Salts of Therapeutic Agents: Chemical, Physicochemical and Biological Considerations

Gupta, Divender; Bhatia, Deepak; Dave, Vivek S; Sutariya, Vijaykumar; Gupta, Sheeba Varghese

doi:10.20944/preprints201804.0187.v1

Cited by 34 publications

(1 citation statement)

References 13 publications

(13 reference statements)

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“…At present, fifty percent of the drugs approvals issued by the United States Food and Drug Administration (US FDA) involve pharmaceutical ingredients formulated as salts, and the same percentage of the top 200 prescription drugs consists of pharmaceutical salts [46]. In particular, sodium is among the most commonly preferred cations utilized in oral or parenteral formulations, as well as in topical products [46]. Moreover, 95% of the existing medications for ophthalmic infections are comprised of eye drops and hydrophilic drugs.…”

Section: Discussionmentioning

confidence: 99%

Tetracycline: structural characterization and antimicrobial properties of its water-soluble di-anionic bi-sodium salt

Tsigara,

Banti,

Hatzidimitriou

et al. 2024

Dalton Trans.

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Section: Discussionmentioning

confidence: 99%

Tetracycline: structural characterization and antimicrobial properties of its water-soluble di-anionic bi-sodium salt

Tsigara,

Banti,

Hatzidimitriou

et al. 2024

Dalton Trans.

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Multimodal Role of Amino Acids in Microbial Control and Drug Development

et al. 2020

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Amino acids are ubiquitous vital biomolecules found in all kinds of living organisms including those in the microbial world. They are utilised as nutrients and control many biological functions in microorganisms such as cell division, cell wall formation, cell growth and metabolism, intermicrobial communication (quorum sensing), and microbial-host interactions. Amino acids in the form of enzymes also play a key role in enabling microbes to resist antimicrobial drugs. Antimicrobial resistance (AMR) and microbial biofilms are posing a great threat to the world’s human and animal population and are of prime concern to scientists and medical professionals. Although amino acids play an important role in the development of microbial resistance, they also offer a solution to the very same problem i.e., amino acids have been used to develop antimicrobial peptides as they are highly effective and less prone to microbial resistance. Other important applications of amino acids include their role as anti-biofilm agents, drug excipients, drug solubility enhancers, and drug adjuvants. This review aims to explore the emerging paradigm of amino acids as potential therapeutic moieties.

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AG1®, a Novel Synbiotic, Demonstrates Superior Mineral Bioaccessibility and Bioavailability Compared to a Tablet Multivitamin and Mineral Supplement Using an In Vitro Model of the Upper Gastrointestinal Tract

Sapp,

Townsend,

Kirby

et al. 2023

Applied Biosciences

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While traditional multivitamin and mineral (MVM) supplements generally come in tablet form, new powder forms of MVM supplements are available with theoretically higher bioavailability relative to tablet MVM supplements. The purpose of this study was to assess the bioaccessibility and bioavailability of minerals (magnesium (Mg), zinc (Zn), calcium (Ca), and potassium (K)) in a tablet MVM supplement compared to a novel powder Foundational Nutrition supplement (AG1®), containing minerals, vitamins, phytochemicals, and pre-/probiotics, in the upper gastrointestinal tract. The tablet MVM supplement was specifically formulated for this study, with matched mineral contents and identical chemical structures. The adapted Simulator of the Human Intestinal Microbial Ecosystem (SHIME®) model was used to assess the bioaccessibility and bioavailability of soluble minerals using a simulated upper gastrointestinal tract and dialysis membrane to mimic human digestion and absorption. The bioaccessibility was assessed at the end of the stomach and duodenum. The bioaccessibility and bioavailability were assessed at 1, 2, and 3 h following dialysis. The preliminary soluble mineral analysis of the tablet (crushed to a powder) and AG1 powder demonstrated significantly higher (p < 0.05) soluble fractions of Zn and Ca, but lower Mg in the AG1 powder vs. the tablet. The total soluble mineral percentages at the stomach and duodenum end were all significantly higher for the AG1 powder vs. the tablet (p < 0.05). Mg, Ca, and Zn were more (p < 0.05) bioaccessible and bioavailable in the powder compared to the tablet during the small intestine simulation. The bioaccessible fraction of K was higher (p < 0.05) only at 3 h for the tablet vs. the powder. These preclinical data demonstrate that the AG1 powder has superior dissolution and disintegration characteristics compared to the tablet, leading to increased bioaccessibility and bioavailability in vitro.

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Salts of Therapeutic Agents: Chemical, Physicochemical and Biological Considerations

Cited by 34 publications

References 13 publications

Tetracycline: structural characterization and antimicrobial properties of its water-soluble di-anionic bi-sodium salt

Tetracycline: structural characterization and antimicrobial properties of its water-soluble di-anionic bi-sodium salt

Multimodal Role of Amino Acids in Microbial Control and Drug Development

AG1®, a Novel Synbiotic, Demonstrates Superior Mineral Bioaccessibility and Bioavailability Compared to a Tablet Multivitamin and Mineral Supplement Using an In Vitro Model of the Upper Gastrointestinal Tract

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