Stable lenalidomide oral solid preparation

Abstract

The invention discloses a lenalidomide oral solid preparation which is based on 10000 solid preparation units and is prepared by the following components: 10-500g of lenalidomide, 300-1200g of premixed powder, 50-200g of cross-linked sodium carboxymethyl cellulose, 1-50g of magnesium stearate and 100-500ml of 10% (percent weight in volume) povidone absolute ethyl alcohol solution, wherein the premixed powder is the mixture of lactose and microcrystalline cellulose which have the weight ratio of 2:3. In addition, the invention also discloses a preparation method of the lenalidomide oral solid preparation and usage thereof. The lenalidomide oral solid preparation has the advantages that a sample can be reserved for a long time with stable quality; and the lenalidomide oral solid preparation can be released within a short time so as to be easily absorbed by the human body completely.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, more specifically, relates to an oral pharmaceutical preparation of lenalidomide which is stable, releases quickly in a short period of time and is completely easily absorbed by the human body. Background technique [0002] Lenalidomide, an immunomodulator with antiangiogenic and antineoplastic properties, has the chemical name 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2- Base)-2,6-piperidinedione, its chemical structural formula is as follows: [0003] [0004] Lenalidomide has piperidinedione and indoline residues, and an asymmetric center in the structure, and the currently approved lenalidomide is a racemic compound. [0005] Chinese patent application CN 1239959A (published on December 29, 1999) discloses a chewable tablet containing 75 mg of lenalidomide, and its auxiliary materials include mannose, lactose, talcum powder, glycine, stearic acid, saccharin and 5% Gelatin solution (E...

AI Technical Summary

Problems solved by technology

[0009] Because lenalidomide is insoluble in water, it affects the dissolution rate of its oral solid preparation and then directly affects the bioavailability of the drug. The prior art solves this problem by micronization or strong salt; in addition, the oral solid preparation auxiliary material The type may affect the stability of the preparation. For example, due to the amino group in the molecular structure of lenalidomide, the "Maillard reaction" may occur if the preparation excipient uses lactose as the excipient, which increases the impurity content of the solid oral preparation and is prone to Change in appearance color (see, Raymond C Rowe et al., eds., Handbook of Pharmaceutical Excipients, 5th ed., 2006, the Pharmaceutical Press)

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