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Tadalafil solid dispersion system and preparation method thereof

A tadalafil, solid dispersion technology, applied in respiratory system diseases, urinary system diseases, cardiovascular system diseases, etc., can solve problems such as poor effect, achieve good reproducibility, simple process operation, and improve bioavailability The effect of degree and stability

Inactive Publication Date: 2017-11-10
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the effects of improving drug dissolution and bioavailability are not good.

Method used

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  • Tadalafil solid dispersion system and preparation method thereof
  • Tadalafil solid dispersion system and preparation method thereof
  • Tadalafil solid dispersion system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] This embodiment provides a tadalafil solid dispersion system (F1), which is mainly made of tadalafil and soluplus, wherein, by weight g, tadalafil is 1 g, and soluplus is 9 g.

[0045] This embodiment provides also a kind of method for preparing tadalafil solid dispersion system:

[0046] Acetone and water were mixed at a volume ratio of 9:1, and then the tadalafil raw material was added so that the content of the tadalafil raw material in the mixed solvent was 1% (W / V). The inlet temperature of spray drying is 85°C, the outlet temperature is 30°C, and the hot air volume is 35m 3 / h, peristaltic pump flow rate 2mL / min, atomizing gas flow rate 100L / h.

[0047] After fully mixing 1 g of tadalafil and 9 g of soluplus uniformly, the mixed mixture is added into a hot-melt extruder for heating, melting and extrusion. Specifically, the mixture was melted at a temperature of 180° C., stirred at a rotation speed of 50 rpm, and extruded at a speed of 1.2 g / min at a temperature ...

Embodiment 2

[0049] This embodiment provides a tadalafil solid dispersion system (F2), which is mainly made of tadalafil and soluplus, wherein, in terms of weight g, tadalafil is 2 g, and soluplus is 8 g.

[0050] This embodiment provides also a kind of method for preparing tadalafil solid dispersion system:

[0051] Acetone and water were mixed at a ratio of 8:1 by volume, and then a mixture of 2 g of tadalafil and 8 g of soluplus was added, and the content of the mixture in the mixed solvent was 1.5% (W / V). The inlet temperature of spray drying is 95°C, the outlet temperature is 30°C, and the hot air volume is 33.5m 3 / h, peristaltic pump flow rate 2.5mL / min, atomizing gas flow rate 400L / h.

[0052] The spray-dried mixture is added to a hot-melt extruder for heat-melting and extrusion. Specifically, after melting the mixture at a temperature of 160° C. and stirring at a rotation speed of 100 rpm, the mixture is extruded at a temperature of 130° C. at a speed of 0.5 g / min. The extruded...

Embodiment 3

[0054] This embodiment provides a tadalafil solid dispersion system (F3), which is mainly made of tadalafil and soluplus, wherein, in terms of weight g, tadalafil is 3 g, and soluplus is 7 g.

[0055] This embodiment provides also a kind of method for preparing tadalafil solid dispersion system:

[0056] Acetone and water were mixed at a volume ratio of 8.5:1, and then a mixture of 3 g of tadalafil and 7 g of soluplus was added, and the content of the mixture in the mixed solvent was 2% (W / V). The inlet temperature of spray drying is 80°C, the outlet temperature is 60°C, and the hot air volume is 15m 3 / h, peristaltic pump flow rate 3mL / min, atomizing gas flow rate 500L / h.

[0057] The spray-dried mixture is added into a hot-melt extruder to be heated, melted and extruded. Specifically, after melting the mixture at a temperature of 190° C. and stirring at a rotation speed of 70 rpm, the mixture is extruded at a temperature of 130° C. at a speed of 15 g / min. The extruded mix...

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Abstract

The invention relates to the field of solid dispersion system pharmacy, and in particular relates to a tadalafil solid dispersion system and a preparation method of the tadalafil solid dispersion system. The tadalafil solid dispersion system is mainly prepared from tadalafil and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer, specifically, 1-4 weight parts of tadalafil, and 6-9 weight parts of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer. For the tadalafil solid dispersion system, the stability of the preparation is good, the amorphous stability of the medicine is good, and the bioavailability of the medicine is also good.

Description

technical field [0001] The invention relates to the field of solid dispersion system pharmacy, in particular to a tadalafil solid dispersion system and a preparation method thereof. Background technique [0002] Combinatorial chemistry and high-throughput screening are used in the drug development process to screen out a large number of pharmacologically active compounds with poor water solubility. In new drug research and development, about 70% of candidate new drug compounds have poor water solubility, and about 40% of the raw materials of oral immediate release preparations are poorly soluble drugs. The water solubility of a drug is a key factor in its dissolution rate. Low dissolution rates due to low solubility often lead to low bioavailability of orally administered drugs, and compounds with water solubility below 100 μg / mL often suffer from solubility-limited absorption. At present, various methods to overcome the poor water solubility of drug candidates have been s...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4985A61K47/34A61P15/10A61P9/12A61P11/00A61P13/08
CPCA61K9/146A61K31/4985
Inventor 李庆国陆明关世侠黄德恩
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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