Flunarizine hydrochloride matrix sustained-release tablets and preparing method thereof

Abstract

Flunarizine hydrochloride matrix sustained-release tablets are prepared from, by weight, 25-55 parts of flunarizine hydrochloride, 35-55 parts of a matrix material, 5-10 parts of diluent, 3-5 parts of a binding agent and 2-5 parts of a lubricating agent. A preparing method of the flunarizine hydrochloride matrix sustained-release tablets comprises the following steps that flunarizine hydrochloride, the matrix material, the diluent the lubricating agent and the binding agent are mixed evenly and them directly pressed into the tablets in a powder mode or flunarizine hydrochloride, the matrix material, the diluent and the binding agent are mixed to be prepared into granules, the granules are then mixed with the lubricating agent evenly, and the tablets are obtained through tabletting. The flunarizine hydrochloride matrix sustained-release tablets overcome the defect that in the prior art, multiple times of administration needs to be conducted due to the short relative half-life period of flunarizine hydrochloride, and it can be avoided that to maintain the blood concentration with the effective amount to reach a treatment effect, initial over-doses in the initial administration period occur, and consequently many side effects are caused; the problem that due to insufficient doses, the pain of a patient cannot be relieved, and the treatment effect cannot be achieved is also solved.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and in particular relates to flunarizine hydrochloride skeleton sustained-release tablets and a preparation method thereof. Background technique [0002] Flunarizine hydrochloride (FNZ), as a diphenylpiperazine derivative, is a selective Ca 2+ Antagonist, white or off-white crystal or crystalline powder; odorless, tasteless. Slightly soluble in methanol or ethanol, slightly soluble in chloroform, very slightly soluble in water, almost insoluble in benzene. Its chemical name is: (E)-1-[bis(4-fluorophenyl)methyl]-4-(2-propenyl-3-phenyl)-piperazine dihydrochloride. Flunarizine hydrochloride selectively inhibits Ca 2+ Enter cerebral artery vascular smooth muscle cells, increase blood flow, improve brain oxygen supply, prevent cell damage caused by intracellular pathological calcium overload caused by ischemia and other reasons, and can treat cerebral arterial ischemic d...

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Problems solved by technology

[0004] Moreover, the existing dosage form of flunarizine hydrochloride has a short half-life, and the effective blood concentration in the body after oral administration maintains a very short time. The patient takes a large dose each time, and the drug dissolves and contacts with the gastrointestinal mucosa at a high concentration, which is easy to produce irritation. , produce adverse reactions such as stomach discomfort, nausea and vomiting, so the compliance is poor; in addition, the time interval between taking the medicine in the evening and the morning is long, and the blood drug concentration is very low in the morning, and there is a "peak-valley" phenomenon, and the drug effect cannot be stable. play, the side effects are also large

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