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Preparation method of nicergoline tablet

A nicergoline tablet and technology for nicergoline, applied in the field of medicine, can solve the problems of low absolute bioavailability, low bioavailability, low dissolution rate and the like, and achieve the effects of increasing shelf life, increasing affinity, and increasing dissolution rate

Inactive Publication Date: 2020-11-10
SHANDONG FANGMING PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of Nicergoline, most of the oral preparations of Nicergoline currently on the market have the problems of low dissolution rate, poor absorption and low bioavailability after taking it. After testing, Nicergoline is rapidly absorbed after oral administration. , the absolute bioavailability is less than 5%

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] A kind of preparation method of Nicergoline tablet, (1) Nicergoline, carboxymethyl starch sodium, hypromellose, starch, mannitol, water are mixed uniformly to make pill ointment, and pill ointment is molded (2) add Nicergoline, oil for injection, phosphatidylglycerol, pregelatinized starch, microcrystalline cellulose in ethanol and stir until Nicergoline is completely dissolved at a rotating speed of 500r / min, then Remove ethanol, and add corn fiber to obtain the main medicinal ointment, the surface of the pill is coated with the main medicinal ointment, dried, and pressed into tablets to obtain a pill coated with the second main medicinal layer; (3) gum arabic, lactose, pectin, medicine Mix gelatin, cornstarch and pigment evenly to prepare a coating paste, put the pills coated with the second main drug layer in a fluidized bed coating device for bottom spraying and coating, and dry to obtain the inner layer of the coating. (4) coating the main drug ointment on the surf...

Embodiment 2

[0023] A kind of preparation method of Nicergoline tablet, (1) Nicergoline, carboxymethyl starch sodium, hypromellose, starch, mannitol, water are mixed uniformly to make pill ointment, and pill ointment is molded (2) add Nicergoline, oil for injection, phosphatidylglycerol, pregelatinized starch, microcrystalline cellulose in ethanol and stir until Nicergoline is completely dissolved at a rotating speed of 500r / min, then Remove ethanol, and add corn fiber to obtain the main medicinal ointment, the surface of the pill is coated with the main medicinal ointment, dried, and pressed into tablets to obtain a pill coated with the second main medicinal layer; (3) gum arabic, lactose, pectin, medicine Mix gelatin, cornstarch and pigment evenly to prepare a coating paste, put the pills coated with the second main drug layer in a fluidized bed coating device for bottom spraying and coating, and dry to obtain the inner layer of the coating. (4) coating the main drug ointment on the surf...

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Abstract

The invention relates to the technical field of medicine, in particular to a preparation method of a nicergoline tablet. The nicergoline tablet is sequentially provided with a pill, a second main medicine layer, a coating inner layer, a first main medicine layer and a coating outer layer from inside to outside; and the thickness ratio of the second main medicine layer to the coating inner layer tothe first main medicine layer to the coating outer layer is (1-2):(4-5):(1-2):(1-2). a tablet inner layer is arranged, so that the medicine can be disintegrated hierarchically, the action time of themedicine is prolonged, and absorption is facilitated; and the nicergoline is uniformly dispersed in phospholipid, so that the affinity between the nicergoline and grease is increased, the dissolutionrate of the nicergoline is further increased, and the utilization rate is increased. By arranging a hollow tablet shell, the dissolution time of the tablet shell is shortened, the medicine is exposedas soon as possible to play a role, and a patient is treated with the medicine early; in addition, the tablet shell contains gelatin and corn starch, so that the tablet shell is softened and decomposed when meeting water and can be absorbed by the human body, and the dissolution time of the tablet shell is also shortened;.

Description

technical field [0001] The application belongs to the technical field of medicine, in particular to a preparation method of Nicergoline tablets. Background technique [0002] Nicergoline is a semi-synthetic ergot alkaloid derivative with alpha-receptor blocking and vasodilator effects. It can strengthen the metabolism of brain cell energy, increase the utilization of oxygen and glucose, promote the conversion of neurotransmitter dopamine to enhance nerve conduction, strengthen brain protein biosynthesis, and improve brain function. [0003] Nicergoline is prepared as a raw material to obtain pharmaceutical preparations, including tablets, capsules, water injections, and freeze-dried powder injections. Due to the poor water solubility of Nicergoline, most of the oral preparations of Nicergoline currently on the market have the problems of low dissolution rate, poor absorption and low bioavailability after taking it. After testing, Nicergoline is rapidly absorbed after oral a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/40A61K9/36A61K9/30A61K47/42A61K47/36A61K47/24A61K47/46A61K31/48A61P25/00
CPCA61K9/209A61K9/2873A61K9/286A61K9/282A61K9/288A61K9/2893A61K31/48A61P25/00
Inventor 刘长江赵亭吴双俊段义杰刘存领赵海桥王正雯尹彩霞
Owner SHANDONG FANGMING PHARMACEUTICAL CO LTD
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