Salts of Therapeutic Agents: Chemical, Physicochemical, and Biological Considerations

The physicochemical and biological properties of active pharmaceutical ingredients (APIs) are greatly affected by their salt forms. The choice of a particular salt formulation is based on numerous factors such as API chemistry, intended dosage form, pharmacokinetics, and pharmacodynamics. The approp...

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Published inMolecules (Basel, Switzerland) Vol. 23; no. 7; p. 1719
Main Authors Gupta, Deepak, Bhatia, Deepak, Dave, Vivek, Sutariya, Vijaykumar, Varghese Gupta, Sheeba
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 14.07.2018
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Abstract The physicochemical and biological properties of active pharmaceutical ingredients (APIs) are greatly affected by their salt forms. The choice of a particular salt formulation is based on numerous factors such as API chemistry, intended dosage form, pharmacokinetics, and pharmacodynamics. The appropriate salt can improve the overall therapeutic and pharmaceutical effects of an API. However, the incorrect salt form can have the opposite effect, and can be quite detrimental for overall drug development. This review summarizes several criteria for choosing the appropriate salt forms, along with the effects of salt forms on the pharmaceutical properties of APIs. In addition to a comprehensive review of the selection criteria, this review also gives a brief historic perspective of the salt selection processes.
AbstractList The physicochemical and biological properties of active pharmaceutical ingredients (APIs) are greatly affected by their salt forms. The choice of a particular salt formulation is based on numerous factors such as API chemistry, intended dosage form, pharmacokinetics, and pharmacodynamics. The appropriate salt can improve the overall therapeutic and pharmaceutical effects of an API. However, the incorrect salt form can have the opposite effect, and can be quite detrimental for overall drug development. This review summarizes several criteria for choosing the appropriate salt forms, along with the effects of salt forms on the pharmaceutical properties of APIs. In addition to a comprehensive review of the selection criteria, this review also gives a brief historic perspective of the salt selection processes.
Author Bhatia, Deepak
Sutariya, Vijaykumar
Varghese Gupta, Sheeba
Dave, Vivek
Gupta, Deepak
AuthorAffiliation 3 Wegmans School of Pharmacy, St. John Fisher College, Rochester, NY 14618, USA; vdave@sjfc.edu
1 Department of Pharmaceutical Sciences, School of Pharmacy, Lake Erie College of Osteopathic Medicine, Bradenton, FL 34211, USA; dgupta@lecom.edu
2 ICPH Fairfax Bernard J. Dunn School of Pharmacy, Shenandoah University, Fairfax, VA 22031, USA; dbhatia@su.edu
4 Department of Pharmaceutical Sciences, USF College of Pharmacy, Tampa, FL 33612, USA; vsutariya@health.usf.edu
AuthorAffiliation_xml – name: 3 Wegmans School of Pharmacy, St. John Fisher College, Rochester, NY 14618, USA; vdave@sjfc.edu
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– name: 2 ICPH Fairfax Bernard J. Dunn School of Pharmacy, Shenandoah University, Fairfax, VA 22031, USA; dbhatia@su.edu
– name: 1 Department of Pharmaceutical Sciences, School of Pharmacy, Lake Erie College of Osteopathic Medicine, Bradenton, FL 34211, USA; dgupta@lecom.edu
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  orcidid: 0000-0002-7243-2625
  surname: Bhatia
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  surname: Dave
  fullname: Dave, Vivek
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  organization: Wegmans School of Pharmacy, St. John Fisher College, Rochester, NY 14618, USA. vdave@sjfc.edu
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  givenname: Vijaykumar
  surname: Sutariya
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  givenname: Sheeba
  surname: Varghese Gupta
  fullname: Varghese Gupta, Sheeba
  email: svarghes@health.usf.edu
  organization: Department of Pharmaceutical Sciences, USF College of Pharmacy, Tampa, FL 33612, USA. svarghes@health.usf.edu
BackLink https://www.ncbi.nlm.nih.gov/pubmed/30011904$$D View this record in MEDLINE/PubMed
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Keywords chemistry
salt
degradation
routes of administration
water solubility
physicochemical
stability
Language English
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Snippet The physicochemical and biological properties of active pharmaceutical ingredients (APIs) are greatly affected by their salt forms. The choice of a particular...
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SubjectTerms Biological properties
Chemical compounds
chemistry
degradation
Drug development
Organic chemistry
Pharmaceuticals
Pharmacodynamics
Pharmacokinetics
Pharmacology
physicochemical
Review
Reviews
routes of administration
salt
Salts
stability
water solubility
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Title Salts of Therapeutic Agents: Chemical, Physicochemical, and Biological Considerations
URI https://www.ncbi.nlm.nih.gov/pubmed/30011904
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Volume 23
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