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Medicinal tadalafil composition tablets for treating urological diseases

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

Inactive Publication Date: 2015-12-30
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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  • Medicinal tadalafil composition tablets for treating urological diseases
  • Medicinal tadalafil composition tablets for treating urological diseases
  • Medicinal tadalafil composition tablets for treating urological diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Preparation of tadalamorph crystals

[0034] Dissolve tadalafil in a mixed solvent of dimethyl sulfoxide and 3-picoline whose volume is 5 times the weight of tadalafil at 35°C, and the volume ratio of dimethyl sulfoxide to 3-picoline is 3 : 1; first add the mixed solvent A of water and tetrahydrofuran whose total volume is 9 times the weight of tadalafil at a speed of 25ml / min, the volume ratio of water and tetrahydrofuran is 4:1.5, stir while adding, and control the temperature 35 DEG C, crystal growth for 1 hour; then add the mixed solvent B of water and tetrahydrofuran whose total volume is 12 times the weight of tadalafil at a speed of 15ml / min, the volume ratio of water and tetrahydrofuran is 3:1, and the After crystallization for 2.5 hours, cool down to -5°C at a speed of 20°C / hour, then maintain a stirring speed of 260 rpm to stir and crystallize, and grow crystals for 2 hours; filter, dry at 45°C and reduce pressure to obtain the tadalamorphic compo...

Embodiment 2

[0036] Example 2: Preparation of tadalafil tablets:

[0037] Prescription: in parts by weight, 2 parts of tadala amorphous compound prepared in Example 1, 4.3 parts of sodium starch glycolate, 3.5 parts of starch, 21 parts of lactose, 4 parts of microcrystalline cellulose, lauryl sulfate 0.1 part of sodium, 16 parts of purified water, 0.2 part of magnesium stearate.

[0038] Preparation:

[0039] (1) Processing of raw and auxiliary materials: use a vibrating sieve to pass lactose through a 80-mesh sieve, and pass microcrystalline cellulose through a 40-mesh sieve;

[0040] (2) Weighing: Weigh each raw and auxiliary material according to the prescription quantity;

[0041] (3) Pre-mixing of raw and auxiliary materials: After manual pre-mixing of the ratio of tadalafil and 2 / 7 lactose in the prescribed amount, put them in a pulverizer and pulverize together with 100 meshes;

[0042] (4) Adhesive preparation: add the prescribed amount of sodium lauryl sulfate to purified wat...

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Abstract

The invention relates to medicinal tadalafil composition tablets for treating urological diseases, and belongs to the technical field of medicine. The tablets are prepared from an internally added original accessory, an adhesive and a lubricant, wherein the internally added original accessory consists of tadalafil, sodium starch glycolate, starch, lactose and microcrystalline cellulose; the adhesive is prepared from sodium dodecyl sulfate and purified water; the lubricant is magnesium stearate. The tadalafil is a compound of a novel crystal form, an X-ray powder diffraction pattern measured by Cu-K alpha rays is shown in picture 1, the tadalafil is different from that reported in the prior art, and a test shows that the compound of the novel crystal form has obviously improved water solubility, low impurity content and high stability; compared with the prior art, the tablets prepared from the tadalafil compound of the novel crystal form are high in dissolubility and stability and low in impurity content, and safety in clinical application is improved.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical technology and involves a drug in the treatment of urological diseases. Background technique [0002] He is currently sold as Cialis.CIALIS was developed by Elililly for the treatment of impotence.In terms of performance, it is reported that Dalafi works by inhibiting cyclolar genoscopic acid (CGMP)-specific phosphate 5 (PDE5).The suppression of PDE5 probably reduces the yang by increasing the amount of CGMP caused by the amount of smooth muscle relaxation and increased blood flow. [0003] The phenomenon of homogeneity, that is, different crystals, are the characteristics of some molecules and molecular matches.Single molecules, such as Dalafi, may produce many crystals. They have different crystal structures and physical properties, such as melting points, X -ray diffraction diagrams, infrared absorption fingerprints and solid NMR spectrum.A crystal may produce a heat activity method different from the ...

Claims

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Application Information

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