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Compound sustained-release pellet tablet containing nifedipine and atenolol and preparation thereof

A technology for sustained-release pellets and sustained-release pellets, which is applied in the directions of medical preparations containing active ingredients, pill delivery, pharmaceutical formulations, etc., and can solve the problem of process stoppage, equipment damage, inability to press the drug-containing pellets into tablets, etc. problem, to achieve good mixing uniformity

Inactive Publication Date: 2010-01-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the composition, particle size, density and fluidity of powders and granules are far from those of drug-containing pellets, it is impossible to protect the uniformity of mixing in the process of industrial mass production. Due to the vibration of the hopper of the machine, the ingredients will also be seriously stratified, resulting in the uncontrollable content of the ingredients of the compound; at the same time, the normal tablet force may not be able to compress a high proportion of drug-containing pellets into tablets, resulting in process stoppage and equipment damage; There may also be different degrees of rupture or fusion of the drug-containing pellets between the tablets prepared by compression, and the drug release behavior is difficult to control

Method used

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  • Compound sustained-release pellet tablet containing nifedipine and atenolol and preparation thereof
  • Compound sustained-release pellet tablet containing nifedipine and atenolol and preparation thereof
  • Compound sustained-release pellet tablet containing nifedipine and atenolol and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Weigh 5g atenolol, 5g microcrystalline cellulose and 3g tartaric acid, mix them evenly, use a 2% aqueous solution of povidone K30 as a binder to make a soft material, extrude and spheronize to prepare atenolol-containing pellet cores, sieve Take 30-40 mesh and set aside.

[0052] Weigh the above-mentioned 10g atenolol-containing pellets in a fluidized bed. Add 0.267g talc powder and 0.002g bright blue lake into 15ml water and mix and stir to obtain a suspension. Just before use, add 0.533g methyl methacrylate: butyl acrylate 1:1.5 polymer, 15ml water and 15ml ethanol. In the coating liquid, the wind speed, temperature and flow rate of the coating liquid are adjusted to ensure a good fluidization state, and the weight gain of the coating is about 8%. Atenolol sustained-release pellets are prepared with a drug content of 35.6%.

[0053] Weigh 10g of nifedipine and 20g of polyethylene glycol 6000 to prepare a solid dispersion. Weigh 10g of the above solid dispersion and 10g of...

Embodiment 2

[0059] Weigh 5g atenolol, 5g microcrystalline cellulose and 3g tartaric acid, mix them evenly, use a 2% aqueous solution of povidone K30 as a binder to make a soft material, and prepare atenolol-containing pellet cores by centrifugal granulation coating , Sieve 30-40 mesh for later use.

[0060] Weigh the above-mentioned 10g atenolol-containing pill core in a centrifugal granulation coating machine. Add 0.833g talc powder and 0.002g bright blue lake into 15ml water and mix and stir to obtain a suspension. Just before use, add 1.667g methyl methacrylate: ethyl acrylate 1:2 polymer, 15ml water and 15ml ethanol In the coating liquid, the wind speed, temperature and flow rate of the coating liquid are adjusted to increase the weight of the coating by about 25% to prepare atenolol sustained-release pellets with a drug content of about 30.77%.

[0061] Weigh 10g of nifedipine and 20g of polyethylene glycol 4000 to prepare a solid dispersion. Weigh 10g of the above solid dispersion and 1...

Embodiment 3

[0067] Weigh 5g of atenolol, 10g of microcrystalline cellulose and 3g of tartaric acid, mix them evenly, use a 2% aqueous solution of povidone K30 as a binder to make a soft material, and prepare atenolol-containing pellet cores in a fluidized bed in one step. Sieve 30-40 mesh for later use.

[0068] Weigh the above-mentioned 10g atenolol-containing pellets in a fluidized bed. Add 0.5g of talc and 0.002g of bright blue lake into 15ml of water and mix and stir to obtain a suspension. Just before use, add 1g of methyl methacrylate: butyl acrylate 1:2 polymer, 15ml of water and 15ml of ethanol. In the coating liquid, the wind speed, temperature and flow rate of the coating liquid are adjusted to ensure a good fluidization state, and the weight gain of the coating is about 15% to prepare atenolol sustained-release pellets with a drug content of 24.15%.

[0069] Weigh 10g of nifedipine and 40g of polyethylene glycol 6000 to prepare a solid dispersion. Weigh 10g of the above solid dispe...

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Abstract

The invention relates to the pharmaceutical preparation field, in particular to a compound controlled release pellet tablet of nifedipine and atenolol, and is characterized in that: controlled release pellet of nifedipine, controlled release pellet of atenolol and blank pellet are pelletized to obtain the compound controlled release pellet tablet of nifedipine and atenolol, wherein the controlled release pellet of nifedipine and the controlled release pellet of atenolol are respectively obtained from drug contained core coated with acrylic resin; the weight of coating of the controlled release pellet of nifedipine is added by 10 to 30 percent while the weight of coating of the controlled release pellet of atenolol by 8 to 25 percent; the blank pellet comprises microcrystaline cellulose and one of macrogol 6000, macrogol 4000 and stearic acid or the mixture of one or two of the macrogol 6000, the macrogol 4000 and the stearic acid, wherein the blank pellet takes up 50 to 70 percent of the total weight of the compound controlled release pellet tablet of nifedipine and atenolol.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nifedipine and atenolol compound sustained-release pellets and a preparation method thereof. Background technique [0002] Nifedinpine (NF) is a calcium antagonist; Atenolol (Atenolol, AT) is a selective β1 receptor blocker. The combination of the two in the treatment of hypertension and angina can enhance the efficacy and reduce the dosage , To counteract adverse reactions, and does not affect normal blood sugar and blood lipids. At present, the market and clinics are mostly dominated by a single preparation of nifedipine or atenolol, which has problems such as inconvenience in medication and uncoordinated drug release behavior. Compound preparations developed abroad are ordinary preparations or slow-release nifedipine mixed with immediate-release atenolol and filled in capsules, such as Beta-Adalat from ICI-PHARMA , Plenacor of Ethypharm / Nordat And Astra Zeneca’s TE...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4422A61K31/165A61K9/20A61P9/12A61P9/10
Inventor 朱家壁杨燕陈盛君
Owner CHINA PHARM UNIV
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