Medication composition of containing macrolides

Abstract

A composite medicine with higher biologic utilization rate contains the microemulsified and pre-concentrated solutions of macrocyclic lactone compound, 1,2-propanediol, hydrophilic surfactant, and medium-and long-chain saturated or unsaturated lipophilic glyceride of fatty acid.

Description

technical field [0001] The invention relates to a pharmaceutical composition, which is a microemulsion preconcentrate containing macrolide compounds, has excellent self-emulsification performance, and is used in the medical field. Background technique [0002] The macrolide compound referred to in the active ingredient of the present invention is a macrolide compound with a tricyclic lactam structure produced by microorganisms of the genus Streptomyces hygroscopicus, including rapamycin, FK506, ascomycin and their analogs Or derivatives, these tricyclic compounds have strong immune activity, antibacterial activity and other pharmacological activities, and are mainly used clinically for the treatment of organ transplantation or tissue transplantation against rejection and autoimmune diseases. [0003] The common point of these above-mentioned macrolide compounds is that they are water-insoluble drugs, and have the disadvantage of low oral bioavailability. Oral absorption is ...

AI Technical Summary

Problems solved by technology

Due to the poor dissolution effect, the drug absorption of these two dosage forms is largely affected by the patient's body condition, and the individual differences are very large. The coefficient of variation CV (%) of absorption is about 45, which is relatively difficult to maintain an effective therapeutic concentration. , Improper use will increase toxic and side effects, and at the same time, they are all strongly affected by food, and must be taken under constant eating conditions to ensure a stable blood drug concentration

[0006] For the solid preparations of rapamycin studied in the past, such as solid dispersions, β-cyclodextrin inclusion complexes, etc. (Chinese invention patent application number 96196788.9), the formed solid dispersions have to be ground, and the average particle size is 100-500um. Although it can improve the dissolution rate of rapamycin and increase the bioavailability, the preparation process is relatively complicated and requires special equipment. At the same time, there are organic solvents, and solvent recovery and explosion-proof safety issues must be considered.

This kind of prescription preparation is still not ideal

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