Gabapentin Novel Co-Crystals: an Attempt to Enhance Physicochemical Parameters
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Published:15 Dec 2023
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Special Collection: 2023 ebook collection
R. Samineni, J. Chimakurthy, M. Billapati, S. B. Bodduluru, S. S. K. Kurra, and V. G. Madasu, in Current Trends in Drug Discovery, Development and Delivery (CTD4-2022), ed. M. Murahari, B. N. Nalluri, and G. Chakravarthi, Royal Society of Chemistry, 2023, vol. 358, pp. 400-413.
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Co-crystals are used to overcome the limitations of poor solubility and poor oral bioavailability of pharmaceuticals. The multiple components of co-crystals are interacting non-covalently with solvent where API properties are improved. The current research mainly focuses on formulating and evaluating Gabapentin (GBP) cocrystals with various coformers like L-Ascorbic acid and Acetyl salicylic acid. The current study of Novel co-crystals is prepared by using the co-grinding method in different stoichiometric ratios of 1:1 and 1:3. FTIR, PXRD, SEM, flow characteristics, inherent solubility, and in vitro dissolution are used to describe synthesized crystals. The FTIR analysis was interpreted that Gabapentin forms a hydrogen bond with the complimentary carboxyl groups of L-Ascorbic acid and Acetyl salicylic acid. PXRD analyses of GBP-L-ASC CF are showing a high degree of Crystallinity compared to other co-former Cocrystals. Flow properties for prepared Cocrystals are showing excellent while compared to pure drug. Particle size analysis by SEM revealed that 1:3 ratio prepared Cocrystals (GBP-ASA CF-2, and GBP-ASA CF-4) showed less size than 1:1 ratio prepared Cocrystals. GBP-ASA CF-2 and GBP-ASA CF-4 showed 44.63 folds and 59.12 folds increased solubility. The invitro dissolution test showed that GBP-ASA CF-4 and GBP-ASC CF-2 showed a higher dissolution rate (99.87%, and 97.84%) than pure Gabapentin. GBP-ASA CF-4 and GBP-ASC CF-2 showed modification in the chemical environment, intermolecular interactions were established, and improved flow properties with enhanced intrinsic solubility and invitro dissolution rate than a pure drug by decreasing Cocrystals particle size.