共查询到20条相似文献,搜索用时 31 毫秒
1.
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
2.
Neeraj Kumar Shishu Goindi Balraj Saini Gulshan Bansal 《Journal of Thermal Analysis and Calorimetry》2014,115(3):2375-2383
The current study was performed to investigate possible interactions between triazole antifungal drug itraconazole (ITR) with selected excipients commonly used for development of solid lipid nanoparticles. The excipients included common lipids (glyceryl behenate (Compritol 888 ATO?), glyceryl monostearate, stearic acid, and cetyl palmitate), charge inducers (dicetyl phosphate and stearlyamine), and surfactants (sodium cholate and sodium deoxycholate). Differential scanning calorimetry, isothermal stress testing, Fourier transform infrared spectral analysis, optical microcopy, and X-ray powder diffraction analysis were performed for assessing the compatibility between the drug and the excipients. Results of the study suggest that the stearic acid exhibited drug–excipient interactions, whereas all other excipients used in the study were found to be compatible with ITR. 相似文献
3.
Rui Gao Bai-Wang Sun Jun Lin Xiao-Li Gao 《Journal of Thermal Analysis and Calorimetry》2014,117(2):731-739
Studies of active drug-excipient compatibility represent an important phase in the preformulation stage of the development of all dosage forms. For the development of conjugation estrogens and medroxyprogesterone acetate (MPA) double-layer tablets, techniques of thermal, isothermal stress testing (IST), and molecular vibrational spectroscopy analysis were performed to access the compatibility. Differential scanning calorimetry (DSC) studies were used as an important and complementary tool during preformulation to determine drug-excipient compatibility. On the basis of DSC results, MPA was found to be compatible with polyethylene glycol 6000. However, the results of Raman and IST studies showed that all the excipients defined in the prototype formula were found to be compatible with MPA. Overall, the compatibility of selected excipients with MPA was successfully evaluated using a combination of thermal and IST methods, and the formulations developed using the compatible excipients were found to be stable. 相似文献
4.
A simple, fast, precise, specific and economical reverse phase liquid chromatographic method was developed for determination of nitrate (NIT) impurity from nicorandil (NIC) and its tablet dosage form. NIT is process impurity as well as a degradation product of NIC. This article is based on application of amino propyl silane (APS) column for determination of NIT in presence of NIC and various excipients using potassium nitrate as a standard. The developed method was validated for its intended use by evaluating various important parameters like linearity, accuracy, recovery and specificity. The developed method was applied to evaluate the compatibility study of NIC with various excipients by monitoring the NIT content. 相似文献
5.
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
6.
K. Terada T. Masuda Y. Yoshihashi E. Yonemochi 《Journal of Thermal Analysis and Calorimetry》2006,85(3):675-680
Isothermal
microcalorimetry was used to evaluate excipient compatibility of solid dosage
form. Oxybutynin hydrochloride and cefaclor were used as model drugs for compatibility
test with excipients. The calorimetric data for compatibility test were compared
with those of HPLC data. Evaluation of compatibility between drug and excipient
of solid dosage form might be possible to use isothermal microcalorimetry
instead of conventional method. By using microcalorimetric method, the evaluation
of the compatibility between drug and excipient could be successfully performed
with a simple operation in a short time. The application of the isothermal
microcalorimetry would be useful for the screening test of the drug compatibility
with excipients. 相似文献
7.
Dumitru Tita Tunde Jurca Adriana Fulias Eleonora Marian Bogdan Tita 《Journal of Thermal Analysis and Calorimetry》2013,112(1):407-419
This study is part of a research project aimed to find and optimize methods by which drug-excipient compatibility can be reliably and quickly assessed. The objective of the present study was to evaluate the compatibility of the acetylsalicylic acid (ASA), an non-steroidal anti-inflammatory drug, with pharmaceutical excipients of common use including diluents, binders, disintegrants, lubricants and solubilising agents. In order to investigate the possible interactions between ASA and eleven excipients differential scanning calorimetry (DSC) and thermogravimetry/derivative thermogravimetry analysis completed by Fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffraction were used for compatibility study. The DSC has proven to be, among the selected analytical techniques, the most sensitive and specific in assessing the compatibility. The samples, as physical mixtures, were prepared by mixing the analyte and excipients in a proportion of 1:1 (w:w). On the basis of thermal results (especially DSC), confirmed by FT-IR and X-ray analysis, a possible chemical interaction was found between the ASA with polyvinylpyrrolidone K30 (PVP) and magnesium stearate, respectively a possible physical interaction with colloidal silicon dioxide and stearic acid (Ac. St.). 相似文献
8.
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
9.
Marta B. Lopes 《Analytica chimica acta》2009,633(1):149-75
Near infrared chemical imaging (NIR-CI) analysis was performed on 55 counterfeit Heptodin™ tablets obtained from a market survey and an additional 11 authentic Heptodin™ tablets for comparison. The aim of the study was to investigate whether NIR-CI can be used to detect the counterfeit tablets and to classify/source them so as to understand the possible number of origins to aid investigators and authorities to shut down counterfeiting operations. NIR-CI combined with multivariate analysis is particularly suited to compare chemical and physical properties of samples, since it is a quick and non-destructive method of analysis. Counterfeit tablets were easily distinguished from the authentic ones. Principal component analysis (PCA) and k-means clustering were performed on the data set. The results from both analyses grouped the counterfeit tablets in 13 main groups. The main groups found with both methods were quite consistent. Out of the 55 tablets only 18% contained the correct active pharmaceutical ingredient (API), i.e., the anti-viral drug lamivudine. The remaining 82% of counterfeit tablets contained talc and starch as main excipients. The API containing tablets classified into three main groups, based mainly on the amount of lamivudine present in the tablet. The group which had close to the correct amount of lamivudine sub-classified into three groups. From the analysis carried out, it is likely that the counterfeit tablets originate from as many as 15 different sources. 相似文献
10.
Howdle MD Eckers C Laures AM Creaser CS 《Journal of the American Society for Mass Spectrometry》2009,20(1):1-9
Gas-phase ion mobility studies of mixtures containing polyethylene glycols (PEG) and an active pharmaceutical ingredient (API),
lamivudine, have been carried out using electrospray ionization-ion mobility spectrometry-quadrupole-time-of-flight mass spectrometry
(ESI-IMS-Q-TOF). In addition to protonated and cationized PEG oligomers, a series of high molecular weight ions were observed
and identified as noncovalent complexes formed between lamivudine and PEG oligomers. The noncovalent complex ions were dissociated
using collision induced dissociation (CID) after separation in the ion mobility drift tube to recover the protonated lamivudine
free from interfering matrix ions and with a drift time associated with the precursor complex. The potential of PEG excipients
to act as “shift reagents,” which enhance selectivity by moving the mass/mobility locus to an area of the spectrum away from
interferences, is demonstrated for the analysis of lamivudine in a Combivir formulation containing PEG and lamivudine. 相似文献
11.
Yan Wang Yang-Hui Luo Jing Zhao Bai-Wang Sun 《Journal of Thermal Analysis and Calorimetry》2014,115(3):2391-2400
For the development of dispersible tablets of itraconazole (ITR), techniques of thermal, Raman spectroscopy, and isothermal stress testing (IST) were used to assess the compatibility of ITR with selected excipients. Initially, differential scanning calorimeter (DSC) was used to evaluate the compatibility. Raman spectrum of drug–excipient mixture was also compared with that of pure drug and excipient. Compatibility of excipients defined in the prototype formula was tested using IST. Based on the DSC results alone, PEG-4000 was found to exhibit interaction with ITR. However, the results of Raman and IST studies showed that all the excipients used in the formula were compatible with ITR. Overall, compatibility of excipients with ITR was successfully evaluated using the combination of DSC, Raman spectroscopy, and IST techniques. 相似文献
12.
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
13.
Laura Sbrcea Ionu-Mihai Tnase Adriana Ledei Denisa Cîrcioban Gabriela Vlase Paul Barvinschi Marinela Miclu Renata-Maria Vru Oana Suciu Ionu Ledei 《Molecules (Basel, Switzerland)》2021,26(6)
Risperidone (RSP) is an atypical antipsychotic drug used in treating schizophrenia, behavioral, and psychological symptoms of dementia and irritability associated with autism. The drug substance is practically insoluble in water and exhibits high lipophilicity. It also presents incompatibilities with pharmaceutical excipients such as magnesium stearate, lactose, and cellulose microcrystalline. RSP encapsulation by randomly methylated β-cyclodextrin (RM-β-CD) was performed in order to enhance drug solubility and stability and improve its biopharmaceutical profile. The inclusion complex formation was evaluated using thermal methods, powder X-ray diffractometry (PXRD), universal-attenuated total reflectance Fourier transform infrared (UATR-FTIR), UV spectroscopy, and saturation solubility studies. The 1:1 stoichiometry ratio and the apparent stability constant of the inclusion complex were determined by means of the phase solubility method. The compatibility between the supramolecular adduct and pharmaceutical excipients starch, anhydrous lactose, magnesium stearate, and cellulose microcrystalline was studied employing thermoanalytical tools (TG-thermogravimetry/DTG-derivative thermogravimetry/HF-heat flow) and spectroscopic techniques (UATR-FTIR, PXRD). The compatibility study reveals that there are no interactions between the supramolecular adduct with starch, magnesium stearate, and cellulose microcrystalline, while incompatibility with anhydrous lactose is observed even under ambient conditions. The supramolecular adduct of RSP with RM-β-CD represents a valuable candidate for further research in developing new formulations with enhanced bioavailability and stability, and the results of this study allow a pertinent selection of three excipients that can be incorporated in solid dosage forms. 相似文献
14.
Akhilesh Vikram Singh Lila Kanta Nath 《Journal of Thermal Analysis and Calorimetry》2012,108(1):307-313
In this study, highly substituted starch acetate was prepared by reaction with native moth bean starch and acetic anhydride.
Physicochemical characterization of this modified starch was done using scanning electron microscopy, X-ray diffraction, and
thermogravimetric analysis. Their formation was confirmed by titrimetric analysis and highest degree of substitution was observed
with a value of 2.35. The synthesized modified starch was further studied for compatibility with model drug lamivudine using
differential scanning calorimetry and isothermal stress testing for its controlled release tablet formulation. 相似文献
15.
Studies are constantly being conducted on the elaboration of efficient methods to confirm the compatibility of active pharmaceutical ingredients (APIs) and excipients, since medicinal products, apart from their APIs, also contain numerous excipients that not only have important functions in pharmaceutical preparations but can also initiate or participate in interactions with drug substances, which eventually lead to a decline in drug quality. With this in mind, research was undertaken to evaluate two of the most often applied pattern recognition methods, hierarchical cluster analysis (HCA) and principal component analysis (PCA), as supporting techniques in the identification of potential physicochemical interactions that may occur during the preformulation of solid dosage forms. The investigation performed with the use of baclofen and selected excipients has shown that with thermogravimetric analysis, HCA and PCA fulfill their role as supporting techniques in the interpretation of the data obtained. Based on these methods, it is possible to detect incompatibilities between baclofen and excipients, and the data obtained concur strongly with the results of differential scanning calorimetry and IR spectrometry analyses. 相似文献
16.
Monica Felts de La Roca Soares José Lamartine Soares-Sobrinho Keyla Emanuelle Ramos da Silva Lariza Darlene Santos Alves Pablo Queiroz Lopes Lidiane Pinto Correia Fábio Santos de Souza Rui Oliveira Macêdo Pedro José Rolim-Neto 《Journal of Thermal Analysis and Calorimetry》2011,104(1):307-313
The ornidazole drug substance presents melt at approximately 90 °C (∆T = 85–98 °C), which is critical for its use on pharmaceutical manufacturing process. This work aimed the thermal characterization
of ornidazole raw-material synthesized by three different manufacturers from India, China, and Italy, using the thermoanalytical
techniques of DTA, DSC, and TG, besides the verification of its stability and compatibility as a solid pharmaceutical product
by the analysis of its binary mixtures (BM) with excipients and a tablet formulation. The characterization includes the thermal
decomposition kinetic investigation by Ozawa model using Arrhenius equation and drug purity determination by Van’t Hoff equation.
The DSC purity determination and precision were compared with results from UV–Vis spectrophotometric and liquid chromatography,
showing an adequate correlation before being recommended as a general method for purity assay. The drug raw-materials presented
similar quality and zero-order kinetic behavior, besides showing differences on thermal stability. The drug presented compatibility
with the tested excipients since the BM studied presented melting at the same temperature range as the drug and a decomposition
temperature similar to the drug for two of the BM, and at a higher temperature for the others three of the BM evaluated, which
presented excipients with higher molecular structure, capable of spatial coating on the small drug molecule promoting a physical
interaction pharmaceutical acceptable. The tablet was processed by wet granulation and compressed under normal conditions
of pressure and temperature, maintaining the physical properties of solid drug approving the manufacturing process used. In
this study, the thermal analysis was used with success as an alternative method to characterize, quantify, and perform a preformulation
study. 相似文献
17.
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
18.
Eleftheria Roumeli Angelina Tsiapranta Eleni Pavlidou Georgios Vourlias Kyriakos Kachrimanis Dimitrios Bikiaris Konstantinos Chrissafis 《Journal of Thermal Analysis and Calorimetry》2013,111(3):2109-2115
Thermal analysis is an essential, analytic tool used in preliminary studies and preparation of new pharmaceutical formulations. This study was performed to investigate the possible interactions between trandolapril and three commonly used natural excipients, namely α-lactose monohydrate, microcrystalline cellulose, and pregelatinized starch. The compatibility studies were carried out using thermoanalytic along with other complementary techniques. Differential scanning calorimetry and thermogravimetric analysis have proved that trandolapril is fully compatible with all the studied excipients until 100 °C. The complementary techniques used in this study were X-ray powder diffraction, Fourier transform-infrared spectroscopy, and scanning electron microscopy which confirmed the findings of thermal analysis. 相似文献
19.
The chemical and physical surface properties of a biomaterial are of high importance for the blood compatibility of an implant. Blends of poly(propylene-co-ethylene) with various amounts of poly(ethylene-co-vinyl acetate) (PPE/EVA-blends) were examined because of the varying surface hydrophilicity. Surface characterizations were performed by means of X-ray Photoelectron Spectroscopy (XPS), Infrared Spectroscopy in Attenuated Totalreflexion Mode (IR-ATR) in relation to dynamic contact angle and zeta potential measurements. The examination of the blood compatibility of the polymer surfaces was carried out in vitro in a modified BOWRY blood chamber with native whole human blood. A balanced ratio of polar and dispersive surface free energy and a zeta potential of −4 mV are the conditions for a good blood compatibility of the investigated PPE/EVA-blends. 相似文献
20.
Dr. Mohd Asim Dr. Abuzar Khan Dr. Aasif Helal Dr. Wael Alshitari Usman A. Akbar Dr. Mohd Yusuf Khan 《化学:亚洲杂志》2021,16(13):1839-1848
Poly(ether-block-amide)/g-PTAP mixed matrix membranes (MMMs) were developed by incorporating different wt.% (1–10%) of a novel 2D g-PTAP nanofiller and its effects on membrane structure and gas permeability were studied. The novel 2D material g-PTAP was synthesized and characterized by various analytical techniques including field-emission scanning electron microscopy (FESEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and Raman spectroscopy. The fabricated MMMs were investigated to study the interaction and compatibility between Pebax and g-PTAP. The MMMs showed an effective integration of g-PTAP nanofiller into the Pebax matrix without affecting its thermal stability. Gas permeation experiments with MMMs showed improved CO2 permeability and selectivity (CO2/N2) upon incorporation of g-PTAP in the Pebax polymer matrix. The maximum CO2 permeability enhancement from 82.3 to 154.6 Barrer with highest CO2/N2 selectivity from 49.5 to 83.5 were found with 2.5 wt.% of nanofiller compared to neat Pebax membranes. 相似文献