Thermal analysis of lipoic acid and evaluation of the compatibility with excipientes

Moyano, María Alejandra; Broussalis, Adriana M.; Segall, Adriana Inés

doi:10.1007/s10973-009-0351-6

Cited by 35 publications

(17 citation statements)

References 27 publications

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“…These minor changes in the drug endotherm could be attributed to the presence of polymer, which lowers the drug purity. 29 This result suggests no interaction between the drug and the polymer during the preparation process.…”

Section: Microspheres For Once-and Twice-daily Administrationsmentioning

confidence: 91%

Design and <i>In Vitro</i> Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior

Bolourchian

Bahjat

2019

tjps

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Bu araştırmanın amacı, emülsiyon çözücü buharlaştırma kullanarak hazırlanan Eudragit (Eud) RL ve RS mikro küreleri ile günde bir ve iki kez uygulama için diltiazem hidroklorürün (DL) uzatılmış salım formülasyonunu geliştirmektir. Gereç ve Yöntemler: Farklı etken madde-polimer konsantrasyonlarına sahip formülasyonlar üretilmiş ve verim, enkapsülasyon etkinliği (EE), partikül büyüklüğü ve yüzey morfolojisi açısından karakterize edilmiştir. Mikrokürelerin etken madde salınımı ve termal davranışı da incelenmiştir. Seçilen mikro küreler daha sonra mikro kürelerin özelliklerini modifiye ve hızlı ilk salınımını değiştirmek için sürekli çözücü buharlaştırma yoluyla Eud RS ile kaplanmıştır. Bulgular: Sonuçlara göre, kaplanmamış mikroküreler için EE %56-%93 aralığındadır. Mikrokürelerin ortalama partikül büyüklüğü, çeşitli formülasyon değişkenlerine bağlı olarak 470 ila 1000 um'nin üzerinde olmuştur. Eud RL ve Eud RS ile hazırlanan partiküllerin ortalama ortalama partikül büyüklüğü arasında bir fark gözlenmemiştir. Mikroküreler, etken madde: polimer oranının yanı sıra partikül boyutundan etkilenen sürekli salım davranışı göstermiştir. Mikrokürelerin kaplanması sadece EE değerlerini iyileştirmemiş (%82-%92), aynı zamanda hızlı ilk çıkış yanı sıra ortalama çözünme oranınıda (MDR) azaltmıştır. Objectives: The aim of this investigation was to develop an extended release formulation of diltiazem hydrochloride (DL) for once-and twice-daily administration, based on Eudragit (Eud) RL and RS microspheres using emulsion solvent evaporation. Materials and Methods: Formulations with different drug-polymer concentrations were produced and characterized in terms of yield, encapsulation efficiency (EE), particle size, and surface morphology. The drug release and thermal behavior of the microspheres were also investigated. Selected microspheres were then coated with Eud RS by continuous solvent evaporation, in order to modify the microspheres' properties and burst release. Results: According to the results, the EE was in the range of 56%-93% for uncoated microspheres. The mean particle size of microspheres was different from 470 to above 1000 µm, based on various formulation variables. No difference was observed between the mean size of particles prepared with Eud RL and Eud RS. Microspheres showed sustained release behavior, which was affected by the drug:polymer ratio as well as particle size. Coating the microspheres not only improved the EE values (82%-92%) but also reduced the mean dissolution rate as well as the burst release. Conclusion: Microspheres prepared with DL:Eud RL ratios of 1:3 and 1:4 showed release profiles in accordance with the USP criteria for a DL extended release product for dosing every 12 and 24 h, respectively.

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Section: Microspheres For Once-and Twice-daily Administrationsmentioning

confidence: 91%

Design and <i>In Vitro</i> Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior

Bolourchian

Bahjat

2019

tjps

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“…Consequently, they identified important incompatibilities to many of the excipients analyzed. In the literature, there are many other examples of preformulation studies applying thermoanalytical techniques with strong evidences of interactions and incompatibilities [20][21][22][23].…”

Section: Introductionmentioning

confidence: 99%

“…Moyano et al [21] evaluated the thermal compatibility between lipoic acid and some cosmetic excipients obtaining suggestive results of interactions. Consequently to confirm these results, avoid misinterpretation and unreliable conclusions through the evaluation, binary mixtures were analyzed by other analytical techniques, such as IR spectroscopy and isothermal stress testing (IST) with the HPLC support.…”

Section: Introductionmentioning

confidence: 99%

“…Several reports are described in the literature to evaluate the interactions between API and excipients using thermal and non-thermal techniques, for example Fourier transformed infrared spectroscopy (FTIR), HPLC, LC-MS/TOF and LC/UV applying mathematical and statistical models to correlate and analyze the results obtained [21][22][23][24][25][26][27][28][29][30].…”

Section: Introductionmentioning

confidence: 99%

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Compatibility study between ferulic acid and excipients used in cosmetic formulations by TG/DTG, DSC and FTIR

Bezerra

Pereira

Ostrosky

et al. 2016

J Therm Anal Calorim

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Ferulic acid (4-hydroxy-3-methoxycinnamic acid) is a phytochemical constituent from the polyphenols group commonly found in whole grains, spinach, parsley, grapes and rhubarb. It has been widely applied in skin care formulations as photoprotective agent and delayer of cutaneous photoaging processes. This work aims to establish a protocol to the development of cosmetic formulations using thermoanalytical techniques (TG/DTG and DSC) and Pearson's correlation by FTIR data, in order to evaluate the compatibility between ferulic acid and excipients used in skin care formulations. The results obtained from the thermoanalytical techniques indicated compatibility between ferulic acid and the following excipients: passion fruit seed oil, Carbopol Ò Ultrez 30, EDTA, Crodabase CR2 Ò , Crodamol TM GTCC and Dow Corning Ò RM 2051. Nevertheless, the analysis also demonstrated the possibility of some interaction between ferulic acid and the following excipients: glyceryl stearate, Rapithix Ò A-60 and Optiphen Ò . To validate these results, it was demonstrated by Pearson's correlation that passion fruit seed oil, Carbopol Ò Ultrez 30, EDTA, Crodabase CR2 Ò , Crodamol TM GTCC, Dow Corning Ò RM 2051, glyceryl stearate and Rapithix Ò A-60 do not have any incompatibility that may compromise ferulic acid properties. Finally, it was also proved a meaningful incompatibility between ferulic acid and Optiphen Ò using Pearson's correlation. Thus, it is not recommended to use Optiphen Ò in the development of cosmetic formulations to carry ferulic acid.

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“…Thus, conclusions based on DSC results alone can often be misleading or inconclusive. Moreover, the presence of a solid-solid interaction does not necessarily indicate pharmaceutical incompatibility, as it might instead be advantageous, e.g., as a more desirable form of the drug delivery system [9][10][11][12][13]. Therefore, the use of other analytical techniques, such as Fourier transform infrared spectroscopy, X-ray powder diffractometry, and high performance liquid chromatography (HPLC) as complementary tools to assist in the interpretation of DSC findings is greatly advisable [14][15][16][17].…”

Section: Introductionmentioning

confidence: 99%

Study of stability and drug-excipient compatibility of estradiol and pharmaceutical excipients

Gao

Jin

Yang

et al. 2014

J Therm Anal Calorim

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Estradiol (E 2 ) is the main drug used in menopause therapy. This study aimed to evaluate the drugexcipient compatibility of binary mixtures (BMs) (1:1 BMs, w/w), initially by differential scanning calorimetry (DSC), and subsequently, by complementary techniques such as X-ray powder diffraction (XRPD) and high performance liquid chromatography (HPLC) if there was any evidence of interaction. The samples were stored under accelerated stability conditions (40°C at 75 % relative humidity). The DSC curves of estradiol and the BMs with excipients (corn starch, lactose, xanthan gum, microcrystalline cellulose, magnesium stearate, dibasic calcium phosphate, and talc) were obtained. The results show that estradiol was compatible with all the selected excipients. XRPD and HPLC analysis were instrumental in interpreting the DSC results and excluding relevant pharmaceutical incompatibilities in all cases. Overall, the compatibility of the selected excipients with estradiol was successfully evaluated using a combination of thermal and spectroscopic methods, and the formulations developed using the compatible excipients were found to be stable.

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Thermal analysis of lipoic acid and evaluation of the compatibility with excipientes

Cited by 35 publications

References 27 publications

Design and <i>In Vitro</i> Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior

Design and <i>In Vitro</i> Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior

Compatibility study between ferulic acid and excipients used in cosmetic formulations by TG/DTG, DSC and FTIR

Study of stability and drug-excipient compatibility of estradiol and pharmaceutical excipients

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