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Carbamazepine oral sustained release preparation and preparation method thereof

A sustained-release preparation, the technology of carbamazepine, is applied in the field of oral sustained-release preparations of carbamazepine, and can solve the problems of environmental damage, high technical barriers of osmotic pump preparations, and difficulty in imitation.

Inactive Publication Date: 2018-06-08
SHANGHAI ANBISON LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Since the launch of the original drug Tegretol XR, no generic drug for osmotic pump preparations has been on the market so far, and the US patent US 5284662 of the original drug discloses a coating system using dichloromethane-methanol as a solvent, but both dichloromethane and methanol are ICH II toxic solvents, industrial production causes great damage to the environment
On the one hand, due to the high technical barriers of osmotic pump preparations, and on the other hand, due to the special coating system using dichloromethane as the coating solvent, no one has broken through the problem of imitating the original drug Tegretol XR. Strict requirements make it even more difficult to imitate the original drug Tegretol XR

Method used

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  • Carbamazepine oral sustained release preparation and preparation method thereof
  • Carbamazepine oral sustained release preparation and preparation method thereof
  • Carbamazepine oral sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1~3

[0064] Embodiment 1 ~ 3 core

[0065]

[0066] Preparation Process

[0067] Core preparation: add the core material components 1-10 into a tank mixer or a high-shear wet granulator and mix for 15 minutes, then add purified water for mixing and granulation. Wet and soft materials are sieved and granulated, and then dried in an oven or fluidized bed at 80°C. Magnesium stearate was added to the dry granules, mixed for 5 minutes, and then compressed using a high-speed rotary tablet press. The above-mentioned carbamazepine is anhydrous carbamazepine.

Embodiment 4~11

[0068] Embodiment 4~11 membrane control coating system

[0069]

[0070] Preparation: The coating materials of Examples 4-6 were dispersed in a mixed solvent of 85:15 acetone-water, and then sprayed onto the surface of the tablet cores of Examples 1-3 respectively. After the coating is dry, the coating is perforated by mechanical or laser.

[0071]

[0072] Preparation: Dissolve the materials of Examples 7-9 in a 90:10 mixed solvent of ethanol-water to prepare a coating solution with a solid content of 7%, and then spray them on the surface of the tablet cores of Examples 1-3 respectively. After the coating is dry, the coating is perforated by mechanical or laser. figure 2 Comparison chart of the dissolution of the carbamazepine sustained-release preparation prepared in Example 4 / 6 / 7 and Tegretol XR under USP conditions. It can be seen that Example 7 has particularly outstanding properties.

[0073] Example 10 Sample preparation is carried out according to the exampl...

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Abstract

The invention relates to a carbamazepine oral sustained release preparation and a preparation method thereof. The sustained release preparation is a perforated single-chamber osmotic pump sustained release preparation; the sustained release preparation comprises 30 to 60 percent by weight of nonaqueous carbamazepine; the sustained release preparation further comprises a film-controlled coating system; the film-controlled coating system is prepared from 1 to 10 percent by weight of water-insoluble film-forming material; a coating agent does not need to be an ICHII type solvent or a higher-toxicity solvent. The sustained release preparation disclosed by the invention has pharmacokinetics parameters being statistically equivalent to an original drug under the condition of not using any toxicand efficient solvent.

Description

technical field [0001] The invention relates to an oral sustained release preparation of carbamazepine. The invention also relates to a preparation method of carbamazepine oral sustained-release preparation. Background technique [0002] Carbamazepine or 5H-dibenzo[b,f]azepine-5-carboxamide is commonly used in the clinical treatment of epilepsy, triangular neuralgia and bipolar syndrome. The drug was synthesized by Schneider in 1961 and marketed in the form of tablets by Ciba-Geigy in 1968 under the trade name Tegretol. So far, the international brands mainly include: Tegretol® (Novartis), Carbatrol®(Shire), equetrotm (Validus), Epitol® (TEVA) and Teril®(Taro). The dosage forms on the market have also developed from ordinary tablets to chewable tablets, oral suspensions, and delayed-release preparations. In 1996, FDA approved delayed-release tablets 400mg, 200mg, and 100mg (TEGRETOL-XR, Novartis). In 1997, Shire's sustained-release capsule (CARBATROL) was approved by the...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/22A61K47/38A61K31/55A61P25/08A61P25/02A61P29/00A61P25/18
CPCA61K9/2866A61K31/55
Inventor 陆鑫雷继峰沙平谢东方施钰文
Owner SHANGHAI ANBISON LAB