Unlock instant, AI-driven research and patent intelligence for your innovation.

Tadalafil freeze-dried flash release tablet and preparation process thereof

A tadalafil, freeze-dried and flash-release technology, applied in the field of medicine, can solve the problems of insufficient improvement of drug utilization, widely varying effects, adverse reactions, etc., and achieve the effect of improving bioavailability, reducing waiting time, and good molding

Active Publication Date: 2022-06-24
湖北菲瑞生物药业有限公司
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem is that the orally disintegrating film preparation of tadalafil prepared by the invention does not appear oral absorption, resulting in the drug not taking effect quickly enough, and the first-pass effect of the liver cannot be avoided, the unit drug utilization rate is low, and adverse reactions may occur
[0006] Patent CN112972405A discloses a tadalafil freeze-dried orally disintegrating tablet and its preparation method. The tadalafil freeze-dried orally disintegrating tablet prepared by the invention includes tadalafil and pullulan. It shows that although different types of thickeners can be used to prepare freeze-dried orally disintegrating tablets, the effects in actual use vary widely. Only when pullulan is used as the thickener can the prepared product be achieved. The appearance is well formed, the effect is quicker when taken, and it has good compliance, which improves the bioavailability
The problem with this invention is that pullulan has strong hydrophilicity and has no significant synergistic effect on the direct absorption of tadalafil in the mucosa, resulting in a low absorption through the mucosa and insufficient improvement in the utilization rate of the unit drug. make further improvements

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Tadalafil freeze-dried flash release tablet and preparation process thereof
  • Tadalafil freeze-dried flash release tablet and preparation process thereof
  • Tadalafil freeze-dried flash release tablet and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] A preparation method of tadalafil freeze-dried flash-release tablet, comprising the following steps:

[0050] S1 Measure 300mL of water and place it in a beaker, heat it in a water bath at 50°C, weigh 16.5g of pullulan into the beaker, stir to dissolve it completely, and cool to 25°C to obtain an aqueous solution of pullulan;

[0051] S2 Weigh 0.9g of sucralose, 17.5g of mannitol, and 10g of tadalafil into the pullulan aqueous solution, stir to dissolve completely, add water and dilute to 500mL to obtain a feed solution;

[0052] S3 emulsifying the feed liquid in an emulsifier at a rotational speed of 10,000 rpm for 10 min; after emulsification, the feed liquid is degassed in vacuum for 10 min to obtain the degassed feed liquid;

[0053] S4 divide the degassed feed liquid into the blisters of the blister sheet by 0.5mL / piece to obtain the blister sheet after filling the feed liquid;

[0054] S5 put the blister plate after filling the material liquid into the -100 ℃ liq...

Embodiment 2

[0058] A preparation method of tadalafil freeze-dried flash-release tablets, the steps are the same as those in Example 1, except that the production formula is different.

[0059] raw material Usage amount (g) Tadalafil 10.0 Mannitol 15.0 Pullulan 17.5 Sucralose 0.9

Embodiment 3

[0061] A preparation method of tadalafil freeze-dried flash-release tablets, the steps are the same as those in Example 1, except that the production formula is different.

[0062]

[0063]

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
radiusaaaaaaaaaa
Login to View More

Abstract

The invention discloses a tadalafil freeze-dried flash release tablet and a preparation process thereof. The tadalafil freeze-dried flash release tablet comprises the following components: 1-10 parts of tadalafil, 1-20 parts of a propping agent, 1-20 parts of an adhesive and 0.1-5 parts of a sweetening agent. Wherein when the proppant is mannitol and the adhesive is pullulan, the freeze-drying flash release tablet is good in forming and short in disintegration time, and the optimal addition amount of mannitol and pullulan is determined through experiments. The tadalafil freeze-dried flash-release tablet prepared by the invention is good in forming and rapid in disintegration, can improve the bioavailability of the medicine, is convenient for a patient to take medicine, takes effect rapidly, and reduces the waiting time after the medicine is taken.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a freeze-dried flash-release tablet of tadalafil and a preparation process. Background technique [0002] Tadalafil, chemical name is (6R-12aR)-6-(1,3-benzodioxolan-5-yl)-2-methyl-2,3,6,7,12 ,12a-Hexahydropyrazino[1',2'-1,6]-pyrido[3,4-b]indole-1,4-dione, is a cyclic guanosine monophosphate (cGMP) specific Sex phosphodiesterase 5 (PDE5) inhibitor, by increasing the level of cGMP in the corpus cavernosum to relax smooth muscle, resulting in increased penile blood flow and play a role in the treatment of male erectile dysfunction (ED), and other drugs for the treatment of ED In contrast, tadalafil has the advantages of high selectivity, long half-life and good tolerance. In 2003, it was approved by the FDA to be listed in the United States as a drug for the treatment of ED. Tadalafil has a rapid onset of action and a long duration of action, and is the only drug among the four anti-ED dr...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/26A61K47/36A61K31/4985A61P15/10
CPCA61K9/2095A61K9/2018A61K9/205A61K9/006A61K31/4985A61P15/10
Inventor 蔡孟杰
Owner 湖北菲瑞生物药业有限公司