Novel Tanshinone II A ternary solid dispersion pellets prepared by a single-step technique: In vitro and in vivo evaluation

Li, Jin; Liu, Pan; Liu, Jianping; Zhang, Wenli; Yang, Jikun; Fan, Yilin

doi:10.1016/j.ejpb.2011.11.003

Cited by 48 publications

(23 citation statements)

References 47 publications

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“…Pure TSIIA ( Figure 3A) showed a sharp melting peak at an onset temperature of 205.6°C, which indicated its crystalline nature. Observations similar to ours have been reported by Li et al 54 The DSC spectra of PMs ( Figure 3C) showed that the endothermic peak of the drug was found at 205.6°C, which indicated no interaction between TSIIA and silica nanoparticles in the PMs and that TSIIA existed in a virgin form in the system. DSC of the SDs prepared at a TSIIA/silica nanoparticle ratio of 1:5 ( Figure 3D) showed that the characteristic peak of TSIIA had completely vanished, which suggested that the drug may have been present in the SDs in an amorphous state, and thus was responsible for increasing the dissolution of the drug.…”

Section: Dscsupporting

confidence: 77%

“…[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%

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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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Section: Dscsupporting

confidence: 77%

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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“…The in vivo test showed that the AUC 0-t and C max were increased 5.40 and 8.97 times more than that of TSIIA. T max value was shortened (3.80 ± 0.398) h, compared to TSIIA with (5.52 ± 0.738) h [85]. Moreover, a solid dispersion (weight ratio 1 : 9) of TSIIA with lowmolecular-weight chitosan (molecular weight 3.0 × 10 3 , degree of deacetylation 90 %) was developed and evaluated the in vitro dissolution and in vivo performance.…”

mentioning

confidence: 99%

Effects of Salvia miltiorrhiza on CNS Neuronal Injury and Degeneration: A Plausible Complementary Role of Tanshinones and Depsides

Bonaccini

Karioti²,

Bergonzi

et al. 2015

Planta Med

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“…Additionally, as reported, rabbits are often used as the animal for the prediction of skin irritation effects in humans, and the findings verified that the rabbit irritation data are useful in identifying human health risks (30). On the other hand, no reference has been found to prove that rabbits were used as the animal models for the study of oral irritation, but many literatures have been reported that rabbits were used as experiment animals to study in vivo pharmacokinetics of pellets (31,32). Hence, rabbits were chosen for oral administration in our study.…”

Section: In Vivo Pharmacokinetics Studiesmentioning

confidence: 97%

Preparation and In Vitro–In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability

Huang

Omari‐Siaw

et al. 2015

AAPS PharmSciTech

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Abstract. Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and antiinflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets of capsaicin to enhance its oral bioavailability. The pellets comprised of a core of soliddispersed capsaicin mixed with microcrystalline cellulose (MCC) and hydroxypropyl cellulose (HPMC) and subsequently coating with ethyl cellulose (EC) were obtained by using the technology of extrusion/ spheronization. The physicochemical properties of the pellets were evaluated through scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD). Besides, the in vitro release, in vivo absorption, and in vitro-in vivo correlation were also assessed. More importantly, the relative bioavailability of the sustained-release matrix pellets was studied in fasted rabbits after oral administration using free capsaicin and solid dispersion as references. The oral bioavailability of the matrix pellets and sustained-release matrix pellets of capsaicin was improved approximately 1.98-fold and 5.34-fold, respectively, compared with the free capsaicin. A good level A IVIVC (in vitro-in vivo correlation) was established between the in vitro dissolution and the in vivo absorption of sustainedrelease matrix pellets. All the results affirmed the remarkable improvement in the oral bioavailability of capsaicin owing to the successful preparation of its sustained-release matrix pellets.

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Novel Tanshinone II A ternary solid dispersion pellets prepared by a single-step technique: In vitro and in vivo evaluation

Cited by 48 publications

References 47 publications

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

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

Effects of Salvia miltiorrhiza on CNS Neuronal Injury and Degeneration: A Plausible Complementary Role of Tanshinones and Depsides

Preparation and In Vitro–In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability

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