A kind of flunarizine hydrochloride matrix sustained-release tablet and preparation method thereof

A technology of flunarizine hydrochloride and sustained-release tablets, which can be applied to pharmaceutical formulas, medical preparations containing active ingredients, extracellular fluid diseases, etc., and can solve the problem of short maintenance time of effective blood drug concentration and unstable drug effects , easy to produce irritation and other problems, to achieve the effect of maintaining blood concentration, improving bioavailability, and improving drug safety

Active Publication Date: 2019-06-28
ZHENGZHOU BARY ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

Method used

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  • A kind of flunarizine hydrochloride matrix sustained-release tablet and preparation method thereof
  • A kind of flunarizine hydrochloride matrix sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The flunarizine hydrochloride matrix sustained-release tablet in this embodiment is a hydrophilic gel matrix sustained-release tablet, and the sustained-release tablet is made of the following components in parts by weight: 35 parts of flunarizine hydrochloride, matrix material (hydroxyl Propyl methyl cellulose) 45 parts, diluent (lactose) 10 parts, binder (95% ethanol) 5 parts, lubricant 5 parts (magnesium stearate 2 parts, talc powder 3 parts).

[0025] Its preparation method is: pulverize flunarizine hydrochloride and pass through a 120-mesh sieve, mix evenly with hydroxypropyl methylcellulose and lactose, add ethanol solution with a volume fraction of 95% to moisten, and then granulate, 45-55 ℃ drying, passing through a 24-mesh sieve for granulation, then adding magnesium stearate and talc powder, mixing evenly, and directly pressing into tablets to obtain flunarizine hydrochloride matrix sustained-release tablets.

Embodiment 2

[0027] The flunarizine hydrochloride matrix sustained-release tablet in this embodiment is an inertable matrix sustained-release tablet, and the sustained-release tablet is made of the following components by weight: 35 parts of flunarizine hydrochloride, matrix material (ethyl Cellulose) 45 parts, diluent (lactose) 10 parts, binder (povidone) 5 parts, lubricant 5 parts (magnesium stearate 2 parts, talc powder 3 parts).

[0028] Its preparation method is: pulverize flunarizine hydrochloride and pass through a 120-mesh sieve, mix evenly with lactose, ethyl cellulose, povidone, magnesium stearate and talcum powder, and directly compress the whole powder into tablets to obtain fluorine hydrochloride Cinnarizine Matrix Extended Release Tablets.

Embodiment 3

[0030] The flunarizine hydrochloride matrix sustained-release tablet in this example is a mixed matrix sustained-release tablet, which is made of the following components by weight: 40 parts of flunarizine hydrochloride, 45 parts of matrix material (hydroxyl Propyl methyl cellulose 35 parts, glyceryl monostearate 10 parts), diluent (lactose) 5 parts, binder (hypromellose) 5 parts, lubricant 5 parts (magnesium stearate 2 parts, talcum powder 3 parts).

[0031] The preparation method is as follows: pulverize flunarizine hydrochloride, pass through a 120-mesh sieve, mix with lactose, hydroxypropyl methylcellulose, glyceryl monostearate, hypromellose, magnesium stearate and talcum powder Evenly, the whole powder is directly compressed into tablets to obtain flunarizine hydrochloride matrix sustained-release tablets.

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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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/495A61P9/10A61P7/02A61P27/16A61P25/06A61P25/08
CPCA61K9/0002A61K9/2031A61K9/205A61K9/2054A61K31/495
Inventor 陈长青王福芳周衡邓俊陈慧娟王颖丁佳丽
Owner ZHENGZHOU BARY ANIMAL PHARMA
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