A kind of nifedipine long-acting sustained-release pellets and preparation method thereof

A technology of sustained-release pellets and nifedipine, which is applied in the fields of cardiovascular system diseases, bulk delivery, drug combination, etc., and can solve the problem that the drug release rate cannot be effectively controlled, the solubility of nifedipine is small, and the release rate of sustained-release preparations Low-level problems, to achieve the effect of improving bioavailability, prolonging transit and absorption time, reducing aggregation and caking

Inactive Publication Date: 2017-12-12
BAOTOU MEDICAL COLLEGE OF INNER MONGOLIA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low solubility of nifedipine, the release rate of the sustained-release preparations made by the general polymer block method is very low, resulting in low bioavailability, and the release rate of the drug cannot be effectively controlled, which easily causes a large increase in blood drug concentration. Amplitude fluctuation

Method used

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  • A kind of nifedipine long-acting sustained-release pellets and preparation method thereof
  • A kind of nifedipine long-acting sustained-release pellets and preparation method thereof
  • A kind of nifedipine long-acting sustained-release pellets and preparation method thereof

Examples

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Effect test

example 1

[0030] A preparation method of the nifedipine long-acting sustained-release pellets, comprising the steps of:

[0031] Step 1: Add 10 parts by weight of nifedipine into a mixed solvent of ethanol and dichloromethane and stir until dissolved to obtain a nifedipine solution, then take 19 parts by weight of polyethylene glycol 4000 and 10 parts by weight of sorbitol in a 95°C water bath After melting, add in the nifedipine solution, stir evenly, cool down and pulverize to obtain the nifedipine dispersion;

[0032] Step 2: After mixing the nifedipine dispersion with 49 parts by weight of welan gum, 5 parts by weight of stearic acid, 5 parts by weight of lactose, and 2 parts by weight of talcum powder, add 25 parts by weight of 15% aqueous ethanol to moisturize Wet to get soft material;

[0033] Step 3: extrude the soft materials through an extruder at a speed of 34r / min, and spheronize at a speed of 1100r / min in a spheronizer to prepare a spherical product, and dry at 45°C for 20...

example 2

[0035] A preparation method of the nifedipine long-acting sustained-release pellets, comprising the steps of:

[0036] Step 1: Add 12 parts by weight of nifedipine into a mixed solvent of ethanol and dichloromethane and stir until dissolved to obtain a nifedipine solution, then take 19 parts by weight of polyethylene glycol 4000 and 14 parts by weight of sorbitol in a water bath at 100°C After melting, add in the nifedipine solution, stir evenly, cool down and pulverize to obtain the nifedipine dispersion;

[0037] Step 2: After mixing the nifedipine dispersion with 30 parts by weight of welan gum, 10 parts by weight of stearic acid, 10 parts by weight of lactose, and 5 parts by weight of micropowdered silica gel, add 30 parts by weight of 20% ethanol aqueous solution to moisturize Wet to get soft material;

[0038] Step 3: Extrude the soft material through an extruder at a speed of 30r / min, and spheronize at a speed of 1080r / min to prepare a spherical product, and dry at 50°...

example 3

[0040] A preparation method of the nifedipine long-acting sustained-release pellets, comprising the steps of:

[0041] Step 1: Add 10 parts by weight of nifedipine into a mixed solvent of ethanol and dichloromethane and stir until dissolved to obtain a nifedipine solution, then take 18 parts by weight of polyethylene glycol 4000 and 12 parts by weight of sorbitol in a 97°C water bath After melting, add in the nifedipine solution, stir evenly, cool down and pulverize to obtain the nifedipine dispersion;

[0042] Step 2: After mixing the nifedipine dispersion with 42 parts by weight of welan gum, 7 parts by weight of stearic acid, 8 parts by weight of lactose and 3 parts by weight of sodium lauryl sulfate, add 27 parts by weight of 17% Wetting the ethanol aqueous solution to obtain soft materials;

[0043] Step 3: Extrude the soft material through an extruder at a speed of 32r / min, and spheronize at a speed of 1050r / min to prepare a spherical product, and dry it at 47°C for 25 ...

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Abstract

The invention provides a nifedipine long-acting sustained-release pellet, which comprises the following materials in parts by weight: 8-12 parts of nifedipine, 30-49 parts of welan gum, 5-10 parts of stearic acid, polyethylene glycol Diol 4000 15-20 parts, sorbitol 10-15 parts, lactose 5-10 parts, lubricant 2-5 parts. The preparation method is as follows: firstly, the nifedipine dispersion is prepared with polyethylene glycol and sorbitol as the carrier, then mixed evenly with other raw materials in the sustained-release pellets, added with ethanol aqueous solution to moisten to obtain a soft material, and then the The soft material is respectively prepared into a spherical product through an extrusion machine and a spheronizer, and dried at 45-50° C. for 20-30 hours to obtain sustained-release pellets. The preparation method of the invention is simple, easy to be prepared in large quantities, and the process reproducibility is good. The obtained long-acting sustained-release pills are uniform and stable, can effectively control the release speed of the medicine, and basically have no stimulating effect on the gastrointestinal mucosa.

Description

technical field [0001] The invention relates to a nifedipine long-acting sustained-release pellet and a preparation method thereof. More specifically, the present invention relates to a kind of nifedipine sustained-release pellets which can effectively improve drug stability and have excellent long-acting sustained-release performance and a preparation method thereof. Background technique [0002] Nifedipine is currently one of the first-choice drugs for the clinical treatment of hypertension and angina pectoris. Its rapid antihypertensive effect has brought good curative effect to patients, but it also brings many risks. Clinically, common dosage forms have poor curative effect and large fluctuations in blood drug concentration in the body. The incidence of adverse reactions in common dosage forms of this drug is nearly 20%. In addition, common preparations of nifedipine have a strong stimulating effect on the gastrointestinal mucosa, and can also cause symptoms such as ab...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4422A61K47/10A61K47/36A61P9/12A61P9/10
Inventor 高洪波方欣齐瑞芳薛永志薛焱常燕琴徐继辉
Owner BAOTOU MEDICAL COLLEGE OF INNER MONGOLIA UNIV OF SCI & TECH
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