Rotundine Nasal Spray

Rotundine was accepted as an anodyne by Chinese pharmacopoeia. It is one of the active components of the corydalis yanhusuoW.T.Wang. Rotundine is effective on the chronic persistent pain and has sedative and hypnotic effects with no addition. Therefore, it was applied for the patients whose pain caused by tension or insomnia. Nowadays more attentions were paid on the effect of analgesic than sedative and hypnotic. The injection and the oral tablets have been used already. In this paper, Rotundine nasal spray was studied combined its properties with intranasal characteristics. The aim is to get fast absorption, better bioavailability and good compliance.Firstly, the prescription of Rotundine nasal spray has been optimized. The pH was adjusted to increase the solubility of the Rotundine to 50mg·ml-1.The enhancer was screened to enhance the absorption of the drug. It showed that 2.5%E was optimistical to get 1.51 times permeability by the nasal mucosa of the sheep in vitro. The dosage of enhancer E was determined through toadish palate mucosa cilia toxicity test. In the final, prescription screening was completed.Secondly, a reliable HPLC method was established to control the quality of the Rotundine nasal spray. the method is good accuracy and precision, and its linear range is 12.5~300μg·ml-1(r=0.9999).The effect factor study showed that the index fluctuate was in the receivable range. The stability study on the prescription indicated it was stable, nearly without any changes.Finally, the toxicity and pharmacodynamics were carried out on the Rotundine nasal spray. The rabbit eyes and nose mucosal toxicity showed the prescription had no obvious toxicity. On the other hand, the sedative-hypnotic effects of nasal spray was better than injection and oral administration under the equal dosage.The pharmacodynamic study of the preparation on rabbits showed that the sedative-hypnotic effects of nasal spray is better than intravenous administration and oral administration, and it effects more rapidly.In this paper, the results showed the quality of Rotundine nasal spray stabile and controllable. Nasal administration was better than intravenous and oral. It is expected to provide a new dosage form of sedative and hypnotic.