Polymorphic substance of yonkenafil hydrochloride and preparation method thereof
A polymorph, hydrochloric acid technology, applied in the field of medicine, can solve the problems such as the inability to compare accurate doses, the lack of research on compound crystal forms, etc., and achieve the effects of good physical and chemical stability and easy industrial production.
Active Publication Date: 2015-04-22
YANGTZE RIVER PHARM GRP CO LTD
View PDF3 Cites 7 Cited by
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
The patent only describes the preparation method of the compound in detail, but the research on the crystal form of the compound does not involve
[0004] The form of a pharmaceutical compound is important and it involves the study of the appropriate dosage form, because if the form of the compound cannot be kept constant during clinical and stability studies, then the exact dosage applied and determined from one batch to another cannot be determined. Compare
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0041] At room temperature, eucnafil hydrochloride type B polymorph (1.0 g, see comparative example for its preparation method) and 95 volume % ethanol aqueous solution (6 mL) were added into the flask, stirred for 2 h, and separated by filtration, the obtained solid Drying under reduced pressure gave ecanafil hydrochloride type A polymorph (0.8 g). Its X-RD diffraction pattern is as figure 1 As shown, DSC such as figure 2 shown.
Embodiment 2
[0043] At room temperature, eucnafil hydrochloride type B polymorph (1.0g) and 50% by volume methanol aqueous solution (3mL) were added to the flask, heated to 70°C to dissolve, cooled to -10°C, and filtered to obtain The solid was dried under reduced pressure to obtain polymorphic form A of eucnafil hydrochloride (0.8 g).
Embodiment 3
[0045] At room temperature, add eucnafil hydrochloride type A polymorph (0.5g), type B polymorph (0.5g) and water (2mL) into the flask, heat to 90°C to dissolve, cool to Filter at -5°C, and dry the obtained solid under reduced pressure to obtain polymorph A of eucnafil hydrochloride (0.7 g).
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More PUM
| Property | Measurement | Unit |
|---|---|---|
| density | aaaaa | aaaaa |
| melting point | aaaaa | aaaaa |
| unit cell | aaaaa | aaaaa |
Login to View More
Abstract
The invention discloses a polymorphic substance of yonkenafil hydrochloride. A powder diffraction pattern of a crystal comprises diffraction peaks at the following three or more 2 theta values selected from 8.4 + / - 0.2 degrees, 11.3 + / - 0.2 degrees, 13.9 + / - 0.2 degrees, 14.2 + / - 0.2 degrees, 14.7 + / - 0.2 degrees, 16.8 + / - 0.2 degrees, 17.1 + / - 0.2 degrees, 19.7 + / - 0.2 degrees, 21.0 + / - 0.2 degrees, 21.7 + / - 0.2 degrees, 22.4 + / - 0.2 degrees, 23.3 + / - 0.2 degrees, 23.8 + / - 0.2 degrees, 26.8 + / - 0.2 degrees, 27.5 + / - 0.2 degrees and 28.0 + / - 0.2 degrees. In addition, the invention also discloses a preparation method of the polymorphic substance. The polymorphic substance is easily subjected to industrial production, and is a pharmaceutically acceptable and stable novel crystal form of yonkenafil hydrochloride.
Description
technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to polymorphs of phosphodiesterase 5 inhibitor ecanafil hydrochloride and a preparation method thereof. Background technique [0002] Erectile dysfunction (Erectile dysfunction, ED) is the persistent inability to achieve and / or maintain a sufficient erection for a satisfactory sexual life. According to different etiologies, ED can be divided into three categories: psychogenic, organic and mixed. It is closely related to age but not an inevitable disease in the aging process. Primary risk factors for ED include: hypertension, hyperlipidemia, diabetes, coronary and peripheral vascular disease, pelvic organ or spinal cord injury or surgery. According to statistics, about 150 million men worldwide suffer from ED to varying degrees, and the number of such patients will double by 2025. There are many treatment options for ED, such as oral drugs phosphodiesterase 5 (PDE5) i...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More Application Information
Patent Timeline
Login to View More Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P15/10A61P15/00A61P15/06A61P13/08A61P13/10A61P9/10A61P9/12A61P9/04A61P11/06A61P37/08A61P11/00A61P11/02A61P27/06A61P1/00A61P1/04A61P25/08A61P25/00A61P3/10A61P25/02A61P25/28A61P17/06A61P17/00A61P35/04A61P17/14
CPCC07D487/04C07B2200/13A61K31/519A61P1/00A61P1/04A61P11/00A61P11/02A61P11/06A61P13/00A61P13/08A61P13/10A61P15/00A61P15/06A61P15/10A61P17/00A61P17/06A61P17/14A61P25/00A61P25/02A61P25/08A61P25/28A61P27/06A61P35/04A61P37/08A61P43/00A61P9/00A61P9/04A61P9/10A61P9/12A61P3/10
Inventor 张海波陈令武路显锋梁慧兴王永峰施连勇骆宏鹏
Owner YANGTZE RIVER PHARM GRP CO LTD