Roxithromycin monohydrate crystal, preparation method thereof and compound dry suspension containing roxithromycin monohydrate crystal and ambroxol hydrochloride composition

Abstract

The invention relates to a roxithromycin monohydrate crystal, a preparation method thereof and a compound dry suspension containing the roxithromycin monohydrate crystal and an ambroxol hydrochloride composition. The roxithromycin monohydrate crystal provided by the invention has a molecular formula of C41H76N2O15.H2O. The preparation method comprises the steps of sample dissolving, devitrifying,smashing, water exchanging and drying. The invention also provides a composition containing the crystal, and the composition comprises 30-70 parts by weight of roxithromycin monohydrate crystals, 5-15 parts by weight of ambroxol hydrochloride, 10-30 parts by weight of xanthan gum, 10-50 parts by weight of hydroxypropyl methylcellulose, 2870-2920 parts by weight of cane sugar and a proper amount of banana essence. The crystal provided by the invention has low moisture absorption and good stability. The composition provided by the invention contains the roxithromycin monohydrate crystal, the suspension is in a good condition, the dissolution rate of medicaments is increased, and the bioavailability is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a roxithromycin monohydrate crystal, a preparation method thereof and a composition dry suspension containing the crystal and ambroxol hydrochloride. Background technique [0002] Pulmonary bacterial infection is a common and frequently-occurring disease of the respiratory system. The main clinical manifestations are cough and expectoration, and antibiotics are usually used for treatment. However, in some cases of bacterial respiratory tract infection with a large amount of sputum, although antibiotics are used reasonably, sometimes the desired curative effect cannot be obtained. The reason may be related to the unobstructed drainage of sputum. The lung is a highly perfused organ. Generally speaking, the concentration of antibacterial drugs in the lung is similar to that in plasma. However, the blood is difficult to perfuse in the abscess cavity and bronchial secretions...

AI Technical Summary

Problems solved by technology

[0005] Chinese patent application CN1582954A discloses a kind of compound preparation of roxithromycin and ambroxol hydrochloride, and its concrete disclosed preparation form has capsule and tablet, but the compound roxithromycin of this common capsule and tablet form, in After oral administration, the dissolution in the body is relatively slow, and it is difficult to achieve complete dissolution, resulting in a decrease in the bioavailability of the drug, and the ideal antibacterial effect cannot be achieved

[0007] CN101712707A discloses that the roxithromycin compound has three solid substance forms of crystal A type, crystal B type and crystal C type. It is found that the crystal form affects the absorption rate of the active ingredient of roxithromycin solid medicine in the organism, enhances or reduces the biological Blood drug concentration in the body thus affects the therapeutic effect of the drug in clinical practice

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