The Development of Glibenclamide-Saccharin Cocrystal Tablet Formulations to Increase the Dissolution Rate of the Drug

Budiman, Arif; Husni, Patihul; Shafira,; Alfauziah, Tazyinul Qoriah

doi:10.22159/ijap.2019v11i4.33802

Cited by 11 publications

(9 citation statements)

References 14 publications

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“…These are indicative of good granule flow property for the BM leaf extract and all excipients. [ 13 ]…”

Section: R Esult and Discussionmentioning

confidence: 99%

“…The granules consisting of BM leaf extract and excipient were evaluated using flow properties, determined with angle of repose and compressibility parameters by Carr’s index, as well as tapped and bulk density. [ 12 13 ]…”

Section: Aterials and M Ethodsmentioning

confidence: 99%

“…Also, 20 tablets were individually weighed using an electronic balance, and the values obtained were compared to the average tablet weight, and the results presented as mean ± standard deviation (SD). [ 13 ]…”

Section: Aterials and M Ethodsmentioning

confidence: 99%

“…These were subsequently brushed and reweighed, and then the percent of weight loss was calculated using the formula: % friability = ([initial weight – final weight]/initial weight) × 100. [ 13 ]…”

Section: Aterials and M Ethodsmentioning

confidence: 99%

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The formulation of lozenge using black mulberries (Morus nigra L.) leaf extract as an α-glucosidase inhibitor

et al. 2020

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A BSTRACT Background: Diabetes mellitus is a chronic metabolic disease, which possibly leads to kidney, brain, heart failure, and other organ complications, subsequently harming human health. These symptoms have been prevented using the leaf of black mulberry (BM), as a traditional medicine, because the phenolic compounds contained are able to decrease blood glucose concentration. Meanwhile, previous reports have shown that BM contains 1-deoxynojirimycin, with strong activity as an α-glucosidase inhibitor. The aim of this study, therefore, was to formulate and evaluate BM leaf extract in lozenge dosage form as an α-glucosidase inhibitor. Materials and Methods: The leaves of BM were extracted using the maceration method, where ethanol (70%) served as a solvent, and the inhibitory activity of the sourced α-glucosidase enzyme was determined through in vitro study. Subsequently, the extract was formulated into lozenge dosage form and evaluated for physical stability and also the effect of α-glucosidase enzyme. Results: The result showed an inhibitory activity of BM leaf extract against the enzyme α-glucosidase, with a half maximal inhibitory concentration (IC 50 ) value of 357.6 μg/mL, whereas the lozenge formulation containing 43% of extract as well as 5% polyvinylpyrrolidone showed the best physical stability as compared to other formulas. However, the lozenge inhibits α-glucosidase enzyme with an IC 50 value of 549.7 μg/mL. Conclusion: It was established that the lozenge of BM leaf extract possesses activity as an α-glucosidase inhibitor.

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“…These are indicative of good granule flow property for the BM leaf extract and all excipients. [ 13 ]…”

Section: R Esult and Discussionmentioning

confidence: 99%

Section: Aterials and M Ethodsmentioning

confidence: 99%

Section: Aterials and M Ethodsmentioning

confidence: 99%

Section: Aterials and M Ethodsmentioning

confidence: 99%

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The formulation of lozenge using black mulberries (Morus nigra L.) leaf extract as an α-glucosidase inhibitor

et al. 2020

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“…The distinct and novel peaks in the FT-IR spectra of cocrystals were indicative of the formation of new intermolecular hydrogen bonding. FT-IR spectrums of cocrystals were recorded on a Perkin Elmer FT-IR spectrophotometer (USA) using the KBr pellet method in the spectral range 4000-500 cm -1 with a resolution of 2 cm -1 Scanning electron microscopy [40].…”

Section: Fourier Transform Infrared Spectroscopymentioning

confidence: 99%

Enhancement of Solubility and Dissolution Rate of Acetylsalicylic Acid via Co-Crystallization Technique: A Novel Asa-Valine Cocrystal

et al. 2021

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Objective: This study aims to synthesize acetylsalicylic acid (ASA) cocrystals using valine as a coformer via a co-crystallization technique to increase the solubility and dissolution rate of ASA. Methods: The ASA-valine cocrystal (1:1 molar ratio) was prepared using the solvent evaporation technique with ethanol: water (50:50). The cocrystal was characterized using Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), melting point to confirm the formation of cocrystal. The evaluation of cocrystal was done by drug content determination, solubility and dissolution studies. Results: The prepared cocrystal was successfully confirmed for the formation of a hydrogen bond. The melting point of prepared cocrystal was decreased compared to pure ASA and valine, which indicated the formation of a new crystalline form. The FT-IR studies showed the formation of a new hydrogen bond by shifting the-O-H,-C=O and-N-H functional groups. SEM studies ensured that the prepared cocrystals were in needle-like appearance. Finally, DSC and PXRD studies were also indicated the successful formation of ASA-valine cocrystal. The drug release of cocrystal was found to be 100% at 60th min. Where in the case of pure ASA and marketed product of ASA exhibited the dissolution rate of 59% and 69% at 60th min respectively. Conclusion: The co-crystallization technique can be adopted as the best strategy to increase the solubility and dissolution rate of BCS class 2 drugs. Therefore the prepared ASA-valine cocrystal can be a greater alternative to increase the solubility and dissolution rate compared with pure and marketed ASA.

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Norfloxacin Cocrystals: Mechanochemical Synthesis and Scale-up Viability Through Solubility Studies

Ferreira¹,

Almeida²,

Costa³

et al. 2023

Journal of Pharmaceutical Sciences

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The Development of Glibenclamide-Saccharin Cocrystal Tablet Formulations to Increase the Dissolution Rate of the Drug

Cited by 11 publications

References 14 publications

The formulation of lozenge using black mulberries (Morus nigra L.) leaf extract as an α-glucosidase inhibitor

The formulation of lozenge using black mulberries (Morus nigra L.) leaf extract as an α-glucosidase inhibitor

Enhancement of Solubility and Dissolution Rate of Acetylsalicylic Acid via Co-Crystallization Technique: A Novel Asa-Valine Cocrystal

Norfloxacin Cocrystals: Mechanochemical Synthesis and Scale-up Viability Through Solubility Studies

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