Glaucocalyxin derivative, and pharmaceutically acceptable salt dosage forms thereof

Abstract

The invention relates to a glaucocalyxin derivative, and pharmaceutically acceptable salt dosage forms thereof. A pharmaceutically acceptable salt of the glaucocalyxin derivative is taken as a main material; and dosage forms, comprising one or a plurality of forms selected from injection, solid preparation, external preparation, suppository, and aerosol preparation, are prepared from the pharmaceutically acceptable salt of the glaucocalyxin derivative and a plurality of additives. The glaucocalyxin derivative and the pharmaceutically acceptable salt dosage forms thereof possess excellent water solubility; and oral administration bioavailability is excellent when the glaucocalyxin derivative and the pharmaceutically acceptable salt dosage forms are applied to the field of medicine. The glaucocalyxin derivative and the pharmaceutically acceptable salt dosage forms thereof can be applied to the field of anti-autoimmune disease drug and antitumor drug exploitation, and drug blank of systemic lupus erythematosus, psoriasis, and triple negative breast cancer can be filled.

Description

technical field [0001] The invention belongs to the field of chemistry and medicine, in particular to a ramacine derivative, and in particular to a dosage form of a ramacine derivative and a pharmaceutically acceptable salt thereof. Background technique [0002] Kaur-16-ene-3, whose structure is shown in formula Ⅰ, is also known as Wangzaozi B, which is extracted from the whole herb of the Lamiaceae plant, Kaur-16-ene-3. ,15-dione,(7α,14R)-, molecular formula: C 20 h 28 o 4 , molecular weight 332.43. Its structure is similar to that of Rubescensin, which belongs to ent-kaurane diterpenes, and also has antitumor pharmacophore α, β-unsaturated ring similar to Rubescensin in the structure Pentanone structural unit. [0003] It has been shown in published literature that it is effective against various human cancer cell lines (CE-1, U87, A549, MCF-7, Hela, K562, HepG2, NCI-H460, KB, JEG-3, K562, HL-60 etc. have significant anti-proliferation effects, especially for non-hor...

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Problems solved by technology

[0005] However, cerulein A has low polarity and poor water solubility, so it is not suitable for direct administration as a drug; therefore, on the premise of retaining the pharmacophore α, β-unsaturated cyclopentanone, the structure of the double bond outside the ring is modified , the synthesis of derivatives with stronger anti-autoimmunity and anti-tumor effects is an effective way to solve the defects existing in them as drugs

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