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Gabapentin Novel Co-Crystals: an Attempt to Enhance Physicochemical Parameters

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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.
Title: Gabapentin Novel Co-Crystals: an Attempt to Enhance Physicochemical Parameters
Description:
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.

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