Strychnine-hydroxypropyl-beta-cyclodextrin liposome, preparation method and applications thereof

Abstract

The present invention discloses a strychnine-hydroxypropyl-beta-cyclodextrin liposome, which contains, by weight, 0.5-2 parts of strychnine, 2-20 parts of a strychnine-HP-beta-cyclodextrin inclusion compound, 20-200 parts of soybean lecithin, and 5-20 parts of cholesterol. The present invention further discloses a strychnine-hydroxypropyl-beta-cyclodextrin liposome preparation method, which comprises: carrying out inclusion on strychnine with hydroxypropyl-beta-cyclodextrin, and then preparing into the liposome. According to the present invention, drug loading capacity is improved, an elimination half-life of the strychnine is prolonged, stability is improved, lymphatic system targeting is achieved, toxic and side effects on heart and central nervous system are reduced, and bioavailability is improved.

Description

technical field

[0001] The invention relates to the preparation technology of anti-inflammatory and analgesic drugs, in particular to a strychnine-hydroxypropyl-β-cyclodextrin liposome and its preparation method and application. Background technique

[0002] Strychnine is the active ingredient of Strychnos nux-vomica L or SPierriana A.W.Hill, a plant of the family Strychnosaceae. It is an effective drug for the treatment of rheumatoid arthritis. Oral administration of strychnine can easily cause abdominal pain and diarrhea. Long-term use of strychnine can damage renal tubular epithelial cells, cause renal function damage, and can excite the central nervous system to produce heart and central side effects. At the same time, it metabolizes quickly in the body and has low bioavailability. The promotion of sub-alkaline in clinical application.

[0003] Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a hydroxyalkyl derivative of β-cyclodextrin (β-CD). It has an excellent enveloping ...