Preparation and Evaluation of Solid Dispersions of Nitrendipine Prepared with Fine Silica Particles Using the Melt-Mixing Method

Wang, Liang; Cui, Fu De; Sunada, Hisakazu

doi:10.1248/cpb.54.37

Cited by 60 publications

(42 citation statements)

References 32 publications

(36 reference statements)

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“…A great deal of research has been conducted using porous and nonporous, hydrophilic and hydrophobic fine silica particles as carriers for solid dispersions (17,18). The porous silica materials showed higher dissolution rates because of their ability to decrease the crystallinity of the drugs compared to nonporous silica materials (19).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Patel¹,

Dave²

2013

AAPS PharmSciTech

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Abstract. Colloidal solid dispersion is an innovative breakthrough in the pharmaceutical industry that overcomes the solubility-related issue of poorly soluble drugs by using an amorphous approach and also the stability-related issue by means of a complex formation phenomenon using different carrier materials. In the present study, a newly developed adsorption method is introduced to incorporate a high-energy sulfathiazole-polyvinylpyrrolidone (Plasdone® K-29/32) solid dispersion on porous silicon dioxide (Syloid® 244FP). Different ternary systems of sulfathiazole-Plasdone® K-29/32-Syloid® 244FP were prepared (1:1:2, 1:1:3, and 1:2:2) and categorized depending on the mechanism by which Syloid® 244FP was incorporated. Modulated differential scanning calorimetry (MDSC), X-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were conducted to characterize the ternary systems. The X-ray diffraction and MDSC data showed a lack of crystallinity in all internal and external ternary systems, suggesting a loss of the crystallinity of sulfathiazole compared to the physical mixtures. USP apparatus II was used to measure the in vitro dissolution rate of the prepared systems at 75 rpm in different media. The dissolution rate of the optimum ratio (1:2:2) containing an internal ternary solid dispersion system was found to be three times higher than that of the external and physical systems. Thus, the porous silicon dioxide incorporated into the conventional binary solid dispersion acted as a carrier to disperse the complex and increase the dissolution rate.

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Section: Introductionmentioning

confidence: 99%

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Patel¹,

Dave²

2013

AAPS PharmSciTech

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“…Kinoshita et al (4), reported an increase in dissolution and solubility of TAS-301 melt adsorbed on amorphous calcium silicate. An improvement in dissolution and/or solubility of drugs such as nitrendipine (24), tolbutamide (25), indomethacin (15), phenytoin (26), and meclozine hydrochloride (27) co-processed with silicates have been well documented. In a previous study, we reported physical and chemical stability of indomethacin amorphized by co-grinding with Neusilin US2 (28).…”

Section: Introductionmentioning

confidence: 99%

Amorphization Alone Does Not Account for the Enhancement of Solubility of Drug Co-ground with Silicate: The Case of Indomethacin

Bahl

Bogner

2008

AAPS PharmSciTech

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Abstract. The solubility advantage of indomethacin amorphized by co-grinding with Neusilin US2 in various media was investigated. Physical mixtures of γ-indomethacin and Neusilin US2 (in the ratios 1:1, 1:4 and 1:5) were amorphized at room temperature employing 75% RH in a porcelain jar mill using zirconia balls. The crystallinity of the samples was determined using ATR-FTIR and PXRD. The solubility and dissolution profiles of co-ground powders and crystalline counterparts were evaluated in 0.1 N HCl, water and phosphate buffer (pH 6.8) in a USP type II dissolution apparatus at 250 rpm and 37°C. Very high concentrations of dissolved indomethacin as compared to the solubility of γ-indomethacin (~500 times in water and~3.7 times in phosphate buffer) were attained. However, the presence of other polymorphs detected by PXRD and a change in the pH of the medium made interpretation of the results difficult. In 0.1 N HCl the solubility (i.e., the peak in a concentration versus time plot) of the amorphized drug in a 1:5 ratio with Neusilin increased to 109 times the solubility of crystalline γ-indomethacin alone. An increase in amount of drug and Neusilin in the same ratio added to the dissolution medium also increased peak and plateau dissolution concentrations. The presence of silicic acid and ions (Mg 2+ and Al 3+ ) in the dissolution media were found to cause the increase in the plateau concentration of indomethacin. Amorphization alone does not account for all of the dissolution enhancement; acidity, ions, and silicic acid are major contributors to dissolution enhancement.

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“…The commercial success of the SMEF, Neoral ® drew greater attention to the development of SMEFs. Many poorly water-soluble drugs such as acyclovir, atorvastatin, and fenofibrate have been reported to offer improved oral bioavailability by SMEFs (Wang et al, 2006;Shen, Zhong, 2006;Patel, Vavia, 2007). Postolache et al (2002) compared the bioavailability of two cyclosporine capsule products with different pharmaceutical formulations.…”

Section: Self-microemulsifying Formulationsmentioning

confidence: 99%

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa¹,

Nair²,

Kumria³

2011

Braz. J. Pharm. Sci.

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Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.Uniterms: Lipid based formulations. Self-emulsifying therapeutic system. Self-emulsification.O sistema terapêutico auto-emulsionante (SETs) fornece solução eficaz e inteligente para os vários problemas relativos à formulação de fármacos hidrofóbicos com solubilidade limitada no fluido gastrintestinal. Embora a utilidade potencial dos SETs seja bem conhecida, só recentemente se compreendeu, mecanisticamente,o impacto desses sistemas na disposição de fármacos. Estes sistemas de formação de emulsão in situ têm alta estabilidade, quando incorporados em várias formas de dosagem. Os SETs têm sido considerados como sistemas que podem resolver problemas associados à liberação de fármacos pouco solúveis em água. O conhecimento profundo dos lipídios e tensoativos que podem ser utilizados para estes sistemas e o critério para a sua seleção e proporção na qual eles são utilizados são alguns dos fatores cruciais que determinam o desempenho do sistema in vivo. Este artigo apresenta o relato abrangente de vários tipos de formulações auto-emulsificantes, com ênfase em sua composição e exemplos das preparações que são correntemente comercializadas.Unitermos: Formulações baseadas em lipídio. Sistema terapêutico auto-emulsificante. Autoemulsificação.

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Preparation and Evaluation of Solid Dispersions of Nitrendipine Prepared with Fine Silica Particles Using the Melt-Mixing Method

Cited by 60 publications

References 32 publications

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Amorphization Alone Does Not Account for the Enhancement of Solubility of Drug Co-ground with Silicate: The Case of Indomethacin

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

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