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Preparation method of carbamazepine solid dispersion with high drug loading capacity

A solid dispersion, carbamazepine technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, drug combinations, etc., can solve the problems of limited application, small drug loading, etc., achieve fast dissolution rate, good tableting performance effect

Active Publication Date: 2019-03-15
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To maintain a highly dispersed state of the drug, a large amount of carrier material is often required to achieve the ideal dissolution effect, so the drug loading capacity of the solid dispersion is generally small, which severely limits its application in some insoluble drugs with large doses.

Method used

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  • Preparation method of carbamazepine solid dispersion with high drug loading capacity
  • Preparation method of carbamazepine solid dispersion with high drug loading capacity
  • Preparation method of carbamazepine solid dispersion with high drug loading capacity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Take by weighing carbamazepine (Zhejiang Jiuzhou Pharmaceutical Co., Ltd.) 8g, polyacrylic resin Eudragit EPO (Evonik Industrial Group) 8g, mix and add to twin-screw hot-melt extruder (Thermo Fisher Scientific Co., Ltd. company), extruded at 120°C at a speed of 50 rpm, cooled, crushed, and passed through a 120-mesh sieve.

[0024] Get 200mg of gained solid dispersion powder, measure the dissolution rate of medicine by " Chinese Pharmacopoeia " dissolution rate second method, dissolution medium is the hydrochloric acid solution that 500mL pH is 1.2, and rotating speed is 50r min -1 , The sampling time is 5, 10, 20, 30, 45, 60 minutes respectively. As a result, the dissolution in 10min exceeds 80% (see figure 1 ).

Embodiment 2

[0026] Weigh 10g of carbamazepine and 5g of polyacrylic acid resin Eudragit EPO, mix them evenly, add them to a twin-screw hot-melt extruder, extrude them at a speed of 50 rpm at 140°C, crush them after cooling, and pass through a 120-mesh sieve , that is.

[0027] Get product 150mg, according to " Chinese Pharmacopoeia " dissolution rate second method is measured the dissolution rate of medicine, dissolution medium is the hydrochloric acid solution that 500mLpH is 1.2, and rotating speed is 50r min -1 , The sampling time is 5, 10, 20, 30, 45, 60 minutes respectively. As a result, the dissolution in 10min exceeds 80% (see figure 1 ).

Embodiment 3

[0029] Weigh 12g of carbamazepine and 3g of polyacrylic acid resin Eudragit EPO, mix them evenly, add them to a twin-screw hot-melt extruder, extrude them at a speed of 30 rpm at 140°C, crush them after cooling, and pass through a 120-mesh sieve , that is.

[0030] Get product 125mg, measure the dissolution rate of medicine by " Chinese Pharmacopoeia " dissolution rate second method, dissolution medium is the hydrochloric acid solution that 500mLpH is 1.2, and rotating speed is 50r min -1 , The sampling time is 5, 10, 20, 30, 45, 60 minutes respectively. In addition, 100 mg of carbamazepine raw material of 120 mesh and 125 mg of a physical mixture of carbamazepine and acrylic resin with a mass ratio of 4:1 were taken, and the dissolution rate was determined by the same method.

[0031] Result: the dissolution rate of carbamazepine only dissolved 50% in 60min, after adding the polyacrylic acid resin Eudragit EPO of 1 / 4 of drug quality and mixing, the dissolution rate in 60min ...

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Abstract

The invention provides a preparation method of carbamazepine solid dispersion with drug loading capacity of 50% or higher. The method comprises the following steps: weighing carbamazepine and a support material, uniformly mixing carbamazepine and the support material, adding the mixture to a twin-screw hot melting extruder, performing extruding at the temperature of 120-160 DEG C and at the rotating speed of 30-100 r / min, cooling an extruded product to room temperature, smashing the product, and sieving the product with a 60-120-mesh sieve to obtain the carbamazepine solid dispersion. The prepared carbamazepine solid dispersion has higher dissolution rate and good tablet compressing performance.

Description

(1) Technical field [0001] The invention relates to a method for preparing a carbamazepine solid dispersion with a drug loading of more than 50% and a faster drug dissolution rate. (2) Background technology [0002] Carbamazepine is a common antiepileptic drug, which is mainly used to treat various epilepsy except petit mal, and is also commonly used in the treatment of trigeminal neuralgia, glossopharyngeal neuralgia, diabetes insipidus and pain syndrome. Carbamazepine was first synthesized by Schneider in Switzerland in 1961, and Novartis in 1968 as Tablets are on the market, and various dosage forms such as chewable tablets, suspensions and sustained-release preparations are now on the market. [0003] Carbamazepine is almost insoluble in water, and its solubility does not change with the pH value, but it has good mucosal permeability and belongs to a typical BCSII drug. The bioavailability of ordinary carbamazepine tablets is often affected by the limitation of solubi...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/32A61K47/38A61K31/55A61P25/08A61P25/02
CPCA61K9/146A61K31/55A61P25/02A61P25/08
Inventor 王文喜冯子琳李梦婷
Owner ZHEJIANG UNIV OF TECH
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