Levetiracetam oral solution and preparation method thereof

Abstract

The invention discloses a levetiracetam oral solution and a preparation method thereof, wherein the levetiracetam oral solution comprises levetiracetam, a preservative, a flavoring agent, a buffer agent and a solvent. The content of levetiracetam is 10 g / 100 ml; the content of the preservative is 120-220 mg / 100 ml, and the preservative is a mixture of methylparaben and propylparaben; the content of the flavoring agent is 22.5-25 g / 100 ml, and the flavoring agent is a mixture of maltitol type I, ammonium glycyrrhetate and potassium acetosulfonate; the solvent is a mixture of glycerol and purified water. The content of the preservative in the levetiracetam oral solution is low, the levetiracetam oral solution not only can satisfy a bacteriostasis effect, but also can reduce adverse reactionsand has high safety. The mixture of maltitol type I, ammonium glycyrrhizinate and potassium acetylsulfonate is used as the flavoring agent, so both the effects of flavor correction and thickening areachieved, and the bitterness is reduced. The levetiracetam oral solution contains alanine and / or taurine and other flavor masking agents and has better taste.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a levetiracetam oral solution and a preparation method thereof. Background technique [0002] Levetiracetam (trade name: Kaiplan) is a new type of antiepileptic drug developed by UCB in Belgium. Adjunctive treatment of partial seizures in adults, children, and infants over one year of age with epilepsy. [0003] Levetiracetam binds to the synaptic vesicle protein SV2A in presynaptic nerve terminals, which inhibits abnormal discharges in the epileptic circuit, thereby blocking seizures. Levetiracetam not only has a high effective rate of clinical treatment, but also has few adverse reactions and high safety. It is one of the ideal therapeutic drugs for children with epilepsy. [0004] According to the usage and dosage of levetiracetam preparations, the initial therapeutic dose for infants aged 1-6 months is 7 mg / kg, and the initial therapeutic dose for infants aged...

AI Technical Summary

Problems solved by technology

[0005] UCB’s Kaiplan prescription contains ingredients such as methylparaben, propylparaben, and maltitol liquid, and the dosages of preservatives methylparaben and propylparaben are 2.7mg / ml and 0.3mg / ml respectively. ml; the composition of this prescription has the following deficiencies: (1) The contents of methylparaben and propylparaben are relatively high, both of which exceed the limit of 2.0mg / ml and 0.2mg / ml stipulated by the US FDA, and there are hidden dangers in drug safety (2) maltitol liquid can reduce the antibacterial ability of methylparaben and propylparaben

[0007] The Chinese invention patent application with the application number 201710080065.5 discloses levetiracetam oral solution and its preparation method. The sweeteners in the levetiracetam oral solution are mannitol, maltitol solution, sorbitol, ammonium glycyrrhizinate, One or more mixtures of stevioside and acesulfame K, and the preservative is one or more mixtures of benzoic acid, sodium benzoate, methylparaben, and propylparaben, which has the following disadvantages : (1) Sorbitol in sorbitol and maltitol solution has incompatibility with preservatives methylparaben and propylparaben, which will reduce the antibacterial effect of preservatives; (2) the consumption of methylparaben in the embodiment The dosage of propylparaben is 0.5g / 100ml, the dosage of propylparaben is 0.1g / 100ml, and the dosage of preservatives exceeds the standard of US FDA

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