Carboxymethyl high amylose starch (CM-HAS) as excipient for Escherichia coli oral formulations

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• 作者：Calinescu ; Carmen ; Mulhbacher ; J??r??me ; Nadeau ; ??ric ; Fairbrother ; John Morris ; Mateescu ; Mircea Alexandru
• 关键词：Carboxymethyl high amylose starch ; Oral administration ; Drug delivery ; Gastric resistance ; Intestinal matrix dissolution ; Escherichia coli ; Probiotics ; Vaccin
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2005
• 出版时间：May, 2005
• 年：2005
• 卷：60
• 期：1
• 页码：53-60
• 全文大小：190 K

文摘

Carboxymethyl high amylose starch (CM-HAS) is proposed as a novel excipient for oral tablet formulation of bioactive agents ensuring their protection in the stomach and delivery in the intestine. Three variants of CM-HAS, with different degrees of substitution, were synthesized by starch treatment with various amounts of monochloroacetic acid. The products were dried in powder form and tablets were obtained by direct compression of mixed powders of polymeric excipient and lyophilized Escherichia coli (E. coli) bacteria. Dosage forms of CM-HAS are unswollen and compact in acidic medium, ensuring protection of active agents against acidity. Release of bacteria from CM-HAS tablets is based on the fast swelling of the tablets during the passage from gastric acidity to alkaline intestinal medium, enzymatic hydrolysis triggering their rapid, almost total dissolution. The bacteria thus formulated displayed higher survival rates in acidic gastric conditions and for longer periods than the free bacteria or than the bacteria formulated with the non-derivatized starch. The CM-HAS selected matrix also assured a good viability of bacteria after 6 months under refrigeration.