The Utility of Sulfonate Salts in Drug Development

Elder, David; Delaney, Ed; Teasdale, Andrew; Eyley, Stephen C.; Reif, Van D.; Jacq, Karine; Facchine, Kevin L.; Oestrich, Rolf Schulte; Sandra, Patrick; David, Frank

doi:10.1002/jps.22058

Cited by 95 publications

(67 citation statements)

References 40 publications

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“…This value was found to be about 70-fold higher than the TTC level of 1.5 µg/day currently applied to EMS based on the generic linear back extrapolation model for genotoxins acting via non-threshold mechanisms. Other literatures highlighted this conservative limit as well (Gocke et al, 2009b;Elder et al, 2010a;Snodin, 2010). In addition, Gocke et al (2009b) reported that the accidental exposure of viracept patients did not result in an increased likelihood for adverse genotoxic, teratogenic or cancerogenic effects.…”

Section: Resultsmentioning

confidence: 99%

“…Sulfonic acid salts tend to be an exception to this rule, since they exhibit both high melting points as well as good solubility. In addition, as mentioned in the literature, the high solubility and high surface area of haloperidol mesylate result in enhanced dissolution rates (<2 min in pH 2 simulated gastric media), which are more rapid than the competing common ion formation (Elder and Snodin, 2009;Elder et al, 2010a). On the other hand, sulfonic acids can react with low molecular weight alcohols such as methanol, ethanol, or isopropanol to form the corresponding sulfonate esters.…”

Section: Genotoxic Impurities (Gis)mentioning

confidence: 92%

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Genotoxic Impurities in Pharmaceuticals

Jouyban¹,

Parsa²

2012

Toxicity and Drug Testing

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Section: Resultsmentioning

confidence: 99%

Section: Genotoxic Impurities (Gis)mentioning

confidence: 92%

Genotoxic Impurities in Pharmaceuticals

Jouyban¹,

Parsa²

2012

Toxicity and Drug Testing

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“…The process of ion exchange leads to a condition of equilibrium. 9,10,11 In this present study sulfonic acid counter ions are analyzed by anion ion chromatography, the developed method was simple, rapid, and accurate for analysis of counter ions from API's salts of doxazosin, amlodipine and clopidogrel.…”

Section: Introductionmentioning

confidence: 84%

“…Quantitative determinations of counter ions (salts) very important aspect in drug development. 1,2,3,8 Classical titration methods are not much accurate compared to instrumental techniques and are subjective for end point observations. So it has become necessary to quantify the counter ions with more accuracy and more precision then existing analytical methods.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2016

IJPSR

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ABSTRACT:The present paper deals with the analysis of methane sulfonic acid, benzene sulfonic acid and camphor sulfonic acid counter anions in pharmaceutical ingredients (doxazosin mesylate, amlodipine besylate and clopidogrel camphor sulfonate) by suppressed conductivity anion chromatography. The diluent used for the preparation of sample solution was Milli-Q Water and injected into a standard chromatographic system connected with 250 mm length, 4.0 mm ID, 5.0 µm particle size, Metrosep A Supp1 column and suppressed conductivity detector. The developed analytical method was highly precise and accurate compared to titration methods and HPLC-UV detection methods to analyze counter ions in drug substance. Calibration curves were linear with correlation coefficient of > 0.999 for anions. The % RSD of area response of anions in standard injections was below 2.0, which demonstrates the method precision of the test procedure. The accuracy of the method was also studied and observed between 97% and 102%. The developed method was validated according to ICH guidelines for the quantitative determination of anions in API taken for the study.

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“…Various strategies to solubilize water-insoluble drugs have been tried, which include using cosolvent (Malick et al, 2007) or surfactants (Strickley, 2004), solid dispersion (Janssens and Van den Mooter, 2009), inclusion complex ( Van de Manakker et al, 2009), salt formation (Elder et al, 2010) or colloidal systems such as microemulsion (He et al, 2010), micelles (Trivedi et al, 2010), polymeric nano-/micro-particles (Kumari et. al, 2009 ), liposomes (Cukierman and Khan, 2010), emulsions (Mirtallo et al, 2010) and solid lipid nanoparticles (SLNs) (Souto and Müller, 2010).…”

mentioning

confidence: 99%

Solid Lipid Nanoparticles as Drug Delivery System for Water-Insoluble Drugs

Li¹,

Lim²,

Choi³

et al. 2010

Journal of Pharmaceutical Investigation

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− Solid lipid nanoparticles (SLNs) have emerged to combine the advantages of polymeric nanoparticles and lipid emulsions in early 1990s. SLNs can present several desirable properties derived from the solid state core. When formulating SLNs, there should be careful considerations about the physical state of the inner solid lipid core and its polymorphism and supercooling behavior. In this review, SLNs were compared to lipid emulsion and emulsion of supercooled melt to understand the unusual behaviors compared to lipid emulsions and to have insights into stability and release mechanism. SLNs have been regarded as biocompatible system because lipids are usually well-tolerable ingredients than polymers. Several studies showed good tolerability of SLNs in terms of cytotoxicity and hemolysis. Similar to various other nanoparticulate drug delivery systems, SLNs can also change biodistribution of the incorporated drugs in a way to enhance therapeutic effect. Most of all, large scale production of SLNs was extablished wihtout using organic solvents. Although there is no SLN product in the market till date, several advantagious properties of SLNs and the progress we have seen so far would make commercial product of SLNs possible before long and encourage research community to apply SLN-based formulations for water-insoluble drugs.

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The Utility of Sulfonate Salts in Drug Development

Cited by 95 publications

References 40 publications

Genotoxic Impurities in Pharmaceuticals

Genotoxic Impurities in Pharmaceuticals

Untitled

Solid Lipid Nanoparticles as Drug Delivery System for Water-Insoluble Drugs

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