Carbamazepine cocrystal solid dispersion and preparation method thereof

A carbamazepine co-crystal and solid dispersion technology, which is applied in the field of medicine, can solve the problems of slow dissolution rate, poor absorption effect, and low bioavailability, and achieve fast dissolution rate, high dissolution rate, and reduced dosage. Effect

Inactive Publication Date: 2014-09-17
天津新济复兴药业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide a kind of insoluble drug eutectic solid dispersion for the dissolution rate that carbamazepine oral preparation exists is slow, and absorption effect is poor, and bioavailability is low, increases the solubility and the dissolution rate of insoluble drug, Thereby improving the oral bioavailability of poorly soluble drugs, reducing dosage and side effects

Method used

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  • Carbamazepine cocrystal solid dispersion and preparation method thereof
  • Carbamazepine cocrystal solid dispersion and preparation method thereof
  • Carbamazepine cocrystal solid dispersion and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Embodiment 1 Carbamazepine eutectic solid dispersion

[0038] Prepared from the following components:

[0039] Carbamazepine (poorly soluble drug, Wuhan Yuancheng Technology Development Co., Ltd.) 2.72g

[0040] Niacinamide (eutectic ligand, Shanghai Jingchun Reagent Co., Ltd.) 1.29g

[0041] Copovidone VA64 (polymer carrier material, German BASF company) 4.01g

[0042] The preparation method of the carbamazepine eutectic solid dispersion of embodiment 1 is eutectic-melting method, comprises the following steps:

[0043] (1) Preparation of eutectic

[0044] Dissolve 0.0115mol (1.29g) of nicotinamide in 16ml of absolute ethanol, add 0.0115mol (2.72g) of carbamazepine, heat to 65°C until carbamazepine is completely dissolved, then cool down to 55°C to facilitate carbamazepine The carbamazepine-nicotinamide co-crystal is precipitated, and the temperature is further lowered to 20°C to promote the further precipitation of the crystal. The Buchner funnel is used to filter...

Embodiment 2

[0048] Embodiment 2 Carbamazepine eutectic solid dispersion

[0049] Prepared from the following components:

[0050] Carbamazepine (poorly soluble drug, Wuhan Yuancheng Technology Development Co., Ltd.) 2.72g

[0051] Niacinamide (co-crystal ligand, Shanghai Jingchun Reagent Co., Ltd.) 1.29g

[0052] Copovidone VA64 (polymer carrier material, German BASF company) 4.01g

[0053] The preparation method of the carbamazepine eutectic solid dispersion of embodiment 2 is eutectic-hot-melt extrusion method, comprises the following steps:

[0054] (1) Preparation of eutectic

[0055] Dissolve 0.0115mol (1.29g) of nicotinamide in 16ml of absolute ethanol, add 0.0115mol (2.72g) of carbamazepine, heat to 65°C until carbamazepine is completely dissolved, then cool down to 55°C to facilitate carbamazepine For the precipitation of the mazepine-nicotinamide co-crystal, the temperature is further lowered to 20°C to promote the further precipitation of the crystal, which is separated by s...

Embodiment 7

[0059] Embodiment 7 Carbamazepine eutectic solid dispersion

[0060] Prepared from the following components:

[0061] Carbamazepine (poorly soluble drug, Wuhan Yuancheng Technology Development Co., Ltd.) 2.72g

[0062] Niacinamide (co-crystal ligand, Shanghai Jingchun Reagent Co., Ltd.) 1.29g

[0063] Copovidone VA64 (polymer carrier material, German BASF company) 6.02g

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Abstract

The invention discloses a carbamazepine cocrystal solid dispersion and a preparation method thereof. According to the invention, a cocrystal ligand and a polymer carrier material are employed to prepare the carbamazepine cocrystal solid dispersion by a melting technique and a hot melting extrusion technique, thus improving the equilibrium solubility and dissolution rate of carbamazepine. By adding the cocrystal ligand to form the cocrystal with carbamazepine, the drug's melting point can be adjusted, the selection range of the temperature and polymer carrier material for preparation of the solid dispersion through the melting technique and the hot melting extrusion technique is expanded, and the problem that the melting technique and the hot melting extrusion technique are likely to cause drug thermal decomposition is effectively solved. The preparation method provided by the invention can improve the oral bioavailability of carbamazepine, lower the dosage of administration, and reduce adverse drug reaction. With high production efficiency, the method is suitable for industrial application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a carbamazepine eutectic solid dispersion and a preparation method thereof. Background technique [0002] Carbamazepine (CBZ) is the drug of choice for the treatment of epilepsy, and is also commonly used in the treatment of trigeminal neuralgia, manic depression, arrhythmia, etc. It is a commonly used drug in clinical practice and has a huge market. It was synthesized by Schneider in Switzerland in 1961. In 1968, Novartis went on the market with Tegretol ~ tablets. So far, the main international brands are Tegretol (Novartis), Carbatrol (Shire), EquetroTM (Shire), Epitol (TEVA company), Teril (Taro company). The dosage forms on the market have also developed from simple tablets to chewable tablets, suspensions and sustained-release preparations. In 1997, Carbatrol, a sustained-release capsule composed of immediate-release, sustained-release, and enteric-coated pel...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/16A61K9/20A61K9/48A61K31/55A61K47/22A61K47/12A61P25/08
Inventor 崔景柏吴传斌梁华辉张乃军
Owner 天津新济复兴药业科技有限公司
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