3 and 5 evenly, granulate with the aqueous solution of 4 in a high-speed wet granulator for 3-5 minutes, the stirring speed is 500rpm, and the shearing speed is 1000rpm. The soft material is extruded in an extruder at 50 rpm, spheronized in a spheronizer at 1500-2000 rpm for 3-6 minutes, dried and sieved.

[0045] Coating prescription:

[0046]

[0047] Preparation of coating solution: firstly, povidone and talcum powder are dispersed in aqueous solution (components 1, 2, and 3 in the coating prescription), and passed through a 60-mesh sieve to make a coating solution for the isolation layer for subsequent use. Disperse components 4, 5, and 6 in the coating formulation in 85% ethanol solution (component 7 in the coating formulation), mix and stir evenly, pass through a 60-mesh sieve to prepare a slow-release coating solution for future use.

[0048] Coa...

Embodiment 3

[0050] Prescription with pill core:

[0051]

[0052] Preparation method of pellet core: Take 3, 4, 75% of 1 and half of 6 of the above components and mix well, moisten with appropriate amount of water in a high-speed wet granulator and pass through a 30-mesh sieve to remove the mother. The material is placed in a centrifugal granulator, the centrifugal speed is controlled at 300-500rpm, the material temperature is 40-50°C, the blast flow rate is 12-15L / min, the jet pressure is 1.2-1.6bar, the fan frequency is 25-30HZ, and the liquid supply flow rate is 5- 8g / min, powder supply speed 4~6g / min, component 2 and the remaining 1 and 6 are mixed evenly as the powder supply material, and the aqueous solution of 5 is sprayed while supplying powder to gradually enlarge the granulation, and the particle size of the pellet is controlled to be about 600~1000μm Or so, dry and get the drug-containing pellet core.

[0053] Coating prescription:

[0054]

[0055] Preparation of coati...

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Abstract

The invention discloses a mesalazine microparticle preparation having a time dependent releasing mechanism and a preparation method thereof. According to the preparation and the preparation method thereof, mesalazine is used as an effective pharmacologic ingredient and is combined with pharmaceutically common auxiliary materials to prepare quickly released pill cores by adopting an extrusion-spheronization technology or a centrifugal granulation technology. An outer layer of each quickly released pill core is covered with an isolation layer which enables the surface of a small pill to be smooth and rounded, wherein the isolation layer mainly comprises one or more of water-soluble macromolecules and antiadhesion agent; a slowly released material is used as the outmost layer and is coated with a slowly released coating, such that the drug is released sustainably and slowly. The slowly released preparation is prepared from mesalazine having a granularity distribution of D10=2 to 6mu m, D50=7 to 18mu m, and D90=20 to 40mu m, and has the function of releasing 5 to 25 percent of mesalazine at 1 h, releasing 30 to 50 percent of mesalazine at 2 h, releasing 60 to 80 percent of mesalazine at 4 h, and releasing 85 percent of mesalazine at 8 h within in simulate intestine liquid having a pH of 7.5. The slowly released micropills are simple in preparation process, low in cost, good in process reproducibility and suitable for mass production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a mesalazine microparticle preparation (or pellet preparation) with a time-dependent release mechanism. In addition, the present invention also relates to the preparation method of the mesalamine microparticle preparation with the time-dependent release mechanism. Background technique [0002] Ulcerative colitis is a chronic non-specific inflammatory disease that mainly involves the rectum and colon. The clinical symptoms are mainly abdominal pain, diarrhea, mucus and bloody stools, and tenesmus, with periods of attack and remission appearing alternately. The disease mostly occurs in young and middle-aged people, and the incidence rate of men and women is equal. In recent years, the incidence rate has an upward trend. In the past, sulfasalazine (SASP) was mainly used as a commonly used drug in clinical practice, but it was often discontinued due to severe s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K9/52A61K31/606A61P1/04A61P1/00
CPCA61K9/0002A61K9/4866A61K9/5047A61K9/5073A61K31/606
Inventor 陈茜陆阳嵇栋梁吕敏
Owner PIVOT PHARMA TECH SHANGHAI