Atenolol non-pH-dependent sustained release pellets and preparation method thereof

A technology of sustained-release micropills and micropills, which is applied in the direction of bulk delivery, cardiovascular system diseases, drug combination, etc., and can solve the problems of complex preparation process and easy adhesion

Inactive Publication Date: 2010-08-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process is relatively complicated, and the coated pellets are all in the range of 30-40 mesh, which is very easy to stick when coating

Method used

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  • Atenolol non-pH-dependent sustained release pellets and preparation method thereof
  • Atenolol non-pH-dependent sustained release pellets and preparation method thereof
  • Atenolol non-pH-dependent sustained release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The dosage of each auxiliary material in every 1000 grams of atenolol non-pH dependent sustained-release pellet preparation:

[0046] Microcrystalline Cellulose 590g

[0047] Adipic acid 150g

[0048] Atenolol 250g

[0049] Crospovidone 10g

[0050] Binder: 4% PVP-K30 aqueous solution

[0051] Isolation layer coating material: 5% Opadry 75% ethanol solution (Shanghai Colorcon Company)

[0052] Sustained-release coating layer material: 10% Surelease water dispersion (Shanghai Colorcon Company)

[0053] Preparation of pill core: Pass microcrystalline cellulose, adipic acid, atenolol, and crospovidone through a 100-mesh sieve, mix well, add binder to make soft material, extrude at about 25 rpm, and roll into a ball The speed is about 1500rpm, the ball is spheronized for about 8 minutes, and it is dried in a constant temperature box at 40°C. The yield of the 20-40 mesh pellet core is about 75%.

[0054] Coating: Put 20-40 mesh pill cores in the fluidized bed, coat the...

Embodiment 2

[0056] The dosage of each auxiliary material in every 1000 grams of atenolol non-pH dependent sustained-release pellet preparation:

[0057] Microcrystalline Cellulose 640g

[0058] Fumaric acid 100g

[0059] Atenolol 250g

[0060] Sodium carboxymethyl starch 10g

[0061] Binder: 2% HPMC-E5 aqueous solution

[0062] Isolation layer coating material: 4% Opadry 50% ethanol solution (Shanghai Colorcon Company)

[0063] Sustained-release coating layer material: 15% Surelease water dispersion (Shanghai Colorcon Company)

[0064] Preparation of pill core: Pass microcrystalline cellulose, fumaric acid, atenolol, and sodium carboxymethyl starch through a 100-mesh sieve and mix evenly, add binder to make soft material, extrude at about 25 rpm, and roll into a ball The speed is about 1200rpm, rounded for 12 minutes, and placed in a 40°C thermostat to dry to obtain the drug-containing core. The yield of the 20-40 mesh drug-containing core is about 80%.

[0065] Coating: Put 20-40 m...

Embodiment 3

[0067] The dosage of each auxiliary material in every 1000 grams of atenolol non-pH dependent sustained-release pellet preparation:

[0068] Starch 400g

[0069] Dextrin 200g

[0070] Adipic acid 150g

[0071] Atenolol 250g

[0072] Adhesive: 25% ethanol aqueous solution Isolation layer Coating material: 80% ethanol solution of 3% HPMC-E5 (containing 15% PEG4000, 20% micropowder silica gel) Sustained release coating layer material: 8% Surelease water dispersion ( Shanghai Colorcon Company)

[0073] Preparation of pill cores: Pass starch, dextrin, adipic acid, and atenolol through a 100-mesh sieve and mix evenly, add binders to make soft materials, extrusion speed 25rpm, spheronization speed 1200rpm, spheronization 9min, set Dried in a constant temperature box at 40°C to obtain the drug-containing core, the yield of the 20-40 mesh drug-containing core is about 75%.

[0074] Coating: Put 20-40 mesh-containing pill cores in the fluidized bed, use 3% HPMC-E5 80% ethanol solut...

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a non-pH-dependent sustained release pellet preparation containing atenolol and a preparation method thereof. The atenolol non-pH-dependent sustained release pellet preparation mainly consists of atenolol-containing pellet cores and coating materials, and is characterized in that the atenolol-containing pellet cores contain a certain proportion of solid organic acid, wherein the solid organic acid is one or more selected from fumaric acid, sorbic acid and adipic acid. The atenolol-containing pellet cores are prepared by the extrusion-spheronization method. The results show that the prepared pellets have good roundness, and the sustained release preparation can be smoothly released in different pH release media.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a non-pH dependent sustained-release pellet preparation containing atenolol and a preparation method thereof. Background technique [0002] Atenolol (AT for short) belongs to the second generation of β-receptor blockers. It reaches the peak concentration in 2-4 hours after oral administration, and its half-life in the blood is 5-7 hours. It can selectively block β-blockers. 1 The receptor is more selective for the heart than blood vessels, has no endogenous sympathomimetic activity, no membrane stability, and no inhibitory effect on myocardial contractility. In 1982, the US FDA approved it for the treatment of hypertension, angina pectoris, early acute myocardial infarction and arrhythmia. The raw materials, tablets and injections have all been listed in the British Pharmacopoeia and the United States Pharmacopoeia. The Chinese Pharmacopoeia has included atenolol raw m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/165A61K47/12A61P9/12A61P9/10A61P9/06
Inventor 刘建平董晨东
Owner CHINA PHARM UNIV
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