Solubility measurement of polymorphic compounds via the pH-metric titration technique

Fioritto, Ann; Bhattachar, Shobha; Wesley, James A.

doi:10.1016/j.ijpharm.2006.09.003

Cited by 25 publications

(12 citation statements)

References 21 publications

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“…This technique allows one to have a precise control of the rate of transformation of one form into the other, depending on the conditions of the experiment used. This approach has been applied to numerous compounds (bases, acids and zwitterions), generally obtaining the more stable polymorph; in many cases they proved to be newly-identified polymorphs [1,66,[71][72][73][74].…”

Section: Potentiometric Cycling For Polymorph Creation [Pc]mentioning

confidence: 99%

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]mentioning

confidence: 99%

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

et al. 2016

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“…The former is due to a phase transition to a higher temperature-stable form, and the latter is due to the melting endotherm. 35) These characteristic peaks were also observed in the PM and the Milled FUR, indicating that FUR in the two preparations is still crystal. On the other hands, different peaks are found in the DSC thermogram of FUR-K12, an endothermic peak at ca.…”

Section: Discussionmentioning

confidence: 87%

“…It has already been reported that several polymorphisms are confirmed for FUR. 35,36) Bulk FUR is likely form I. In Fig.…”

Section: Discussionmentioning

confidence: 99%

Novel Strategy for the Systemic Delivery of Furosemide Based on a New Drug Transport Mechanism

Kimura

Kiriyama

Nishimura

et al. 2018

Biological & Pharmaceutical Bulletin

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We reported a novel transport mechanism of curcumin, independent of improved solubility, which involved direct contact of amorphous solid particles with the cell membrane. This mechanism has potential as a novel systemic delivery system of poorly water-soluble drugs. In this study, the transport mechanism of furosemide (FUR), which is transported by the same novel mechanism, was examined. In vitro cell permeation studies under air-interface conditions (AICs) revealed that the permeation from powders sprayed on cell monolayers was significantly higher than that under liquid-covered conditions (LCCs) from their solutions. The permeation from amorphous solid particles was faster than that from crystals. Similar results were derived from in vitro studies using an artificial membrane, with which the permeation of FUR could be examined without water. These findings clearly indicated that the transport mechanism of FUR is the same as that of curcumin. For the application of this new transport mechanism, the in vivo absorption of FUR was examined after pulmonary insufflation, which allows the solid particles to make direct contact with the epithelial cells. Pulmonary absorption of FUR from the amorphous powder was almost complete and was faster than that after intragastric administration of the solution, suggesting that FUR was absorbed from the lung by the same mechanism as the in vitro study. This new transport mechanism, which is independent of water dissolution, could be exploited to develop a novel delivery system for poorly water-soluble drugs, using pulmonary powder inhalation.

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“…In the solubility assay, a phase transition was not observed for form II, whereas form I converted to the hemihydrate under identical conditions (Fioritto et al, 2007).…”

Section: Cephalexin Erythromycin Ciprofloxacin Sulfamethoxazole Amentioning

confidence: 95%

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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Solubility measurement of polymorphic compounds via the pH-metric titration technique

Cited by 25 publications

References 21 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

Novel Strategy for the Systemic Delivery of Furosemide Based on a New Drug Transport Mechanism

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

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