Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process

Won, Dong Han; Kim, Min Soo; Lee, Sibeum; Park, Jeong Sook; Hwang, Sung Joo

doi:10.1016/j.ijpharm.2005.05.017

Cited by 176 publications

(80 citation statements)

References 20 publications

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“…The highest ABZ dissolution rate was achieved from the microparticles of HPMC in 1:1 ratio (P< 0.05). This is in agreement with our previous study in which the highest dissolution of indomethacin from its microparticles achieved with the lower HPMC content [17].This finding can be explained by the fact that the microparticles with low polymer content were expected to be more porous than those with high polymer content, which might facilitate the release of the residual drug from the microparticles [22]. Also, the thickness of the hydrogel layer increases with high polymer content due to polymer swelling and forming a gel layer which retarded drug diffusion [23].…”

Section: Resultssupporting

confidence: 92%

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Alanazi

2007

Sci Pharm

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The aim of this work was to improve the dissolution rate of albendazole (ABZ) by preparing its microparticles with certain hydrophilic polymers such as hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), and polyvinyl pyrrolidone (PVP) using spray drying technique. Microparticles of ABZ with these polymers were prepared in different ratios of 1:1, 1:2, and 1:4 by spray drying technique. Morphology and characterization of the prepared ABZ microparticles was studied and photographed using a biological microscope and examined by scanning electron microscope. Smooth surface and spherical microparticles of ABZ were detected by these methods which indicating the coating of drug crystals by the studied polymers. Physicochemical properties of drug alone and its spray dried microparticles were investigated using differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD). DSC and PXRD analysis showed that ABZ transformed from the crystalline state to amorphous state by spray drying with these polymers as confirmed by disappearance of its melting peak and characteristic crystalline peaks. Dissolution rate of ABZ from the prepared microparticles was determined and compared to its corresponding physical

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Section: Resultssupporting

confidence: 92%

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Alanazi

2007

Sci Pharm

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“…Incubator shaker was used to keep samples at 37 °C during the test with agitation of 150 rpm for 72 hours (until achieve the equilibrium condition) (Marín, Margarit, Salcedo, 2002;Okumu, Dimaso, Löbenberg, 2009;United States, 2000;Won et al, 2005). After this period, samples were immediately filtered (0.45 µm) and diluted in a volumetric flask with the corresponding media.…”

Section: Buffersmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

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Solubility and dissolution rate of drugs are of major importance in pre-formulation studies of pharmaceutical dosage forms. The solubility improvement allows the drugs to be potential biowaiver candidates and may be a good way to develop more dose-efficient formulations. Solubility behaviour of lamivudine, stavudine and zidovudine in individual solvents (under pH range of 1.2 to 7.5) was studied by equilibrium solubility and intrinsic dissolution methods. In solubility study by equilibrium method (shake-flask technique), known amounts of drug were added in each media until to reach saturation and the mixture was subjected to agitation of 150 rpm for 72 hours at 37 °C. In intrinsic dissolution test, known amount of each drug was compressed in the matrix of Wood's apparatus and subjected to dissolution in each media with agitation of 50 rpm at 37 °C. In solubility by equilibrium method, lamivudine and zidovudine can be considered as highly soluble drugs. Although stavudine present high solubility in pH 4.5, 6.8, 7.5 and water, the solubility determination in pH 1.2 was not possible due stability problems. Regarding to intrinsic dissolution, lamivudine and stavudine present high speed of dissolution. Considering a boundary value presented by Yu and colleagues (2004), all drugs studied present high solubility characteristics in intrinsic dissolution method. Based on the obtained results, intrinsic dissolution seems to be superior for solubility studies as an alternative method for biopharmaceutical classification purposes.Uniterms: Drugs/solubility. Drugs/dissolution rate. Intrinsic dissolution/method/biopharmaceutical classification. Biopharmaceutical Classification System.A solubilidade e a taxa de dissolução de fármacos são de grande importância em estudos de pré-formulação de formas farmacêuticas. A melhora na solubilidade permite que os fármacos sejam candidatos potenciais à bioisenção, podendo ser uma boa maneira para desenvolver formulações dose-eficientes. O comportamento de solubilidade da lamivudina, estavudina e zidovudina em solventes individuais (sob faixa de pH 1,2 a 7,5) foi estudado pelos métodos de solubilidade em equilíbrio e dissolução intrínseca. No estudo de solubilidade pelo método do equilíbrio (método de agitação de frascos), conhecidas quantidades do fármaco foram adicionadas em cada meio até atingirem a saturação e a mistura foi submetida à agitação de 150 rpm por 72 horas a 37 °C. No ensaio de dissolução intrínseca, conhecida quantidade de cada fármaco foi comprimida na matriz do aparato de Wood e submetida à dissolução em cada meio com agitação de 50 rpm a 37 °C. No método de solubilidade em equilíbrio, a lamivudina e a zidovudina podem ser consideradas como fármacos altamente solúveis. Embora a estavudina apresente alta solubilidade nos meios pH 4,5, 6,8, 7,5 e água, a determinação da solubilidade em pH 1,2 não foi possível devido a problemas de estabilidade. Com relação à dissolução intrínseca, a lamivudina e a estavudina apresentaram alta velocidade de dissolução. Considerando o valor ...

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“…In this method, the thermal decomposition of drugs or carriers can be prevented, since organic solvent evaporation occurs at low temperature 54 . A basic process of preparing solid dispersions of this type consists of dissolving the drug and the polymeric carrier in a common solvent, such as ethanol, chloroform 55 , or a mixture of ethanol and dichloromethane.…”

Section: Solvent Evaporation Methodmentioning

confidence: 99%

“…Normally, the resulting films are pulverized and milled. Super Critical fluid is the one where substances existing as a single fluid phase above their critical temperature and critical pressure, was shown to be efficient in obtaining solid dispersions 38,54,56 . It ensured a very fine dispersion of the hydrophobic drug in the hydrophilic carrier 53 .…”

Section: Solvent Evaporation Methodmentioning

confidence: 99%

Untitled

2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process

Cited by 176 publications

References 20 publications

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

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