The effect of pH on polymorph formation of the pharmaceutically active compound tianeptine

Liana Orola; Mikelis V. Veidis; Inese Sarcevica; Andris Actins; Sergey Belyakov; Aleksandrs Platonenko

doi:10.1016/j.ijpharm.2012.04.061

The effect of pH on polymorph formation of the pharmaceutically active compound tianeptine

Liana Orola
, Mikelis V. Veidis^*
, Inese Sarcevica
, Andris Actins
, Sergey Belyakov
, Aleksandrs Platonenko

^*Šī darba korespondējošais autors

University of Latvia
Latvian Institute of Organic Synthesis

Zinātniskās darbības rezultāts: Devums žurnālam › Zinātniskais raksts (žurnālā) › koleģiāli recenzēts

20 Atsauces (Scopus)

Kopsavilkums

The anti-depressant pharmaceutical tianeptine has been investigated to determine the dynamics of polymorph formation under various pH conditions. By varying the pH two crystalline polymorphs were isolated. The molecular and crystal structures have been determined to identify the two polymorphs. One polymorph is an amino carboxylic acid and the other polymorph is a zwitterion. In the solid state the tianeptine moieties are bonded through hydrogen bonds. The zwitterion was found to be less stable and transformed to the acid form. During this investigation an amorphous form was identified.

Oriģinālvaloda	Angļu
Lapas (no-līdz)	50-56
Lapu skaits	7
Žurnāls	International Journal of Pharmaceutics
Sējums	432
Izdevuma numurs	1-2
DOIs	https://doi.org/10.1016/j.ijpharm.2012.04.061
Publikācijas statuss	Publicēts - 1 aug. 2012

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title = "The effect of pH on polymorph formation of the pharmaceutically active compound tianeptine",

abstract = "The anti-depressant pharmaceutical tianeptine has been investigated to determine the dynamics of polymorph formation under various pH conditions. By varying the pH two crystalline polymorphs were isolated. The molecular and crystal structures have been determined to identify the two polymorphs. One polymorph is an amino carboxylic acid and the other polymorph is a zwitterion. In the solid state the tianeptine moieties are bonded through hydrogen bonds. The zwitterion was found to be less stable and transformed to the acid form. During this investigation an amorphous form was identified.",

keywords = "Crystal structure, Crystallization, Polymorph, Tianeptine, X-ray diffractometry, pH",

author = "Liana Orola and Veidis, \{Mikelis V.\} and Inese Sarcevica and Andris Actins and Sergey Belyakov and Aleksandrs Platonenko",

year = "2012",

month = aug,

day = "1",

doi = "10.1016/j.ijpharm.2012.04.061",

language = "English",

volume = "432",

pages = "50--56",

journal = "International Journal of Pharmaceutics",

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TY - JOUR

T1 - The effect of pH on polymorph formation of the pharmaceutically active compound tianeptine

AU - Orola, Liana

AU - Veidis, Mikelis V.

AU - Sarcevica, Inese

AU - Actins, Andris

AU - Belyakov, Sergey

AU - Platonenko, Aleksandrs

PY - 2012/8/1

Y1 - 2012/8/1

N2 - The anti-depressant pharmaceutical tianeptine has been investigated to determine the dynamics of polymorph formation under various pH conditions. By varying the pH two crystalline polymorphs were isolated. The molecular and crystal structures have been determined to identify the two polymorphs. One polymorph is an amino carboxylic acid and the other polymorph is a zwitterion. In the solid state the tianeptine moieties are bonded through hydrogen bonds. The zwitterion was found to be less stable and transformed to the acid form. During this investigation an amorphous form was identified.

AB - The anti-depressant pharmaceutical tianeptine has been investigated to determine the dynamics of polymorph formation under various pH conditions. By varying the pH two crystalline polymorphs were isolated. The molecular and crystal structures have been determined to identify the two polymorphs. One polymorph is an amino carboxylic acid and the other polymorph is a zwitterion. In the solid state the tianeptine moieties are bonded through hydrogen bonds. The zwitterion was found to be less stable and transformed to the acid form. During this investigation an amorphous form was identified.

KW - Crystal structure

KW - Crystallization

KW - Polymorph

KW - Tianeptine

KW - X-ray diffractometry

KW - pH

UR - https://www.scopus.com/pages/publications/84861582679

U2 - 10.1016/j.ijpharm.2012.04.061

DO - 10.1016/j.ijpharm.2012.04.061

M3 - Article

C2 - 22569228

AN - SCOPUS:84861582679

SN - 0378-5173

VL - 432

SP - 50

EP - 56

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1-2

ER -

The effect of pH on polymorph formation of the pharmaceutically active compound tianeptine

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