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Doina Piciu - One of the best experts on this subject based on the ideXlab platform.
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Thermal stability of synthetic thyroid hormone l-thyroxine and l-thyroxine sodium salt hydrate both pure and in pharmaceutical Formulations.
Journal of pharmaceutical and biomedical analysis, 2016Co-Authors: Ionuţ Ledeţi, Adriana Ledeţi, Gabriela Vlase, Titus Vlase, Petru Matusz, Vasile Bercean, Lenuţa-maria Şuta, Doina PiciuAbstract:In this paper, the thermal stability of pure l-thyroxine (THY) and l-thyroxine sodium salt hydrate (THYSS) vs. two pharmaceutical Solid Formulations commercialized on both Romanian and European market (with a content of 100μg, respectively 200μg THYSS per tablet) were investigated. In order to determine whether the presence of excipients affects the thermal stability of the active pharmaceutical ingredient (API), the preliminary study of thermal stability in air atmosphere was completed with an in-depth Solid-state kinetic study. By kinetic analysis, the non-isothermal degradation of the selected active pharmaceutical ingredients vs. the Solid Formulation with strength of 200μg THYSS per tablet was investigated. Isoconversional methods (Kissinger-Akahira-Sunose, Flynn-Wall-Ozawa and Friedman) were employed for the estimation of activation energies values, at five different heating rates, β=5, 7, 10, 12 and 15°Cmin(-1). Also, a fourth method was applied in the processing of data, namely NPK, allowing an objective separation in the physical and chemical processes that contribute to the thermal degradation of the selected compounds. A discussion of thermal stability from the kinetic point of view is also presented.
Todd E. Shelly - One of the best experts on this subject based on the ideXlab platform.
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Capture of Bactrocera fruit flies in traps baited with liquid versus Solid Formulations of male lures in Malaysia
Journal of Asia-Pacific Entomology, 2013Co-Authors: Suk-ling Wee, Todd E. ShellyAbstract:Abstract Approximately 70 species of Bactrocera fruit flies (Diptera: Tephritidae) are polyphagous economic pests that attack many important agricultural crops. Several of these Bactrocera species are also highly invasive, and many countries operate continuous, large-scale trapping programs to detect incipient infestations. Detection programs rely heavily on traps baited with male lures, with males of some species responding to raspberry ketone (RK; or its synthetic analogue cue-lure [CL]) and males of other species responding to methyl eugenol (ME). These lures (plus naled, an insecticide) are currently applied as liquids, although this procedure is time-consuming and may expose workers to health risks. Recent field tests, conducted largely in Hawaii, have shown that traps baited with a Solid Formulation (termed a wafer) that contains both RK and ME (plus dichlorvos, an insecticide) capture as many or more B . dorsalis (Hendel) and B . cucurbitae (Coquillett) males as traps baited with the standard liquid lures. While these results are promising, a more complete evaluation of the Solid Formulation requires testing in a region with a diverse assemblage of Bactrocera species, since interspecific variation in male response to lures has been reported. The objective of the present investigation was to assess the relative effectiveness of liquid versus Solid Formulations of male lures in Malaysia, a country known to harbor a large assemblage of Bactrocera species. Based on a 12-week sampling period, we found that, contrary to the Hawaiian results, traps baited with the wafer captured significantly fewer males than traps baited with liquid lures for all five ME-responding taxa analyzed and for one of the three RK/CL-responding species analyzed. Possible explanations for the discrepancy between these and earlier findings are offered.
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Field Capture of Male Melon Flies, Bactrocera cucurbitae (Coquillett), in Jackson Traps Baited with Cue-Lure Versus Raspberry Ketone Formate in Hawaii
2012Co-Authors: Todd E. Shelly, Rick Kurashima, Jon I. NishimotoAbstract:The melon fly, Bactrocera cucurbitae (Coquillett), is an invasive worldwide pest of vegetables, particularly various species of squashes and melons. Because it poses a serious economic threat, many countries operate continuous trapping programs to detect incipient infestations. Detection currently relies on traps baited with a chemical (cue-lure, CL) that is attractive to males of this species. Earlier research suggested that a chemically similar compound (raspberry ketone formate, RKF) is more attractive than CL and thus might improve surveillance efforts. The present study describes the results of field experiments in Hawaii that compare captures of B. cucurbitae males in traps baited with (1) CL liquid versus a Solid Formulation (so-called plugs) of RKF or (2) CL liquid versus RKF liquid. In the first experiment, the traps with CL liquid captured more males than traps baited with RKF plugs in three of the four study sites, with no difference observed between lures at the remaining area. In the second experiment, the traps baited with CL liquid captured more males than traps baited with RKF liquid at two of the four study areas, with no difference observed between lures at the remaining two sites. The discrepancy between earlier studies and the present one highlights the need for additional field testing of RKF to assess its value as a replacement for CL.
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Capture of Bactrocera fruit flies (Diptera: Tephritidae) in traps baited with liquid versus Solid Formulations of male lures
Journal of Asia-Pacific Entomology, 2011Co-Authors: Todd E. Shelly, Rick Kurashima, Jon I. Nishimoto, A. Diaz, J. Leathers, Mamadou War, D. JosephAbstract:Bactrocera dorsalis (Hendel) and B. cucurbitae (Coquillett) (Diptera: Tephritidae) are important agricultural pests of the Pacific region. Detection and control of these species rely largely on traps baited with malespecific attractants (parapheromones), namely methyl eugenol for B. dorsalis and cue lure for B. cucurbitae. Presently, these lures (plus naled, an insecticide) are applied in liquid form, although this procedure is timeconsuming, and naled as well as methyl eugenol may pose human health risks. Recently, a Solid Formulation (termed a wafer) has been developed that contains both male lures (plus DDVP, an insecticide), and here we present data from field tests in California and Hawaii that compare the effectiveness of liquid versus Solid Formulations of the lures in capturing marked, released males of these two Bactrocera species. For both species and in both California and Hawaii, traps baited with the Solid Formulation of the male lure captured similar or significantly more released flies than the liquid Formulation for both fresh and aged baits. Traps in Hawaii also captured wild (unmarked) males of both B. dorsalis and B. cucurbitae, and the results obtained for wild flies were similar to those recorded for released flies for both species. Collectively, the results presented suggest that the Solid dispenser of the male lures constitutes a reliable substitute for the liquid Formulation in detecting incipient Bactrocera outbreaks.
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Capture of Bactrocera Males (Diptera: Tephritidae) in Parapheromone-Baited Traps: A Comparison of Liquid versus Solid Formulations
2010Co-Authors: Todd E. ShellyAbstract:Bactrocera cucurbitae (Coquillett) and B. dorsalis (Hendel) (Diptera: Teph- ritidae) are important agricultural pests of the Pacific region. Detection and control of these species rely largely on traps baited with male-specific attractants (paraphero - mones), namely cue lure for B. cucurbitae and methyl eugenol for B. dorsalis. Pres- ently, these lures (plus naled, an insecticide) are applied in liquid form, although this procedure is time-consuming, and naled as well as methyl eugenol may pose human health risks. Recently, a Solid Formulation (termed a wafer) has been developed that contains both chemicals (plus DDVP, an insecticide), and here we present data from field tests that compare the effectiveness of liquid versus Solid Formulations of the lures in attracting males of these two Bactrocera species. Trapping in two areas of Oahu, Hawaii, yielded consistent results: Jackson traps baited with wafers captured (1) similar numbers of B. cucurbitae males and (2) significantly greater numbers of B. dorsalis males than Jackson traps baited with standard liquid lures. Additional tests examined the effect of ageing on the attractiveness of the wafers and revealed that Jackson traps baited with wafers aged for 6 or 8 weeks captured similar or significantly more males of both Bactrocera species than Jackson traps baited with fresh liquid lures.
Seh Hyon Song - One of the best experts on this subject based on the ideXlab platform.
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Solid Formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability
Oncotarget, 2017Co-Authors: Dong Woo Yeom, Bo Ram Chae, Jin Han Kim, Jun Soo Chae, Dong Jun Shin, Chang Hyun Kim, Sung Rae Kim, Ji Ho Choi, Seh Hyon SongAbstract:// Dong Woo Yeom 1, * , Bo Ram Chae 1, 2, * , Jin Han Kim 1 , Jun Soo Chae 1 , Dong Jun Shin 1 , Chang Hyun Kim 1 , Sung Rae Kim 1 , Ji Ho Choi 1 , Seh Hyon Song 2 , Dongho Oh 2 , Se Il Sohn 2 and Young Wook Choi 1 1 College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of Korea 2 Daewon Pharm. Co., Ltd, Seoul 04994, Republic of Korea * These authors have contributed equally to this work Correspondence to: Young Wook Choi, email: ywchoi@cau.ac.kr Keywords: valsartan; SMEDDS; Solid carrier; tablet; optimization Received: June 27, 2017 Accepted: September 20, 2017 Published: October 09, 2017 ABSTRACT In order to improve the dissolution and oral bioavailability of valsartan (VST), and reduce the required volume for treatment, we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) composed of VST (80 mg), Capmul ® MCM (13.2 mg), Tween ® 80 (59.2 mg), Transcutol ® P (59.2 mg), and Poloxamer 407 (13.2 mg). In the present study, by using Florite ® PS-10 (119.1 mg) and Vivapur ® 105 (105.6 mg) as Solid carriers, VST-loaded Solidified SuSMEDDS (S-SuSMEDDS) granules were successfully developed, which possessed good flow properties and rapid drug dissolution. By introducing croscarmellose sodium (31 mg) as a superdisintegrant, S-SuSMEDDS tablets were also successfully formulated, which showed fast disintegration and high dissolution efficiency. Preparation of granules and tablets was successfully optimized using D-optimal mixture design and 3-level factorial design, respectively, resulting in percentage prediction errors of
Dong Woo Yeom - One of the best experts on this subject based on the ideXlab platform.
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Solid Formulation of a supersaturable self-microemulsifying drug delivery system for valsartan with improved dissolution and bioavailability
Oncotarget, 2017Co-Authors: Dong Woo Yeom, Bo Ram Chae, Jin Han Kim, Jun Soo Chae, Dong Jun Shin, Chang Hyun Kim, Sung Rae Kim, Ji Ho Choi, Seh Hyon SongAbstract:// Dong Woo Yeom 1, * , Bo Ram Chae 1, 2, * , Jin Han Kim 1 , Jun Soo Chae 1 , Dong Jun Shin 1 , Chang Hyun Kim 1 , Sung Rae Kim 1 , Ji Ho Choi 1 , Seh Hyon Song 2 , Dongho Oh 2 , Se Il Sohn 2 and Young Wook Choi 1 1 College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of Korea 2 Daewon Pharm. Co., Ltd, Seoul 04994, Republic of Korea * These authors have contributed equally to this work Correspondence to: Young Wook Choi, email: ywchoi@cau.ac.kr Keywords: valsartan; SMEDDS; Solid carrier; tablet; optimization Received: June 27, 2017 Accepted: September 20, 2017 Published: October 09, 2017 ABSTRACT In order to improve the dissolution and oral bioavailability of valsartan (VST), and reduce the required volume for treatment, we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) composed of VST (80 mg), Capmul ® MCM (13.2 mg), Tween ® 80 (59.2 mg), Transcutol ® P (59.2 mg), and Poloxamer 407 (13.2 mg). In the present study, by using Florite ® PS-10 (119.1 mg) and Vivapur ® 105 (105.6 mg) as Solid carriers, VST-loaded Solidified SuSMEDDS (S-SuSMEDDS) granules were successfully developed, which possessed good flow properties and rapid drug dissolution. By introducing croscarmellose sodium (31 mg) as a superdisintegrant, S-SuSMEDDS tablets were also successfully formulated, which showed fast disintegration and high dissolution efficiency. Preparation of granules and tablets was successfully optimized using D-optimal mixture design and 3-level factorial design, respectively, resulting in percentage prediction errors of
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Fujicalin^®-based Solid supersaturable self-emulsifying drug delivery system (S-SEDDS) of tacrolimus for enhanced dissolution rate and oral absorption
Journal of Pharmaceutical Investigation, 2015Co-Authors: Dae Ro Lee, Dong Woo Yeom, Young Han Kim, Keun Won Park, Hyuck Jun Jung, Ha Ra Cho, Jun Seo Park, Yong Seok Choi, Young Wook Choi, Myung Joo KangAbstract:The aim of the study was to formulate the Solid dosage form of the supersaturable self-emulsifying drug delivery system (S-SEDDS) for tacrolimus, a poorly water-soluble immunosuppressant, to enhance the dissolution rate and oral absorption. A Solid Formulation was prepared by adsorbing the liquid S-SEDDS onto porous carriers including Fujicalin^® (dibasic calcium phosphate). Macroscopic observation using scanning electron microscopy and drug crystallinity determination using X-ray powder diffraction revealed that the calcineurin inhibitor was effectively held within the intact porous carriers in a solubilized form. In an in vitro dissolution test in simulated gastric fluid (pH 1.2), there were no remarkable differences in the release rate and extent of dissolution between liquid and Fujicalin^®-based Solid S-SEDDS, achieving over 90 % drug release after 15 min. Moreover, the pharmacokinetic parameters for tacrolimus in the liquid and Fujicalin^®-based Solid S-SEDDS after oral administration at a dose of 5 mg/kg were statistically equivalent in rats ( p > 0.05). This study suggests that Solidification of liquid S-SEDDS using Fujicalin^®, a soluble adsorbent in acidic medium, can be a promising approach to obtain the free-flowing powder form of liquid S-SEDDS while preserving the high and fast dissolution rate of the liquid self-emulsifying system.
Yukiko Yasuhara - One of the best experts on this subject based on the ideXlab platform.
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visualization of protonation deprotonation of active pharmaceutical ingredient in Solid state by vapor phase amine selective alkyne tagging and raman imaging
Journal of Pharmaceutical Sciences, 2017Co-Authors: Kei Moriyama, Yukiko YasuharaAbstract:Abstract Here, we report a simple and direct method to visualize the protonation/deprotonation of an amine active pharmaceutical ingredient (API) in the Solid state using a Solid-vapor reaction with propargyl bromide and Raman imaging for the assessment of the API during the manufacturing process of Solid Formulations. An alkyne tagging occurred on the free form of Solid haloperidol by the vapor phase reaction, and a distinct Raman signal of alkyne was detected. Alkyne signal monitoring by Raman imaging enabled us to visualize the distribution of the free-form haloperidol in a Solid Formulation. On the other hand, haloperidol hydrochloride did not react with propargyl bromide in the Solid-vapor reaction, and the alkyne signal was not observed. Using the difference in reactivity, the protonation/deprotonation of the amine API in the Solid state could be visualized. As an example of application, we tried to visually assess the protonation/deprotonation state when the free-form haloperidol was ground with acids using the Solid-vapor reaction and Raman imaging and found that haloperidol was partially protonated when ground with 2 equivalents of hydrogen chloride. Furthermore, we demonstrated the relationship between the degree of protonation and the amount of water added as a medium for grinding haloperidol with succinic acid.
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Visualization of Protonation/Deprotonation of Active Pharmaceutical Ingredient in Solid State by Vapor Phase Amine-Selective Alkyne Tagging and Raman Imaging
Journal of pharmaceutical sciences, 2017Co-Authors: Kei Moriyama, Yukiko Yasuhara, Hiromi OtaAbstract:Here, we report a simple and direct method to visualize the protonation/deprotonation of an amine active pharmaceutical ingredient (API) in the Solid state using a Solid-vapor reaction with propargyl bromide and Raman imaging for the assessment of the API during the manufacturing process of Solid Formulations. An alkyne tagging occurred on the free form of Solid haloperidol by the vapor phase reaction, and a distinct Raman signal of alkyne was detected. Alkyne signal monitoring by Raman imaging enabled us to visualize the distribution of the free-form haloperidol in a Solid Formulation. On the other hand, haloperidol hydrochloride did not react with propargyl bromide in the Solid-vapor reaction, and the alkyne signal was not observed. Using the difference in reactivity, the protonation/deprotonation of the amine API in the Solid state could be visualized. As an example of application, we tried to visually assess the protonation/deprotonation state when the free-form haloperidol was ground with acids using the Solid-vapor reaction and Raman imaging and found that haloperidol was partially protonated when ground with 2 equivalents of hydrogen chloride. Furthermore, we demonstrated the relationship between the degree of protonation and the amount of water added as a medium for grinding haloperidol with succinic acid.