PMID- 34400960
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20210818
IS  - 1735-0328 (Print)
IS  - 1726-6890 (Electronic)
IS  - 1726-6882 (Linking)
VI  - 20
IP  - 1
DP  - 2021 Winter
TI  - Development and Comparison of Intramuscularly Injected Long-acting Testosterone 
      Undecanoate Nano-/Microcrystal Suspensions with Three Different Particle Size.
PG  - 307-317
LID - 10.22037/ijpr.2019.14408.12370 [doi]
AB  - The aim of this study was to develop and compare the pharmacokinetic property of 
      testosterone undecanoate (TU) nano-/microcrystal suspension with three different 
      particle sizes after intramuscular (i.m.) administration. TU nano-/microcrystal 
      suspensions were prepared by high pressure homogenization method and the mean 
      particle size was 0.30 +/- 0.11 mum (A), 1.21 +/- 0.37 mum (B), and 4.83 +/- 0.60 mum (C), 
      respectively. Scanning electron microscope (SEM) was employed to observe the 
      morphology of nano-/microcrystal suspensions after operation. X-ray Powder 
      diffraction (XRPD) confirmed the crystalline state of TU in nano-/microcrystal 
      suspension. After storage at 4  degrees C and 25  degrees C under mechanical shaking for 2 
      months, physical and chemical stabilities of nano-/microcrystal suspensions were 
      measured by particle size analyzer and high performance liquid chromatography. 
      There was no obvious change in particle size distribution and content of TU. 
      After i.m. administration of suspension C to rats, the concentration of TU in 
      plasma lasted for nearly 12 days that was comparative with the commercial 
      testosterone undecanoate injection. The results showed that microcrystal C with a 
      larger particle size had long-acting effect comparing with other two suspensions. 
      The muscle irritation test in rabbits showed that the local irritation of TU 
      nano-/microcrystal suspensions was lower than that of commercial testosterone 
      undecanoate injection. It can be concluded that appropriate particle size of 
      nano-/microcrystal suspensions for i.m. administration of TU was important to 
      achieve better therapeutic effect.
FAU - Jia, Lihua
AU  - Jia L
AD  - Department of Pharmacy, Beijing Beiya Orthopedics Hospital, Beijing, China.
AD  - L. J. and J. X. contributed equally to this work.
FAU - Xiao, Jiachao
AU  - Xiao J
AD  - State Key Laboratory of Toxicology and Medical Countermeasures, Beijing, China.
AD  - Department of Pharmaceutics, Institute of Pharmacology and Toxicology, Beijing, 
      China.
AD  - L. J. and J. X. contributed equally to this work.
FAU - Yang, Xi
AU  - Yang X
AD  - State Key Laboratory of Toxicology and Medical Countermeasures, Beijing, China.
AD  - Department of Pharmaceutics, Institute of Pharmacology and Toxicology, Beijing, 
      China.
FAU - Gao, Jing
AU  - Gao J
AD  - State Key Laboratory of Toxicology and Medical Countermeasures, Beijing, China.
AD  - Department of Pharmaceutics, Institute of Pharmacology and Toxicology, Beijing, 
      China.
FAU - Zhang, Hui
AU  - Zhang H
AD  - State Key Laboratory of Toxicology and Medical Countermeasures, Beijing, China.
AD  - Department of Pharmaceutics, Institute of Pharmacology and Toxicology, Beijing, 
      China.
FAU - Yu, Fanglin
AU  - Yu F
AD  - State Key Laboratory of Toxicology and Medical Countermeasures, Beijing, China.
AD  - Department of Pharmaceutics, Institute of Pharmacology and Toxicology, Beijing, 
      China.
FAU - Zheng, Aiping
AU  - Zheng A
AD  - State Key Laboratory of Toxicology and Medical Countermeasures, Beijing, China.
AD  - Department of Pharmaceutics, Institute of Pharmacology and Toxicology, Beijing, 
      China.
LA  - eng
PT  - Journal Article
PL  - Netherlands
TA  - Iran J Pharm Res
JT  - Iranian journal of pharmaceutical research : IJPR
JID - 101208407
PMC - PMC8170747
OTO - NOTNLM
OT  - Microcrystal
OT  - Nanocrystal
OT  - Particle size
OT  - Pharmacokinetics
OT  - Testosterone undecanoate
EDAT- 2021/08/18 06:00
MHDA- 2021/08/18 06:01
PMCR- 2021/01/01
CRDT- 2021/08/17 07:28
PHST- 2021/08/17 07:28 [entrez]
PHST- 2021/08/18 06:00 [pubmed]
PHST- 2021/08/18 06:01 [medline]
PHST- 2021/01/01 00:00 [pmc-release]
AID - 10.22037/ijpr.2019.14408.12370 [doi]
PST - ppublish
SO  - Iran J Pharm Res. 2021 Winter;20(1):307-317. doi: 10.22037/ijpr.2019.14408.12370.