共查询到20条相似文献,搜索用时 31 毫秒
1.
Rahul B. Chavan Nalini R. Shastri 《Journal of Thermal Analysis and Calorimetry》2018,131(3):2129-2139
Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, and hot-stage microscopy were employed to evaluate the drug–excipient compatibility of atovaquone with commonly used tablet excipients. The DSC curves of pure drug and excipients were compared with their physical mixtures. Microcrystalline cellulose, titanium dioxide, colloidal silica, ferric oxide, lactose monohydrate, and sodium starch glycolate were compatible, while magnesium stearate, polyethylene glycol (PEG) 8000, Poloxamer 188, and hydroxypropyl methyl cellulose (HPMC) E15 showed incompatibility with the drug. Heat–cool–heat analysis of the physical and the ground mixture of later three excipients showed polymorphic transformation of atovaquone form III to form I, which occurred via amorphization with HPMC E15 and through solubilization mechanism with remaining two excipients. These outcomes were further supported by hot-stage microscopy. Results of milling experiments revealed a milling time-dependent polymorphic transformation and solubilization with HPMC E15 and PEG 8000, respectively. This study highlights the importance of compatibility assessment for selection of excipients in specific unit operations such as milling and grinding. 相似文献
2.
H. K. Stulzer P. O. Rodrigues T. M. Cardoso J. S. R. Matos M. A. S. Silva 《Journal of Thermal Analysis and Calorimetry》2008,91(1):323-328
Captopril (CAP) was the first commercially available angiotensine-converting enzyme (ACE) inhibitor. In the anti-hypertensive
therapy is considered the selected drug has to be therapeutically effective together with reduced toxicity. CAP is an antihypertensive
drug currently being administered in tablet form. In order to investigate the possible interactions between CAP and excipients
in tablets formulations, differential scanning calorimetry (DSC) and thermogravimetric (TG) analysis completed by X-ray powder
diffraction (XRPD) and Fourier transform infrared spectroscopy (FTIR) were used for compatibility studies. A possible drug-excipient
interaction was observed with magnesium stearate by DSC technique. 相似文献
3.
Adina Magdalena Musuc Mihaela Badea-Doni Luiza Jecu Adriana Rusu Vlad Tudor Popa 《Journal of Thermal Analysis and Calorimetry》2013,113(1):169-177
The purpose of this research study was evaluation of the utility of two common multivariate techniques, agglomerative cluster analysis (CA) and principal component analysis (PCA), as supplementary means of detecting incompatibilities, which can occur between active pharmaceutical ingredients and excipients at the preformulation stage of a solid dosage form. For the detection of incompatibilities between atenolol (beta blocker) and selected excipients (mannitol, lactose, starch, methylcellulose, β-cyclodextrin, meglumine, chitosan, polyvinylpyrrolidone and magnesium stearate), the thermogravimetry (TG), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) were chosen. The results have shown that compatibility between atenolol and an excipient can be identified in a CA dendrogram by two large clusters, from which one groups an excipient and physical mixtures with a high concentration of the excipient. Another cluster encompasses atenolol and mixtures with a high content of the drug. In the PCA plot, all samples are located along the first principal component axis (PC1), beginning from a single component located with the most negative PC1 value, through mixtures with gradually varying concentration of both ingredients, till the second component located close to the most positive PC1 values. The results have shown that CA and PCA fulfil their role as supporting techniques in the interpretation of the data acquired from the TG curves, and the obtained data are compatible with the results of DSC and FTIR analyses. 相似文献
4.
C. D. Bertol A. P. Cruz H. K. Stulzer F. S. Murakami M. A. S. Silva 《Journal of Thermal Analysis and Calorimetry》2010,102(1):187-192
Primaquine (PQ) is the drug of choice for the radical cure of Plasmodium vivax malaria, and currently being administered in solid dosage form. In this study, the compatibility studies were carried out
using differential scanning calorimetry (DSC), thermogravimetry (TG), and fourier transformed infrared (FT-IR). Non-isothermal
and isothermal methods were employed to investigate kinetic parameters under nitrogen and air atmospheres using TG. The DSC
investigations obtained by physical mixtures showed slight alterations in the melting temperatures of PQ with some excipients.
The FT-IR confirmed the possible interactions obtained by DSC for the physical mixtures with PQ and lactose, magnesium stearate
and mannitol. The results showed that the thermal decomposition followed a zero order kinetic in both atmospheres in non-isothermal
method. The activation energy in both methods using nitrogen atmosphere was similar, and in air atmosphere the activation
energy decreased. 相似文献
5.
D. Abbas J. Kaloustian C. Orneto P. Piccerelle H. Portugal A. Nicolay 《Journal of Thermal Analysis and Calorimetry》2008,93(2):353-360
The 4,6-bis[2′(diethylamino)ethoxy]2,8,10-trimethylpyrido[3,2-g]quinoline (BG 637) is one of the compound from the pyrido[3,2-g] quinolines
family. This compound had in vitro activity against the resistant cells and can reverse the multidrug resistance developed
during the chemotherapeutic treatments.
To characterize BG 637, techniques such as differential scanning calorimetry (DSC), Fourier transform infrared spectrometer
(FTIR), ultra violet spectrophotometry (UV), gas chromatography coupled with mass spectrometry (GC/MS), nuclear magnetic resonance
(NMR) and X-ray powder diffraction (XRPD) were used. Several of them were also used to show the stability of the drug during
various storage conditions.
DSC, FTIR and UV were used as screening techniques for assessing the compatibility of BG 637 with several commonly used pharmaceutical
excipients. We compared the properties of the pure drug with those of binary mixture drug/excipient. Studied excipients were
lactose monohydrate, microcrystalline cellulose, polyvinylpyrrolidone, sodium croscarmellose and magnesium stearate. Melting
temperature and enthalpy of BG 637 in binary mixtures were similar to theoretical values. These results showed that BG 637
is a very stable compound and compatible with several pharmaceutical excipients. 相似文献
6.
M. Łaszcz B. Kosmacińska K. Korczak B. Śmigielska M. Glice W. Maruszak A. Groman H. Beczkowicz Ł. Żelazko 《Journal of Thermal Analysis and Calorimetry》2007,88(2):305-310
Differential scanning calorimetry and thermogravimetric
analysis with the support of X-ray powder diffraction and infrared spectroscopy
were used as screening techniques for the compatibility testing of imatinib
mesylate, with following excipients: magnesium stearate, polyvinylpyrrolidone,
microcrystalline cellulose. In order to maximize the probability of interactions
1:1 (by mass) drug: excipient binary mixtures were analysed and compared to
individual components. Additionally an influence of storage at temperatures
of 25 and 40°C on physico-chemical stability on drug – excipient
binary mixtures was investigated.
The largest visible changes
were observed in the DSC curves of imatinib mesylate – magnesium stearate
mixtures. 相似文献
7.
S. Shantikumar G. Sreekanth K. V. SurendraNath S. JaferValli N. Satheeshkumar 《Journal of Thermal Analysis and Calorimetry》2014,115(3):2423-2428
Differential scanning calorimetry (DSC) is a primary technique for measuring the thermal properties of materials, which reflects the physico-chemical properties of drug substances. In the present study, it is used as a screening technique for assessing the compatibility of sitagliptin with some currently employed pharmaceutical excipients. The influence of processing conditions and their effects (simple blending, co-grinding or kneading) on drug stability was evaluated. Sitagliptin showed a sharp endothermic peak at 212.1 °C with an enthalpy change of 131.5 J g?1 indicating melting of drug. Facile transformation of dehydrated sitagliptin to monohydrate form was observed in some mixtures, disappearance of sharp melting endothermic peak of sitagliptin was observed in some mixtures. On the basis of DSC results, sitagliptin was found to be compatible with micro crystalline cellulose, croscarmellose, and pregelatinized starch. Some excipient interaction was observed with magnesium stearate, ascorbic acid, and citric acid. X-ray diffractometry and FT-IR were used as supportive tools in interpreting the DSC results. Overall, the excipients selected were compatible with the API and the mixtures are stable within the tested conditions. These results would be useful for formulation development of the film coated tablets of sitaglitptin. 相似文献
8.
Tamíris A. Júlio Igor F. Zâmara Jerusa S. Garcia Marcello G. Trevisan 《Journal of Thermal Analysis and Calorimetry》2013,111(3):2037-2044
The evaluation of sildenafil citrate (SC), the best-selling drug for treatment of impotence, for compatibility with various excipients was investigated using thermal and isothermal stress testing. Differential scanning calorimetry (DSC), hot-stage microscopy (HSM) and liquid chromatography (LC) with ultraviolet detection were successfully employed to investigate the compatibility between SC and various excipients commonly used in solid form in the pharmaceutical industry. The studies were performed using 1:1 (m/m) drug/excipient physical mixtures and samples were stored under accelerated stability conditions (40 °C at 75% relative humidity). All excipients tested (such as colloidal silicon dioxide, croscarmellose sodium, lactose, mannitol and sucrose) showed potential incompatibilities by DSC and LC analysis after accelerated stability testing. However, some incompatibilities were not detected by the DSC method and were observed only when LC analysis was performed. HSM was able to differentiate active pharmaceutical ingredient degradation from solubilisation, supporting the interpretation of DSC in excipients where thermal events either overlapped or disappeared. The combination of both the analytical techniques (DSC and LC) and use of a stability chamber is extremely helpful in detecting incompatibilities and providing more robust and accurate approaches for pre-formulation studies. 相似文献
9.
Naiana G. P. B. Lima Igor P. B. Lima Denise M. C. Barros Thays S. Oliveira Fernanda N. Raffin Túlio F. A. de Lima e Moura Ana C. D. Medeiros Ana P. B. Gomes Cícero F. S. Aragão 《Journal of Thermal Analysis and Calorimetry》2014,115(3):2311-2318
Psoralens are widely used for the treatment of psoriasis. Trioxsalen is a drug prescribed low-dose, belonging to the group of substituted psoralen. The aim of this study was to evaluate the compatibility of trioxsalen with pharmaceutical excipients used in the solid forms by analytical techniques. Binary mixtures between the trioxsalen and pharmaceutical excipients (namely, magnesium stearate, α-lactose, microcrystalline cellulose 102, pregelatinized starch, mannitol, sodium lauryl sulfate, sodium starch glycolate, and croscarmellose sodium) were examined. The trioxsalen–sodium lauryl sulfate mixture displayed some physical interaction based on the DTA and DSC results, but the FTIR study ruled out any chemical change. 相似文献
10.
The thermal techniques of analysis were used to assess the compatibility between ibuprofen (IB) and some excipients used in
the development of extended released formulations. This study is a part of a systematic study undertaken to find and optimizes
a general method of detecting the drug–excipient interactions, with the aim of predicting rapidly and assuring the long-term
stability of pharmaceutical product and speeding up its marketing. The thermal properties of IB and its physical association
as binary mixtures with some common excipients were evaluated by thermogravimetry/derivative thermogravimetry (TG/DTG) and
differential scanning calorimetry. FT-IR spectroscopy and X-ray powder diffraction (XRPD) were used as complementary techniques
to adequately implement and assist in interpretation of the thermal results. Based on their frequent use in preformulations
nine different excipients: starch; microcrystalline cellulose (PH 101 and PH 102); colloidal silicon dioxide; lactose (monohydrate
and anhydre); polyvinylpyrrolidone; magnesium stearate and talc were blended with IB. The samples were prepared by mixing
the analyte and excipients in a proportion of 1:1 (w:w). The TG/DSC curves of the IB have shown a single stage of mass loss
between 175 and 290 °C, respectively, an endothermic peak at 78.5 °C, which corresponds to the melting (literature T
m = 75–78 °C). 相似文献
11.
Z. Aigner R. Heinrich E. Sipos G. Farkas A. Ciurba O. Berkesi P. Szabó-Révész 《Journal of Thermal Analysis and Calorimetry》2011,104(1):265-271
The compatibility of aceclofenac with various tableting excipients was investigated by means of differential scanning calorimetry
(DSC) and Fourier transform infrared spectroscopy (FT-IR). The excipients applied in the direct pressing retard tablets were
Carbopol 940, hydroxypropyl-methyl-cellulose, microcrystalline cellulose, Aerosil 200 and magnesium stearate. The ingredients
alone and their 1:1 (w/w) binary mixtures were investigated before and after accelerated storage. An interaction was observed
only between aceclofenac and magnesium stearate. The DSC and FT-IR examinations indicated formation of the magnesium salt
of aceclofenac. For the other mixtures, there was no incompatibility between the components. 相似文献
12.
Nihar Ranjan Pani Lila Kanta Nath Sujata Acharya Biswanath Bhuniya 《Journal of Thermal Analysis and Calorimetry》2012,108(1):219-226
Experiments were done to assess the compatibility of nateglinide (NTG) with selected excipients in the development of immediate
release tablets of NTG by thermal and isothermal stress testing (IST) techniques. To evaluate the drug excipient compatibility,
different techniques such as differential scanning calorimetric (DSC) study, infrared (IR) spectrophotometric study, and IST
were adopted. The results of DSC study showed that magnesium stearate exhibited some interaction with NTG. However, the results
of IR and IST studies showed that all the excipients used in the formula were compatible with NTG. The optimized formulation
developed using the compatible excipients were found to be stable after 3 months of accelerated stability studies (40 ± 2 °C
and 75 ± 5% RH). Overall, compatibility of excipients with NTG was successfully evaluated using the combination of thermal
and IST methods and the formulations developed using the compatible excipients was found to be stable. 相似文献
13.
Bogdan Tita Ionut Ledeti Geza Bandur Dumitru Tita 《Journal of Thermal Analysis and Calorimetry》2014,118(2):1293-1304
Thermal analysis is a routine method for analysis of drugs and substances of pharmaceutical interest. Thermogravimetry/derivative thermogravimetry (TG/DTG) and differential scanning calorimetry (DSC) are thermoanalytical methods which offer important information about the physical and chemical properties of drugs (purity, stability, phase transition, polymorphism, compatibility, kinetic analysis, etc.). This work exemplifies a general method of studying the drug-excipient interactions with the aim of predicting rapidly and inexpensively the long thermal stability of their mixtures. The TG/DTG and DSC were used as screening techniques for assessing the compatibility between indomethacin (IND) and its physical associations as binary mixtures with some common excipients. Based on their frequent use in preformulations eleven different excipients: corn starch, microcrystalline cellulose (PH 101; PH 102), colloidal silicon dioxide, lactose (monohydrate and anhydre), polyvinilpyrrolidone K30, magnesium stearate, talc, stearic acid, and manitol were blended with IND. The samples were prepared by mixing the analyte and excipients in a proportion of 1:1 (w:w). In order to investigate the possible interactions between the components, the thermal curves of IND and each selected excipient were compared with those of their 1:1 (w/w) physical mixtures. FT-IR spectroscopy and X-ray powder diffraction were used as complementary techniques to adequately implement and assist in interpretation of thermal results. On the basis of thermal results, confirmed by FT-IR and X-ray analyses, a possible interaction was found between IND with polyvinylpyrrolidone K30, magnesium stearate, and stearic acid. 相似文献
14.
Fátima Duarte Freire C. Flávio Soares Aragão T. Flávio Accioly de Lima e Moura Fernanda Nervo Raffin 《Journal of Thermal Analysis and Calorimetry》2009,97(1):355-357
Chlorpropamide ((4-chloro-N-(propylamino)-carbonyl)-benzenesulfonamide) belongs to compounds having sulfonylurea group and is widely used as an oral
antidiabetic agent. In this work differential scanning calorimetry (DSC) was used during pre-formulation of chlorpropamide
tablets to determine the drug-excipients compatibility. The DSC curves of chlorpropamide and binary mixtures with excipients
(sodium croscarmellose, sodium lauryl sulfate, microcrystalline cellulose, magnesium stearate and calcium carbonate) showed
that chlorpropamide exhibited interaction with magnesium stearate and sodium lauryl sulfate. The binary mixtures of chlorpropamide–magnesium
stearate presented a single endothermic process at 96–108 °C and chlorpropamide–sodium lauryl sulfate showed a wide endotherm
at 99–120 °C. 相似文献
15.
Isabela P. Veronez Josiane S. P. Daniel Jerusa S. Garcia Marcello G. Trevisan 《Journal of Thermal Analysis and Calorimetry》2014,115(3):2407-2414
Desloratadine (DL) is a selective antagonist of the histamine H1 receptor, which has been widely used to treat allergic symptoms, and stands out from other drugs in this therapeutic class because it does not cause sedative effects. In the present study, the physico-chemical properties of DL were fully characterized using six analytical techniques such as Differential Scanning Calorimetry (DSC), Thermogravimetric analysis (TG/DTG), Fourier transform infrared spectroscopy (FT-IR), Raman spectroscopy, Powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The DSC curve shows a sharp endothermic event at 158.4 °C, and the TG/DTG curve presents two decomposition events between 178.4 and 451.9 °C. A compatibility study involving DL and nine pharmaceutical excipients generally used in pharmaceutical formulations was performed. Physical binary mixtures of DL with each excipient were prepared in a 1:1 (w/w) ratio. After preparation, the samples were analyzed immediately and the results reveal solid-state interaction with anhydrous lactose, microcrystalline cellulose, magnesium stearate, and stearic acid. 相似文献
16.
J. P. Sousa e Silva J. M. Sousa Lobo 《Journal of Thermal Analysis and Calorimetry》2010,102(1):317-321
Study of excipients incompatibility with drugs in an early phase of pharmaceutical development is still a persistent difficulty
within the pharmaceutical industry. We examine here the compatibility between an experimental drug (nebicapone) and common
excipients using differential scanning calorimetry (DSC), high sensitivity DSC (HSDSC) and a conventional heat stress test.
The results obtained indicate that nebicapone may be compatible with lactose monohydrate and sodium croscarmellose but is
incompatible with magnesium stearate. This study concludes that HSDSC, in stepwise isothermal mode, may be used as a potential
tool for detecting excipient incompatibilities. 相似文献
17.
Edilene Pereira Lavor Marco Vinícius M. Navarro Fátima D. Freire Cícero F. S. Aragão Fernanda Nervo Raffin Euzébio Guimarães Barbosa Túlio F. A. de Lima e Moura 《Journal of Thermal Analysis and Calorimetry》2014,115(3):2303-2309
First-line drugs (rifampicin, RIF; isoniazid, INH; ethambutol, ETA; and pyrazinamide, PZA) recommended in conventional treatment of tuberculosis were analyzed in 1:1 w/w binary mixtures with microcrystalline cellulose MC 101 (CEL) and lactose supertab® (LAC) by differential scanning calorimetry (DSC), thermogravimetry (TG), differential thermal analysis (DTA), and Fourier transformed infrared analysis (FTIR) as part of development of fixed dose combination (FDC) tablets. Evidence of interaction between drug and pharmaceutical excipients was supposed when peaks disappearance or shifting were observed on DTA and DSC curves, as well as decreasing of decomposition temperature onset and TG profiles, comparing to pure species data submitted to the same conditions. LAC was showed to interact with RIF (absence of drug fusion and recrystallization events on DSC/DTA curves); INH (thermal events of the mixtures different from those observed for drug and excipient pure in DSC/DTA curves); PZA (decrease on drug fusion peak in DSC/DTA curves), and ETA (shift on drug onset fusion and absence of pure LAC events on DSC/DTA curves). In all cases, an important decrease on the temperature of drug decomposition was verified for the mixtures (TG analysis). However, FTIR analysis showed good correlation between theoretical and experimental drug-LAC spectra except for INH–LAC mixture, evidencing high incompatibility between these two species and suggesting that those interactions with PZA and RIF were thermally induced. No evidence of incompatibilities in CEL mixtures was observed to any of the four-studied drugs. 相似文献
18.
L. S. Bernardi P. R. Oliveira F. S. Murakami M. A. S. Silva S. H. M. Borgmann S. G. Cardoso 《Journal of Thermal Analysis and Calorimetry》2009,97(2):729-733
The thermal analytical study of venlafaxine hydrochloride, a third generation antidepressant, was investigated using thermogravimetry
(TG) and differential scanning calorimetry (DSC). The DSC curves have shown a sharp endothermic event at 211 °C and TG demonstrated
a single stage of mass loss between 254 and 283 °C. Solid-state characterization was carried out by DRIFT, SEM, and XRPD demonstrating
the drug physicochemical properties including crystallinity. Drug-excipient compatibility studies investigated by DSC have
shown a possible physical interaction of the drug with magnesium stearate, microcrystalline cellulose and starch. Nevertheless,
these results where not confirmed by DRIFT and SEM analyses. 相似文献
19.
Brown M. E. Antunes E. M. Glass B. D. Lebete M. Walker R. B. 《Journal of Thermal Analysis and Calorimetry》1999,56(3):1317-1322
Differential scanning calorimetry was used to examine the thermal behaviour of mixtures of the drug prochlorperazine with standard excipients, to assess potential interactions, and of mixtures with cyclodextrins, to investigate inclusion complexation which could increase the photostability of the drug. For most of the excipients (magnesium stearate, stearic acid, Explotab®, Ac-Di-Sol®, Encompress® and Ludipress®, lactose and Starch 1500) disappearance or broadening of the melting endotherm of the drug indicated interactions. Lubritab® was the only 'inert' excipient tested. Mixtures of prochlorperazine and the cyclodextrins gave incomplete inclusion complexation as shown by only partial disappearance of the melting endotherm of the drug. 相似文献
20.
H. Salvio Neto Cs. Novák J. R. Matos 《Journal of Thermal Analysis and Calorimetry》2009,97(1):367-374
Differential Scanning Calorimetry (DSC), thermogravimetry/derivative thermogravimetry (TG/DTG) and infrared spectroscopy (IR) techniques were used to investigate the compatibility between prednicarbate and several excipients commonly used in semi solid pharmaceutical form. The thermoanalytical studies of 1:1 (m/m) drug/excipient physical mixtures showed that the beginning of the first thermal decomposition stage of the prednicarbate (T onset value) was decreased in the presence of stearyl alcohol and glyceryl stearate compared to the drug alone. For the binary mixture of drug/sodium pirrolidone carboxilate the first thermal decomposition stage was not changed, however the DTG peak temperature (T peak DTG) decreased. The comparison of the IR spectra of the drug, the physical mixtures and of the thermally treated samples confirmed the thermal decomposition of prednicarbate. By the comparison of the thermal profiles of 1:1 prednicarbate:excipients mixtures (methylparaben, propylparaben, carbomer 940, acrylate crosspolymer, lactic acid, light liquid paraffin, isopropyl palmitate, myristyl lactate and cetyl alcohol) no interaction was observed. 相似文献