The Investigation of the Pharmacokinetics of Pulsatile-Release Salbutamol Sulfate with pH-Sensitive Ion Exchange Resin as the Carriers in Beagle Dogs

• Published in: Chemical & Pharmaceutical Bulletin Vol. 55; no. 3; pp. 480 - 481
• Main Authors: Hongfei LIUa, b, Tianhui SUNa, Feiqian YUa, Xin ZHAOb, Hong GUOa, Weisan PANa
• Format: Journal Article
• Language: Japanese
• Published: Pharmaceutical Society of Japan 2007
• ISSN: 0009-2363

We previously reported the preparation of the salbutamol sulfate pulsatile-release capsules with the pH-sensitive ion exchange resin as the carriers. In the present study, we investigated the pharmacokinetics of the salbutamol sulfate pulsatile-release capsules in beagle dogs. The analysis method was established for the drugs in vivo by HPLC method. The pharmacokinetics parameters of pulsatile-release salbutamol sulfate and reference tablet were AUC0-24 (ng, h/ml) 1031.8±23.1, 1112.6±118.24, Cmax (ng/ml) 172.4±21.4, 179.3±26.1, Tmax(h) 3.8±0.6, 1.5±0.5, Tlag(h) 2.7±0.5, 0.3±0.2. The results showed that the test dosage forms was bioequivalent with reference dosage form, and had an obviously pulsatile-release effect. Salbutamol sulfate (SS) is used to treat diseases such as asthma, emphysema and bronchitis. ) According to the human circadian rhythm 2) asthma and related conditions often occur in the early hours of the morning and so prove very disturbing to the patient. So, if we can prepare a pulsatile-release salbutamol sulfate which can be released after a 2-3 h lag-time, this will greatly benefit the patients. But now all the SS pulsatile dosage forms are the coated tablets. 3) If the patients break the coated tablets during taking medicine, the pulsatile-release effect will disappear. So if we can prepare the particulate SS pulsatile dosage form will afford a new method for the clinical application. However, to our knowledge, few investigations have been published on the preparation of the particulate SS pulsatile dosage form and the in vitro-in vivo study. In our previously study, we have reported the preparation of the particulate salbutamol sulfate pulsatile-release capsules with the novel pH-sensitive ion exchange resin as the carriers. 4) The results showed that a novel pH-sensitive ion exchange resin was successfully prepared and the SS dissolution in vitro results exhibited an obvious pulsatile release characteristic.