Study On Tablet Of Thenorphine Hydrochloride And Quality Control

Thenorphine Hydrochloride (ThH) is a 1st category new drug of China which was developed by Institute of Pharmacology and Toxicology, the Academy of Military Medicinal Science (the Property Right holder).The drug is a sectional opioid receptor antagonist with a novel configuration. ThH is known to produce strong antalgic effect and long duration of action with a small dose. ThH has unique characteristics which set it apart from other opioid receptor antagonist such as, for example, Buprenorphine.ThH have a good oral absorption, marking antimorphine effect and high Reliable Index(500~1000) while has not been shown to produce tolerance, physical dependence, or abuse potential. So, ThH has a exploitation perspective as an ideal drug for antalgic and for Off-the-Habit. In order to provide lab data of ThH for the preclinical and clinic study, we planed to study on the tablet of ThH and its quality control.Firstly, considering the drug's dissolubility and dosage, we optimized the formulation and process with the index of preparation's dissolution and uniformity of content. Based on the study above, the optimal formulation was determined. The result showed that the formulation is reasonable and the Spec is 0.1, 0.2, 0.5mg/tab. The preparation's dissolution and uniformity of content were consistent with regulation.Secondly, we studied on the preparation's quality control, which was the key work in our study. HPLC method was established for the analysis. The method had a good selectivity and reproducibility while the adjuvants and decomposition method of assay and stability test is exact, sensitive ,the adjuvants and decomposition products could be well separated from thenorphine hydrochloride. The stability study on preparation indicated that it was stable, nearly without any changes during the stability study.The formulation and process of thenorphine hydrochloride were confirmed.On the meantime,the quality standard of the preparation was established.No report about it was found. The innovation of the formulation was verified by the pharmacodynamic studies of thenorphine hydrochloride tablet.The preclinical study of it as lnd category new drug of China have been finished basically and the formulation has been patented.