Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): In vivo evaluation

Tanaka, Nobuyuki; Imai, Kazunori; Okimoto, Kazuto; Ueda, Satoshi; Tokunaga, Yuji; Ibuki, Rinta; Higaki, Kazutaka; Kimura, Takeshi

doi:10.1016/j.jconrel.2006.01.020

Cited by 75 publications

(37 citation statements)

References 20 publications

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“…This suggested that the therapeutic period of Cur was extended after it was presented in the SRSD. Cur suspension upon oral administration resulted in a sharp C max within 0.66 h and the plasma concentration of the drug decreased rapidly, indicating a rapid metabolism of Cur, which was proven by the obtained higher k el and shorter t 1/2 , whereas a relatively slow increase and sustained plasma concentration of Cur for a longer time was observed after the administration of the SRSD, with significantly delayed t max and prolonged K el and K a , suggesting that an obvious sustained release of Cur from the formulation successfully resulted in the sustained absorption of Cur in vivo (7,25,26). Consequently, SRSD persisted for a longer period of time with a higher relative bioavailability of 701.64%.…”

Section: In Vivo Studymentioning

confidence: 93%

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

et al. 2011

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Abstract. Curcumin (Cur), one of the most widely used natural active constituents with a great variety of beneficial biological and pharmacological activities, is a practically water-insoluble substance with a short biologic half-life. The aim of this study was to develop a sustained-release solid dispersion by employing water-insoluble carrier cellulose acetate for solubility enhancement, release control, and oral bioavailability improvement of Cur. Solid dispersions were characterized by solubility, in vitro drug release, Fourier transform infrared spectroscopy, X-ray diffractometry, and differential scanning calorimetry studies. The in vivo performance was assessed by a pharmacokinetic study. Solid-state characterization techniques revealed the amorphous nature of Cur in solid dispersions. Solubility/ dissolution of Cur was enhanced in the formulations in comparison with pure drug. Sustained-release profiles of Cur from the solid dispersions were ideally controlled in vitro up to 12 h. The optimized formulation provided an improved pharmacokinetic parameter (C max =187.03 ng/ml, t max =1.95 h) in rats as compared with pure drug (C max =87.06 ng/ml, t max =0.66 h). The information from this study suggests that the developed solid dispersions successfully enhanced the solubility and sustained release of poorly water-soluble drug Cur, thus improving its oral bioavailability effectively.

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Section: In Vivo Studymentioning

confidence: 93%

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

et al. 2011

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“…Many researchers have concluded that an improvement in the release profiles of these drugs by suitable formulation can enhance their bioavailability and reduce side effects (2,3). Class II drugs are considered the best candidates for intervention by formulation, and several methods have been developed to overcome their low aqueous solubility.…”

mentioning

confidence: 99%

Dissolution Behavior and Thermodynamic Stability of Fused-Sugar Dispersions of a Poorly Water-Soluble Drug

Singh¹,

Chhabra²,

Pathak³

2011

Dissolution Technol.

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The current research was undertaken to develop and evaluate dissolution profiles of thermodynamically stabilized sugar dispersions of the poorly water-soluble, model drug etoricoxib (ETX). Fused-sugar dispersions were formulated using sorbitol, xylitol, and maltose separately, and the binary systems were stabilized by incorporation of the antiplasticizing agents poloxamer 407 and PVP K30 to obtain ternary and quaternary systems. The sugar dispersions (F1-F12) were subjected to in vitro dissolution studies, and based on model-independent dissolution parameters, ETX-sorbitol binary/ ternary/composite systems were selected for thermodynamic stability study. The aged ETX-sorbitol composite dispersion (SF8) displayed the highest percent dissolution efficiency (%DE 80min of 78.48), the minimum t 50% of 4.45 min, and the least tendency to recrystallize (D cryst of 0.68), confirming maximum amorphization and thermodynamic stability among all the composite dispersions. The SEM photomicrographs reveal complete miscibility of drug in the aged quaternary dispersion SF8, and its diffuse reflectance (DR) spectrum confirms the absence of any chemical change. Conclusively, sorbitol binary systems can be effectively stabilized by incorporation of PVP K30-poloxamer 407 and retain the dissolution characteristics of sugar dispersions upon aging.

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“…[8][9][10] Drug release is a crucial and limiting step in oral drug bioavailability 11,12 especially for drugs with low gastrointestinal solubility and high permeability. [13][14][15] Previous studies have shown that the formation of solid dispersions (SDs) is a promising strategy for increasing the dissolution rate and solubility of drugs [16][17][18][19][20] belonging to class II of the Biopharmaceutical Classification System. 21 Dissolution can be improved by reducing the particle size of the drug and increasing the surface area; 22,23 drug wettability can be improved by mixing the drug with a high concentration of the carrier in the surrounding solution; 24,25 and the drug can be transformed from a crystalline to an amorphous state.…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

Jiang¹,

Zhang²,

Liu³

et al. 2013

IJN

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Abstract:We prepared solid dispersions (SDs) of tanshinone IIA (TSIIA) with silica nanoparticles, which function as dispersing carriers, using a spray-drying method and evaluated their in vitro dissolution and in vivo performance. The extent of TSIIA dissolution in the silica nanoparticles/TSIIA system (weight ratio, 5:1) was approximately 92% higher than that of the pure drug after 60 minutes. However, increasing the content of silica nanoparticles from 5:1 to 7:1 in this system did not significantly increase the rate or extent of TSIIA dissolution. The physicochemical properties of SDs were investigated using scanning electron microscopy, differential scanning calorimetry, X-ray powder diffraction, and Fourier transforms infrared spectroscopy. Studying the stability of the SDs of TSIIA revealed that the drug content of the formulation and dissolution behavior was unchanged under the applied storage conditions. In vivo tests showed that SDs of the silica nanoparticles/TSIIA had a significantly larger area under the concentration-time curve, which was 1.27 times more than that of TSIIA (P , 0.01). Additionally, the values of maximum plasma concentration and the time to reach maximum plasma concentration of the SDs were higher than those of TSIIA and the physical mixing system. Based on these results, we conclude that the silica nanoparticle based SDs achieved complete dissolution, increased absorption rate, maintained drug stability, and showed improved oral bioavailability compared to TSIIA alone.

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Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): In vivo evaluation

Cited by 75 publications

References 20 publications

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

Dissolution Behavior and Thermodynamic Stability of Fused-Sugar Dispersions of a Poorly Water-Soluble Drug

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

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