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Carvedilol supersaturatable self-microemulsion dispersible tablets and preparing method thereof

A technology of carvedilol and self-microemulsion, applied in the field of medicine

Inactive Publication Date: 2017-05-31
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] In view of this, the present invention designs a kind of novel self-emulsifying preparation means, combines supersaturated self-microemulsifying preparation and dispersible tablet, solves the security problem and stability problem that traditional self-emulsifying preparation exists to a certain extent, simultaneously Improve the solubility of poorly soluble drugs, promote drug absorption and increase oral bioavailability

Method used

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  • Carvedilol supersaturatable self-microemulsion dispersible tablets and preparing method thereof
  • Carvedilol supersaturatable self-microemulsion dispersible tablets and preparing method thereof
  • Carvedilol supersaturatable self-microemulsion dispersible tablets and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1 A kind of carvedilol supersaturated self-microemulsion dispersible tablet, each raw material proportioning of this preparation is as follows:

[0035]

[0036] A total of 1000 carvedilol dispersible tablets were made

[0037] Preparation process: Weigh the oil phase, surfactant and co-surfactant in the prescribed amount, mix them evenly to obtain a homogeneous solution, add the drug in the prescribed amount and the supersaturation accelerator poloxamer 407, and stir well to obtain carvetidine Low supersaturated self-microemulsion preparation. Add the excipient microcrystalline cellulose KG802, after the adsorption and mixing are complete, add the filler microcrystalline cellulose 102 (which also acts as a binder) and the disintegrant crospovidone, mix well, and finally add the prescription amount The lubricating agent micropowder silica gel and magnesium stearate were passed through an 80-mesh sieve for 3 times, mixed evenly, and compressed into tablets...

Embodiment 2

[0038] Embodiment 2 A kind of carvedilol supersaturated self-microemulsion dispersible tablet, each raw material proportioning of this preparation is as follows:

[0039]

[0040] A total of 1000 carvedilol dispersible tablets were made

[0041] Preparation process: Weigh the oil phase, surfactant and co-surfactant in the prescribed amount, mix them evenly to obtain a homogeneous solution, add the drug in the prescribed amount and the supersaturation accelerator Soluplus, and stir fully to obtain carvedilol supersaturated self- Microemulsions. Add the excipient microcrystalline cellulose 101, after the absorption and mixing are complete, add the filler direct pressure mannitol, the binder low-substituted hydroxypropyl cellulose and the disintegrant crospovidone, mix well, and finally add Lubricant micropowder silica gel and magnesium stearate of the prescribed amount are passed through an 80-mesh sieve for 3 times, mixed evenly, and compressed into tablets, and the tablet ...

Embodiment 3

[0042] Embodiment 3 A kind of carvedilol supersaturated self-microemulsion dispersible tablet, each raw material proportioning of this preparation is as follows:

[0043]

[0044] A total of 1000 carvedilol dispersible tablets were made

[0045] Preparation process: Weigh the oil phase, surfactant and co-surfactant in the prescription amount, mix evenly to obtain a homogeneous solution, add the drug in the prescription amount, supersaturation accelerator Soluplus and Poloxamer 407, and stir well to obtain Carvet Dirol supersaturated self-microemulsion preparation. Add the solid adsorption material microcrystalline cellulose KG802. After the adsorption and mixing are complete, add the filler microcrystalline cellulose 102 (which also acts as a binder) and the disintegrating agent crospovidone, mix well, and finally add the prescription amount Lubricant talcum powder and magnesium stearate were passed through an 80-mesh sieve for 3 times, mixed evenly, and compressed into ta...

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Abstract

The invention relates to the technical field of pharmaceutic preparations, in particular to carvedilol supersaturatable self-microemulsion dispersible tablets and a preparing method thereof. A carvedilol supersaturatable self-microemulsion preparation is prepared by combining an oil phase, a surfactant, a cosurfactant and a supersaturation promoter according to a certain ratio and mixed with other auxiliary materials after being adsorbed by an excipient, and then tabletting is conducted on powder directly to obtain the carvedilol supersaturatable self-microemulsion dispersible tablets. The prepared carvedilol supersaturatable self-microemulsion dispersible tablets can form microemulsion with particle size within 200 nm through spontaneous emulsification in the body after being orally taken. By the adoption of the supersaturatable self-microemulsion dispersible tablets, the dissolution rate of carvedilol in the gastrointestinal tract can be increased, bioavailability can be improved, usage of the surfactant and the cosurfactant in the prescription can be reduced, irritation to the gastrointestinal tract can be reduced, drug use safety can be improved, and market prospects are broad.

Description

technical field [0001] The invention relates to a carvedilol supersaturated self-microemulsion dispersible tablet and a preparation method and application thereof, belonging to the technical field of medicine. Background technique [0002] Carvedilol (Carvedilol, CAR), the chemical structure is (±)-1-(9H-carbazole-4-amino)-3-[2-(2-methoxyphenoxyethyl)-amino] -2-propanol, molecular formula C 24 h 26 N 2 o 4 , with a molecular weight of 406.5 and the following chemical structure. Carvedilol is white or off-white crystalline powder, odorless, easily soluble in glacial acetic acid, soluble in chloroform, slightly soluble in methanol or ethyl acetate, insoluble in water. [0003] [0004] Carvedilol is a third-generation β-receptor blocker that also blocks α 1 Drugs with adrenergic receptor effects. Originally obtained by SmithKline Beecham from Boehringer Mannhein in the United States, it was used clinically in 1985 and was first listed in the United States in 1991 und...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/107A61K31/403A61P9/12A61P9/10A61P9/04
CPCA61K9/2054A61K9/1075A61K31/403A61K47/10A61K47/34
Inventor 刘建平郑春丽柴夫娟
Owner CHINA PHARM UNIV
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