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Glycine anhydride eutectic serving as medicinal premixing adjuvant, preparation method and application

A technology of glycine anhydride and premixed excipients is applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. The effect of water absorption

Active Publication Date: 2016-11-09
GUANGZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Moreover, although there are many types of tablet excipients on the market, most of them need to be compatible with each other to meet the requirements. Enterprises often have to try different excipient formulas for each drug in industrial production, and the cost of excipients is too high

Method used

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  • Glycine anhydride eutectic serving as medicinal premixing adjuvant, preparation method and application
  • Glycine anhydride eutectic serving as medicinal premixing adjuvant, preparation method and application
  • Glycine anhydride eutectic serving as medicinal premixing adjuvant, preparation method and application

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preparation example Construction

[0025] The preparation method of described glycine anhydride, comprises the steps:

[0026] (1) Glycine anhydride and 3,5-dihydroxybenzoic acid are weighed in proportion, and ground after the two are mixed;

[0027] (2) Ball milling the powder after step (1) grinding.

[0028] Specifically, the molar ratio of glycine anhydride to 3,5-dihydroxybenzoic acid is preferably 1:2. The ball milling condition in step (2) is preferably 20 Hz, time 20 min, but not limited thereto.

Embodiment 1

[0030] Use glycine anhydride and 3,5-dihydroxybenzoic acid to synthesize glycine anhydride co-crystal, comprising the following steps:

[0031] (1) Weigh glycine anhydride and 3,5-dihydroxybenzoic acid in a molar ratio of 1:2, mix them and grind them.

[0032] Specifically, 50 g of glycine anhydride and 135 g of 3,5-dihydroxybenzoic acid were weighed, mixed and ground in a mortar to obtain high-purity glycine anhydride eutectic. In this embodiment, the grinding time is 30 minutes, but it is not limited thereto.

[0033] (2) Ball milling the powder after step (1) grinding. The ball milling condition is preferably 20 Hz, and the time is 20 min, but not limited thereto.

[0034] see figure 1 , which is a schematic diagram of the basic structural unit of the glycine anhydride co-crystal prepared in this example. The basic structural unit of the glycine anhydride co-crystal includes one glycine anhydride molecule and two 3,5-dihydroxybenzoic acid molecules. Among them, each gl...

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Abstract

The invention discloses glycine anhydride eutectic serving as medicinal premixing adjuvant. A basic structural unit of the glycine anhydride eutectic comprises a glycine anhydride molecule and two 3,5-dihydroxy benzoic acid molecules, wherein the glycine anhydride molecule and carboxylic acid on the two opposite 3,5-dihydroxy benzoic acid molecules form a stable R22(8) synthon, and the two adjacent opposite 3,5-dihydroxy benzoic acid molecules are connected through intermolecular hydrogen bonds to form a stable laminated structure; a space group of the glycine anhydride eutectic is a triclinic system. Compared with the prior art, glycine anhydride in the glycine anhydride eutectic and 3,5-dihydroxy benzoic acid have no biotoxicity, the formed eutectic has good preforming performance, can serve as an auxiliary filler and can also serve as a lubricating agent, formed hydrogen bonds absorb water and break easily and disintegrate easily, and eutectic is uniform in matching.

Description

technical field [0001] The invention belongs to the field of medicine and health food processing, in particular to the field of pharmaceutical excipients, and in particular relates to a glycine anhydride eutectic as a medicinal premixed auxiliary material, its preparation method and application. Background technique [0002] In recent years, the preparation of drug co-crystals using supramolecular chemistry and crystal engineering has become a research hotspot in the fields of chemistry and medicine. Drug co-crystals are favored due to their unique physical and chemical properties. Pharmaceutical co-crystals refer to co-crystal formers (CCFs) between active pharmaceutical ingredients (API) and other physiologically acceptable acids, bases or non-ionic compounds, through hydrogen bonds, van der Waals forces, π- Crystals formed by the combination of π-stacking, halogen bonds and other non-covalent forces, in which the pure states of API and CCFs are solid at room temperature. ...

Claims

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Application Information

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IPC IPC(8): C07D241/08C07C51/43C07C65/03A61K31/616A61K47/22A61K47/12A61K9/20
Inventor 王子舟郑舒硕吴春燕吴梓恩李志刚
Owner GUANGZHOU UNIVERSITY
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