Compound Berberine Hydrochloride Liposome Preparation And Quality

Objective:Take berberine hydrochloride and Radix Aucklandiae volatile oil as model drug to prepare oral liposomes, set up preparation technology that liposomes can encapsulate the amphiphilic drug and lipophilic volatile components at the same time, and to establish an experimental basis of increasing the biological availability and the new clinical application of berberine hydrochloride, and reducing the volatile oil loss and stimulation of essential oil.Method:Extract Radix Aucklandiae volatile oil by steam distillation,and select the best technology factors according to orthogonal design. To Establish To prepare compound berberine hydrochloride liposome by film hydration- pH gradient- probe ultrasonic-method, take encapsulation efficiency, particle size distribution, sample status as the infactors to screen the best prescription and technology. With SephadexG-50 gel column chromatography,PBS (pH7.0) as mobile phase elution liposomes and free drug,demulsify by alcohol and ultrasonic,detect berberine hydrochloride and Radix Aucklandiae volatile oil by HPLC and UV,and calculate the encapsulation efficiency. From the encapsulation efficiency, drug loading, particle size and distribution, vitro release etc, establish quality evaluation.Results:The best distillation conditions of Radix Aucklandiae volatile oil:crush the medical material into raw powder to20-40 mesh, add 10 times of water, soak 0.5h, extraction 10h, extraction rate:0.856%(g/g).SPC S100 (Lipoid), cholesterol (Sigma) was determinated to prepare liposomes. The best formulation and preparation are as follows:SPC concentration of 15mg/mL,SPC/cholesterol/berberine hydrochloride/Radix Aucklandiae volatile oil/=3000:1000:150:25:6;ultrasoniced 3min (ultra 3s, stop 3s, power 360w) in ice water bath,adjusted the external phase to pH7.0, incubated at 60℃20min,prepared compound berberine hydrochloride liposome encapsulation efficiency was: Berberine:91.8% Essential Oil:77.1%.Verify three batches of liposome encapsulation efficiency,the results showed that the technology of preparation and particle size uniformity, system stability. Methodological study meet the analysis requirements. Conclusions:The appearance of the liposomes, microscopic morphology, particle size and distribution, pH value, encapsulation efficiency, leakage rate, the quality such as in vitro release study, the compound berberine hydrochloride liposome quality indexes to agent design. This study achieves the desired purpose of the experiment.