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Prucalopride succinate pharmaceutical composition free of silicon dioxide and preparation method of prucalopride succinate pharmaceutical composition

A technology of prucalopride and silicon dioxide, which can be used in drug combinations, medical preparations containing active ingredients, and pharmaceutical formulations, etc., can solve the problems of hidden safety hazards, high prices, and very high fluidity requirements, and can achieve guaranteed Accuracy, reduced production costs, improved particle flowability

Active Publication Date: 2015-02-18
CHENGDU SINO STRONG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the solvent dispersion method is adopted, the uniformity of the main components in the auxiliary materials can be guaranteed, but it can be seen from the information disclosed in the prior art that the prucalopride succinate preparation cannot be produced by conventional wet production processes. , because prucalopride succinate can form a lactose adduct with the product diluent lactose monohydrate during the shelf life, this is a special excipient impurity, which has potential safety hazards in clinical practice
The information disclosed in the prior art shows that the powder used in the production process is directly compressed into tablets, but this process has very high requirements on the fluidity of the tablet machine and the material, and it is generally necessary to add a glidant to the formula, such as silicon dioxide (micronized silica gel) etc., all other auxiliary materials are required to be direct-pressed auxiliary materials, and the price of such auxiliary materials is more expensive than the same type of ordinary auxiliary materials

Method used

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  • Prucalopride succinate pharmaceutical composition free of silicon dioxide and preparation method of prucalopride succinate pharmaceutical composition
  • Prucalopride succinate pharmaceutical composition free of silicon dioxide and preparation method of prucalopride succinate pharmaceutical composition
  • Prucalopride succinate pharmaceutical composition free of silicon dioxide and preparation method of prucalopride succinate pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Weigh the raw materials according to formula 1, carry out jet milling of prucalopride succinate, collect the materials, and measure the particle size distribution (dry method measurement), requiring D10=0.1~8um, D50=10~30um, D90<60um. Then, the lactose monohydrate, the microcrystalline cellulose, and the corn starch are pulverized to control the particle size distribution D90<75um respectively. Using the doubling method, first mix prucalopride succinate and lactose monohydrate with particle size distribution meeting the requirements, and mix each time for 2 to 5 minutes; mix prucalopride succinate with lactose monohydrate After completion, mix with 50% of the prescription amount of microcrystalline cellulose for 2 to 5 minutes, then add the remaining microcrystalline cellulose and cornstarch, and mix for 10 to 20 minutes. After mixing, take 10 samples at different positions of the mixer to measure the content, and the RSD value is required to be less than 1.0%. Put the...

Embodiment 2-4

[0043] Example 2-4 Formula 2-4 was used and prepared according to the method of Example 1.

Embodiment 5

[0045] Particle content uniformity detection. The detection method is UV method; the detection wavelength is 274nm, the solvent is 0.001mol / L hydrochloric acid solution, and the measured concentration is 10ug / ml.

[0046] sample number Prescription 1 Prescription 2 Prescription 3 4 prescriptions 1# 0.414％ 0.423％ 0.811％ 0.812％ 2# 0.415％ 0.422％ 0.813％ 0.814％ 3# 0.416％ 0.424％ 0.814％ 0.811％ 4# 0.415％ 0.425％ 0.815％ 0.809％ 5# 0.414％ 0.423％ 0.811％ 0.808％ 6# 0.415％ 0.422％ 0.810％ 0.816％ 7# 0.415％ 0.424％ 0.810％ 0.812％ 8# 0.413％ 0.423％ 0.811％ 0.811％ 9# 0.416％ 0.426％ 0.812％ 0.810％ 10# 0.415％ 0.421％ 0.815％ 0.813％ RSD 0.22％＜1.0％ 0.35％＜1.0％ 0.24％＜1.0％ 0.29％＜1.0％

[0047] Table 2 Determination data of tablet content uniformity

[0048]

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Abstract

The invention discloses a prucalopride succinate pharmaceutical composition free of a silicon dioxide. The prucalopride succinate pharmaceutical composition comprises the following raw materials in parts by weight: 1-5 parts of prucalopride succinate (based on tiapride prucalopride), 100-280 parts of a diluent, 90-140 parts of a disintegrating agent and 1-10 parts of a lubricating agent. The invention also discloses a preparation method of the pharmaceutical composition. Due to adoption of the composition and the preparation method thereof disclosed by the invention, the specific surface area of the main ingredient prucalopride succinate can be increased; the particle mobility is improved by virtue of a dry granulator production process; the influence on content uniformity caused by a direct pressure technology without the silicon dioxide is solved; the accuracy of the clinical administration dosage is ensured; meanwhile, the pharmaceutical composition can be solved by common production equipment and auxiliary materials; and the industrial production cost is lowered.

Description

technical field [0001] The application relates to a silicon dioxide-free prucalopride succinate pharmaceutical composition and a preparation method, belonging to the field of pharmaceutical preparations. Background technique [0002] The chemical name of prucalopride succinate is: 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7 - Benzofuran carboxamide succinate, molecular formula: C 18 h 26 ClN 3 o 3 ·C 4 h 6 o 4 , molecular weight: 485.96. Prucalopride is a dihydrobenzofuran carboxamide compound, which is a selective and high-affinity serotonin (5-HT4) receptor agonist with intestinal motility-promoting activity. The results of in vivo and in vitro studies show that prucalopride can enhance the peristaltic reflex and propulsive motor pattern in the gastrointestinal tract through 5-HT4 receptor activation, and it is clinically used to treat chronic constipation in adult female patients who cannot be adequately relieved by laxatives symptom. ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4525A61K47/38A61K47/26A61P1/10A61J3/10
Inventor 蒲洪黄汉伟荣利许娟陈小宁
Owner CHENGDU SINO STRONG PHARMA
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