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Pharmic tadalafil composition granules for treating urological diseases

A technology of tadalafil and urology, applied in the field of medicine, can solve the problems of low bioavailability, large ineffective dose, unfavorable discharge response, etc., and achieve the effects of high bioavailability, improved water solubility, and good stability

Inactive Publication Date: 2015-12-02
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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  • Pharmic tadalafil composition granules for treating urological diseases
  • Pharmic tadalafil composition granules for treating urological diseases
  • Pharmic tadalafil composition granules for treating urological diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation of tadalamorph crystals

[0030] Get the tadalafil raw material drug, add 30 ℃ of volumes in the mixed solvent A of the dimethyl sulfoxide that is 7 times of tadalafil weight, carbon tetrachloride, the volume ratio of dimethyl sulfoxide, carbon tetrachloride is 3 : 1, obtain solution; Apply the constant magnetic field that magnetic field strength is 0.9T then on the horizontal direction of the liquid level of gained solution, and drop volume in solution under the condition of this constant magnetic field be tadalafil weight 6 times two Mixed solvent B of methyl chloride and isopropyl ether, the volume ratio of dichloromethane and isopropyl ether is 4:1; after the dropwise addition, cool down to -5°C, let stand for 3 hours, filter, wash, and dry in vacuum to obtain The tadalamorph crystal.

[0031] The X-ray powder diffraction pattern obtained by measuring the obtained tadalamorph crystal using Cu-Kα rays is as follows: figure 1 shown.

Embodiment 2

[0032] Example 2: Preparation of Tadalafil Granules

[0033] Prescription: in parts by weight as shown in Table 1

[0034] Table 1 Tadalafil composition prescription

[0035]

[0036] Preparation:

[0037] 1) Processing of raw and auxiliary materials: pass tadalafil through a 40-mesh sieve with a vibrating sieve;

[0038] 2) Weighing: Weigh each raw and auxiliary material according to the prescription amount;

[0039] 3) Granulation: Add the prescribed amount of tadalafil, sucrose, glucose, glycine, and polyethylene glycol into the high-speed mixing granulator, turn on the stirring motor for low-speed mixing for 15 minutes, add the prescribed amount of purified water, and wet at a low speed Mix 220-250 seconds to make soft materials, choose 18-mesh nylon mesh and install it in a swinging granulator to granulate;

[0040] 4) Drying and sieving: Control the inlet air temperature of the boiling dryer at 55°C-60°C, place the wet granules in the boiling dryer, check the up...

Embodiment 3

[0043] Example 3: Preparation of tadalafil granules:

[0044] Prescription: in parts by weight as shown in Table 2

[0045] Table 2 Tadalafil composition prescription

[0046]

[0047] Preparation:

[0048] 1) Processing of raw and auxiliary materials: pass tadalafil through a 40-mesh sieve with a vibrating sieve;

[0049]2) Weighing: Weigh each raw and auxiliary material according to the prescription amount;

[0050] 3) Granulation: Add the prescribed amount of tadalafil, sucrose, glucose, glycine, and polyethylene glycol into the high-speed mixing granulator, turn on the stirring motor for low-speed mixing for 15 minutes, add the prescribed amount of purified water, and wet at a low speed Mix 220-250 seconds to make soft materials, choose 18-mesh nylon mesh and install it in a swinging granulator to granulate;

[0051] 4) Drying and sieving: Control the inlet air temperature of the boiling dryer at 55°C-60°C, place the wet granules in the boiling dryer, check the up...

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Abstract

The invention discloses pharmic tadalafil composition granules for treating urological diseases, and belongs to the technical field of medicament. A composition is prepared from tadalafil, saccharose, glucose, glycine, polyethylene glycol and purified water. The tadalafil is a novel crystal-type compound, an X-ray powder diffraction pattern measured through a Cu-K alpha-ray is shown in graph 1, and the tadalafil is different from that reported in the prior art; according to experiments, it is found that the compound with the novel crystal-type structure has significantly improved water solubility and is low in impurity content and good in stability; the granules prepared from the novel crystal-type tadalafil compound is good in stability, low in impurity content and high in bioavailability, and the safety of clinical applications is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a tadalafil composition granule 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, 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 may ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4985A61P15/10C07D471/14
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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