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Multi-cell ranolazine slow-release pellet tablet

A technology of sustained-release pellets and sustained-release pellets, which is applied in the fields of pill delivery, medical preparations of non-active ingredients, cardiovascular system diseases, etc., and can solve problems such as pellet rupture, adhesion, and impact on formability, and achieve High bioavailability, large distribution area, good clinical significance effect

Active Publication Date: 2015-06-10
FUREN PHARMA GROUP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are very few domestic related studies, and foreign reports are only on low-drug-loaded pellets, and there are few reports and patents on high-drug-loaded pellets. The main reason is that the formability of pellets is affected by drugs and Influence of the properties of excipients, it is necessary to investigate the relationship between the properties of different ingredients in the formulation and the formability of pellets
Tabletting is a challenge for sustained-release pellets. Direct use of conventional sustained-release membrane materials and tableting excipients will cause rupture and adhesion of pellets. At the same time, the pressure during tablet compression and the change of tablet filler will have different effects on drug release. degree of influence

Method used

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  • Multi-cell ranolazine slow-release pellet tablet
  • Multi-cell ranolazine slow-release pellet tablet
  • Multi-cell ranolazine slow-release pellet tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]Weigh 60g of ranolazine, 25g of microcrystalline cellulose, 7g of lactose, 7g of precrossified starch, 1g of sodium lauryl sulfate, pass through a 100-mesh sieve and mix evenly, and use a 10% aqueous solution of povidone K30 as a binder to prepare Soft material, extruded and spheronized to prepare ranolazine drug-containing pellets, wherein the extrusion screen has an aperture of 0.6 mm, an extrusion speed of 25 r / min, dried at 40°C in a fluidized bed for 1 hour, and sieved to 20-40 mesh for use.

[0041] Put the screened ranolazine pellets in a fluidized bed, prepare a coating solution, adjust the fan frequency to 25HZ, the air inlet temperature to 30°C, the material temperature to 25°C and the flow rate of the coating solution to 0.4rpm, and control the coating weight gain to 5%. Ranolazine sustained-release pellets were prepared.

[0042] Coating solution ratio:

[0043] Sustained release material Acrylic resin 15%

[0044] Plasticizer Diethyl phthalate 3%

[0045]...

Embodiment 2

[0049] Weigh 80g of ranolazine, 15g of microcrystalline cellulose, 2g of lactose, 2g of starch, 0.8g of sodium lauryl sulfate, pass through a 100-mesh sieve and mix evenly, use 5% hypromellose E50M aqueous solution as a binder to make soft material, extruded and spheronized to prepare ranolazine drug-containing pellets, wherein the extrusion screen has an aperture of 0.8 mm, an extrusion speed of 25 r / min, dried at 40° C. in a fluidized bed for 1 hour, and sieved to 20-40 meshes for use.

[0050] The screened ranolazine pellets are placed in a fluidized bed to prepare a coating solution. Adjust the fan frequency to 25HZ, the air inlet temperature to 30°C, the material temperature to 25°C, and the flow rate of the coating solution to 0.4rpm, and control the coating weight gain to 5%, to prepare ranolazine sustained-release pellets.

[0051] Coating solution ratio:

[0052] Sustained release material Hypromellose 40%

[0053] Plasticizer triethyl citrate 5%

[0054] Anti-stic...

Embodiment 3

[0059] Weigh 95g of ranolazine, 3g of microcrystalline cellulose, 1g of lactose, and 1g of sodium lauryl sulfate, pass through a 100-mesh sieve and mix evenly, use 5% hypromellose K100M aqueous solution as a binder to make a soft material, and extrude Prepare ranolazine drug-containing pellets by spheronizing, wherein the extrusion screen has an aperture of 0.6mm, an extrusion speed of 25r / min, and is dried in a fluidized bed at 40°C for 1 hour, and sieved to 20-40 mesh for use.

[0060] The screened ranolazine pellets are placed in a fluidized bed to prepare a coating solution. Adjust the fan frequency to 25HZ, the air inlet temperature to 30°C, the material temperature to 25°C, and the flow rate of the coating solution to 0.4rpm, and control the coating weight gain to 5%, to prepare ranolazine sustained-release pellets.

[0061] Coating solution ratio:

[0062] Sustained release material Polyethylene glycol 5%

[0063] Plasticizers Diethyl phthalate, Dimethyl phthalate 6% ...

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a multi-cell ranolazine slow-release pellet tablet, which is formed by tabletting a ranolazine slow-release pellet and filling auxiliary materials, wherein the ranolazine slow-release pellet is prepared from polymer film coating containing a pellet core and capable of being permeated by medicines in a non-water-soluble manner; the polymer film also contains a water-soluble polymer; the weight of the ranolazine slow-release pellet coating is increased by 1-20%; the filling auxiliary materials are one or more of a group including microcrystalline cellulose, lactose, starch, pre-crossed starch, crossed sodium carboxymethylcellulose, crossed polyvinylpyrrolidone, hydroxy propyl cellulose, povidone, magnesium stearate and colloidal silicon dioxide, wherein the weight of the filling auxiliary materials is 5-20% of the total weight of the tablet; the multi-cell ranolazine slow-release pellet tablet disclosed by the invention can be rapidly disintegrated into pellet cells in digestive juice; the pellet cells can achieve the 12-h slow-release effect in gastrointestinal tracts.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a ranolazine multi-unit sustained-release pellet tablet and a preparation method thereof. Background technique [0002] Ranolazine, a piperazine derivative, is a partial fatty acid oxidase (pFOX) inhibitor. It treats chronic angina by changing the metabolism of the heart and reducing the oxygen consumption of the heart. Under normal conditions, the heart uses fatty acid oxidation as its main energy source, and once this source is reduced by pFOX inhibitors, another energy source—glucose oxidation—is increased. Since the oxidation of glucose produces more energy per unit of oxygen than the oxidation of fatty acids, the heart can do more work under the condition of available oxygen without affecting blood pressure and heart rate. There are controlled-release tablets or capsules of its acceptable salts and esters, and ranolazine sustained-release tablets. Chinese patent...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/495A61K47/38A61K47/32A61K47/34A61P9/10
Inventor 赵永星陈永强路存真王新军韩萌萌李沙沙李嘉朱来峰赵艺丹刘丹崔浩方水霞程功华
Owner FUREN PHARMA GROUP
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