Pectin-adriamycin coniuncate lyophilized preparation, and preparation method thereof

Abstract

The invention belongs to the field of pharmacy, and specifically relates to a pectin-adriamycin coniuncate lyophilized preparation, and a preparation method thereof. In order to solve the dissolving difficulty of pectin-adriamycin coniuncate (PAC for short), to improve the biomass utilance, and to produce preparations conveniently, the inventor produces PAC into a nano-sized suspension. However, because the long-term stability of the nano-sized suspension is poor, the nano-sized suspension is then produced into a lyophilized preparation. The preparation method comprises the steps that: PAC which is hard to dissolve is prepared into a suspension or a nano-sized suspension; a lyophilizing proppant is added to the suspension or the nano-sized suspension; lyophilization is carried out upon the suspension, and a lyophilized preparation is obtained. When the nano-sized suspension is prepared into the lyophilized preparation, stability of nano-particle size is improved, and stability of drugloading capacity is improved. The invention assists in providing a novel scheme for the clinic application of PAC.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a freeze-dried preparation and a preparation method of a pectin-doxorubicin conjugate. Background technique [0002] The name of the Chinese patent application is solid tumor passive targeting anticancer prodrug and its preparation method, and the application number is 200910311854.0. Medicine, which is obtained by reacting small molecule pectin with Mw (Mw, that is, weight-average molecular weight, weight-average molecular weight, which belongs to one of the molecular weight expression methods of polymer compounds) of 0.5 to 45,000 and doxorubicin is 100,000 to 1,000,000 pectin-doxorubicin conjugates, made into a suspension, processed by a nano ultra-high pressure homogenizer to obtain a particle size of 100nm-200nm, and a melting point of 220°C to 245°C. Passive targeted anticancer for solid tumors Prodrug; wherein, pectin and doxorubicin are connected through amide bonds, ...

AI Technical Summary

Problems solved by technology

[0003] The pectin-adriamycin conjugate is called pectin-adriamycin conjugate (Pectin-adriamycin coniuncate, hereinafter referred to as PAC) in this patent, and the inventor found that its solubility was very poor when applying PAC, and many times Solubility test shows that it is insoluble

There are two major problems in the clinical application of poorly soluble drugs. One is the low solubility of the drug, which leads to low bioavailability. The other is that the conventional preparation methods also have certain restrictions on the application of poorly soluble drugs.

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