Ivabradine hydrochloride sustained-release preparation as well as preparation method and application thereof

Abstract

The invention provides an ivabradine hydrochloride sustained-release preparation as well as a preparation method and application thereof, and belongs to the field of pharmaceutical preparations. The ivabradine hydrochloride sustained-release preparation is composed of a blank pellet core, a drug-containing layer, an isolation coating layer, a sustained-release coating layer and a protective coating layer. The ivabradine hydrochloride sustained-release preparation prepared by the invention consists of a plurality of small-unit pellets and is filled in a hard capsule, so that the peak valley phenomenon of the blood concentration of a common preparation can be effectively avoided, the medicine taking frequency can be reduced, the sudden release phenomenon possibly occurring in a single-element sustained-release preparation can be avoided, the side effect of the medicine can be reduced, and the medication compliance of a patient is enhanced. The capsule preparation is convenient to take, the preparation process is simple, the technical difficulty is low, and industrial large-scale production is easy to realize.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an ivabradine hydrochloride sustained-release preparation and a preparation method and application thereof. Background technique [0002] Ivabradine hydrochloride (Ivabradine hydrochloride), the chemical name is 3-[3-[[[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-triene -7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepine-2-one hydrochloride Salt is the first selective and specific inhibitor of sinoatrial node If current. Its simple heart rate slowing effect is the most important progress in the treatment of stable angina pectoris in the past 20 years. Ivabradine hydrochloride is the first pure heart rate-lowering factor, the first selective and specific IF (controlling spontaneous diastolic depolarization and regulating heart rate in the sinus node) inhibitor, which has a selective effect on the sinus node and a There was no e...

AI Technical Summary

Problems solved by technology

This technique requires heating the drug and excipients to 130°C, which may be detrimental to the stability of the drug

In addition, the preparation process of this technology is complicated, and industrial production is difficult

[0006] CN102908327B discloses a sustained-release preparation of ivabradine hydrochloride, which is prepared into a sustained-release matrix tablet; although the preparation is a slow-release drug, it is not a constant-rate drug release, and the gastrointestinal environment in the human body affects the release and release of the drug. Absorption is greatly affected, there is a certain phenomenon of blood drug fluctuations, and individual differences are large

However, this type of osmotic pump is mostly suitable for the preparation of osmotic pump preparations for insoluble drugs. During the drug release process, the swelling of the polymer layer generates a driving force to push the drug suspension out of the release hole. Inquire about the product review of the original Servier company listed in Australia. Review document (Attachment: Product Information: Ivabradine (doc, 631KB), https: / / www.tga.gov.au / auspar / auspar-ivabradine), it can be seen that the solubility of ivabradine hydrochloride in water is 50mg / ml (ie 100g 5g of ivabradine hydrochloride can be dissolved in water), which is a soluble drug. It is prepared into a double-layer osmotic pump tablet. If water enters the tablet core, it may still cause the local drug concentration to be too high and cause sudden release of the drug.

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