Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process

Park, Junsung; Cho, Wonkyung; Ho, Kwang; Ahn, Junhyun; Han, Kang; Hwang, Sung Joo

doi:10.1016/j.ijpharm.2012.12.020

Cited by 63 publications

(37 citation statements)

References 33 publications

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“…More uncommon preparation methods which are not widely used and established industrially for the preparation of amorphous formulations such as supercritical fluid impregnation /solvent-antisolvent (84,92,102,149), electrospinning /electrospraying (72,91,141,153,174), confined impinging jet (107) and pressurized gyration (161) have also been explored even though the applicability in large scale is still a question.…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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“…However, SM-SD-SEDS showed a cumulative release of more than 90% in the first 5 min, whereas less than 70% release was observed from SM-SD-SE at 5 min. This may be due to the decreased particle size and reduced surface tension of the dissolution medium [26] when using supercritical fluid technology.…”

Section: In Vitro Dissolution Testmentioning

confidence: 99%

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Yang

Zhao

Feng

et al. 2015

Asian Journal of Pharmaceutical Sciences

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Available online xxxKeywords: Silymarin Solution-enhanced dispersion by supercritical fluids Solid dispersion Dissolution Bioavailability a b s t r a c tThe objective of this study was to improve the dissolution and bioavailability of silymarin (SM). Solid dispersions (SDs) were prepared using solution-enhanced dispersion by supercritical fluids (SEDS) and evaluated in vitro and in vivo, compared with pure SM powder.The particle sizes, stability, and contents of residual solvent of the prepared SM-SDs with SEDS and solvent evaporation (SE) were investigated. Four polymer matrix materials were evaluated for the preparation of SM-SD-SEDS, and the hydrophilic polymer, polyvinyl pyrrolidone K17, was selected with a ratio of 1:5 between SM and the polymer. Physicochemical analyses using X-ray diffraction and differential scanning calorimetry indicated that SM was dispersed in SD in an amorphous state. The optimized SM-SD-SEDS showed no loss of SM after storage for 6 months and negligible residual solvent (ethanol) was detected using gas chromatography. In vitro drug release was increased from the SM-SD-SEDS, as compared with pure SM powder or SM-SD-SE. In vivo, the area under the rat plasma SM concentration-time curve and the maximum plasma SM concentration were 2.4-fold and 1.9-fold higher, respectively, after oral administration of SM-SD-SEDS as compared with an aqueous SM suspension. These results illustrated the potential of using SEDS to prepare SM-SD, further improving the biopharmaceutical properties of this compound. © 2014 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/ licenses/by-nc-nd/4.0/).

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“…Supercritical fluid technologies were applied in micronization for their advantages in producing solvent-free drug particles and homogeneous size distribution. The micronized technology was proven to be feasible for hesperidin and nimodipine 29, 30 in improving bioavailability, while KW-2581 and telmisartan did not achieve the expected effect for decomposition 31, 32 . Hence, the application of micronization to herbal medicines with low solubility and bioavailability ingredients needs to be studied case by case.…”

Section: Introductionmentioning

confidence: 99%

Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers

Xing

Tan

Cheng

et al. 2017

Sci Rep

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Salvia miltiorrhiza (SM) is widely used to treat microcirculatory disturbance-related diseases; its lipophilic components play important roles in this application. Cryptotanshinone (CTS), tanshinone I (TSI) and tanshinone IIA (TSA) are the most widely-studied lipophilic ingredients, but low oral bioavailability limits their clinical application. It has been proven that micronization could improve the bioavailability of some drugs, so we’ve conducted this randomized study to investigate whether micronized granular powder (GP) of SM could improve the bioavailability of tanshinones compared with traditional decoction (TD). An oral dose of TD or GP of SM was administrated to subjects and blood samples were collected at predetermined time points. The plasma concentrations of tanshinones were detected by a validated method and pharmacokinetic parameters were calculated using a non-compartmental model. GP of SM resulted in a significant increase in mean maximum plasma concentration (C max), elimination half-life and area under concentration-time curve (AUC) of tanshinones, with the plasma AUC of CTS, TSI and TSA in GP 5–184, 4–619 and 5–130 times higher than TD. In addition, the individual variances of C max and AUC were much lower after GP administration. Summarily, tanshinones in micronized GP of SM had higher oral bioavailability and lower individual variances, thus we speculate that it may indicate a better clinical efficacy and be a better choice than current treatments.

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Solubilization of the poorly water soluble drug, telmisartan, using supercritical anti-solvent (SAS) process

Cited by 63 publications

References 33 publications

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers

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