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Tadalafil drug compound for treating male erectile dysfunction

A technology for erectile dysfunction and tadalafil, which is applied in the field of medicine and can solve problems such as visual impairment, loss, and large ineffective doses

Inactive Publication Date: 2015-11-18
QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] 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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  • Tadalafil drug compound for treating male erectile dysfunction
  • Tadalafil drug compound for treating male erectile dysfunction
  • Tadalafil drug compound for treating male erectile dysfunction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Preparation of tadalafil compound

[0034] (1) Grind the crude tadalafil, pass through an 80-mesh sieve, and then add it to a mixed solution of dimethyl sulfoxide and ethanol whose volume is 8 times the weight of tadalafil, the volume of dimethyl sulfoxide and ethanol The ratio is 4.5:1, 100 rpm stirring for 15 minutes;

[0035] (2) Add dimethyl sulfoxide whose volume is 8 times the weight of tadalafil under stirring at 80 rpm, and raise the temperature to 30°C at the same time;

[0036] (3) After adding the solution, let it stand for 2 hours, and add deionized water at 0°C dropwise under the condition of stirring at 150 rpm. The volume of deionized water is 7 times the weight of tadalafil, and add dropwise at a uniform speed within 1 hour complete;

[0037] (4) After the dropwise addition was completed, the temperature was lowered to -10°C, and stirring was continued for 1 h at a stirring rate of 20 rpm, and crystals were precipitated after standing for ...

Embodiment 2

[0039] Example 2: Preparation of tadalafil compound

[0040] (1) Grind the crude tadalafil, pass through a 90-mesh sieve, and then add it to a mixed solution of dimethyl sulfoxide and ethanol whose volume is 9 times the weight of tadalafil, the volume of dimethyl sulfoxide and ethanol The ratio is 4.5:1, 110 rpm stirring for 20 minutes;

[0041] (2) Add dimethyl sulfoxide whose volume is 10 times the weight of tadalafil under stirring at 85 rpm, and raise the temperature to 32.5°C at the same time;

[0042] (3) After adding the solution, let it stand still for 2.5 hours, and add deionized water at 2.5°C dropwise under the condition of stirring at 160 rpm. The volume of deionized water is 8 times the weight of tadalafil, and add dropwise at a constant speed within 1 hour complete;

[0043] (4) After the dropwise addition, the temperature was lowered to -2.5°C, and the stirring was continued for 1.5 h at a stirring rate of 25 rpm, and the crystals were precipitated after sta...

Embodiment 3

[0045] Example 3: Preparation of tadalafil compound

[0046] (1) Grind the crude tadalafil, pass through a 100-mesh sieve, and then add it to a mixed solution of dimethyl sulfoxide and ethanol whose volume is 10 times the weight of tadalafil, the volume of dimethyl sulfoxide and ethanol The ratio is 4.5:1, stirring at 120 rpm for 25 minutes;

[0047] (2) Add dimethyl sulfoxide whose volume is 12 times the weight of tadalafil under stirring at 90 rpm, and raise the temperature to 35°C at the same time;

[0048] (3) After adding the solution, let it stand for 3 hours, and add deionized water at 5°C dropwise under the condition of stirring at 170 rpm. The volume of deionized water is 9 times the weight of tadalafil, and add dropwise at a constant speed within 1 hour complete;

[0049] (4) After the dropwise addition was completed, the temperature was lowered to 5°C, and stirring was continued at a stirring rate of 30 rpm for 2 hours, and crystals were precipitated after stand...

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PUM

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Abstract

The invention belongs to the technical field of medicine, particularly relates to a tadalafil drug compound for treating male erectile dysfunction. The X-ray powder diffraction diagram of the tadalafil drug compound obtained through measurement by using Cu-K-alpha rays is shown in Figure 1. The tadalafil drug compound provided by the invention has significantly improved water solubility, low impurity content and good stability.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a drug tadalafil compound for treating male erectile dysfunction. Background technique [0002] Tadalafil is currently marketed as Cialis. Cialis was developed by Eli Lilly for the treatment of impotence. In this regard, tadalafil is reported to act by inhibiting cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Inhibition of PDE5 reduces impotence presumably by increasing the amount of cGMP leading to smooth muscle relaxation and increased blood flow. [0003] Polymorphism, ie, the appearance of different crystal forms, is characteristic of some molecules and molecular complexes. A single molecule, such as tadalafil, may give rise to many crystalline forms with distinct crystal structures and physical properties such as melting points, X-ray diffraction patterns, infrared absorption fingerprints, and solid-state NMR spectra. One crystalline form ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14A61K31/4985A61P15/10
CPCC07D471/14C07B2200/13
Inventor 邢继华
Owner QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD