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Pharmaceutical tadalafil composition tablet for treating urological diseases

A tadalafil and urology technology, applied in the field of medicine, can solve problems such as low bioavailability, large ineffective dose, and visual impairment, and achieve the effects of improving safety, improving water solubility, and high dissolution rate

Inactive Publication Date: 2016-01-13
QINGDAO HUAZHICAO PHARMA 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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  • Pharmaceutical tadalafil composition tablet for treating urological diseases
  • Pharmaceutical tadalafil composition tablet for treating urological diseases
  • Pharmaceutical tadalafil composition tablet for treating urological diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Preparation of tadalamorph crystals

[0032] (1) Take the tadalafil raw material and add it to dimethyl sulfoxide, the volume of dimethyl sulfoxide is 5 times the mass of tadalafil;

[0033] (2) Stir until completely dissolved, and adjust the pH to 6-9;

[0034] (3) Add activated carbon for decolorization and filter to obtain a clear solution;

[0035] (4) Move the clarified solution into a pressure vessel, add isobutanol dropwise at 5°C under the condition that the pressure in the pressure vessel is controlled at 1.3Mpa and stirred, the stirring speed is controlled at 40rmp, and the volume of isobutanol is two 3 times the volume of methyl sulfoxide;

[0036] (5) Release the pressure after the dropwise addition, cool the solution down to -10°C at a rate of 10°C / min, let it stand for 2 hours, filter, wash, and dry under reduced pressure to obtain tadalamorph crystals.

[0037] The X-ray powder diffraction pattern obtained by measuring the obtained tadalam...

Embodiment 2

[0038] Example 2: Preparation of tadalafil composition tablet

[0039] Prescription: 2 parts by weight of the tadala amorphous compound prepared in Example 1, 9 parts by weight of lactose, 10 parts by weight of pregelatinized starch, 3 parts by weight of polyvinyl butyral, 2 parts by weight of Carbopol, the magnesium stearate of 0.15 parts by weight.

[0040] Preparation:

[0041] (1) Processing of raw and auxiliary materials: sieve tadalafil to 80 mesh;

[0042] (2) Weighing: Weighing according to the prescription;

[0043] (3) Total mixing: Add tadalafil, lactose, pregelatinized starch, polyvinyl butyral, carboxyvinyl, and magnesium stearate to the three-dimensional motion mixer, set the premixing speed to 15 rpm, Mixing time 10 minutes;

[0044] (4) Tablet compression: calculate the theoretical loading range according to the content of the materials obtained from the total blending, and then perform tablet compression;

[0045] (5) Packaging.

Embodiment 3

[0046] Example 3: Preparation of tadalafil composition tablet

[0047] Prescription: 2 parts by weight of tadala amorphous compound prepared in Example 1, 10 parts by weight of lactose, 10.1 parts by weight of pregelatinized starch, 4 parts by weight of polyvinyl butyral, 2.5 parts by weight of Carbopol, the magnesium stearate of 0.2 weight part.

[0048] Preparation:

[0049] (1) Processing of raw and auxiliary materials: sieve tadalafil to 80 mesh;

[0050] (2) Weighing: Weighing according to the prescription;

[0051] (3) Total mixing: Add tadalafil, lactose, pregelatinized starch, polyvinyl butyral, carboxyvinyl, and magnesium stearate to the three-dimensional motion mixer, set the premixing speed to 15 rpm, Mixing time 10 minutes;

[0052] (4) Tablet compression: calculate the theoretical loading range according to the content of the materials obtained from the total blending, and then perform tablet compression;

[0053] (5) Packaging.

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Abstract

The invention discloses a pharmaceutical tadalafil composition tablet for treating urological diseases and belongs to the technical field of medicine. A composition is made from tadalafil, lactose, pregelatinized starch, polyvinyl butyral, carboxyvinyl polymer and magnesium stearate. The tadalafil is a novel-crystal form compound, an X-ray powder diffraction pattern obtained by measurement using Cu-Ka ray is shown in 1, the tadalafil is one different from the prior art, testing shows that the novel-crystal form compound has significantly improved water solubility, low impurity content and good stability, a tablet prepared with the tadalafil novel-crystal form compound has higher dissolution than the prior art, good stability and low impurity content and is safer to clinically apply.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a tadalafil composition tablet for treating urological diseases. 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 is a 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 may produce a different pattern of thermal acti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4985C07D471/14A61P13/00A61P15/10
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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