O/w type matrine percutaneous absorption microemulsion

Abstract

The invention provides a matrine percutaneous administration new dosage form, namely an o / w type matrine percutaneous absorption microemulsion, and a preparation method thereof. The o / w type matrine percutaneous absorption microemulsion comprises matrine, a surfactant, a cosurfactant, an oil phase and water, and is characterized in that the particle diameter range of the matrine microemulsion is 20-70 cm, and the mean particle size is 31.2 nm. The formula of the o / w type matrine percutaneous absorption microemulsion comprises the following components in percentage by weight: 7% of matrine, 23% of the surfactant, 15% of the cosurfactant, 4.5% of the oil phase, and 0.5% of the water. The o / w type matrine percutaneous absorption microemulsion provided by the invention has the advantage of overcoming the defects of the available matrine injection and matrine oral preparation, such as rapid in vivo release, instable blood concentration and low bioavailability; and the microemulsion permeates skin to enter blood with zero-order kinetics, and has improved bioavailability compared with the oral preparation, so as to provide convenience for infants and chronic disease patients needing long-term administration. The microemulsion also has a distinct effect on inhibiting hypertrophic scar of rabbit ears, and is hopeful to become a candidate medicament for treating hypertrophic scar.

Description

Technical field: [0001] The invention relates to the technical field of medicine, and relates to a novel drug delivery system of matrine-O / W type matrine transdermal absorption microemulsion. technical background: [0002] Matrine is a natural monomer compound extracted from leguminous plants Sophora flavescens, broad bean root and Sophora sophora. The melting point is 76°C. Free matrine is soluble in water. It has anti-inflammation, anti-virus, anti-fibrosis, liver protection and enzyme reduction, anti-cancer, white blood cell increase and anti-arrhythmia effects. At present, matrine preparations used clinically mainly include injections and oral preparations, which have achieved certain effects in the treatment of chronic hepatitis B and liver cirrhosis. However, matrine injection is extremely inconvenient for infants and young children and chronic hepatitis B patients who need long-term medication, and the half-life of the drug is short, so the blood drug concentration c...

AI Technical Summary

Problems solved by technology

However, matrine injection is extremely inconvenient for infants and young children and chronic hepatitis B patients who need long-term medication, and the half-life of the drug is short, and the blood drug concentration cannot be stabilized for a long time

Although oral preparations overcome the problem that patients are difficult to adhere to long-term injections, their oral drug bioavailability is poor, the number of administrations is frequent, and the drug must be taken tid, which is inconvenient for patients and has large fluctuations in blood drug concentration, which is not convenient for rational drug use.

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