PMID- 35230851
OWN - NLM
STAT- MEDLINE
DCOM- 20220503
LR  - 20220509
IS  - 1543-8392 (Electronic)
IS  - 1543-8384 (Linking)
VI  - 19
IP  - 5
DP  - 2022 May 2
TI  - Insoluble Salt of Memantine with a Unique Fluorescence Phenomenon.
PG  - 1389-1399
LID - 10.1021/acs.molpharmaceut.1c00931 [doi]
AB  - Alzheimer's disease is a chronic disease, and the long-term treatment of chronic 
      diseases has always been a concern. Memantine (Mem) is approved by the US Food 
      and Drug Administration for the treatment of moderate to severe Alzheimer's 
      disease. In this study, reactions of memantine (Mem) with pamoic acid (Pam) were 
      carried out to form insoluble salts (Mem-Pam). Four polymorphic forms (Forms 
      I-IV) of Mem-Pam were successfully obtained through polymorphic screening, which 
      were systematically characterized by X-ray powder diffraction (PXRD), thermal 
      analysis (TGA and DSC), single-crystal X-ray diffraction (SXRD), and solid-state 
      fluorescence. Compared with the hydrochloride form, the dissolution and release 
      rates of these four forms are lower. The presence of pamoic acid reduces the 
      release rate of memantine and makes it possible to achieve a sustained release of 
      the drug. Interestingly, because of the presence of memantine, each polymorphic 
      solid crystal of Mem-Pam has unique fluorescence emission. Therefore, memantine 
      and pamoic acid have a synergistic effect on the fluorescence performance and can 
      be expected to be used for real-time monitoring in continuous and controlled 
      release drug delivery systems. In addition, the polymorphic solid crystals also 
      exhibit reversible mechanochromic luminescence under the fumigation of 
      acetonitrile vapor, which has a guiding role in the fluorescence design and 
      synthesis of Pam substances and is expected to be used for information security, 
      visual inspection of organic substances, etc.
FAU - Kuang, Wenjie
AU  - Kuang W
AD  - State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin 300072, 
      P. R. China.
FAU - Liu, Jian
AU  - Liu J
AD  - State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin 300072, 
      P. R. China.
FAU - Lin, Xia
AU  - Lin X
AD  - School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, P. R. China.
FAU - Wu, Songgu
AU  - Wu S
AUID- ORCID: 0000-0003-4329-4654
AD  - State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin 300072, 
      P. R. China.
FAU - Gong, Junbo
AU  - Gong J
AUID- ORCID: 0000-0002-3376-3296
AD  - State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin 300072, 
      P. R. China.
FAU - Yin, Qiuxiang
AU  - Yin Q
AUID- ORCID: 0000-0001-8812-0848
AD  - State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin 300072, 
      P. R. China.
FAU - Wang, Jingkang
AU  - Wang J
AD  - State Key Laboratory of Chemical Engineering, Tianjin University, Tianjin 300072, 
      P. R. China.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20220301
PL  - United States
TA  - Mol Pharm
JT  - Molecular pharmaceutics
JID - 101197791
RN  - 0 (Powders)
RN  - 451W47IQ8X (Sodium Chloride)
RN  - W8O17SJF3T (Memantine)
SB  - IM
MH  - *Alzheimer Disease/drug therapy
MH  - Humans
MH  - *Memantine
MH  - Powders
MH  - Sodium Chloride
MH  - X-Ray Diffraction
OTO - NOTNLM
OT  - insoluble salts
OT  - memantine
OT  - pamoic acid
OT  - physicochemical property
OT  - polymorphism
EDAT- 2022/03/02 06:00
MHDA- 2022/05/04 06:00
CRDT- 2022/03/01 17:11
PHST- 2022/03/02 06:00 [pubmed]
PHST- 2022/05/04 06:00 [medline]
PHST- 2022/03/01 17:11 [entrez]
AID - 10.1021/acs.molpharmaceut.1c00931 [doi]
PST - ppublish
SO  - Mol Pharm. 2022 May 2;19(5):1389-1399. doi: 10.1021/acs.molpharmaceut.1c00931. 
      Epub 2022 Mar 1.