| Objective : to prepare Huang-Ma Slow-Release Membrane Spray Agent.Methods:（1） To determine the detection wavelength of strychnine and berberine hydrochloride by using UV scanning method.（2） HPLC is determined by drawing standard curves, investigation precision and stability of strychnine and berberine hydrochloride.（3） To optimize appropriate film-forming agent by determine the properties of coating materials such as PVP K30, PVA-1788 and CMC-Na with its dissolve situation in the liquid.（4） To optimize the Spray Agent prescription by studying the effects of PVA-1788 quality concentration, dosage of ethanol and glycerol to its film-forming, and screening penetration enhancer.（5） To study drug-loaded spray agent′s release behavior in vitro by using Franz diffusion pool method.（6） To establish the HPLC content determination method of strychnine and berberine hydrochloride.（7） To evaluate its safety by investigating the skin irritation.（8） To investigate spray agent preliminary stability by observing reserved sample.Results:（1） The UV detection indicates that strychnine and berberine hydrochloride both have significant absorption at 254 nm.（2） Strychnine has good linear relationship between peak area and concentration in which concentration range was 2.875 μg·m L-1 46μg·m L-1; Berberine hydrochloride has good linear relationship between peak area and concentration in which concentration range was 5.75μg·m L-1 92 μg·m L-1; with good instrument precision; The strychnine and berberine hydrochloride were both relatively stable at room temperature in 24 hours.（3） Optimizing the PVA-1788 as film-forming substrate, glycerol as a moisturizer and it has a good release and permeation without penetration enhancers.（4） Optimizing the PVA-1788 concentration was 5 %, the dosage of glycerol was 6 % and ethanol was 15 %.（5） Diffusion cells results showed that the release curves and transdermal absorption curves in vitro of strychnine and berberine hydrochloride were both in conformity to the first-order kinetic equation;The experiments showed that the drug transdermal process is the main limit factor to percutaneous absorption.（6） HPLC detection wavelength was 254 nm, mobile phase:methanol-0.1 mol·L-1 sodium dihydrogen phosphate solution-0.025 mol·L-1lauryl sodium sulfate solution（50:25:25）, column temperature was 30 ℃;the method was accurate, simple, easy and could effectively measure the content of strychnine and berberine hydrochloride in spray agent.（7） The skin irritation test showed that Huang-Ma slow-release spray agent has almost no irritation to skin.（8） Stability test results showed that the preparation should be stored at shade place, preparation traits, appearance and contents of drugs did not change significantly in 0 6 months, has a good stability.Conclusion: The preparation technology of the spray agent is reasonable, reliable, quality control method is feasible; drug loaded in spray agent had little irritation to skin and has slow-release effect. It is a new drug delivery dosage form which provided theoretical foundation of being better used in clinical. |
