January 17, 2018
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Sulfobutyl Ether-β-cyclodextrin Sodium salt(SBE- beta -CD), as a derivative of beta -CD, has been widely applied in medicine field because of its high safety, strong solubilization and inclusion ability. Because it can not only improve the stability and safety of the drug, it can reduce the irritation of the injection to the injection site, the blood concentration of drug to achieve fast, prolong the time of drug action, making it as injection accessories have wide application foreground.
Fentanyl (Fentanyl) is a synthetic opioid receptor agonist, which is a potent analgesic and is used for sedation and analgesia before, during and after anesthesia. Due to the large effect of oral first pass, it is usually used for injection. Shandong Binzhou Zhiyuan Biotechnology Co.Ltd, the researchers studied the company's flagship product SBE- beta -CD and HP- beta -CD as an excipient in improving the potential utility of fentanyl injection. The results showed that all two kinds of beta -CD derivatives could form 1:1 inclusion complexes with fentanyl, and the solubility of the drugs increased with the increase of the concentration of beta -CD. By drawing the phase solubility curve, can choose the suitable concentration of beta -CD, making the drug exist at the same time free drug injection and. The minimum effective amount of the free drug dose can ensure injection, involved drugs as drug reservoir, release the drug slowly, so as to achieve the purpose of long-term. These results suggest that the use of SBE- beta -CD as a solubilizer and stabilizer is possible for the preparation of a long effect injection of fentanyl.
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