title: Pharmacokinetics of dimemorfan phosphate tablets in healthy Chinese volunteers.
abstract: OBJECTIVE
  Investigate the pharmacokinetic properties of the antitussive dimemorfan phosphate tablets in healthy male and female Chinese volunteers after single and multiple-dose administration; and to evaluate the food-effect on pharmacokinetics of dimemorfan.
  
  
  METHODS
  12 subjects received a single dose of 10 mg and 40 mg dimemorfan phosphate tablets, respectively in study stage 1. Another 12 subjects received a single dose of 20 mg dimemorfan phosphate tablets under fed conditions, a single dose of 20 mg dimemorfan phosphate tablets under fasting conditions and multiple-dosing of 20 mg dimemorfan phosphate tablets 3 times per day, respectively in study stage 2. The washout between each treatment was 1 week. Plasma dimemorfan was quantified by a high pressure liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method.
  
  
  RESULTS
  After single-dosing of 10 mg, 20 mg and 40 mg dimemorfan phosphate tablets, Cmax, AUC0-tand AUC0-∞were dose proportional, which achievd 6.19 ± 7.61 ng·mL-1, 101 ± 171 and 117 ± 210 ng·mL-1·h, respectively after single-dosing of 40 mg dimemorfan phosphate tablets. Tmaxranged from 2.75 to 3.96 h and t1/2ranged from 10.6 to 11.4 h. After multiple-dosing of 20 mg dimemorfan phosphate tablets, the Accumulation Index (AI) was 2.65 ± 1.11. The pharmacokinetic parameters after single-dosing of 20 mg dimemorfan phosphate tablets under fed conditions were similar with those under fasting conditions. Sex did not affect the pharmacokinetics of dimemorfan phosphate tablets.
  
  
  CONCLUSIONS
  Single-dosing of dimemorfan phosphate tablets exhibited linear kinetic characteristics. Multiple-dosing of 20 mg dimemorfan phosphate tablets 3 times per day caused obvious accumulation. No food effect or sex effect on the pharmacokinetics of dimemorfan phosphate tablets was observed. Chictr.org identifier: ChiCTR-ONC-14004851.
authors.affiliation: Department of Abdominal Oncology, Cancer Center, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Yali
authors.initials: Y
authors.lastname: Shen
authors.affiliation: GCP Center / Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China. luozhu720@163.com.
authors.forename: Zhu
authors.identifier: http://orcid.org/0000-0003-1030-2320
authors.initials: Z
authors.lastname: Luo
authors.affiliation: GCP Center / Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Qin
authors.initials: Q
authors.lastname: Yu
authors.affiliation: GCP Center / Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.affiliation: GCP Center / Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Jin
authors.initials: J
authors.lastname: Xiang
authors.affiliation: GCP Center / Institute of Drug Clinical Trials, West China Hospital, Sichuan University, Chengdu, 610041, People's Republic of China.
authors.forename: Jia
authors.initials: J
authors.lastname: Miao
mesh_terms: D000996:Antitussive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D044466:Asian People; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004305:Dose-Response Relationship, Drug; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D009019:Morphinans / Q000008:administration & dosage / Q000493:pharmacokinetics*; D013607:Tablets; D053719:Tandem Mass Spectrometry / Q000379:methods*; D055815:Young Adult
chemical_list: D000996:Antitussive Agents; D009019:Morphinans; D013607:Tablets; C012621:dimemorfan
keywords: Dimemorfan phosphate; HPLC-MS/MS; Pharmacokinetics