Rhein-arginine eutectic compound, and preparation method, purification method and application thereof in preparation of medicines for treating diabetic complications
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A technology of masarginic acid and co-crystals, applied in the field of masarginic acid co-crystals, its preparation, purification and its application in the preparation of drugs for the treatment of diabetic complications, which can solve problems such as male sexual dysfunction
Active Publication Date: 2012-07-25
南京瑞因大健健康科技有限公司
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[0022] The above inventions have not yet involved the use of rhein or rhein compound compounds to treat diabetic complications, including the treatment of diabetic cardiomyopathy; diabetic macroangiopathy; male sexual dysfunction
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Embodiment 1
[0197] Example 1, take 2.0 g of rhein and 1.23 g of arginine, mix them, add 200 mL of water, heat to 90° C., keep warm for 1 hour, and filter while hot. Add ethanol to the filtrate so that the alcohol content is 80%. Under a water bath at 60°C, recover the solvent under reduced pressure until the volume is reduced by half, cool down to 4-10°C, let stand, crystallize, filter, and dry to obtain a large Type I crystallization of succinic acid.
Embodiment 2
[0198] Example 2, take 2.0 g of rhein and 1.23 g of arginine, mix them, add 200 mL of water, heat to 80° C., keep warm for 1.5 h, and filter while hot. Add ethanol to the filtrate to make the alcohol content 60%, recover the ethanol solvent under reduced pressure in a water bath at 50°C until the volume is reduced by half, cool down to 4-10°C, let stand, crystallize, filter, and dry to obtain the Type I crystallization of succinic acid.
Embodiment 3
[0199] Example 3, take 2.0 g of rhein and 1.23 g of arginine, mix them, add 250 mL of water, heat to 75° C., keep warm for 2 hours, and filter while hot. Add ethanol to the filtrate to make the alcohol content 40%, recover the solvent under reduced pressure in a water bath at 65°C until the volume is reduced by half, cool down to 20-30°C, keep it warm for 4 hours, then cool down to 4-10°C, Stand still, crystallize, filter, and dry to obtain type I crystals of macrospermic acid. Take an appropriate amount of rhein type I crystal product, add water, heat to dissolve, add dilute hydrochloric acid to adjust the pH to 2, collect the precipitate, wash the precipitate with water until neutral, and dry to obtain the purified rhein product.
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Abstract
The invention relates to a rhein-arginine eutectic compound, and a preparation method, a purification method and application thereof in preparation of medicines for treating diabetic complications. The rhein-arginine eutectic compound is an eutectic substance formed by rhein and L-arginine, the mol ratio of the active medicine component of the rhein to the L-arginine is 1:1, and the X-ray diffractogram of the eutectic powder has the characteristic peaks of 9.22 degrees, 10.34 degrees, 12.28 degrees, 26.05 degrees, 26.58 degrees and 27.57 degrees 2theta. The medicines for treating diabetic complications are medicines for treating diabetic cardiopathy, medicines for treating diabetic macroangiopathy, medicines for treating diabetic nephropathy, medicines for treating diabetic orchiopathy, medicines for treating complicated male sexual dysfunction of diabetes, or medicines for treating diabetic impotence. The invention can increase the solubility and dissolution of the medicines, enhance the purity and stability of the rhein-arginine eutectic compound, reduce the impurity content and hygroscopicity, enhance the bioavailability and improve the release characteristic.
Description
technical field [0001] The present invention relates to a compound of rhein arginine, which uses supramolecular chemical co-crystal technology to prepare co-crystal-arginine (Argirein), that is, the active pharmaceutical ingredient rhein (rhein) and co-crystal A co-crystal (a kind of complex) formed by crystal former L-arginine (L-arginine), the present invention also relates to the preparation method of this large spermatic acid co-crystal compound, this large-arginic acid co-crystal compound A purification method with rhein, and the application of the macrospergic acid co-crystal in the preparation of drugs for treating diabetic complications. Background technique [0002] Diabetes and its complications are common and frequently-occurring diseases. The incidence of diabetes remains high, showing a trend of high incidence. The incidence rate in China is higher. Diabetes is mainly type II, which affects the middle-aged and elderly people. It is highly pathogenic and has b...
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