Abstract
Classical mixed micelle systems make excellent parenteral drug carriers for lipophilic or poorly soluble drugs, but many formulations details are not fully understood and need further study. Thus, we constructed mixed micelle systems with lecithin and either glycocholic acid sodium salt or deoxycholic acid sodium salt in order to investigate the differences between the bile salts. Vitamin K1, a lipid‐soluble drug, was encapsulated in the mixed micelles, and the influence of bile salts on the quality and stability of the mixed micelle systems was analyzed. Both bile salts displayed similar profiles, and the amounts of bile salts used in formulating clear solutions did not differ. Mixed micelle systems formed from glycocholic acid sodium were physically stable at low pH levels (5.5), whereas those formed from deoxycholic acid required higher pH (>8.5). High pH levels hurt active pharmaceutical ingredients that are prone to hydrolytic and oxidative degradation. Hence, when mixed micelle systems formed from deoxycholic acid sodium were sterilized, unexpected chemical unstability occurred. Therefore, we conclude that glycocholic acid sodium salt is more suitable than deoxycholic acid sodium salt for the preparation of mixed micelle injections.
Highlights
Classical mixed micelle (MM) systems, composed of natural phospholipids and bile salts, offer a nontoxic, highly biocompatible, and parenterally well‐tolerated drug carrier for lipophilic and poorly soluble drugs
Has been approved for the pharmaceutical market; while a few published results have described the influence of lecithin/bile salt ratios and the effect of total concentration on the size and shape of MMs (Krishnadas, Rubinstein, & Önyüksel, 2003; Lichtenberg, Robson, & Dennis, 1983; Shankland, 1970), many other factors are not fully understood
An ultraviolet‐visible spectrophotometer (U‐3010, Hitachi) was used to analyze the transmittance of MM systems at 650 nm in order to elucidate the influence of bile salt or phospholipid (PC) concentrations on the formation of clear solutions in the presence of 1% (m/v) vitamin K1
Summary
Classical mixed micelle (MM) systems, composed of natural phospholipids and bile salts, offer a nontoxic, highly biocompatible, and parenterally well‐tolerated drug carrier for lipophilic and poorly soluble drugs. KEYWORDS deoxycholic acid salt, glycocholic acid salt, mixed micelle injection, physiochemical stability, Vitamin K1 Glycocholic acid sodium deoxycholic acid sodium how they differ, we constructed MM systems from lecithin and bile (GAS or DAS) salts.
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