Investigation of the influence of cellulose polymer on solid phase transformation of carbamazepine

Investigation of the influence of cellulose polymer on solid phase transformation of carbamazepine

•The solubility of Carbamazepine anhydrous forms decreases when they convert to dihydrate.•The anhydrous form converts to Carbamazepine dihydrate via solution mediated mechanism.•HPMC inhibits the transformation of carbamazepine Anhydrous to dihydrate in the gel layer of hydrated tablets. Crystallin...

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Bibliographic Details
Published in:Journal of crystal growth Vol. 575; p. 126358
Main Authors: Wadher, Kamlesh J., Bajaj, Girija S., Trivedi, Rashmi V., Trivedi, Sagar S., Umekar, Milind J.
Format: Journal Article
Language:English
Published: Amsterdam Elsevier B.V 01-12-2021
Elsevier BV
Subjects:
Aqueous solutions
Carbamazepine
Crystal growth
Fourier transforms
Gel layer
HPMC K4M
Infrared spectrophotometers
Manufacturing
Phase transformations
Phase transitions
Polymers
Premixing
Solid phases
Solid state
Crystal growth
Gel layer
Phase transformations
Carbamazepine
HPMC K4M
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Summary:•The solubility of Carbamazepine anhydrous forms decreases when they convert to dihydrate.•The anhydrous form converts to Carbamazepine dihydrate via solution mediated mechanism.•HPMC inhibits the transformation of carbamazepine Anhydrous to dihydrate in the gel layer of hydrated tablets. Crystalline anhydrous drugs can get potentially transformed in to the hydrate form during manufacturing processes that involve water. To control the solid-state form of the drug it is important to understand the process of manipulating these transformations. The use of polymers to inhibit solid state transformations is an imperative concept in drug delivery. Recently tremendous investigation is going on using various polymers to prevent the anhydrate to hydrate transformation during manufacturing. The aim of this work was to investigate the influence of specific ratio of hydroxypropyl methylcellulose K 4 M on the phase transformation and release profile of carbamazepine. The surface topography of the crystal for assessing the crystal habit was done using scanning electron microscope, Fourier Transform Infrared Spectrophotometer and differential scanning calorimetry. Powder dissolution profile concluded that anhydrate exhibited significantly higher dissolutionrate. HPMC K4 M was found to inhibit the transformation of carbamazepine to carbamazepine dihydrate in the gel layer of hydrated tablets and in aqueous solutions. Upon exposure to aqueous medium, the anhydrateform rapidly converts to the dihydrate. However, premixing ofanhydrate with HPMC K4M in specific ratio, in the presence of water exhibited inhibition of the solution mediated phase transformation of carbamazepine anhydrate to dihydrate.
ISSN:0022-0248
1873-5002
DOI:10.1016/j.jcrysgro.2021.126358