The application of Hydroxypropyl Beta Cyclodextrin in injection.
Hydroxypropyl betacycline dextrin (HPBCD) could increases the solubility of insoluble drugs, thus avoiding the use of organic solvents, surfactants and esters.HPBCD in 1999, the FDA has approved of itraconazole intravenous fluids as excipient, immunosuppression uninfected rat once a day of intravenous itraconazole HPBCD solution (40%), continuous dosing 7 d, itraconazole doses were 10, 20, 30 or 40 mg kg - 1, observed 28 d, LD was 24.5 mg, 1 kg -, d - 1 to 7.
HPBCD can also reduce the toxicity and irritation of drugs.Solid tumor patients, respectively, the static note mitomycin preparations containing HPBCD MitroExtra and mitomycin, human pharmacokinetic parameters of no significant difference, but accept MitroExtra subjects injected local erythema, ulcers, skin toxicity response is decreased obviously.HPBCD can also relieve the pain caused by etomidate injection.
At 0.05mol/L HPBCD, the solubility of nimodipine can be increased by 60 times, and the AUC of rabbits can be increased by about 2.5 times within 24h of im, and the stimulation to muscles will be reduced.
After intrabscabbard, cerebrospinal fluid and epidural injection of HPBCD inclusion compound, the inclusion compound is slowly dissociated at the injection site and can achieve sustained release.The analgesic effect of fentanyl -HPBCD inclusion compound was significantly prolonged after epidural injection.