Pro-drug containing lignum vitae sodium gualenate and preparation method of pro-drug

Abstract

The invention discloses a pro-drug containing lignum vitae sodium gualenate. The pro-drug containing lignum vitae sodium gualenate comprises 5%-10% of sodium gualenate, 10%-15% of glutamic acid, 30%-45% of polyethylene glycol compound, 10%-25% of sodium sulfamate, and the balance of distilled water by mass percent. A preparation method prepares the product by taking the various materials by mass percent, adding the distilled water, sodium gualenate, glutamic acid, polyethylene glycol and sulfamate compound sequentially into a vessel, and stirring for 1 hour at the room temperature. Firstly, the sodium gualenate containing compound pro-drug does not contain iodine in the formula, promotes the metabolism of the oral mucosa, reduces the bioactivity of the salivary protease, and belongs to a medicine product. Secondly, the source of the crude drug of the pro-drug containing polyethylene glycol is wide, the preparation process is simple, multiple hydroxyls in the formula is beneficial for the release of the drug, the vesical is formed, the degree of coverage of the drug on the surface of the oral cavity is increased, and multiple layers of protection films are formed on the surface of the oral cavity.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, in particular to a prodrug containing sodium guaiazulene sulfonate and a preparation method thereof. Background technique [0002] 1,4-Dimethyl-7-isopropylazulene (Guaiazulene, Guaiazulene) is an active ingredient of chamomile, which has various biological activities such as anti-allergic, anti-inflammatory, anti-ulcer, and anti-pepsin (E.H. Ghazvini Zadeh, S. Tang, A.W. Woodward, T. Liu, M.V. Bondar and K.D. Belfield, J. Mater. Chem. C, 2015, 3, 8495-8503.; A. Székely, Péter, K. Aradi, G.L. Tolnai and Z. Novák, Org. Lett., 2017, 19, 954-957.). Moreover, 3,8-dimethyl-5-isopropylazulene-1-sodium sulfonate (sodium azulene sulfonate or water-soluble azulene) is not only clinically used to treat digestive system diseases, but also Marzulene-S ), the main component can also be used alone. It has biological activities such as anti-inflammation, anti-allergy, anti-ulcer, promotion of mucos...

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a composite material containing sodium azulene sulfonate used in the pharmaceutical industry and other fields in view of the existing synthetic schemes, the poor lipophilicity and insufficient stability of the guaiazulene compound. and its preparation method, the preparation method is simple, used to alleviate periodontitis, improve the anti-inflammatory and sustained release of sodium azulene sulfonate in the oral cavity, and overcome the secondary damage to the oral cavity caused by polyethylene glycol

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