Ramosetron hydrochloride effervescent tablet and preparation method thereof

Abstract

The invention discloses a ramosetron hydrochloride effervescent tablet. The ramosetron hydrochloride effervescent tablet is prepared by mixing and compacting a pellet and a tablet excipient, the pellet and the tablet excipient respectively contain at least one pharmaceutically acceptable organic acid and at least one pharmaceutically acceptable alkaline compound, the pellet accounts for 60% or less of the weight of the effervescent tablet, and the pellet is prepared from, by weight, 0.005 parts of ramosetron hydrochloride, 50-120 parts of lactose, 10-40 parts of microcrystalline cellulose, 40-80 parts of the organic acid, 3-8 parts of a flavoring agent and 1-5 parts of a perfume. The ramosetron hydrochloride is stable under high-temperature and high-humidity conditions. An isolation layer coating makes the ramosetron hydrochloride stable to light.

Description

technical field [0001] The invention relates to an effervescent tablet, in particular to a ramosetron hydrochloride effervescent tablet. It belongs to the field of medical technology. Background technique [0002] The chemical name of Ramosetron is (-)-(R)-5-((1-methyl-1H-indol-3-yl)carbonyl)-4,5,6,7-tetrahydro -1H-benzimidazole. [0003] In EP-A-381422, it is disclosed that a series of tetrahydrobenzimidazole derivatives including ramosetron and its pharmaceutically acceptable salts have antagonism on 5HT3 receptors. Based on this effect, the patent proposes that it may inhibit vomiting caused by anticancer drugs (such as cisplatin and radiation exposure), and may prevent and treat migraine, complex headache, trigeminal neuralgia, anxiety, abnormal gastrointestinal motility, digestive Ulcers, irritable bowel syndrome, etc., and the commonly used clinical doses are explained, adult daily 0.1 to 10mg intravenously, and 0.5 to 50mg orally, once a day or divided into multipl...

AI Technical Summary

Problems solved by technology

[0005] However, the active ingredient ramosetron hydrochloride is unstable under light and heat conditions

When it is used as a drug for the treatment of irritable bowel syndrome, according to the results of clinical trials, the effective daily dosage is in the range of 0.001-0.005mg, which is lower than that of 0.1mg orally disintegrating tablets. 20 to 100 times higher, and the ratio of excipients to API (drug active ingredient) will increase by 20 to 100 times. The influence of interaction with excipients, resulting in a decrease in its stability

[0006] As a technique for stabilizing ramosetron against temperature and humidity conditions, it is known that the incorporation of a specific compound with a carbonyl group can improve its stability, but the addition of a carbonyl compound tends to cause sticking and other phenomena

On the other hand, the incorporation of iron oxide, titanium dioxide and other substances with light-shielding effect can reduce the sensitivity of ramosetron to light. Due to its distribution in the tablet and other problems, the expected stable effect is often not obtained.

Among the products already on the market, rapid disintegration, high bioavailability, and light, humidity and heat stability are often not achieved simultaneously

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