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Oral medicinal preparation of tadalafil

A pharmaceutical preparation, tadalafil technology, applied in the field of oral pharmaceutical preparations of tadalafil, can solve the problems of large ineffective dose, adverse response, loss, etc., to improve bioavailability, fresh and sweet mouth, and improve compliance sexual effect

Active Publication Date: 2013-07-10
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Tadalafil is a poorly soluble drug with relatively low bioavailability, so the ineffective dose taken is relatively large, which will produce a variety of adverse reactions, and unreasonable drug use can cause vision damage or loss

Method used

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  • Oral medicinal preparation of tadalafil
  • Oral medicinal preparation of tadalafil
  • Oral medicinal preparation of tadalafil

Examples

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Embodiment Construction

[0060] The following representative examples of the present invention are given to illustrate the content of the present invention, but are not intended to limit the present invention in any respect. The tadalafil in the examples refers to tadalafil or its salt, and the average weight-to-volume ratio (w / v) of the given amount is based on the amount of tadalafil.

[0061] 1. Tadalafil orally disintegrating tablets prepared according to patent 201210236261.4

[0062] Prescription: 1000 tablets

[0063] Tadalafil

[0064] sodium bicarbonate

[0065] Preparation:

[0066] (1) Dissolve tadalafil, adhesives, and fillers in acetone, called solutions a, b, and c, respectively, dissolve citric acid in solution b, and dissolve sodium bicarbonate in solution c.

[0067] (2) The solution a is firstly spray-dried to make the drug in a "boiling" state, and then sprayed into the solutions b and c in sequence, and dried to obtain a powdery or fine-grained solid.

[0068...

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PUM

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Abstract

The invention relates to an oral medicinal preparation of tadalafil and application of the preparation in treatment of male erectile dysfunction. The preparation is characterized in that the main medicne is tadalafil or salt thereof, and the particular formulation can be orally disintegrating tablets, chewable tablets, oral membranes and other preparations capable of being quickly released in the oral cavity; tadalafil is an insoluble medicament, and is low in bioavailability, so that the administrated infective dose is large, multiple adverse responses can be generated, and visual impairment or loss can be caused due to unreasonable administration. Regarding the researches of tadalafil medicinal preparation for improving medicament bioavailability and reducing occurrence of adverse responses, the wide clinical application of tadalafil in treatment of male erectile dysfunction is particularly important. Aiming at the fact that the tadalafil medicinal preparation brings great favor to broad ED patients in improvement of the compliance when the tadalafil medicinal preparation is taken by a patient, particularly in administration in an environment without water and in a non-swallow mode. The oral medicinal preparation is prepared through massive studies based on patients.

Description

technical field [0001] The invention relates to an oral pharmaceutical preparation of tadalafil and its application in treating male erectile dysfunction. Background technique [0002] Tadalafil, trade name Cialis, is a reversible, selective phosphodiesterase-5 inhibitor (PDE5), developed by Eli Lilly and Company for the treatment of male erectile dysfunction (ED), 2003 It was approved for marketing by FDA on November 23, and it is also the third new drug approved by FDA for ED. The specific mechanism of action of tadalafil is as follows: nitric oxide (NO) is the main mediator that causes relaxation and erection of cavernous smooth muscle. Tadalafil is a selective inhibitor of phosphodiesterase (PDE) V, which can enhance the physiological response of penile erection caused by NO release under sexual stimulation. NO is released from nerve endings and endothelial cells and binds to receptors on the smooth muscle of the cavernous body, activating intracellular soluble guanyla...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/70A61K31/4985A61K47/20A61P15/10
Inventor 晁阳包玉胜叶海
Owner NANJING CHIA TAI TIANQING PHARMA
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