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High-drug loading capacity oxcarbazepine controlled-release granule and preparation method thereof

A technology of high drug loading and granules, which is applied in the field of medicine, can solve the problems of transportation, storage, inconvenient portability, enrichment of suspension particles in the suspension medium, and poor oral applicability, so as to improve portability, The effect of high drug loading and small batch-to-batch variation

Inactive Publication Date: 2014-10-29
SHANGHAI AUCTA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the dose factor, the sustained-release tablet is too heavy (600 mg tablet weighs more than 1 g) and is indivisible, so it is not suitable for oral administration of children, the elderly and other patients with dysphagia.
However, suspensions are inconvenient in transportation, storage, and portability. In addition, long-term storage will cause problems such as sedimentation of suspended particles and accumulation of suspension medium at the bottom. It needs to be shaken vigorously before use, and viscous suspensions will Inconvenience to patients

Method used

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  • High-drug loading capacity oxcarbazepine controlled-release granule and preparation method thereof
  • High-drug loading capacity oxcarbazepine controlled-release granule and preparation method thereof
  • High-drug loading capacity oxcarbazepine controlled-release granule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Representative oxcarbazepine extended-release granules (immediate-release pellet cores prepared by extrusion spheronization, coated with Opadry I isolation coating suspension and acrylic resin extended-release coating suspension) are provided in Table 1 middle.

[0026] Table 1 Components of oxcarbazepine sustained-release granules

[0027]

[0028] Preparation steps of immediate-release pellets:

[0029] First, the poloxamer is formulated as a wetting agent with an appropriate amount of water. Weigh the rest of the raw and auxiliary materials in the prescribed amount, sieve and break the blocks, and place them in a wet granulator for dry mixing. Add an appropriate amount of wetting agent to it under stirring, and stir evenly to obtain a soft material; place the soft material in an extruder equipped with a 0.6mm aperture screen and extrude at a speed of 25rpm, and the strips pass through a spheronizer at 800rpm Spheronize for 3 minutes to obtain pellets ...

Embodiment 2

[0038] Example 2 Representative oxcarbazepine extended-release granules (immediate-release pellet cores prepared by hot-melt extrusion process, coated with Opadry I barrier coating suspension and acrylic resin extended-release coating suspension) are provided in Table 2 in.

[0039] Table 2 Components of oxcarbazepine sustained-release granules

[0040]

[0041] Preparation steps of immediate-release pellets:

[0042] The high-loaded oxcarbazepine immediate-release pellet core was prepared by hot-melt extrusion process, and the specific process was as follows:

[0043]1. Preparation of physical mixture: Weigh the raw and auxiliary materials of the prescription amount, sieve and break them, and dry mix them evenly in a mixer;

[0044] 2. Extrusion and granulation: set the temperature f of the conveying section, melting section, mixing section, and metering section of the hot-melt extruder to 40, 60, 60, and 40°C respectively. After preheating for 30 minutes, the above phys...

Embodiment 3

[0047] Example 3 Representative oxcarbazepine sustained-release granules (sodium lauryl sulfate was used instead of poloxamer, pellet cores were prepared by extrusion spheronization) are shown in Table 3.

[0048] Table 3 Components of oxcarbazepine sustained-release granules

[0049]

[0050] Preparation steps of immediate-release pellets:

[0051] Weigh the raw and auxiliary materials of the prescription amount, sieve and break the blocks, and place them in a wet granulator for dry mixing. at 300rpm

[0052] Add an appropriate amount of wetting agent to it under high-speed stirring, and stir evenly to obtain a soft material; place the soft material in an extruder equipped with a 0.6mm aperture screen and extrude at a speed of 35rpm, and the strips pass through a spheronizer at 1000rpm Spheronize for 3 minutes to obtain pellets with uniform particle size; dry the pellets at 60°C until the water content is less than 2%, and sieve the pellets with a size between 500-800 um...

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Abstract

The invention belongs to the field of medicine science and technology, and particularly relates to a high-drug loading capacity oxcarbazepine controlled-release granule and a preparation method thereof. The oxcarbazepine controlled-release granule provided by the invention is prepared by preparing a high-drug loading capacity oxcarbazepine quick-release pellet by oxcarbazepine and accessories via an extrusion rolling process or a hot-melt extrusion process and then coating an isolation layer and a controlled-release layer (collectively referred to as coating layers) through a fluidized bed coating technology. The oxcarbazepine controlled-release granule has an in-vitro release curve similar to that of an oxcarbazepine quick-release tablet. The prepared oxcarbazepine quick-release granule has the advantages of high drug loading capacity, stability in release, uniform granularity and good stability, has the effect of extremely improving the patient taking compliance, and is mainly used for treating the epilepsy attack of children, old people or dysphagia patients.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a sustained-release granule containing oxcarbazepine pharmacologically active components and a preparation method thereof. Background technique [0002] Oxcarbazepine is an oral antiepileptic drug. Both oxcarbazepine and its metabolite hydroxy derivatives in the body have anticonvulsant activity. It is a neurological drug that can be used alone or in combination with other antiepileptic drugs. Localized and generalized seizures. At present, the dosage forms of oxcarbazepine that have been marketed at home and abroad include ordinary tablets, suspensions and sustained-release tablets. Ordinary tablets have three specifications, namely 150mg, 300mg and 600mg (Trex), which are taken twice a day; oral suspensions have one specification, namely 30mg / 5mL, which is suitable for children, the elderly and other patients with dysphagia. Take it twice a day. In October 2012,...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/28A61K31/55A61P25/08A61J3/06
Inventor 卢恩先李守峰马红岩李朋朋
Owner SHANGHAI AUCTA PHARMA CO LTD
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