Trends in Solubility of Polymorphs

Pudipeddi, Madhu; Serajuddin, Abu T.M.

doi:10.1002/jps.20302

Cited by 447 publications

(330 citation statements)

References 64 publications

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“…Using the CheqSol method one avoids the possibility of confounding different forms precipitating, and therefore reporting misleading data (i.e., amorphous vs crystalline, salts vs neutral forms, hydrates vs anhydrous...). Pudipeddi and Serajuddin published a survey in 2005, showing that the difference in solubility of polymorphs is usually less than a factor of two [18]. However our results suggest that polymorphs [71] can have a considerably greater factor than this.…”

Section: Potentiometric Cycling For Polymorph Creation [Pc]contrasting

confidence: 62%

“…Had longer dissolution times been used, the more soluble anhydrous form would likely have converted into the trihydrate. Many anhydrous forms of drugs are near 2-fold higher in solubility than their hydrate counter parts [4,18]. The two profiles are well-described by the simple HH equation.…”

Section: Atorvastatinmentioning

confidence: 99%

“…Several excellent books and reviews serve as background material for the commentary covering the solubility of druglike molecules: general coverage of solubility [7][8][9][10]; salt formation/selection [11][12][13][14][15][16]; polymorphism [17][18][19][20]; analysis of saturated solution speciation [21][22][23][24][25][26][27]; dissolution/solubility of cocrystals [28][29][30][31][32][33][34][35][36][37]; anhydrous forms versus hydrates [16,38,39].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

et al. 2016

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Section: Potentiometric Cycling For Polymorph Creation [Pc]contrasting

confidence: 62%

Section: Atorvastatinmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

et al. 2016

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“…Micronization with supercritical antisolvent has led to an increase in the sulfamethoxazole dissolution rate and has caused the phase transition of polymorph I to II, with a solubility ratio of 1.2 (Pudipeddi et al, 2005;Chang et al, 2008).…”

Section: Cephalexin Erythromycin Ciprofloxacin Sulfamethoxazole Amentioning

confidence: 99%

Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Santos

Reis

Jacon

et al. 2014

Braz. J. Pharm. Sci.

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Polymorphism in solids is a common phenomenon in drugs, which can lead to compromised quality due to changes in their physicochemical properties, particularly solubility, and, therefore, reduce bioavailability. Herein, a bibliographic survey was performed based on key issues and studies related to polymorphism in active pharmaceutical ingredient (APIs) present in medications from the Farmácia Popular Rede Própria. Polymorphism must be controlled to prevent possible ineffective therapy and/or improper dosage. Few mandatory tests for the identification and control of polymorphism in medications are currently available, which can result in serious public health concerns.Uniterms: Polymorphism. Medicines/quality control. Medicines/solubility. Medicines/bioavailability.O polimorfismo em sólidos é um fenômeno frequente em fármacos e pode levar a problemas na qualidade dos medicamentos por alterar suas propriedades físico-químicas, em especial a solubilidade e, consequentemente, a biodisponibilidade. Nesse trabalho realizou-se levantamento bibliográfico sobre os principais estudos e problemas relacionados ao polimorfismo em fármacos presentes nos medicamentos disponibilizados pela Farmácia Popular do Brasil. O polimorfismo deve ser controlado a fim de evitar possível ineficácia terapêutica e/ou dosagem inapropriada dos medicamentos. Destacamos que são poucos os ensaios obrigatórios para identificação e controle desse fenômeno em medicamentos, o que pode acarretar grande problema de saúde pública. Unitermos:Polimorfismo. Medicamentos/controle de qualidade. Medicamentos/solubilidade. Medicamentos/biodisponibilidade.

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“…In fact, when considering polymorphs, the solubility ratio between polymorphs is rarely found to be above 5. In the review from Pudipeddi and coworkers 13 , out of 50 drugs investigated (comprising 81 polymorph comparisons), the solubility ratio never exceeded 5 (except for 1 compound). Similar conclusions could be made for solvates.…”

Section: Crystalline State -Polymorphismmentioning

confidence: 99%

Solubility and Dissolution of Drug Product: A Review

Shahrin

2013

Int. J. Pharma Life Sci.

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The oral route of drug administration is the most common and preferred method of delivery due to convenience and ease of ingestion. From a patients perspective, swallowing a dosage form is a comfortable and a familiar means of taking medication. As a result, patient compliance and hence drug treatment is typically more effective with orally administered medications as compared with other routes of administration, for example, parenteral. Although the oral route of administration is preferred, for many drugs it can be a problematic and inefficient mode of delivery for a number of reasons. Limited drug absorption resulting in poor bioavailability is paramount amongst the potential problems that can be encountered when delivering an active agent via the oral route. Drug absorption from the gastrointestinal (GI) tract can be limited by a variety of factors with the most significant contributors being poor aqueous solubility and/or poor membrane permeability of the drug molecule. When delivering an active agent orally, it must first dissolve in gastric and/or intestinal fluids before it can then permeate the membranes of the GI tract to reach systemic circulation. Therefore, a drug with poor aqueous solubility will typically exhibit dissolution rate limited absorption, and a drug with poor membrane permeability will typically exhibit permeation rate limited absorption. Hence, two areas of pharmaceutical research that focus on improving the oral bioavailability of active agents include: (i) enhancing solubility and dissolution rate of poorly water-soluble drugs and (ii) enhancing permeability of poorly permeable drugs. In this article, solubility and dissolution will be discussed.DOI: http://dx.doi.org/10.3329/ijpls.v2i1.15133 International Journal of Pharmaceutical and Life Sciences Vol.2(1) 2013: 33-41

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Trends in Solubility of Polymorphs

Cited by 447 publications

References 64 publications

Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Solubility and Dissolution of Drug Product: A Review

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