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 in | Molecules (Basel, Switzerland) Vol. 23; no. 7; p. 1719 |
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Main Authors | , , , , |
Format | Journal Article |
Language | English |
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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. |
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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 – name: 4 Department of Pharmaceutical Sciences, USF College of Pharmacy, Tampa, FL 33612, USA; vsutariya@health.usf.edu – 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 |
Author_xml | – sequence: 1 givenname: Deepak surname: Gupta fullname: Gupta, Deepak email: dgupta@lecom.edu organization: Department of Pharmaceutical Sciences, School of Pharmacy, Lake Erie College of Osteopathic Medicine, Bradenton, FL 34211, USA. dgupta@lecom.edu – sequence: 2 givenname: Deepak orcidid: 0000-0002-7243-2625 surname: Bhatia fullname: Bhatia, Deepak email: dbhatia@su.edu organization: ICPH Fairfax Bernard J. Dunn School of Pharmacy, Shenandoah University, Fairfax, VA 22031, USA. dbhatia@su.edu – sequence: 3 givenname: Vivek orcidid: 0000-0002-8074-758X surname: Dave fullname: Dave, Vivek email: vdave@sjfc.edu organization: Wegmans School of Pharmacy, St. John Fisher College, Rochester, NY 14618, USA. vdave@sjfc.edu – sequence: 4 givenname: Vijaykumar surname: Sutariya fullname: Sutariya, Vijaykumar email: vsutariya@health.usf.edu organization: Department of Pharmaceutical Sciences, USF College of Pharmacy, Tampa, FL 33612, USA. vsutariya@health.usf.edu – sequence: 5 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 |
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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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StartPage | 1719 |
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 |
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