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Preparation method of mosapride citrate stomach buoyant sustained-release pellet

A technology of mosapride citrate and sustained-release pellets is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc. It is not good, and the local drug concentration is high, so as to achieve the optimization of gas producing layer and retardation layer, good slow release characteristics, and the effect of expanding production

Active Publication Date: 2018-12-18
CHONGQING MEDICAL & PHARMA COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Gastric floating sustained-release preparations are currently researched mainly as gastric floating tablets, which belong to the unit system. However, this type may cause sudden release and cause local drug concentration to be too high, or individual preparations have poor floating performance and are quickly emptied by the stomach, which cannot be achieved. Anticipated effect, so the present invention prepares mosapride citrate as gastric floating sustained-release pellets

Method used

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  • Preparation method of mosapride citrate stomach buoyant sustained-release pellet
  • Preparation method of mosapride citrate stomach buoyant sustained-release pellet
  • Preparation method of mosapride citrate stomach buoyant sustained-release pellet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] A method for preparing mosapride citrate gastric floating sustained-release pellets, characterized in that it comprises the steps of:

[0064] 1) Preparation of soft materials

[0065] 1.1) Place stearyl alcohol in ethanol solution, and obtain mixture A after completely dissolving;

[0066] The concentration of the ethanol solution is 95%;

[0067] Get described stearyl alcohol 13g, dissolve completely with above-mentioned ethanol solution 220g;

[0068] 1.2) Mix mosapride citrate, microcrystalline cellulose, sodium bicarbonate and the mixture A obtained in step 1.1), and sieve to obtain mixture B;

[0069] Described mosapride citrate, microcrystalline cellulose, sodium bicarbonate weight are respectively 1g, 25g, 3.4g;

[0070] The sieve used in the sieving process is 80 mesh;

[0071] 1.3) Shake the mixture B until it is evenly mixed, then add an aqueous solution of hydroxypropyl methylcellulose to the mixture B to prepare a soft material;

[0072] The mass fract...

experiment example 1

[0103] Randomly take 100 pellets and place them in 900ml of hydrochloric acid solution with a concentration of 0.1mol / L, at 37±0.5°C, and the rotation speed of the stirring paddle is 75rpm;

[0104] The time required for observing the floating rate to be higher than 90% (floating time) was less than 1min, and the floating rate of the pellets was 84.32% in 8h; the time to record the floating rate of the pellets higher than 80% was more than 10h.

experiment example 2

[0106] According to the scheme in Example 1, 3 batches of mosapride citrate gastric floating sustained-release pellets were prepared, and the release rate was measured, specifically: a method for determining the content of mosapride citrate was established by using high performance liquid chromatography Determination of the release rate of the coated sustained-release pellets.

[0107] The chromatographic column is WelchromTMC18 (5μm, 4.6×250mm), the mobile phase is acetonitrile-0.2% phosphoric acid solution (30︰70, v / v), the detection wavelength is 274nm, the column temperature is 30°C, and the flow rate is 1ml / min. Volume: 30 μl.

[0108] The peak eluting time of mosapride citrate was 8.6min, and other excipients did not affect the determination of mosapride citrate.

[0109] After the methodological verification of linearity, precision and recovery, the standard curve equation was established, and the in vitro release of the coated pellets was determined by the rotating ba...

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Abstract

The invention discloses a preparation method of a mosapride citrate stomach buoyant sustained-release pellet. The mosapride citrate stomach buoyant sustained-release pellet is formed by a drug-loadedpellet core, and a gas-generating layer and a retardation layer which wrap the pellet core, the inner layer of the pellet is a light-weight pellet core, the outer layer of the pellet is wrapped with acontrolled-release polymer material, and the middle layer of the pellet is the gas-generating layer produced from NaHCO3 and HPMC used as an adhesive. When the pellet meets a release medium water, the pellet can be quickly hydrated and expand, the pellet and CO2 gas produced by NaHCO3 in the gas-generating layer are prevented from overflowing by the retardation layer, so the pellet can float fora long time, and the release of the drug from the core is controlled; and the mosapride citrate stomach buoyant sustained-release pellet has the advantages of good roundness, good buoyancy in vitro, realization of a 8 h buoying rate reaching 80% or above, and good sustained-release characteristic.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a method for preparing mosapride citrate gastric floating sustained-release pellets. Background technique [0002] The absorption of drugs in the gastrointestinal tract is a complex process affected by many factors. Studies have shown that the degree of drug absorption in the gastrointestinal tract is related to the residence time of the drug in the gastrointestinal tract. [0003] The purpose of the gastric retention drug delivery system is to prolong the residence time of the drug in the stomach to several hours, thereby promoting the release and absorption of the drug in the gastrointestinal tract, and improving the oral bioavailability of the drug. A variety of studies have used different methods to improve the residence time of drugs in the stomach, including mucoadhesion, floating, expansion, and magnetic drug delivery systems. In addition, there are drug delivery syste...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/32A61K47/02A61K47/38A61K47/10A61K31/5375A61P1/14
CPCA61K9/0065A61K9/501A61K9/5026A61K9/5047A61K31/5375A61K47/02A61K47/10A61K47/38A61P1/14
Inventor 何静邱妍川江尚飞王牌李芝邢于政张露
Owner CHONGQING MEDICAL & PHARMA COLLEGE
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