Nimodipine oral fast dissolving tablets and preparation method thereof

Abstract

The invention belongs to the field of medicinal preparations. Nimodipine serving as a clinical cerebrovascular medicament is applied for years; however, the nimodipine has the defects of poor water solubility, obvious first pass effect and the like due to the physicochemical property of the nimodipine, which directly influence clinical medicinal effect. The invention provides nimodipine oral fast dissolving tablets and a preparation method thereof. The preparation method comprises the following steps of: preparing a nimodipine solid dispersion with high water solubility from a nimodipine raw material and a hydrophilic carrier by a spray drying process; mixing the solid dispersion and suitable auxiliary materials; and preparing the oral fast dissolving tablets by a direct powder compression method. The preparation process is simple and industrial production is easy to realize. The prepared nimodipine oral fast dissolving tablets can be administrated without water. After being administrated, the nimodipine oral fast dissolving tablets are rapidly dissolved and absorbed in an oral cavity in 30 seconds so as to avoid the first pass effect of the gastrointestinal tract, greatly improve the dissolution rate of the medicament and improve the bioavailability of the medicament.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an oral instant tablet of nimodipine and a preparation method thereof. Background technique: [0002] Nimodipine, also known as nifedipine, is a second-generation pyridine calcium antagonist. At present, it is mostly used in clinical treatment of cerebrovascular disease, namely for ischemic cerebrovascular disease, treatment of mild or moderate hypertension, prevention and treatment of cerebral vasospasm, sudden deafness, migraine after subarachnoid hemorrhage, etc. . [0003] Nimodipine has been used as a clinical cerebrovascular drug for many years, but due to its own physical and chemical properties, it has shortcomings such as poor water solubility and obvious first-pass effect, which directly affects the clinical efficacy. On the one hand, the saturated solubility of the hydrophobic drug nimodipine in water is only 4 μg / ml. After entering the body, m...

AI Technical Summary

Problems solved by technology

[0005] When nimodipine tablets and capsules are administered orally, they will be metabolized by the liver before being absorbed through the gastrointestinal tract, enter the surrounding capillaries or lymphatic vessels, and then enter the blood circulation. There is a long period of absorption and distribution process in the middle. About 80% is lost in the whole process, and the first-pass effect is very obvious; and although nimodipine injection directly enters the blood circulation and is fully absorbed, it has the disadvantages of being inconvenient to use and unacceptable to patients

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