Development and Chemical Stability Studies of Alcohol-Free Phenobarbital Solution for Use in Pediatrics: a Technical Note

Jelveghari, M.; Nokhodchi, Ali

doi:10.1208/s12249-008-9112-2

Cited by 18 publications

(15 citation statements)

References 10 publications

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“…The solubility of luteolin in water was found to be 0.85 ± 0.03 mg/ml which is approximately similar as reported [28,29]. Drugs having aqueous solubility < 1 mg/ml are considered as very slightly soluble or poorly soluble drugs [76,77]. Poor aqueous solubility of drug is considered as the main cause of poor bioavailability of several drugs [78].…”

Section: Phase Solubility Evaluation Of Luteolinsupporting

confidence: 78%

Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin

Ansari

Alshetaili

Aldayel

et al. 2020

Journal of Taibah University for Science

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The purpose of this study was to develop a self-nanoemulsifying drug delivery system (SNEDDS) for the improvement of solubility and bioavailability of luteolin in order to enhance its therapeutic benefits. Formulations were prepared by spontaneous emulsification method which involved low energy mixing of appropriate amounts ofcastor oil, kolliphor & polyethylene glycol 200. The developed formulae were optimized and characterized for self-nanoemulsifying capacity, thermodynamic stability, size behaviour and solubility. The globule size of the optimized formula F1-A1:1 was 112 ± 15 nm, with narrow PDI (0.31 ± 0.09) and good zeta potential (−16.2 ± 3.2 mV). The optimized formula exhibited approximately 83, 17 and 3-fold enhancement in the solubility in vitro release and ex vivo permeation respectively. The luteolin SNEDD exhibited better antioxidant activity (DPPH scavenging activity) than ascorbic acid. Per cent inhibition in rat paw oedema by the SNEDDS formulation was statistically significant when compared with luteolin suspension at equivalent dose (P < 0.05).

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Section: Phase Solubility Evaluation Of Luteolinsupporting

confidence: 78%

Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin

Ansari

Alshetaili

Aldayel

et al. 2020

Journal of Taibah University for Science

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“…Non-ionic surfactants such as polysorbates, polyoxyethylated castor oil etc. are commonly used for improving the solubilization of the drug (Rangel-Yagui et al, 2005 ; Hsu et al, 2008 ). Solubility of various anti-diabetic drugs such as gliclazide, glyburide and glipizide has been enhanced using the approach of micellar solubilization (Hsu et al, 2008 ).…”

Section: Strategies For Solubilization Of Hydrophobic Drugsmentioning

confidence: 99%

Impact of Dendrimers on Solubility of Hydrophobic Drug Molecules

et al. 2017

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Adequate aqueous solubility has been one of the desired properties while selecting drug molecules and other bio-actives for product development. Often solubility of a drug determines its pharmaceutical and therapeutic performance. Majority of newly synthesized drug molecules fail or are rejected during the early phases of drug discovery and development due to their limited solubility. Sufficient permeability, aqueous solubility and physicochemical stability of the drug are important for achieving adequate bioavailability and therapeutic outcome. A number of different approaches including co-solvency, micellar solubilization, micronization, pH adjustment, chemical modification, and solid dispersion have been explored toward improving the solubility of various poorly aqueous-soluble drugs. Dendrimers, a new class of polymers, possess great potential for drug solubility improvement, by virtue of their unique properties. These hyper-branched, mono-dispersed molecules have the distinct ability to bind the drug molecules on periphery as well as to encapsulate these molecules within the dendritic structure. There are numerous reported studies which have successfully used dendrimers to enhance the solubilization of poorly soluble drugs. These promising outcomes have encouraged the researchers to design, synthesize, and evaluate various dendritic polymers for their use in drug delivery and product development. This review will discuss the aspects and role of dendrimers in the solubility enhancement of poorly soluble drugs. The review will also highlight the important and relevant properties of dendrimers which contribute toward drug solubilization. Finally, hydrophobic drugs which have been explored for dendrimer assisted solubilization, and the current marketing status of dendrimers will be discussed.

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“…The borate buffer solution at a pH 9.6 with 10% of EtOH was used, for it has a better solubility and does not interfere with the wavelength 242 nm (data not shown). A basic pH facilitates the solubility of PB (pKa = 7.3) due to its conversion into an ionized tautomeric form, in addition to increasing its molar absorptivity compared to more acidic pHs (Romer, Donaruma, Zuman, 1977;Jelveghari, Nokhodchi, 2008).…”

Section: Kinetics Of the In Vitro Release Of Pb In Mementioning

confidence: 99%

Phenobarbital loaded microemulsion: development, kinetic release and quality control

Figueiredo

Neves

Silva

et al. 2016

Braz. J. Pharm. Sci.

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This study aimed to obtain and characterize a microemulsion (ME) containing phenobarbital (PB). The PB was incorporated in the proportion of 5% and 10% in a microemulsion system containing Labrasol ® , ethanol, isopropyl myristate and purified water. The physicochemical characterization was performed and the primary stability of the ME was evaluated. An analytical method was developed using spectrophotometry in UV λ = 242 nm. The kinetics of the in vitro release (Franz model) of the ME and the emulsion (EM) containing PB was evaluated. The incorporation of PB into ME at concentrations of 5 and 10% did not change pH and resistance to centrifugation. There was an increase in particle size, a decrease of conductivity and a change in the refractive index in relation to placebo ME. The ME remained stable in preliminary stability tests. The analytical method proved to be specific, linear, precise, accurate and robust. Regarding the kinetics of the in vitro release, ME obtained an in vitro release profile greater than the EM containing PB. Thus, the obtained ME has a potential for future transdermal application, being able to compose a drug delivery system for the treatment of epilepsy.Uniterms: Microemulsion/physicochemical characterization. Microemulsion/In vitro release. Phenobarbital/microemulsion system/evaluation. Nanotechnology.O objetivo deste trabalho foi obter e caracterizar uma microemulsão (ME) contendo fenobarbital (FEN). O FEN foi incorporado na proporção de 5% e 10% em um sistema microemulsionado composto por labrasol ® , etanol, miristato de isopropila e água purificada. Foi realizada a caracterização físico-química e avaliada a estabilidade preliminar da ME. Desenvolveu-se um método analítico por espectrofotometria em UV λ = 242 nm. Foi avaliada a cinética de liberação in vitro (em modelo de Franz) da ME e da emulsão (EM) contendo FEN. A incorporação do FEN em ME nas concentrações de 5 e 10% não alterou o pH e a resistência à centrifugação. Houve aumento do tamanho da partícula, redução da condutividade e alteração do índice de refração em relação à ME placebo. A ME manteve-se estável nos ensaios de estabilidade preliminar. O método analítico demonstrou ser específico, linear, preciso, exato e robusto. Na cinética de liberação in vitro, a ME obteve um perfil de liberação in vitro superior a EM contendo FEN. Desta forma, a ME obtida tem potencial para uma futura aplicação transdérmica, podendo compor um sistema de liberação de fármacos para tratamento da epilepsia.Uniterms: Microemulsão/caracterização físico-química. Microemulsão/cinética de liberação in vitro. Fenobarbital/sistema microemulsionado/avaliação. Nanotecnologia.

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Development and Chemical Stability Studies of Alcohol-Free Phenobarbital Solution for Use in Pediatrics: a Technical Note

Cited by 18 publications

References 10 publications

Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin

Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin

Impact of Dendrimers on Solubility of Hydrophobic Drug Molecules

Phenobarbital loaded microemulsion: development, kinetic release and quality control

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