A kind of oxcarbazepine sustained-release preparation, preparation method and application thereof

Abstract

The invention belongs to the technical field of medicines, and in particular to an oxcarbazepine sustained release preparation and a preparation method thereof. The oxcarbazepine tablet is composed of40-100 parts of oxcarbazepine, 4-20 parts of a framework material, 5-50 parts of a filler, 1-50 parts of an adhesive and 0.05-2 parts of a lubricant. According to the oxcarbazepine sustained releasetablet and the preparation method thereof, conventional sustained-release matrix auxiliary materials are adopted as a framework, other conventional auxiliary materials are combined, wet granulation and tabletting processes are utilized for preparing the oxcarbazepine sustained-release tablet, a cosolvent lauryl sodium sulfate in an original research preparation product is prevented from being used, and nausea, emesis and human body toxicity caused by a preparation finished product are reduced; pH-dependent auxiliary materials in an original research preparation product are not used, so that the influence of food and gastric juice pH is avoided, and the risk of premature burst release after the preparation product enters a human body is avoided; through preparation adjustment, compared witha reference preparation on the market, the oxcarbazepine sustained release tablet has similar in-vitro release curves and consistent in-vivo bioequivalence.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oxcarbazepine sustained-release preparation, a preparation method and an application thereof. [0002] technical background [0003] Epilepsy is a brain disorder characterized by the persistence of long-lasting changes in the brain that produce seizures, with corresponding neurobiological, cognitive, psychological, and sociological consequences. 15%-25% of epilepsy patients whose seizures cannot be controlled by drug treatment are clinically regarded as intractable epilepsy. Intractable epilepsy has different etiologies and clinical manifestations, but most patients do not respond to commonly used antiepileptic drugs. Long-term recurrent seizures seriously affect the quality of life of patients and bring a heavy burden to society and families. [0004] Oxcarbazepine is an oral antiepileptic drug. Both oxcarbazepine and its metabolite 10-monohydroxy metabolite (MHD...

AI Technical Summary

Problems solved by technology

In the examples, the raw and auxiliary materials are required to be mixed and jet milled multiple times, and the particle size of the mixture needs to be controlled to a certain extent (for example: D90 is 25 μm, D50 is 15 μm, and D5 is 5 μm). This process requires relatively high equipment requirements. High, and the process is complicated, resulting in poor reproducibility between batches, low yield of finished products, and high product cost

[0008] If the surfactant and pH-dependent excipients in the original drug are removed, the preparation will be slowed down due to the decrease in the solubility of oxcarbazepine in body fluids and the overall release in the gastrointestinal tract, and due to the removal of pH-dependent excipients, the Unable to form a pH-dependent release in the gastrointestinal tract, thus unable to effectively control the release

[0009] In view of this, there is a lack of a sustained-release preparation of oxcarbazepine clinically, which can avoid unnecessary side effects caused by adding some special excipients, and can be prepared simply and with good batch reproducibility

Images