Solid preparation containing single crystal form
A solid preparation, a single technology, applied in the field of solid preparations of 2--4-methyl-5-thiazole carboxylic acid, can solve the problems such as no records, hints, no proof that A crystal has advantages and the like
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
manufacture example
[0033] The specific production example of this tablet is as follows.
[0034] (1) Granulation process
[0035] The pharmaceutical crystals of the present invention, excipients, disintegrants, and binders are charged into a conventionally known granulator, sprayed with water, and granulated to obtain granules.
[0036] Alternatively, the crystals of the drug of the present invention, excipients, and disintegrants (removing the binder) are charged into a conventionally known granulator, and water is sprayed thereon to perform granulation to obtain granules.
[0037] The moisture content (measured by the dry weight loss method) of the obtained granulated material was about 17 to 26% by weight for the former and about 10 to 16% by weight for the latter. Namely, with the latter method, less water can be used for granulation, and the production time can be shortened. The so-called dry weight loss method refers to the method of heating the powder by infrared radiation to dry it, an...
Embodiment
[0060] As a reference example, the stability, dissolution rate, and solid content of each crystal form of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid were measured. 15 N-NMR, 13 C-NMR.
[0061] The original drug (A, B, C, D, E and G crystals) of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid can be obtained according to WO92 / 09279 specification and the method described in WO99 / 65885 specification to manufacture.
reference example 1
[0063] physical stability
[0064] Store in open and sealed glass bottles under the condition of 40°C / 75%RH, measure the decomposition products by HPLC, measure the crystallization transformation by powder X-ray diffraction and thermal mass measurement, and calculate the 50% transformation time. The results are shown in Table 1, none of the six crystal forms were decomposed. Crystal A, crystal C, and crystal G were still stable after 3 months, while crystal B, crystal D, and crystal E underwent crystal transformation.
[0065] Table 1
[0066]
[0067]
Analytical method
40℃ / 75%RH opening
40℃ / 75%RH sealing
Crystal A
XRD
(no change)
(no change)
B crystal
TG
14 hours
5 days
C crystal
XRD
(no change)
(no change)
D crystal
XRD
0.25 hours
17 days
E crystal
XRD
19 days
55 days
G crystal
XRD
(no change)
(no change)
[0068] Using 2690 m...
PUM
| Property | Measurement | Unit |
|---|---|---|
| particle size | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
Login to View More