Thermal studies of pre-formulates of metronidazole obtained by spray drying technique

Medeiros, Antonilêni F. D.; Santos, Ana Flávia Oliveira; Souza, Fábio Santos de; Júnior, Irinaldo Diniz Basílio; Valdilânio, J.; Procópio, José Valdilânio Virgulino; Santana, Davi Pereira de; Macêdo, Rui Oliveira

doi:10.1007/s10973-007-7874-5

Cited by 17 publications

(6 citation statements)

References 9 publications

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“…The benznidazole purity determination was carried by a Shimadzu® liquid chromatograph with PDA detector and software Class-VP (Kyoto, Japan). The HPLC method used is reported in scientific literature (19). The data obtained by HPLC technique was confronted to the data obtained by differential scanning calorimetry (DSC) and treated by Van't Hoff equation (20).…”

Section: Determination Of the Puritymentioning

confidence: 99%

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A Preformulation Study of a New Medicine for Chagas Disease Treatment: Physicochemical Characterization, Thermal Stability, and Compatibility of Benznidazole

Sobrinho¹,

Soares²,

Lopes³

et al. 2010

AAPS PharmSciTech

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This work aimed the studies of physicochemical characterization, thermal stability, and compatibility of benznidazole (BNZ) drug by spectroscopy (NMR, IR), thermoanalytical (differential thermal analysis, differential scanning calorimetry, and thermogravimetry), and chromatographic (HPLC) techniques, beyond the analytical tools of Van't Hoff equation and Ozawa model. The compatibility study was conducted by binary mixtures (1:1, w/w) of the drug with microcrystalline cellulose 102 and 250, anhydrous lactose, and sodium starch glycolate. The physicochemical characterization confirmed data reported in scientific literature, guaranteeing authenticity of the analyzed raw material. The drug melts at 191.68°C (∆H, 119.71 J g(-1)), characteristic of a non-polymorphic raw material, and a main stage decomposition at 233.76-319.35°C (∆m, 43.32%) occurred, ending the study with almost all mass volatilized. The quantification of drug purity demonstrated a correlation of 99.63% between the data obtained by chromatographic (99.20%) and thermoanalytical technique (99.56%). The Arrhenius equation and Ozawa model showed a zero-order kinetic behavior for the drug decomposition, and a calculated provisional validity time was 2.37 years at 25°C. The compatibility study evidenced two possible chemical incompatibilities between BNZ and the tested excipients, both associated by the authors to the reaction of the BNZ's amine and a polymer carbohydrate's carbonile, being maillard reactions. The BNZ reaction with anhydrous lactose is more pronounced than with the sodium starch glycolate because the lactose has more free hydroxyl groups to undergo reduction by the drug. In this sense, this work guides the development of a new solid pharmaceutical product for Chagas disease treatment, with defined quality control parameters and physicochemical stability.

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Section: Determination Of the Puritymentioning

confidence: 99%

“…The decomposition occurs at 178-296°C. The Ozawa's model was used in the kinetic studies evidencing a zero-order kinetic behavior (19).…”

Section: Introductionmentioning

confidence: 99%

A Preformulation Study of a New Medicine for Chagas Disease Treatment: Physicochemical Characterization, Thermal Stability, and Compatibility of Benznidazole

Sobrinho¹,

Soares²,

Lopes³

et al. 2010

AAPS PharmSciTech

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“…The structures of guanylhydrazones studied in this study are the following: Thermogravimetry (TG) and differential scanning calorimetry (DSC) are thermal techniques widely distributed and used in pharmaceutical analyses. These techniques are used in studies of drug characterization, purity, compatibility studies, polymorphism identification, stability evaluation, thermal decomposition of drugs, and development of pharmaceutical formulations [19][20][21][22][23][24][25][26].…”

Section: Introductionmentioning

confidence: 99%

Thermal characterization of some guanylhydrazones by thermal and nonthermal techniques

galvão

Brito

Dantas

et al. 2014

J Therm Anal Calorim

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2-[(3,5-di-tert-butyl-4-hydroxyphenyl)methylene]-hydrazinecarboximidamide (WE010), 2-([1,1 0 -biphenyl]-4-ylmethylene)-hydrazinecarboximidamide (WE014), and 2-[(3,4-dichlorophenyl)methylene]-hydrazinecarboximidamide (WE017) are guanylhydrazone derivatives widely studied biologically and chemically; however, there are no studies regarding their thermal behaviors. The present study aims to apply the thermal analyses: differential scanning calorimetry (DSC), differential scanning calorimetry coupled to the photovisual system (DSC-photovisual), and thermogravimetry (TG), to characterize the guanylhydrazones, as well as HPLC and FTIR. The DSC curve of WE010 shows a melting process with T onset at 190°C and peak at 193.5°C (DH 41.0 J g -1 ). Due to the symmetry of the melting peaks obtained by DSC, it is possible to calculate the purity of the sample (98.87 %). The DSC curve of WE014 shows the melting process in the range of 208-213°C, with a melting peak at 211°C (DH 61 J g -1 ).The DSC curve of WE017 showed T onset at 215°C and peak temperature of 219°C (DH 55 J g -1 ). The TG curve of WE010, WE014, and WE017 presents initial decomposition temperatures of 186.95, 197.31, and 195.44°C, respectively. The DSC-photovisual confirmed the results of DSC and TG. The HPLC determined the purities of the samples and confirmed the results of DSC. The FTIR confirmed the thermal data. Thus, the use of thermal analysis is an important tool for the characterization of molecules with therapeutic potential contributing to the characterization and evaluation of their stability as well as nonthermal technique with complementary tool.

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“…O método isotérmico termogravimétrico, associado à equação de Arrhenius (Equação 5), é comumente utilizado para acompanhar a cinética de uma reação de decomposição no estado sólido: são traçados vários gráficos de fração decomposta () versus tempo (t) mantendo constantes as temperaturas (T) na região de interesse, para uma faixa definida de perda de massa (FERNANDES et al, 1999 SANTOS-FILHO, MATOS, 2006;MEDEIROS et al, 2007;STULZER et al, 2008). Para os valores de T pico de fusão e T pico do evento de decomposição referido, deve ser observada sua pequena redução nas misturas binárias em relação aos resultados obtidos para substância avaliada isoladamente, por se tratar de uma mistura na proporção MATOS, 2006;MEDEIROS et al, 2007;SANTOS et al, 2008)  Avaliação termoanalítica das emulsões com e sem ácido fítico/kójico.…”

Section: Estudo Cinético De Decomposição Por Tg Isotérmicaunclassified

Estudo termoanalítico envolvendo estabilidade e pré-formulação de ácido fítico livre/emulsão

Daneluti¹

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Documentação do Conjunto das Químicas da USP Da ne lut i, And r é Luís M á ximo D1 7 9e Estudo termoanalítico envolvendo estabilidade e pré-formulação d e á cid o fíti co l ivr e /e mulsã o / André Luís Máximo Daneluti.-S ão P a ulo , 20 1 1. 1 1 2p. Disser tação (mestrado)-F a c uld a de de C iê nc ia s Farmacêuticas d a Uni ve r sid a de d e S ã o P a ul o. Departamento de Farmácia. O r i e n t a d o r : M a t o s , J i va l d o d o R o s á r i o 1. Cosméticos : Análise química 2. Análise térmica : Química 3. Ác id o fític o I. T. II. M a t o s , J i va l d o d o R o s á r i o , o r ie nt ad o r. 6 6 8.5 5 C DD Ao meu amigo e orientador, Prof. Dr. Jivaldo do Rosário Matos, pela acolhida e pelo crédito para a realização deste trabalho.

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Thermal studies of pre-formulates of metronidazole obtained by spray drying technique

Cited by 17 publications

References 9 publications

A Preformulation Study of a New Medicine for Chagas Disease Treatment: Physicochemical Characterization, Thermal Stability, and Compatibility of Benznidazole

A Preformulation Study of a New Medicine for Chagas Disease Treatment: Physicochemical Characterization, Thermal Stability, and Compatibility of Benznidazole

Thermal characterization of some guanylhydrazones by thermal and nonthermal techniques

Estudo termoanalítico envolvendo estabilidade e pré-formulação de ácido fítico livre/emulsão

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