Formulation Optimization of the Volatile Oil Microcapsules of Cinnamomi Ramulus and Angelicae Sinensis Radix and Their Pharmacokinetics in Vivo
10.13748/j.cnki.issn1007-7693.20223396
- VernacularTitle:桂枝、当归挥发油微囊处方优化及体内药动学研究
- Author:
LAI Wensheng
1
;
LIU Yanling
1
;
KUANG Yanhui
2
;
ZHANG Sisi
2
;
ZHANG Chuanping
2
;
LI Chuyuan
2
;
GUO Bohong
1
Author Information
1. School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China
2. Guangzhou Baiyun Mountain and Hutchison Whampoa Ltd., Guangzhou 510515, China
- Publication Type:Journal Article
- Keywords:
Box-Behnken design-response surface method;
Cinnamomi Ramulus and Angelicae Sinensis Radix volatile oil;
microcapsules;
pharmacokinetics;
relative bioavailabilit
- From:
Chinese Journal of Modern Applied Pharmacy
2023;40(16):2251-2259
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To optimize the preparation technology of the volatile oil microcapsules of Cinnamomi Ramulus and Angelicae Sinensis Radix, characterize the microcapsules prepared after the formulation optimization and study pharmacokinetics characteristics in rats. METHODS Spray drying was used to prepare the volatile oil microcapsules of Cinnamomi Ramulus and Angelicae Sinensis Radix. The preparation process was optimized by Box-Behnken response surface method with the drug loading and encapsulation efficiency as indexes. The microcapsules were characterized by Fourier transform infrared spectroscopy(FT-IR) and scanning electron microscopy(SEM). Blood samples were collected after gastric administration at a dose of 100 mg·kg-1. HPLC method was adopted in the plasma concentration determination, and pharmacokinetics behavior in vivo was also compared. RESULTS The optimal formulation: core material-capsules material ratio was 1∶1.7, capsules material concentration was 10.25%, sodium starch octenyl succinate∶maltodextrin was 3.8∶1, high pressure homogenization pressure was 20 MPa and the inlet temperature of spray drying was 185 ℃. Under the optimized conditions, the drug loading was (18.94±1.09)% and the encapsulation rate was (96.03±2.91)%, respectively. The results of FT-IR and SEM showed that the essential oils had been successfully coated in the capsule wall material. The microcapsules were basically spherical in shape, with concave surface but no obvious cracks. The main pharmacokinetic parameters such as tmax, t1/2, CL, AUC0-t, k10,k12, and k21 of microcapsules had significant difference of the volatile oil(P<0.05 or P<0.01). Microcapsules effectively prolonged the circulation time of volatile oil in the body, promoted the absorption of drugs in the body and the oral bioavailability was enhanced to 2.62 times. CONCLUSION The model established by the Box-Behnken design-response surface method can be used to optimize the formulation of volatile oil microcapsules of Cinnamomi Ramulus and Angelicae Sinensis Radix with great prediction effect. The microcapsules prepared by the optimized process has good drug loading properties and the bioavailability of volatile oil is increased.
