10-hydoxy camptothecin self micro emulsifieation composition

Abstract

A self-microemulsifying 10-hydroxycamptothecine composition applied by injection or orally features that its self-microemulsifier is prepared from oil phase, surfactant and cosurfactant. After it is taken into human body, it can automatically microemulsifying for higher biologic utilization rate.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a 10-hydroxycamptothecin self-microemulsion composition and a preparation method thereof. Background technique [0002] 10-hydroxycamptothecin (Hydrocamptothecin, HCPT) is a trace alkaloid with the strongest anti-cancer effect among similar anti-tumor monomers extracted from camphor tree chinensis in the 1960s and 1970s. It is an S-phase specific anti-cancer drug . Systematic pharmacological research. Its anti-cancer mechanism is to inhibit Topo I. It is mainly used clinically in ascites-type liver cancer, head and neck cancer, gastric cancer, bladder cancer and leukemia. The toxic reactions of HCPT are mainly manifested in the inhibition of urinary system, digestive system and hematopoietic function. etc., but its toxicity is significantly lower than that of camptothecin, especially the urinary system reaction is less, and it is easy to be accepted clinically. At prese...

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Problems solved by technology

At present, the main problems of the drug are: short half-life (5min-1h), repeated administration is required, so the side effects are relatively large; fat solubility is strong, and the anticancer activity of the water-soluble sodium salt is reduced by 90%; poor stability , the lactone ring of the drug is sensitive to light and heat, and loses its pharmacological activity after opening the lactone ring

At present, domestic clinical preparations are in the form of ring-opening salts of HCPT (patents 02138930.6 and 02114913.5). The efficacy of such preparations decreases significantly, and the toxicity increases, which limits clinical application.

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