Topiramate granule and preparation method thereof

Abstract

The invention provides a topiramate granule and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The preparation method comprises the steps of firstly, preparing a cyclodextrin inclusion compound from topiramate serving as an active drug; then, screening the inclusion compound, and next, uniformly mixing the screened inclusion compound and pharmaceutically-acceptable auxiliary materials; and granulating by using a wet process or dry process to obtain the granule. The granule is good in uniformity and stability and is easily dissolved into water; the bitter taste of topiramate is completely covered; the taste of the topiramate granule is remarkably improved; the dosage of the topiramate granule can be conveniently selected according to the age and bodyweight of a patient; and the compliance of the old, children and patients having difficulty in swallowing during drug use is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a topiramate granule and a preparation method thereof. Background technique [0002] Topiramate is a new generation of antiepileptic drugs, which is a new type of antiepileptic drugs that replace monosaccharides with sulfamic acid esters. It was synthesized for the first time in 1980 and used to treat the first epilepsy patient in 1986. It was developed by Johnson & Johnson in the United States and launched in the UK in 1995. It was approved by the FDA in 1996 for the treatment of primary epilepsy in adults. Partial epilepsy, approved in 2000 for the treatment of epilepsy in children. In 2004, the FDA approved the drug for the prevention of migraine in adults. In July 2012, the FDA approved the launch of Qsymia, a compound weight-loss drug containing topiramate and phentermine from Vivus Pharmaceuticals of the United States, which is the second n...

AI Technical Summary

Problems solved by technology

[0016] In order to cover up its special bitter taste, it is convenient for children and the elderly to take it, and to ensure good absorption in the body. At the same time, in order to improve the long-term stability and water solubility of the preparation , the present invention provides a granule of topiramate, which can well solve the problems existing in the prior art. This product completely conceals the special bitter taste of the drug, improves the compliance of patients with medication, and is especially suitable for patients with dysphagia. For children and the elderly, the inventor conducted a large number of comparative studies on the problem of poor drug stability, and found that the solution was solved by making the active ingredient of the drug into a cyclodextrin inclusion compound, and unexpectedly found that the cyclodextrin inclusion technology was applied Because the dosage form can increase the water solubility of the main drug, it can significantly improve the dissolution rate and bioavailability of the drug, and at the same time, the drug after cyclodextrin inclusion can be released smoothly in the gastrointestinal tract, reducing the irritation to the gastrointestinal tract. It avoids the peak-valley phenomenon of the blood drug concentration, significantly reduces the adverse reactions of the drug, and improves the safety of the drug, which is beyond the reach of ordinary granules of topiramate

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