Nifedipine A crystal bulk crystal habit and controlled release tablet composition thereof

A nifedipine and composition technology, applied in the field of nifedipine A crystal block crystal habit and its controlled-release tablet composition, can solve the preparation process of large nifedipine controlled-release tablets, the difficulty of controlling the dissolution rate of preparations, the nifedipine Problems such as the poor crystal form of bendipine can facilitate commercial production, avoid the risk of a narrow process operation window, and solve the effects of large release differences

Active Publication Date: 2021-04-02
DISHA PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Purpose of the invention: to provide a nifedipine A crystal block crystal habit that meets the requirements of the preparation process, its controlled release composition, and the preparation process of related raw materials and preparations, so as to solve the problem of poor crystal form of nifedipine in the market and the dissolution of preparations. The rate regulation is difficult, and the preparation process of the existing nifedipine controlled-release tablets is complex and the release is different.

Method used

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  • Nifedipine A crystal bulk crystal habit and controlled release tablet composition thereof
  • Nifedipine A crystal bulk crystal habit and controlled release tablet composition thereof
  • Nifedipine A crystal bulk crystal habit and controlled release tablet composition thereof

Examples

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Effect test

Embodiment 1

[0052] Example 1. Add 4g of nifedipine into a crystallizer filled with 100g of methanol and water mixed solvent (mass ratio: 17:3), stir and dissolve at 40°C, and after continuous stirring for 60 minutes, add purification to the crystallizer Water (conductivity is 3.6μs / cm), flow rate is 2.0mL / min, when the mass fraction of water in the solution is 30%, stop feeding purified water. Then add activated carbon for decolorization and filter. Then move the filtrate into the crystallizer and keep it warm at 40°C, introduce ultrasonic wave to induce crystallization, the ultrasonic frequency is 40KHz, cool down to 20°C within 200 minutes and keep it warm for 2 hours to grow crystals; then stop the ultrasonic wave, and cool down to 5°C within 150 minutes , and turn on the ultrasonic wave, the ultrasonic frequency is 33KHz, and grow the crystal for 2h. Then, it was filtered, and the filter cake was washed with water, and dried at 40° C. under normal pressure for 12 hours. The yield of...

Embodiment 2

[0053] Example 2. Add 6g of nifedipine into a crystallizer filled with 100g of methanol and water mixed solvent (mass ratio: 19:1), stir and dissolve at 50°C, and after continuous stirring for 30 minutes, add purification to the crystallizer Water (conductivity is 4.0μs / cm), flow rate is 1.5mL / min, when the mass fraction of water in the solution is 20%, stop feeding purified water. Then add activated carbon for decolorization and filter. Then move the filtrate into the crystallizer and keep it warm at 45°C, introduce ultrasonic wave to induce crystallization, the ultrasonic frequency is 33KHz, cool down to 30°C within 150 minutes and keep it warm for 1 hour to grow the crystal; then stop the ultrasonic wave, and cool down to 10°C within 100 minutes , and turn on the ultrasonic wave, the ultrasonic frequency is 20KHz, and grow the crystal for 4h. Then, it was filtered, and the filter cake was washed with methanol, and dried at 60° C. under normal pressure for 10 hours. The fi...

Embodiment 3

[0054] Example 3. Add 5g of nifedipine into a crystallizer filled with 100g of methanol and water mixed solvent (mass ratio: 9:1), stir and dissolve at 45°C, and after continuous stirring for 40 minutes, add purification to the crystallizer Water (conductivity is 4.5μs / cm), flow rate is 1.0mL / min, when the mass fraction of water in the solution is 25%, stop feeding purified water. Then add activated carbon for decolorization and filter. Then move the filtrate into the crystallizer and keep it warm at 30°C, introduce ultrasonic wave to induce crystallization, the ultrasonic frequency is 20KHz, cool down to 20°C within 60 minutes and keep it warm for 1 hour to grow the crystal; then stop the ultrasonic wave, and cool down to 10°C within 100 minutes , and turn on the ultrasonic wave, the ultrasonic frequency is 25KHz, and grow the crystal for 3h. Then, it was filtered, and the filter cake was washed with ethanol, and dried at 50° C. under normal pressure for 8 hours. The final ...

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Abstract

The present invention relates to a nifedipine A crystal bulk crystal habit and a controlled release tablet composition thereof, the controlled release tablet composition contains (HPMC) E30 and the nifedipine A crystal habit, the nifedipine A crystal form is cubic, the length, width and thickness ratio is 4-1: 2-1: 1, the particle size range Dv (90) is 120-240 [mu] m, and the mass ratio of HPMC E30 to nifedipine is 2:1 to 3:1. The invention provides the nifedipine bulk crystal habit and a pharmaceutical composition of nifedipine controlled release tablets released at an approximately constantrate.

Description

technical field [0001] The invention relates to a nifedipine A crystal block-like crystal habit and a controlled-release tablet composition, belonging to the technical field of pharmacy. Background technique [0002] Nifedipine is the first generation of dihydropyridine calcium antagonists, and it is one of the best-selling drugs for the treatment of hypertension and angina pectoris. At present, there are few types of nifedipine controlled-release preparations on the market in China, and the quality is not stable. Most of the nifedipine controlled-release tablets that are currently on the market at home and abroad are double-layer tablets based on the principle of osmotic pumps or single-layer tablets based on the principle of gel skeleton. . [0003] The double-layer osmotic pump tablet is composed of a drug-containing layer and a controlled-release layer, covered with a rigid semi-permeable membrane layer, which is laser-drilled and then coated with a film. The requireme...

Claims

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Application Information

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IPC IPC(8): C07D211/90A61K9/22A61K9/36A61K47/38A61K47/26A61K47/10A61K47/02A61K31/4422A61P9/12A61P9/10
CPCC07D211/90A61K9/2866A61K9/2853A61K9/2813A61K9/2054A61K9/2018A61K31/4422A61P9/12A61P9/10C07B2200/13
Inventor 金栋霞王冠侯铁强孙详彧邹韬博
Owner DISHA PHARMA GRP
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