Solid nano-medicine and preparing method thereof

Abstract

A method of preparing low water-soluble medicine into solid nanometer pharmaceutical formulation is disclosed. According to the characters of molecular aggregates such as supramolecular chemical micelles and vesicles, the formulation, which based on the hydroxypropyl-beta-cyclodextrin and phospholipid, is prepared under the condition of hyperthermia sterilization and decompression. Such nanometer formulation is sterile particle or powder with loose porosity. For directly intravenous use, the formulation has targeting activity, sustained release and long circulating characters. While as a solid oral product, it is fast-release, fast-effective, and improved bioavailability characters, and is readily melted in mouth. The formulation utilizes secure accessories, traditional equipments and methods, thus, it is suited to be used and manufactured widely. Also disclosed is intravenous formulation of anticancer paclitaxel, which characterized that there has no polyoxyethylenated castor oil in it. Such intravenous formulation is nonallergic so that it has higher security and efficiency compared to present commercially available paclitaxel formulations.

Description

technical field [0001] The invention relates to a solid nano-medicine and a preparation method thereof, in particular to preparing a solid nano-medicine by combining an insoluble organic drug with an amphiphilic matrix (carrier). The invention also relates to paclitaxel nano-medicine for injection and a preparation method thereof. Background technique [0002] For drugs that are poorly soluble in water, formulations prepared by conventional methods have poor and highly variable bioavailability, which affects drug efficacy. For new active compounds, formula preparations prepared by conventional methods will affect the results of preclinical screening and clinical trials, and even cause screening errors. According to reports, it is estimated that about 40% of the active substances screened by combinatorial chemistry are poorly soluble in water, which is basically the same proportion as the clinically applied poorly soluble drugs. It can be seen that "solubilization" is undou...

AI Technical Summary

Problems solved by technology

However, most of them do not meet the requirements of drug safety and industrial production, and there have been no clinical and marketing reports so far.

Images