PMID- 30944538
OWN - NLM
STAT- MEDLINE
DCOM- 20190603
LR  - 20200225
IS  - 1976-555X (Electronic)
IS  - 1229-845X (Print)
IS  - 1229-845X (Linking)
VI  - 20
IP  - 2
DP  - 2019 Mar
TI  - Preparation, characterization, and in vivo evaluation of a polymorphic form of 
      valnemulin hydrogen tartrate.
PG  - e16
LID - 10.4142/jvs.2019.20.e16 [doi]
LID - e16
AB  - We prepared a polymorphic form of valnemulin hydrogen tartrate (Form I) to 
      overcome the instability and irritating odor of valnemulin hydrochloride that 
      affect its use in the production and application of veterinary drugs. The 
      physicochemical properties of Form I were characterized by scanning electron 
      microscopy, X-ray powder diffraction, infrared spectroscopy, differential 
      scanning calorimetry, and thermogravimetric analysis. The results showed the 
      crystal structure and thermal properties of Form I were very different from those 
      of a commercially available form of valnemulin hydrogen tartrate (Form II). Form 
      I and Form II were more stable than valnemulin hydrochloride after storage under 
      irradiation and high humidity conditions, respectively. The solubility of Form I 
      was 2.6 times that of Form II, and Form I was selected for use in pharmaceutical 
      kinetics experiments in vivo. Compared to valnemulin hydrochloride, after oral 
      administration at a dose of 10 mg/kg in pigs, Form I had similar pharmaceutical 
      kinetic behavior but a slightly higher area under the concentration-time curve 
      from time zero to the last measurable concentration. Consequently, Form I should 
      be suitable for the development of simple formulations and be effective in the 
      clinical application of veterinary drugs.
FAU - Zhu, Xinle
AU  - Zhu X
AUID- ORCID: 0000-0002-8722-8432
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Xu, Shixin
AU  - Xu S
AUID- ORCID: 0000-0003-2506-0109
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Lu, Lianshou
AU  - Lu L
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Wang, Shensen
AU  - Wang S
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Zhao, Qi
AU  - Zhao Q
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Li, Dan
AU  - Li D
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Li, Jian
AU  - Li J
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Zhao, Hui
AU  - Zhao H
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
FAU - Xu, Bingen
AU  - Xu B
AD  - Safety Assessment Department, China Institute of Veterinary Drug Control, Beijing 
      100081, China.
LA  - eng
PT  - Journal Article
DEP - 20190322
PL  - Korea (South)
TA  - J Vet Sci
JT  - Journal of veterinary science
JID - 100964185
RN  - 0 (Anti-Bacterial Agents)
RN  - 0 (Diterpenes)
RN  - 0 (Tartrates)
RN  - 2AHC415BQG (valnemulin)
SB  - IM
MH  - Animals
MH  - Anti-Bacterial Agents/*chemistry/pharmacokinetics/therapeutic use
MH  - Calorimetry, Differential Scanning
MH  - Crystallization
MH  - Diterpenes/chemistry/pharmacokinetics/therapeutic use
MH  - Drug Compounding/veterinary
MH  - Male
MH  - Microscopy, Electron, Scanning
MH  - Spectroscopy, Fourier Transform Infrared
MH  - Swine
MH  - Tartrates/chemistry/therapeutic use
MH  - Thermogravimetry
MH  - X-Ray Diffraction
PMC - PMC6441808
OTO - NOTNLM
OT  - Pharmacokinetics
OT  - pigs
OT  - polymorphism
OT  - solubility
OT  - valnemulin
COIS- Conflict of Interest: The authors declare no conflicts of interest.
EDAT- 2019/04/05 06:00
MHDA- 2019/06/04 06:00
PMCR- 2019/03/01
CRDT- 2019/04/05 06:00
PHST- 2018/12/01 00:00 [received]
PHST- 2019/01/20 00:00 [revised]
PHST- 2019/02/08 00:00 [accepted]
PHST- 2019/04/05 06:00 [entrez]
PHST- 2019/04/05 06:00 [pubmed]
PHST- 2019/06/04 06:00 [medline]
PHST- 2019/03/01 00:00 [pmc-release]
AID - 10.4142/jvs.2019.20.e16 [doi]
PST - ppublish
SO  - J Vet Sci. 2019 Mar;20(2):e16. doi: 10.4142/jvs.2019.20.e16. Epub 2019 Mar 22.