Study on Optimization of Formulation and Technology of Citronellol Submicroemulsion / 中国药房

ABSTRACT

OBJECTIVE：To optimize the p reparation technology of citronellol submicroemulsion. METHODS ：The content of citronellol in Citronellol submicroemulsion was determined by HPLC. Citronellol submicroemulsion by high-speed shearing dispersion-high pressure homogenization method ，with centrifugation stability constant （ke） and particle size were used as evaluation indexes. Its formulation and preparation technology were optimized and validated. Drug-loading amount and encapsulation rate of the preparation were detected. RESULTS ：The linear range of citronellol were 4-64 μg/mL（R 2＝0.999 9）. RSDs of precision ，stability（24 h）and reproducibility tests were all lower than 3％. The recoveries were 97.64％-101.97％（RSD＝ 2.28％，n＝3），97.71％-99.50％（RSD＝1.29％，n＝3），96.87％-101.48％（RSD＝2.86％，n＝3）. The optimal formulation included that total weight of soybean oil and medium chain triglycerides （1 ∶ 1，g/g）was 3.75 g，1.2％ soybean phospholipid was 0.6 g， cholesterol was 0.06 g，citronellol was 1.25 g，0.6 ％ sodium oleate was 0.3 g，15-hydroxystearic acid polyethylene glycol ester was 0.75 g，poloxamer 188 was 0.75 g，water added to 50 mL. After prepared by optimal technology at 4 ℃ which contained shearing speed of 13 000 r/min，lasting for 5 min， primary emulsion was adjusted to pH 7 with dilute hydro- chloric acid ，and homogenized with 600 Bar high pressure for 1434412440@qq.com 5 min. The parameters of Citronellol submicroemulsion accor- ding to optimal formulation and technology contained mean particle size of （91.05±0.26）nm，PDI of （0.20±0.01）， Zeta-potential of （－30.86±0.39）mV，average content of 649511230@qq.com citronellol（100.21±0.01）％，the drug-loading amount was （2.481 7 ± 0.000 7） mg/mL，the encapsulation rate was （99.27 ± 0.03）％ . CONCLUSIONS ：The optimal formulation and technology is stable and feasible.