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Amorphous form of avanafil, preparation method of, application and medicine composition of amorphous form of avanafil

A kind of avanafil and amorphous technology, applied in the field of chemical pharmaceuticals, can solve the problems of reduced probability of interaction, short half-life, etc., and achieve the effect of mild conditions, stable drug properties and good reproducibility

Inactive Publication Date: 2015-05-20
PEKING UNIV FOUNDER GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The short half-life reduces the chance of the drug interacting with other drugs in the body

Method used

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  • Amorphous form of avanafil, preparation method of, application and medicine composition of amorphous form of avanafil
  • Amorphous form of avanafil, preparation method of, application and medicine composition of amorphous form of avanafil
  • Amorphous form of avanafil, preparation method of, application and medicine composition of amorphous form of avanafil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Amorphous

[0025] Add 0.5 g of crude avanafil and 10 ml of ethyl acetate into the reaction flask, stir at room temperature until the avanafil dissolves, keep for 30 minutes, and filter. The filtrate was concentrated to dryness under reduced pressure to obtain a white solid, which was then dried under reduced pressure at 60°C to constant weight to obtain the amorphous avanafil of the present invention, m.p.76.0-77.5°C. The measured content is 98.98%.

[0026] Use the Rigaku Dmax / 2400 type X-ray polycrystalline powder diffractometer (condition: Cu Kα, 40kV, 100mA) to measure and get figure 1 Powder X-ray Diffraction Spectrum shown.

experiment example 1

[0031] Comparing the amorphous drug prepared in Example 1 with the crystalline drug prepared in the comparative example, and administering it orally to rats, the amorphous drug only needs 80% of the dosage of the crystalline drug to achieve the same therapeutic effect.

experiment example 2

[0033] The subjects took a blood sample in the morning, and then took 500mg of avanafil amorphous form, crystalline form and 150ml of water respectively on an empty stomach, and took blood samples at 0.25, 0.5, 1, 1.5, 2, 3, 4 and 6 hours after taking the medicine. Serum was separated and stored at -20°C for future use. Microbial detection technology was used to measure drug concentration data in serum at different times. The experimental results show that the time for the blood concentration of avanafil amorphous form to reach the peak is 35 minutes, and the time for the blood concentration of avanafil amorphous form of the present invention to reach the peak value is 30 minutes. Compared with crystalline drugs, amorphous drugs have faster absorption and better bioavailability.

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Abstract

The invention relates to an amorphous form of avanafil, a preparation method, application and a medicine composition of the amorphous form of avanafil. The amorphous form of avanafil has no obvious characteristic peak in powder X-ray diffraction pattern based on Cu-K alpha radiation and shows a valuable characteristic in drug preparation; the amorphous form is high in purity and stable, and the in-vivo absorption of the amorphous form is superior to that of a crystal form.

Description

technical field [0001] The invention relates to the field of chemical pharmacy, in particular to the amorphous form of the chemical drug avanafil, its preparation method, use and pharmaceutical composition. Background technique [0002] Avanafil is 4-[(3-chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N having the formula -(2-pyrimidinylmethyl)-5-pyrimidinemethanesulfonamide: [0003] [0004] Avanafil (Avanafil) is a PDE5 receptor inhibitor, which can improve the function of penile erection by enhancing the vasodilation effect through the NO / cyclic guanosine monophosphate pathway. The drug has higher selectivity to PDE5 and higher safety, so the incidence of side effects such as visual disturbance, back pain, and muscle pain after taking avanafil is lower, and no effect of avanafil on What is the effect on retinal function. Another feature of the drug is its rapid onset and short half-life. Because ED patients often suffer from other systemic disea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/14A61K31/506A61P15/10A61P15/00A61P9/12A61P11/00A61P9/00
CPCC07D403/14A61K31/506A61K2300/00
Inventor 易崇勤马德君李学义孟宏涛郭欲晓郑少辉
Owner PEKING UNIV FOUNDER GRP CO LTD
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