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Adduct of topiramate and tramadol hydrochloride and uses thereof

A technology for tramadol hydrochloride and adducts, which is applied to the preparation of sugar compounds with non-glycosyl groups, organic compounds, active ingredients of heterocyclic compounds, etc., and can solve the problems of long half-life and short half-life of topiramate

Inactive Publication Date: 2005-08-10
CILAG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Also, the half-lives of topiramate and tramadol are quite different, with tramadol having a relatively short half-life and topiramate having a relatively long half-life

Method used

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  • Adduct of topiramate and tramadol hydrochloride and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: the preparation of formula (I) adduct

[0051] Mix 2 moles of tramadol hydrochloride and 1 mole of topiramate in ethanol, heat to 40°C, and keep the temperature for a sufficient time until the solid drug is completely dissolved. The mixture is then cooled to a temperature of about 2-8°C, whereupon crystallization begins. The whole mixture was left at this temperature for several hours to form the remaining crystals. The entire material was filtered cold and the crystals dried. The resulting 1:1 adduct had a melting point of about 161°C (onset temperature).

Embodiment 2

[0052] Example 2: Composition Example

[0053] Typical pharmaceutical compositions of the invention in dosage unit form suitable for systemic or topical administration to warm-blooded animals are illustrated below.

[0054] capsule

[0055] 50 g of the adduct of formula (I), 12 g of sodium lauryl sulfate, 112 g of starch, 112 g of lactose, 1.6 g of colloidal silicon dioxide, and 2.4 g of magnesium stearate were stirred vigorously. The resulting mixture is then filled into 1000 suitable hard gelatine capsules, each containing 50 mg of the adduct of formula (I).

[0056] Film Coated Tablets

[0057] Preparation of tablet cores

[0058] 500g formula (I) adduct, the mixture of 2850g lactose and 1000g starch is mixed completely, and mixture is mixed with 25g sodium lauryl sulfate and 50g polyvinylpyrrolidone (Kollidon-K 90 TM ) in about 1000ml of water to wet the solution. The wet powder mixture is sieved, dried and re-sifted. Then add 500g microcrystalline cellulose (Avicel)...

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Abstract

This invention relates to a new pharmaceutically useful compound which is a stoichiometrically 1:1 adduct of tramadol hydrochloride and topiramate, to the manufacture and use thereof.

Description

Brief description of the invention [0001] The present invention relates to a new pharmaceutical compound, which is an adduct of tramadol hydrochloride and topiramate in a stoichiometric ratio of 1:1, as well as its preparation and application. Background technique [0002] U.S. Patent 4513006 discloses some effective anticonvulsant drugs, including compound 2,3:4,5-di-O-(1-methylethylene)-β-D-fructopyranose sulfamate, also called topiramate. Topiramate is used in the treatment of epilepsy in humans, effective as adjunctive therapy or as monotherapy in the treatment of simple or complex partial seizures and secondary generalized seizures (E.Faught et.al., Epilepsia 36(S4)33, 1995; S.K. Sachdeo, et al., Epilepsia 36(S4)33, 1995). [0003] Topiramate is currently on the market for the treatment of simple or generalized partial-onset epilepsy with or without secondary generalized seizures. [0004] Recent preclinical trials on topiramate have shown previously unknown pharmaco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/35A61K45/06C07D493/14A61P25/04C07C217/74C07H7/00C07H9/04
CPCC07C217/74C07C2101/14C07H7/00C07H9/04A61K45/06C07C2601/14A61P25/04
Inventor R·奈夫S·斯皮彻尔-胡伯尔T·亨齐克G·劳菲尔
Owner CILAG
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