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Nifedipine framework sustained-release pellets and preparation method and application thereof

A technology for nifedipine and sustained-release pellets, applied in the field of medicine, can solve the problems of poor reproducibility between batches, low yield of pellets, and poor hardness, and achieves improved bioavailability, improved bioavailability, and improved release. effect of behavior

Inactive Publication Date: 2012-05-02
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of a coating granulator has disadvantages such as large dust pollution, low pellet yield and hardness, low drying rate, and poor batch-to-batch reproducibility.
[0009] Although there are many existing nifedipine sustained-release preparations, there are certain limitations in the preparation process. For this reason, it is necessary to research and develop new preparation technologies for nifedipine to further improve the dissolution rate and bioavailability of nifedipine

Method used

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  • Nifedipine framework sustained-release pellets and preparation method and application thereof
  • Nifedipine framework sustained-release pellets and preparation method and application thereof
  • Nifedipine framework sustained-release pellets and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The raw materials of the liquid co-grind are as follows: 500g of nifedipine, 40g of hypromellose E5, 10g of PEG6000, and 500ml of water;

[0042] The raw materials of the pellets are as follows: Nifedipine liquid co-grind 26g, microcrystalline cellulose 15g, mannitol 57g, sodium lauryl sulfate 12g, sodium carboxymethyl starch 2g;

[0043] The raw materials for coating are as follows: 500g of nifedipine matrix pellets, 15g of brown Opadry, 100ml of water;

[0044] The specification is 20mg / capsule.

[0045] Its preparation method is as follows:

[0046] (1) Preparation of liquid co-grind of nifedipine: 500g of nifedipine was suspended in an aqueous solution of a hydrophilic carrier, which was prepared by mixing 40 g of hypromellose E5, 10 g of PEG6000 and 500 ml of water. into, the concentration of the aqueous solution of the hydrophilic carrier is 10% (weight / volume). Put the suspension in a basket mill, and grind it for 4 hours under the condition of a grinding ...

Embodiment 2

[0051] The raw materials of the liquid co-grind are as follows: 400g of nifedipine, 30g of hypromellose E5, 600ml of water;

[0052] The raw materials of the pellets are as follows: 35g of nifedipine liquid co-grind, 18g of microcrystalline cellulose, 54g of lactose, 12g of sodium lauryl sulfate, 3g of croscarmellose sodium;

[0053] The raw materials for coating are as follows: 500g of nifedipine matrix pellets, 20g of brown Opadry, 133.33ml of water;

[0054] The specification is 20mg / capsule.

[0055] Its preparation method is as follows:

[0056] (1) Preparation of nifedipine liquid co-grind: 400g of nifedipine was suspended in an aqueous solution of a hydrophilic carrier, which was prepared by mixing 30 g of hypromellose E5 and 600 ml of water. The concentration of propylmethylcellulose E5 aqueous solution is 5 (w / v)%. The suspension is placed in a basket mill and ground for 4 hours at a grinding speed of 1500 rpm to obtain the product.

[0057] (2) Preparation of n...

Embodiment 3

[0061] The raw materials of the liquid co-grind are as follows: 200g of nifedipine, 30g of hypromellose E5, 30g of compressible starch, 120ml of ethanol, and 480ml of water;

[0062] The raw materials of the pellets are as follows: Nifedipine liquid co-grind 40g, microcrystalline cellulose 20g, mannitol 54g, sodium lauryl sulfate 15g, sodium carboxymethyl starch 2g, sodium bicarbonate 2g;

[0063] The raw materials for coating are as follows: 500g of nifedipine matrix pellets, 25g of titanium dioxide, and 166.67ml of water;

[0064] The specification is 20mg / capsule.

[0065] Its preparation method is as follows:

[0066] (1) Preparation of nifedipine liquid co-grind: 200g of nifedipine was suspended in ethanol aqueous solution of hydrophilic carrier, which was composed of 30g hypromellose E5, 30g compressible starch, It is prepared by mixing 480ml of water and 120ml of ethanol. The concentration of the aqueous solution of the hydrophilic carrier is 10% (weight / volume). The ...

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Abstract

The invention discloses nifedipine framework sustained-release pellets and a preparation method and application thereof, and belongs to the technical field of medicines. The nifedipine framework sustained-release pellets are prepared from the following raw materials in part by weight: 10 to 40 parts of nifedipine liquid co-ground material, 15 to 25 parts of framework material, 40 to 60 parts of diluent, 10 to 20 parts of surfactant, 1 to 5 parts of disintegrating agent and 0 to 5 parts of auxiliary disintegrating agent. Nifedipine and a hydrophilic carrier solution are co-ground, so that the in-vitro release behavior of the medicine can be greatly improved, and the bioavailability of the medicine is improved; and after the nifedipine framework sustained-release pellets prepared by bonding other framework auxiliary materials through the liquid co-ground material serving as a bonding agent are orally taken, a long-acting sustained-release effect is achieved in vivo, and the bioavailability is greatly improved.

Description

technical field [0001] The invention relates to an improved oral sustained-release dosage form, in particular to a nifedipine skeleton-type sustained-release pellet, a preparation method thereof and an application in pharmaceutical preparations, which belong to the technical field of medicine. Background technique [0002] Nifedipine is a dihydropyridine calcium antagonist, which is commonly used in clinical treatment of hypertension and angina pectoris. However, its common oral preparations have many disadvantages such as low bioavailability, significant adverse reactions, and frequent administration. Therefore, nifedipine has long-acting Sustained and controlled release preparations are gradually gaining favor. German Bayer company first developed nifedipine controlled-release tablets, the trade name is Baixintong; then France Aidifa Company successfully developed nifedipine sustained-release capsules, the trade name is Aidiqing. These products can maintain stable blood d...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4422A61K47/38A61K47/32A61K47/34A61K47/36A61P9/12A61P9/10
Inventor 唐星何海冰张宇
Owner SHENYANG PHARMA UNIVERSITY
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