Lacosamide oral solution and preparation method thereof

Abstract

According to the lacosamide oral solution and the preparation method thereof, sodium carboxymethyl cellulose, povidone and polyethylene glycol are used as taste-masking combined matrixes, the viscosity of the oral solution is increased, the contact time of a medicine and a taste bud is shortened, the strong bitter taste of the lacosamide oral solution can be effectively masked under the condition that a sweetening agent is not added, and the taste of the lacosamide oral solution is improved. The attention of a patient on bitter taste is transferred through the cooling effect of menthol, the medication compliance of the patient is improved, the stability of an oral solution is improved, and the validity period of the medicine is prolonged. In the lacosamide oral solution provided by the invention, the variety of auxiliary materials is less, the preparation method is simple, and the lacosamide oral solution has a good taste masking effect and stability.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a lacosamide oral solution and a preparation method thereof. Background technique [0002] Lacosamide is a new anti-epileptic drug developed by SchwarzBioSciences, a German subsidiary of UCB Pharma. In vivo glycine site binding antagonist. The NMDA receptor glycine site-binding antagonist belongs to a new class of functional amino acids and is an anticonvulsant drug with a new dual mechanism of action. It selectively promotes slow inactivation of sodium channels and regulates collapse response mediating protein 22 (CRMP22), which may slow or even prevent epileptic seizures and reduce neuropathic pain in diabetes. [0003] Currently, lacosamide on the market is mainly an oral solid preparation, which is inflexible in dosage, difficult to accurately control the dosage, and difficult to take for patients and children with dysphagia. Oral liquid preparations c...

AI Technical Summary

Problems solved by technology

[0003] At present, lacosamide that has been marketed is mainly oral solid preparation, which is inflexible in medication, difficult to control the dose accurately, and difficult to take for patients with dysphagia and children.

Oral liquid preparations can effectively solve the above problems, but the strong bitterness brought by the raw materials will affect the patient's taste, and a large amount of sweeteners need to be added for flavor correction

[0004] For example, Chinese patent 112022804A discloses a lacosamide oral solution, including lacosamide, solubilizer, thickener, flavoring agent, acidity regulator and preservative; wherein, the mass concentration of flavoring agent is 180-300 mg / mL, the addition of a large number of sweeteners will lead to insufficient stability and taste. For example, when natural sweeteners such as sucrose are added, the heat is high, it is easy to spoil, the solution stability is poor, it is not resistant to storage, and it is not friendly to special groups of people. , but the taste of adding artificial synthetic sweeteners is not pure enough and has a "metallic taste". Excessive consumption of its high sweetness will affect the sensitivity of taste buds, and the safety of most synthetic sweeteners is questionable

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