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Tadalafil spray and preparation method thereof

A technology of tadalafil and spray, which is applied in the field of tadalafil spray and its preparation, can solve problems such as dysphagia, achieve the effects of improving quality of life, improving treatment effect, and relieving psychological pressure

Active Publication Date: 2020-05-08
HEFEI IND PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still some shortcomings in the way of taking the film, such as difficulty in swallowing, and a small amount of water is required to take it together.

Method used

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  • Tadalafil spray and preparation method thereof
  • Tadalafil spray and preparation method thereof
  • Tadalafil spray and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The stability of embodiment 1 solution system

[0042] The stability of the solution system is an important quality index of the spray, and the stability of the solution system directly affects the accuracy of the dosage. Put the spray on a stable horizontal platform, the temperature is 20-25°C, and the humidity does not exceed 70%. Observe the state of the solution in the spray every 2 hours. The thickness of the precipitate should not form obvious lamellar distribution and be easy to disperse after shaking. It is required that the preparation should remain stable within the validity period.

[0043] Experiments show that the stability of products 1-4 in the following examples of the present invention all meet the requirements.

Embodiment 2

[0044] Embodiment 2 The impact of the particle size of tadalafil bulk drug on the solubilization effect of tadalafil

[0045] The results are shown in Table 1. The measurement results show that the undifferentiated treatment of raw materials and the addition of solubilizers help to improve the solubility of tadalafil, which is conducive to the rapid release and absorption of active ingredients in the oral cavity and gastrointestinal tract, and has a positive effect on improving the quality of life of patients. Great significance.

[0046] Table 1 The particle size of tadalafil bulk drug and the influence of cosolvent on the solubilization effect of tadalafil

[0047]

[0048] Note: * indicates that compared with the particle size of 20μm, D 90 There is a significant difference in the solubility of tadalafil at 12 μm;

[0049] # indicates that the solubility of tadalafil has a significant difference when using water+SDS (0.3%) as the solvent compared with water as the sol...

Embodiment 3

[0050] The impact of embodiment 3 bulk drug particle diameter on product quality

[0051] The preparation method of present embodiment tadalafil spray is as follows:

[0052] (1) Grinding, sieving or jet milling methods are used to pulverize the tadalafil raw material drug, and D 90 The particle size is controlled at ≤20μm;

[0053] (2) Add the suspending agent into purified water under stirring, and fully stir evenly at 70°C until the suspending agent is completely dissolved;

[0054] (3) adding a wetting agent to the bulk drug powder obtained in step (1) and fully stirring to obtain a stable and uniform mixed liquid of the bulk drug;

[0055] (4) Add the suspension obtained in step (2) to step (3) and fully stir to obtain a stable and uniform suspension;

[0056] (5) Add a pH regulator to the homogeneous dispersion system obtained in step (4), fully stir and adjust the pH to between 4.0 and 8.0;

[0057] (6) Add preservatives, penetration-promoting agents and taste regul...

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Abstract

The invention belongs to the field of drug preparations, and specifically relates to a tadalafil spray and a preparation method thereof. The tadalafil spray is characterized in that the tadalafil spray includes an active component-tadalafil, a suspending agent, a wetting agent, a taste regulating agent and other pharmaceutically acceptable auxiliary materials; and the weight percentage of the tadalafil in the spray is 1-15%. The spray can start to be absorbed in the mouth and has no disintegration and releasing processes of tablets; the spray can be taken without drinking water, so that the spray is convenient; the spray can maintain stable within the term of validity; through the indication of in vivo absorption tests, compared with commercially available tadalafil tablets, the bioequivalence of t<max> and C<max> can be achieved; and the spray is good in taste and stability and stable in dispersion system, and has no obvious settlement phenomenon at the bottom of a sample.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a tadalafil spray and a preparation method thereof. Background technique [0002] Studies have shown that with the increasing pressure of life and the impact of pollution, half of men over the age of 40 suffer from erectile dysfunction, which seriously affects the quality of life and family stability. The current research on the pathogenesis of ED, especially at the level of signal transduction pathways, has achieved significant research results, proving that the nitric oxide-cyclic guanosine monophosphate (NO-cGMP) signaling pathway is the key pathway for the onset of ED. At present, the research results have been applied clinically, such as the marketing of phosphodiesterase type 5 (PDE-5) inhibitors such as sildenafil, vardenafil, and tadalafil, all of which have achieved remarkable clinical results. Effect. [0003] Tadalafil, its chemical structural formula is: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K47/36A61K47/10A61K31/4985A61P15/10
CPCA61K9/006A61K47/36A61K47/10A61K31/4985A61P15/10A61K9/12
Inventor 何广卫苏峰李庆
Owner HEFEI IND PHARMA INST
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