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  1. Article ; Online: Modulation of biopharmaceutical properties of acidic drugs using cationic counterions: A critical analysis of FDA-approved pharmaceutical salts.

    Bharate, Sonali S

    International journal of pharmaceutics

    2021  Volume 607, Page(s) 120993

    Abstract: Salification has a successful track record in modulating the biopharmaceutical properties of drugs. This is evident from the significant share (40%) of pharmaceutical salts in FDA-approved drugs in the past 80-years. Based on the ionic nature of drugs, ... ...

    Abstract Salification has a successful track record in modulating the biopharmaceutical properties of drugs. This is evident from the significant share (40%) of pharmaceutical salts in FDA-approved drugs in the past 80-years. Based on the ionic nature of drugs, the corresponding cationic or anionic counterions are employed for salification. This review aims to provide the contribution of cationic counterions in FDA-approved drugs from 1939 to 2020. The analysis of 80-years data has shown that the 7.1% of the FDA-approved drugs comprise cationic counterions (98 pharmaceutical salts). Heparin sodium is the pioneering drug in the history of pharmaceutical salts that was approved in 1939 as an anticoagulant medication. Inorganic (sodium, calcium, potassium, magnesium, silver), as well as organic (tromethamine, meglumine, erbumine) cationic counterions, were used in FDA-approved drugs with a major share by sodium (76 drugs). The technical superiority of cationic salts over other salt forms and the parent drug is also exemplified using case studies.
    MeSH term(s) Biological Products ; Cations ; Pharmaceutical Preparations ; Salts ; Solubility
    Chemical Substances Biological Products ; Cations ; Pharmaceutical Preparations ; Salts
    Language English
    Publishing date 2021-08-12
    Publishing country Netherlands
    Document type Journal Article ; Review
    ZDB-ID 428962-6
    ISSN 1873-3476 ; 0378-5173
    ISSN (online) 1873-3476
    ISSN 0378-5173
    DOI 10.1016/j.ijpharm.2021.120993
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Carboxylic Acid Counterions in FDA-Approved Pharmaceutical Salts.

    Bharate, Sonali S

    Pharmaceutical research

    2021  Volume 38, Issue 8, Page(s) 1307–1326

    Abstract: Salification is one of the powerful and widely employed approaches to improve the biopharmaceutical properties of drugs. The FDA's eighty-year trajectory of new drug approvals depicts around one-third of the drugs clinically used as their pharmaceutical ... ...

    Abstract Salification is one of the powerful and widely employed approaches to improve the biopharmaceutical properties of drugs. The FDA's eighty-year trajectory of new drug approvals depicts around one-third of the drugs clinically used as their pharmaceutical salts. Among various cationic and anionic counterions used in FDA-approved pharmaceutical salts, the carboxylic acids have significantly contributed. A total of 94 pharmaceutical salts discovered during 1943-2020 comprises carboxylic acids as counterions with a major contribution of acetate, maleate, tartrate, fumarate, and succinate. Hydrocodone tartrate is the first FDA-approved carboxylate salt approved in 1943. Overall, the analysis shows that fifteen carboxylic acid counterions are present in FDA-approved pharmaceutical salts with a major share of acetate (18 drugs). This review provides an account of FDA-approved carboxylate salts from 1939 to 2020. The decade-wise analysis indicates that 1991-2000 contributed a maximum number of carboxylate salts (24) and least (3) in 1939-1950. The technical advantage of carboxylate salts over free-base or other counterions is also discussed. Graphical Abstract.
    MeSH term(s) Carboxylic Acids/chemistry ; Drug Approval ; Pharmaceutical Preparations/chemistry ; Salts/chemistry ; United States ; United States Food and Drug Administration
    Chemical Substances Carboxylic Acids ; Pharmaceutical Preparations ; Salts
    Language English
    Publishing date 2021-07-23
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 843063-9
    ISSN 1573-904X ; 0724-8741 ; 0739-0742
    ISSN (online) 1573-904X
    ISSN 0724-8741 ; 0739-0742
    DOI 10.1007/s11095-021-03080-2
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  3. Article ; Online: Critical Analysis of Drug Product Recalls due to Nitrosamine Impurities.

    Bharate, Sonali S

    Journal of medicinal chemistry

    2021  Volume 64, Issue 6, Page(s) 2923–2936

    Abstract: A product recall is the outcome of a careful pharmacovigilance; and it is an integral part of drug regulation. Among various reasons for product recall, the detection of unacceptable levels of carcinogenic impurities is one of the most serious concerns. ... ...

    Abstract A product recall is the outcome of a careful pharmacovigilance; and it is an integral part of drug regulation. Among various reasons for product recall, the detection of unacceptable levels of carcinogenic impurities is one of the most serious concerns. The genotoxic and carcinogenic potential of
    MeSH term(s) Carcinogens/analysis ; Drug Contamination/prevention & control ; Drug Industry ; Drug Recalls ; Humans ; Nitrosamines/analysis ; Pharmaceutical Preparations/chemistry ; United States ; United States Food and Drug Administration
    Chemical Substances Carcinogens ; Nitrosamines ; Pharmaceutical Preparations
    Language English
    Publishing date 2021-03-11
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.0c02120
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  4. Article ; Online: Enhancing Biopharmaceutical Attributes of Khellin by Amorphous Binary Solid Dispersions.

    Bharate, Sonali S

    AAPS PharmSciTech

    2021  Volume 22, Issue 8, Page(s) 260

    Abstract: Khellin, a furanochromone isolated from fruits and seeds of Ammi visnaga, is traditionally used in many eastern Mediterranean countries. The plant decoction and the crystalline substance khellin have many pharmacological activities. For instance, it acts ...

    Abstract Khellin, a furanochromone isolated from fruits and seeds of Ammi visnaga, is traditionally used in many eastern Mediterranean countries. The plant decoction and the crystalline substance khellin have many pharmacological activities. For instance, it acts as a bronchodilator and also relieves renal colic and urethral stones, etc. However, the low water solubility (~ 120 µg/mL) and low bioavailability limit its therapeutic application. Thus, the present research explores the development of its binary and ternary solid dispersion formulations to improve its solubility and dissolution behavior. A 24-well plate miniaturized protocol was established to identify the optimal hydrophilic polymer to prepare its solid dispersions. PEG-4000 was recognized as the favorable hydrophilic carrier in preparation of solid dispersion, SSB17. The formulation displayed ~ five-fold enhancement in the aqueous solubility of khellin. The binary solid dispersion SSB17 was manufactured at a gram scale and evaluated using
    MeSH term(s) Biological Products ; Chemistry, Pharmaceutical ; Khellin ; Solubility ; Spectroscopy, Fourier Transform Infrared
    Chemical Substances Biological Products ; Khellin (5G117T0TJZ)
    Language English
    Publishing date 2021-10-27
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2052070-0
    ISSN 1530-9932 ; 1530-9932
    ISSN (online) 1530-9932
    ISSN 1530-9932
    DOI 10.1208/s12249-021-02126-3
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019.

    Bharate, Sonali S

    Drug discovery today

    2020  Volume 26, Issue 2, Page(s) 384–398

    Abstract: Around half of the new molecular entities approved by the US Food and Drug Administration (FDA) are pharmaceutical salts. The pharmaceutical salts have been on a continuous growth trajectory since the approval of the first salt form in 1939. This review ... ...

    Abstract Around half of the new molecular entities approved by the US Food and Drug Administration (FDA) are pharmaceutical salts. The pharmaceutical salts have been on a continuous growth trajectory since the approval of the first salt form in 1939. This review aims to provide updates on pharmaceutical salts approved by the FDA between 2015 and 2019. The five-year drug-approval database contains 61 pharmaceutical salts, featuring a diverse range of counterions; however, hydrochlorides are the most abundant. The chemical structures of all pharmaceutical salts in each class are presented here, along with their therapeutic indications and date of approval. The reason behind the selection of a particular counterion and the technical superiority achieved by the salt form over the free active pharmaceutical ingredient base are also discussed.
    MeSH term(s) Animals ; Databases, Pharmaceutical ; Drug Approval ; Humans ; Pharmaceutical Preparations/chemistry ; Salts/chemistry ; United States ; United States Food and Drug Administration
    Chemical Substances Pharmaceutical Preparations ; Salts
    Language English
    Publishing date 2020-11-19
    Publishing country England
    Document type Comparative Study ; Journal Article ; Review
    ZDB-ID 1324988-5
    ISSN 1878-5832 ; 1359-6446
    ISSN (online) 1878-5832
    ISSN 1359-6446
    DOI 10.1016/j.drudis.2020.11.016
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    Zs.A 4725: Show issues Location:
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  6. Article: Estimating thermodynamic equilibrium solubility and solute-solvent interactions of niclosamide in eight mono-solvents at different temperatures.

    Bhanushali, Jigar S / Bharate, Sonali S

    Journal of molecular liquids

    2022  Volume 367, Page(s) 120359

    Abstract: Niclosamide is an FDA-approved oral anthelmintic drug currently being repurposed for COVID-19 infection. Its interesting applicability in multiple therapeutic indications has sparked interest in this drug/ scaffold. Despite its therapeutic use for ... ...

    Abstract Niclosamide is an FDA-approved oral anthelmintic drug currently being repurposed for COVID-19 infection. Its interesting applicability in multiple therapeutic indications has sparked interest in this drug/ scaffold. Despite its therapeutic use for several years, its detailed solubility information from Chemistry Manufacturing & Controls perspective is unavailable. Thus, the present study is intended to determine the mole fraction solubility of niclosamide in commonly used solvents and cosolvents at a temperature range of 298.15-323.15 K. The polymorphic changes from crystalline to monohydrate forms post-equilibration in various solvents were observed. The maximum mole fraction solubility of niclosamide at 323.15 K is 1.103 × 10
    Language English
    Publishing date 2022-09-16
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1491496-7
    ISSN 1873-3166 ; 0167-7322
    ISSN (online) 1873-3166
    ISSN 0167-7322
    DOI 10.1016/j.molliq.2022.120359
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  7. Article ; Online: Analytical Methods for Furanochromone Natural Product, Khellin and Its Inspired Drug Candidates, Amiodarone and Sodium Cromoglycate.

    Shah, Raj P / Bharate, Sonali S

    Critical reviews in analytical chemistry

    2022  , Page(s) 1–16

    Abstract: Khellin is the key furanocoumarin ... ...

    Abstract Khellin is the key furanocoumarin of
    Language English
    Publishing date 2022-07-01
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 2030019-0
    ISSN 1547-6510 ; 1040-8347
    ISSN (online) 1547-6510
    ISSN 1040-8347
    DOI 10.1080/10408347.2022.2094198
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  8. Article ; Online: Techniques for analytical estimation of COVID-19 clinical candidate, niclosamide in pharmaceutical and biomedical samples.

    Gupta, Deepank S / Bharate, Sonali S

    Separation science plus

    2022  

    Abstract: Niclosamide is a well-known broad-spectrum antiparasitic drug used for human as well as veterinary tapeworm infections. Recently, it attracted attention as an antiviral agent for treating coronavirus disease 2019. It is administered orally in humans to ... ...

    Abstract Niclosamide is a well-known broad-spectrum antiparasitic drug used for human as well as veterinary tapeworm infections. Recently, it attracted attention as an antiviral agent for treating coronavirus disease 2019. It is administered orally in humans to treat tapeworm infections. Furthermore, it is a registered pesticide and molluscicide to control infections in the aquaculture industry. Its chronic environmental exposure has potential toxicities when such contaminated seafood is consumed. Therefore, monitoring its residual concentration in food products (seafood, water, water waste, etc.) and pharmaceuticals (active pharmaceutical ingredients, bulk drugs, and formulations) is imperative. The present review critically investigates the sophisticated techniques employed for analyzing niclosamide, its degradation products, and metabolites in various samples and matrices. The future scope for green analytical methods, green sample extraction and preparation is also deliberated.
    Language English
    Publishing date 2022-09-08
    Publishing country Germany
    Document type Journal Article ; Review
    ISSN 2573-1815
    ISSN (online) 2573-1815
    DOI 10.1002/sscp.202200097
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  9. Article ; Online: Phosphate moiety in FDA-approved pharmaceutical salts and prodrugs.

    Fulmali, Ameya / Bharate, Sonali S

    Drug development research

    2022  Volume 83, Issue 5, Page(s) 1059–1074

    Abstract: The salification and prodrug approaches modulate the physicochemical properties and absorption, distribution, metabolism, excretion, and toxicity parameters of drugs and lead candidates. The "phosphate" is one of the key counterions/promoiety used in the ...

    Abstract The salification and prodrug approaches modulate the physicochemical properties and absorption, distribution, metabolism, excretion, and toxicity parameters of drugs and lead candidates. The "phosphate" is one of the key counterions/promoiety used in the salt formation and prodrug synthesis. Salification with phosphoric acid enhances the aqueous solubility and thereby facilitates the administration of a drug by the parenteral route. Phosphate moiety in prodrug synthesis mainly improves permeability by lipophilic substitution. Histamine phosphate is the first phosphate salt, and hydrocortisone phosphate was the first prodrug approved by FDA in 1939 and 1952, respectively. The orange book enlists 12 phosphate salts and 17 phosphate prodrugs. Phosphate prodrugs, namely combretastatin A-4 diphosphate, combretastatin A-4 phosphate, lufotrelvir, TP-1287, pyridoxal phosphate, riboflavin phosphate, and psilocybin are clinical candidates. This review focuses on the FDA-approved phosphate salts and prodrugs from 1939 to 2021. The biopharmaceutical advantage of phosphate salts and prodrugs over the parent molecule is also deliberated.
    MeSH term(s) Indoles ; Leucine ; Phosphates ; Prodrugs/chemistry ; Pyrrolidinones ; Salts ; Solubility
    Chemical Substances Indoles ; Phosphates ; Prodrugs ; Pyrrolidinones ; Salts ; Leucine (GMW67QNF9C) ; lufotrelvir (XJ51YOB1SC)
    Language English
    Publishing date 2022-06-02
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 604587-x
    ISSN 1098-2299 ; 0272-4391
    ISSN (online) 1098-2299
    ISSN 0272-4391
    DOI 10.1002/ddr.21953
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    Zs.B 2542: Show issues Location:
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  10. Article ; Online: Recent developments in the management of Huntington's disease.

    Devadiga, Shanaika J / Bharate, Sonali S

    Bioorganic chemistry

    2022  Volume 120, Page(s) 105642

    Abstract: Huntington's disease (HD) is a rare, incurable, inheritedneurodegenerative disorder manifested by chorea, hyperkinetic, and hypokinetic movements. The FDA has approved only two drugs, viz. tetrabenazine, and deutetrabenazine, to manage the chorea ... ...

    Abstract Huntington's disease (HD) is a rare, incurable, inheritedneurodegenerative disorder manifested by chorea, hyperkinetic, and hypokinetic movements. The FDA has approved only two drugs, viz. tetrabenazine, and deutetrabenazine, to manage the chorea associated with HD. However, several other drugs are used as an off-label to manage chorea and other symptoms such as depression, anxiety, muscle tremors, and cognitive dysfunction associated with HD. So far, there is no disease-modifying treatment available. Drug repurposing has been a primary drive to search for new anti-HD drugs. Numerous molecular targets along with a wide range of small molecules and gene therapies are currently under clinical investigation. More than 200 clinical studies are underway for HD, 75% are interventional, and 25% are observational studies. The present review discusses the small molecule clinical pipeline and molecular targets for HD. Furthermore, the biomarkers, diagnostic tests, gene therapies, behavioral and observational studies for HD were also deliberated.
    MeSH term(s) Anxiety ; Chorea/drug therapy ; Humans ; Huntington Disease/drug therapy ; Tetrabenazine/therapeutic use
    Chemical Substances Tetrabenazine (Z9O08YRN8O)
    Language English
    Publishing date 2022-01-30
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2022.105642
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