2020
DOI: 10.1021/acsomega.0c00692
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Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid

Abstract: BBC is a drug with a variety of activities but poor solubility. Cocrystal technology is an effective method to improve the solubility and stability of this type of compound. In this work, the cocrystal of BBC with fumaric acid was obtained at a stoichiometric ratio of 2:1. Studies on stabilities and solubilities were carried out using BBC dihydrate and tetrahydrate as reference materials. Results showed that this new cocrystal did not only significantly improve the dissolution rate of BBC but also highly impro… Show more

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Cited by 57 publications
(49 citation statements)
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“…For decades, the multicomponent solid structure has been developed widely as the primary strategy to modulate the performance of active pharmaceutical ingredients (API) [ 1 ]. The combination compound may involve ionic and nonionic bonding [ 2 , 3 ], which, in some cases, are tailored for a particular purpose, such as increased solubility and stability [ 3 , 4 ], also improving the unpleasant taste [ 5 ].…”
Section: Introductionmentioning
confidence: 99%
“…For decades, the multicomponent solid structure has been developed widely as the primary strategy to modulate the performance of active pharmaceutical ingredients (API) [ 1 ]. The combination compound may involve ionic and nonionic bonding [ 2 , 3 ], which, in some cases, are tailored for a particular purpose, such as increased solubility and stability [ 3 , 4 ], also improving the unpleasant taste [ 5 ].…”
Section: Introductionmentioning
confidence: 99%
“…4−8 The efficient delivery of BCl needs to overcome several problems, including (1) low aqueous dissolution, 9,10 (2) bitter taste, 11 and (3) sensitivity of water content to variations in environment humidity and temperature due to phase change among anhydrates, dihydrates, and tetrahydrates. 12 If not overcome, its low aqueous dissolution can lead to poor and highly variable bioavailability. The bitter taste must be masked to improve patient compliance for oral delivery.…”
Section: Introductionmentioning
confidence: 99%
“…From a biological standpoint, solubility determines the concentration of the API in systemic circulation so it must be fine-tuned for achieving the required pharmacological response . From an engineering perspective, solubility curves are necessary for any crystallization process design and development. , Thus, several studies have been devoted to improving API solubility via cocrystallization with a coformer (CF) as well as finding the region in the phase diagram that favors cocrystal formation. For instance, Darwish et al have successfully prepared a new 1:1 theophylline–aspirin cocrystal and then constructed the ternary phase diagram (TPD) to identify stable regions for cocrystal formation …”
Section: Introductionmentioning
confidence: 99%