Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Guedes, Francimary L.; Oliveira, Boaz G.; Hernandes, Marcelo Zaldini; Simone, C. A. De; Veiga, Francisco; Lima, Maria do Carmo Alves de; Pitta, Ivan R.; Galdino, Suely Lins; Rolim-Neto, Pedro José

doi:10.1208/s12249-010-9556-z

Cited by 24 publications

(12 citation statements)

References 18 publications

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“…Many hypotheses have been proposed to explain the mechanism by which formulation as a solid dispersion can ameliorate the disadvantageous pharmaceutical properties of drugs. Generally, the major factors that influence drug solubility and dissolution include degree of crystallinity, wettability, and particle size (23). The XRD results indicated that the drug was in an amorphous form within the crystalline polymer matrix.…”

Section: Discussionmentioning

confidence: 99%

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Hou

Cao

et al. 2013

AAPS PharmSciTech

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Ensuring sufficient drug solubility is a crucial problem in pharmaceutical-related research. For water-insoluble drugs, various formulation approaches are employed to enhance the solubility and bioavailability of lead compounds. The goal of this study was to enhance the dissolution and absorption of a new antitumor lead compound, T-OA. Early-stage preparation discovery concept was employed in this study. Based on this concept, a solid dispersion system was chosen as the method of improving drug solubility and bioavailability. Solid dispersions of T-OA in polyvinylpyrrolidone (PVP) K30 were prepared by the solvent evaporation method. Dissolution testing determined that the ideal drug-to-PVP ratio was 1:5. X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were employed to confirm the formation of solid dispersions. Scanning electron microscopy demonstrated that T-OA was converted into an amorphous form. Both in vitro dissolution testing and the in vivo studies demonstrated that the solubility and bioavailability of T-OA were significantly improved when formulated in a solid dispersion with PVP. The dissolution rate of the T-OA/PVP solid dispersion was greatly enhanced relative to the pure drug, and the relative bioavailability of T-OA solid dispersions was found to be 392.0%, which is 4-fold higher than the pure drug.

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Section: Discussionmentioning

confidence: 99%

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Hou

Cao

et al. 2013

AAPS PharmSciTech

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“…SDs prepared with water-soluble polymer carriers are usually soft and sticky and have poor flow properties, which hinders their application in large-scale pharmaceutical formulation. 11,30,31 In this study, SDs prepared with CNPs were not sticky and flowed freely, which may facilitate the downstream processing of solid formulations. Thus, we can conclude that CNP has great potential for clinical application as a novel and promising SD carrier.…”

Section: Resultsmentioning

confidence: 89%

Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

Ding¹,

Zhang²,

Song³

et al. 2014

IJN

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In this study, a novel carbon nanopowder (CNP) drug carrier was developed to improve the oral bioavailability of apigenin (AP). Solid dispersions (SDs) of AP with CNP were prepared, and their in vitro drug release and in vivo performance were evaluated. The physicochemical properties of the formulations were examined by differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy. Drug release profiles showed that AP dissolution from the CNP-AP system (weight ratio, 6:1) after 60 minutes improved by 275% compared with that of pure AP. Moreover, the pharmacokinetic analysis of SD formulations in rats showed that the AP area under the curve 0–t value was 1.83 times higher for the CNP-AP system than for pure AP, indicating that its bioavailability was significantly improved. In addition, compared with pure AP, SDs had a significantly higher peak and shorter time to peak. Preliminary intestinal toxicity tests indicated that there was no significant difference in the tissues of the rats treated with the CNP-AP system, rats treated with the CNP alone, and controls. In conclusion, CNP-based SDs could be used for enhancing the bioavailability of poorly water-soluble drugs while also improving drug safety.

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“…[1011121314] Dissolution rates can be improved by particle size reduction, increased wettability through mixing with highly soluble carriers, and maintenance of the drug in the amorphous form. [151617] Although the application of SDs has been reported regularly in the pharmaceutical literature, only a few commercial products rely on the SDs strategy.…”

Section: Introductionmentioning

confidence: 99%

An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO₃and poloxamer 188

et al. 2014

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Background:Tanshinone IIA (TSIIA) on solid dispersions (SDs) has thermodynamical instability of amorphous drug. Ternary solid dispersions (tSDs) can extend the stability of the amorphous form of drug. Poloxamer 188 was used as a SD carrier. Nano-CaCO3 played an important role in adsorption of biomolecules and is being developed for a host of biotechnological applications.Objective:The aim of the present study was to investigate the dissolution behavior and accelerated stability of TSIIA on solid dispersions (SDs) by the use of ternary systems with nano-CaCO3 and poloxamer 188.Materials and Methods:The TSIIA tSDs were prepared by a spray-drying method. First, the effect of combination of poloxamer 188 and nano-CaCO3 on TSIIA dissolution was studied. Subsequently, a set of complementary techniques (DSC, XRPD, SEM and FTIR) was used to monitor the physical changes of TSIIA in the SDs. Finally, stability test was carried out under the conditions 40°C/75% RH for 6 months.Results:The characterization of tSDs by differential scanning calorimetry analysis (DSC) and X-ray powder diffraction (XRPD) showed that TSIIA was present in its amorphous form. Fourier transforms infrared spectroscopy (FTIR) suggested the presence of interactions between TSIIA and carriers in tSDs. Improvement in the dissolution rate was observed for all SDs. The stability study conducted on SDs with nano-CaCO3 showed stable drug content and dissolution behavior, over the period of 6 months as compared with freshly prepared SDs.Conclusion:SDs preparation with nano-CaCO3 and poloxamer 188 may be a promising approach to enhance the dissolution and stability of TSIIA.

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Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Cited by 24 publications

References 18 publications

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO₃and poloxamer 188

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Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Cited by 24 publications

References 18 publications

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Preparation and Evaluation of Solid Dispersions of A New Antitumor Compound Based on Early-Stage Preparation Discovery Concept

Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO3and poloxamer 188

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Product

Resources

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An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO₃and poloxamer 188