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2022, Vol. 26 ›› Issue (4): 535-539Optimization of preparation method of atorvastatin calcium sustained-release microspheresLiu Tongbin1, Lin Peng2, Zhang Xiaoming1, Dong Xiling1, Cao Fei1, Wang Le1, Guo Xinxing2
Abstract: BACKGROUND: In recent years, studies have found that statins have significant effects on regulating bone metabolism, repairing bone microstructure, inhibiting inflammation, promoting cell proliferation, repairing vascular endothelium, and regulating signal pathway conduction. OBJECTIVE: To optimize the preparation parameters of atorvastatin calcium sustained-release microspheres, to prepare sustained-release microspheres with large drug loading and regular morphology. METHODS: The bovine serum albumin sustained-release microspheres loaded with atorvastatin calcium were prepared by desolvent method. The main factors affected the preparation of the microspheres were screened out. The four key related factors were bovine serum albumin concentration (40, 70, 100 g/L), pH value (7, 8, 9), dosage of atorvastatin calcium (200, 300, 400 µg), and ethanol addition rate (0.2, 0.5, 1 mL/min). The optimal preparation conditions of large drug loading were screened by orthogonal test. Atorvastatin calcium-loaded bovine serum albumin sustained-release microspheres were prepared under optimal parameters and placed in PBS for sustained-release performance testing. RESULTS AND CONCLUSION: (1) The optimum preparation parameters were as follows. The concentration of bovine serum albumin was 100 g/L; the pH value was 7; the dosage of atorvastatin calcium was 400 µg; the addition rate of ethanol was 0.2 mL/min. (2) The microspheres prepared under this parameter had regular morphology and smooth surface. The particle size was (425.0±13.8) nm and the encapsulation efficiency of drug loaded microspheres was up to 85.70%. The in vitro release time could last for more than 48 hours, and the cumulative release reached 73% which had a relatively good sustained release effect. (3) It is indicated that the stable sustained-release microspheres loaded with atorvastatin calcium were successfully prepared. The sustained-release microspheres with high drug loading and stability can achieve sustained drug release. Key words:materials, bovine serum albumin, microspheres, atorvastatin calcium, drug release, orthogonal experiment, entrapment efficiency |