盐酸四环素胃内漂浮微球的研制

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Abstract Objective To prepare Tetracycline Hydrochloride gastric floating microspheres using ionic gelation method, and to improve drug release percentage and therapeutic effect of anti-Helicobacter pylori. Methods Chitosan and alginate were chosen as the carriers, and NaHCO3 was utilized as the foaming agent. The orthogonal experiment was adopted to investigate the weight ration of tetracycline/alginate and alginate/NaHCO3, as well as the concentration of CaCl2 and chitosan. Therefore, the optimum preparation was determined by evaluating floating performances, drug release, encapsulation efficiency and balling index. Results The optimal conditions were as followed: the concentration of chitosan was 8 mg/mL, the weight ration of alginate/tetracycline was 4∶1, the concentration of CaCl2 was 20 mg/mL, and the weight ration of alginate/NaHCO3 was 2∶1. The microcapsules could float in stomach for 24 h with a floating rate of 95%, and the encapsulation efficiency was 79.90%. The in vitro experiments suggested that these floating microspheres had good sustain-release properties. Conclusion According to the results above, tetracycline gastric floating microspheres meet the requirements of gastric retention, which can increase drug absorption and therapeutic effect of anti-Helicobacter pylori, reduce dosing frequency, and have more selection of dosage forms.

Key words： Tetracycline Hydrochloride Gastric floating microspheres Chitosan Alginate Orthogonal experiment

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	ZHONG Lei1 BIAN Fang1 ZHAO Chaoyang2 ZHANG Hong1

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ZHONG Lei1 BIAN Fang1 ZHAO Chaoyang2 ZHANG Hong1. Study on Tetracycline Hydrochloride gastric floating microspheres[J]. 中国医药导报, 2018, 15(7): 23-26.

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http://www.yiyaodaobao.com.cn/EN/ OR http://www.yiyaodaobao.com.cn/EN/Y2018/V15/I7/23

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