Development of a pharmaceutical cocrystal of a monophosphate salt with phosphoric acid.
We report the first case of a pharmaceutical cocrystal formed between an inorganic acid and an active pharmaceutical ingredient (API), which enabled us to develop a stable crystalline and bioavailable solid dosage form for pharmaceutical development where otherwise only unstable amorphous free form or salts could have been used.
Chen
Alex M
AM
Merck & Co. Inc., PO Box 2000, Rahway, New Jersey 07065, USA. alex_chen2@merck.com
Ellison
Martha E
ME
Peresypkin
Andrey
A
Wenslow
Robert M
RM
Variankaval
Narayan
N
Savarin
Cecile G
CG
Natishan
Theresa K
TK
Mathre
David J
DJ
Dormer
Peter G
PG
Euler
Danielle H
DH
Ball
Richard G
RG
Ye
Zhixiong
Z
Wang
Yaling
Y
Santos
Ivan
I
D003460:Crystallization; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D015394:Molecular Structure; D010710:Phosphates / Q000737:chemistry* / Q000494:pharmacology; D010756:Phosphoric Acids / Q000737:chemistry*
D010710:Phosphates; D010756:Phosphoric Acids; C030242:phosphoric acid