Betadex sulfobutyl ether sodium can not only increase the solubility, stability and safety of the drug, but also reduce the irritation of the injection to the drug delivery site, so that the drug can quickly reach the required blood concentration and prolong the action time of the drug.
At present, Pfizer has successfully developed the injection of ziprasidone, an antipsychotic drug with SBECD as inclusion material, and has been listed in the United States and Sweden. SBECD has many advantages, such as high safety, strong solubilization and inclusion ability, and has broad application prospects as an adjuvant for injection. Examples are as follows:
Fentanyl, a synthetic opioid receptor agonist, is a potent analgesic for sedation and analgesia before, during and after anesthesia. Owing to the large first-pass effect of oral administration, it is generally used for injection. Fentanyl et al. studied the potential of SBECD as excipient in improving the efficacy of fentanyl for injection. The results showed that fentanyl formed a 1:1 inclusion complex, and the encapsulated drug was used as drug storage, releasing the drug slowly, so as to achieve long-term effect. It is possible to prepare long-term fentanyl injection by using SBECD as solventizer and stabilizer.
Amphotericin B is a broad-spectrum polyene antibiotic used in systemic fungal infections. The inclusion compound injection prepared by amphotericin B-SBECD can increase the stability of amphotericin B, improve the safety of drug use, and thus improve the therapeutic window of amphotericin B in clinic.
Amiodarone is a class III antiarrhythmic drug, which is widely used in the treatment of arrhythmia. SBECD can be used as a solvent to prepare safer and more effective amiodarone injection, which can reduce the risk of hypotension after administration.