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Solid dispersion of cilnidipine and preparation method thereof

A solid dispersion and cilnidipine technology, which is applied in pill delivery, cardiovascular system diseases, powder delivery, etc., can solve the problem that cilnidipine dispersion is difficult to achieve disintegration and dissolution effects, and it is difficult to play a role in maintaining hypertension and other issues to achieve good stability

Inactive Publication Date: 2015-05-27
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The cilnidipine dispersion prepared by the above method is still difficult to achieve good disintegration and dissolution effects when it is prepared into tablets, and the dissolution rate can only reach about 70% after testing.
Since the specification and dose of cilnidipine are relatively small, if the dissolution and release of the drug cannot meet the requirements set by the standard within the specified time, it will be difficult to exert its role in the maintenance treatment of hypertension

Method used

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  • Solid dispersion of cilnidipine and preparation method thereof
  • Solid dispersion of cilnidipine and preparation method thereof
  • Solid dispersion of cilnidipine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] 1. Raw materials and prescription composition

[0031]

Weight (g)

cilnidipine

5

polyethylene glycol 6000

45

microcrystalline cellulose

55

lactose

25

Croscarmellose Sodium

52.5

Magnesium stearate

0.7

0.5% hypromellose (dissolved in 95% ethanol)

0.5

[0032] 2. Preparation method:

[0033] 1) Put polyethylene glycol 6000 in a water bath and heat it in a water bath to melt it. Control the temperature of the water bath at 75-80°C, and then add cilnidipine. The weight ratio of cilnidipine to polyethylene glycol 6000 is 1: 5. Stir fully to make it heated evenly and melt until the material melts into a yellow transparent solution and the bubbles completely disappear; the dispersion solution is obtained, and then the dispersion solution is flattened and frozen at a temperature of -13°C to -15°C. Freeze overnight, pulverize, and pass through an 80-mesh sieve to obtain the cilnidi...

Embodiment 2

[0036] 1. Raw materials and prescription composition

[0037]

[0038] 2. Preparation method

[0039] 1) Put polyethylene glycol 6000 in a water bath and heat it in a water bath to melt it. Control the temperature of the water bath at 70-75°C, and then add cilnidipine. The weight ratio of cilnidipine to polyethylene glycol 6000 is 1: 10. Stir fully to make it evenly heated and melted until the material melts into a yellow transparent solution and the bubbles completely disappear; the dispersion solution is obtained, and then the dispersion solution is flattened and frozen at a temperature of -13°C to -15°C. Freeze overnight, pulverize, and pass through an 80-mesh sieve to obtain the cilnidipine dispersion powder;

[0040] 2) Weigh each component according to the formula, add auxiliary materials except binder and magnesium stearate to the cilnidipine dispersion powder, mix well, then add binder to granulate, dry at 45°C, granulate, add Magnesium stearate, direct compressio...

Embodiment 3

[0042] 1. Raw materials and prescription composition

[0043]

[0044] 2. Preparation method

[0045]1) Put polyethylene glycol 6000 in a water bath and heat it in a water bath to melt it. Control the temperature of the water bath at 70-75°C, and then add cilnidipine. The weight ratio of cilnidipine to polyethylene glycol 6000 is 1: 10. Stir fully to make it evenly heated and melted until the material melts into a yellow transparent solution and the bubbles completely disappear; the dispersion solution is obtained, and then the dispersion solution is flattened and frozen at a temperature of -13°C to -15°C. Freeze overnight, pulverize, and pass through an 80-mesh sieve to obtain the cilnidipine dispersion powder;

[0046] 2) Weigh each component according to the formula, add auxiliary materials except binder and magnesium stearate to the cilnidipine dispersion powder, mix well, then add binder to granulate, dry at 45°C, granulate, add Magnesium stearate, direct compression...

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Abstract

The invention relates to a solid dispersion of cilnidipine and a preparation method thereof. The solid dispersion is prepared from the following raw material components: cilnidipine, polyethylene glycol, microcrystalline cellulose, lactose, croscarmellose sodium, magnesium stearate and hydroxypropyl methylcellulose. The dissolution degree of the solid dispersion provided by the invention is not lower than 85%; the contents of related substances conform to the requirements; and the effect is superior to that of the prior art.

Description

technical field [0001] The invention relates to a tablet of cilnidipine, in particular to a solid dispersion of cilnidipine and a preparation method thereof. Background technique [0002] Cilnidipine was developed by Ajinomoto Corporation of Japan and first approved for marketing in Japan in 1995. It is taken orally once a day for the treatment of essential hypertension with high curative effect and good tolerance. This drug is a combination of L-type and Novel calcium antagonists that block N-type calcium channels. Its characteristics are: In addition to acting on L-type calcium channels like most calcium antagonists, this product can also act on N-type calcium channels existing in the sympathetic nerve endings, inhibiting the activation of sympathetic nerves, resulting in unique clinical features- - Does not increase the heart rate of patients with essential hypertension, and can also significantly reduce the patient's cardiothoracic ratio (that is, the ratio of the trans...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/4422A61K47/34A61K9/20A61P9/12
Inventor 李保琴左莉英杜明松
Owner 蚌埠丰原涂山制药有限公司
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