Complex formation with layered double hydroxides for the remediation of hygroscopicity

Chemical & Pharmaceutical Bulletin
Aki HayashiHirokazu Nakayama

Abstract

Layered double hydroxides (LDHs) have been used commercially as antacids, to stabilize drugs, to allow the controlled release of incorporated drugs, and to act as drug carriers to reduce drug accumulation within the body. Several types of LDH were investigated: nitrate type (LDH-NO3); chloride type (LDH-Cl); and carbonate type (LDH-CO3). Each type was added to an aqueous or methanol (MeOH) solution containing a drug (pravastatin or nateglinide). With pravastatin sodium, the interlayer distance expanded after reaction with LDH-NO3 and LDH-Cl in aqueous solution. In contrast, the interlayer distance of LDH-CO3 increased in methanol with nateglinide. Each drug was intercalated into the interlayer space of LDH by ion exchange. The hygroscopicity of the drug substances, complexes, and physical mixtures were determined at 70% relative humidity. Increases in weight (%) of the complexes were less than those of the physical mixtures, which demonstrates that hygroscopicity was reduced upon complexation with LDH due to the layer of LDH over the drugs.

References

Mar 29, 2001·Bulletin of Experimental Biology and Medicine·V P ChekhoninV V Belopasov
Oct 31, 2006·International Journal of Pharmaceutics·Markos Trikeriotis, Demetrios F Ghanotakis
Apr 2, 2008·Journal of Colloid and Interface Science·Nobuo Iyi, Takayoshi Sasaki
Apr 22, 2008·Journal of Pharmaceutical Sciences·Hirokazu NakayamaMitsutomo Tsuhako
Aug 21, 2013·Journal of Radiation Research·Minoru SuzukiAkira Maruhashi

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