Differential Scanning Calorimetric Analysis for Incompatibility: Sodium Stearate/Magnesium Stearate and Acidic Compounds

2020 ◽  
Vol 859 ◽  
pp. 307-312
Author(s):  
Pornsit Chaiya ◽  
Thawatchai Phaechamud
Keyword(s):  
Sodium Stearate ◽  
Pharmaceutical Formulations ◽  
Pharmaceutical Compounds ◽  
Magnesium Stearate ◽  
Differential Scanning Calorimetric ◽  
Salt Form ◽  
Scanning Calorimetry ◽  
Calorimetric Analysis ◽  
Pharmaceutical Excipient ◽  
Acidic Compounds

Compatibility investigation was performed between stearate lubricants (sodium stearate and magnesium stearate) and acidic pharmaceutical compounds (ibuprofen, indomethacin and valproic acid) and citric acid as acidic pharmaceutical excipient using differential scanning calorimetry (DSC). Alteration in DSC thermogram was found in all mixtures. There was a presence of melting endothermic peak of stearic acid in all mixtures (except that of stearate lubricants and indomethacin) indicating breakage of salt form of stearate lubricants depended on the physicochemical properties of drug compounds and pharmaceutical excipient. Therefore, the avoidance for using stearate lubricants with acidic pharmaceutical compounds and excipient should be concerned in development of pharmaceutical formulations.

Compatibility between Magnesium Stearate and Pharmaceutical Acidic Active Compounds/Excipients with DSC

2020 ◽  
Vol 856 ◽  
pp. 190-197
Author(s):  
Pornsit Chaiya ◽  
Thawatchai Phaechamud
Keyword(s):  
Differential Scanning Calorimetry ◽  
Magnesium Stearate ◽  
X Ray Diffraction ◽  
Salt Form ◽  
Scanning Calorimetry ◽  
Powder Mixtures ◽  
X Ray ◽  
Pharmaceutical Excipients ◽  
Drug Compounds ◽  
Ft Ir

Compatibility investigation was performed between magnesium stearate and acidic drug compounds (ibuprofen, indomethacin and valproic acid) and acidic pharmaceutical excipients (lactic acid and citric acid) using differential scanning calorimetry (DSC). DSC study indicated the possible incompatibility for the mixture between magnesium stearate and any compounds. Alteration in DSC thermogram was found in all mixtures. The eutectic phenomenon was found in the powder mixture of magnesium stearate and ibuprofen. In addition, the presence of melting endothermic peak of stearic acid in other powder mixtures except the mixture of magnesium stearate and indomethacin indicating breakage of salt form of magnesium stearate. This alteration could relate to the influence on physicochemical properties of drug compounds and pharmaceutical excipients which powder x-ray diffraction (PXRD) and Fourier Transform Infrared Spectroscopy (FT-IR) should be further analyzed to confirm the interactions between compounds.

scholarly journals Thermal analysis studies on the compatibility of furosemide with solid state and liquid crystalline excipients

2020 ◽  
Vol 74 (1) ◽  
pp. 15-23
Author(s):  
Marilena Vlachou ◽  
Natassa Pippa ◽  
Angeliki Siamidi ◽  
Aimilia Kyrili
Keyword(s):  
Solid State ◽  
Acrylic Acid ◽  
Thermal Behavior ◽  
Liquid Crystalline ◽  
Pharmaceutical Formulations ◽  
Magnesium Stearate ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Poly Ethylene ◽  
Poly Acrylic Acid

In the context of the present study, the thermal behavior of furosemide and the solid state excipients, sodium alginate, poly(ethylene oxide), poly(vinylpyrrolidone), lactose mono-hydrate and magnesium stearate, using Differential Scanning Calorimetry (DSC), was probed. It was found that the thermal behavior of these solid-state pharmaceutical excipients and furosemide correlates nicely with the literature relevant data. Regarding the furosemide-excipients mixtures, the DSC scans appear as a compilation of the thermal curves of each excipient. This suggests that the formulations containing these mixtures, may retain their stability over time. This information, which arises from the cooperativity of materials, their thermal stability and behavioris very helpful for the research and development of safe and effective pharmaceutical formulations. DSC experiments were also carried out with chimeric bilayers (called ?liposomes?), composed of hydrogenated soy phosphatidylcholine (HSPC) and poly(n-butylacrylate)-b-poly(acrylic acid) block copolymer with 70 % content of poly(acrylic acid (PnBA-b-PAA 30/70) with the addition of furosemide at the molar ratio of 9:0.1:1.0 in the system HSPC:PnBA-b-PAA 30/70:furosemide. Chimeric liposomal systems were characterized as ?fluid-like? by their DSC curves, which may be potentially translated as an easy way for release of furosemide from the advanced delivery system.

Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets

2020 ◽  
Vol 16 (7) ◽  
pp. 950-959
Author(s):  
Yu Li ◽  
Xiangwen Kong ◽  
Fan Hu
Keyword(s):  
Sustained Release ◽  
Powder Diffraction ◽  
Magnesium Stearate ◽  
Influential Factor ◽  
High Concentration ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Sustained Release Tablets ◽  
Crystal Transition ◽  
Excipient Compatibility

Background: Clarithromycin is widely used for infections of helicobacter pylori. Clarithromycin belongs to polymorphic drug. Crystalline state changes of clarithromycin in sustained release tablets were found. Objective: The aim of this study was to find the influential factor of the crystal transition of clarithromycin in preparation process of sustained-release tablets and to investigate the possible interactions between the clarithromycin and pharmaceutical excipients. Methods and Results: The crystal transition of active pharmaceuticals ingredients from form II to form I in portion in clarithromycin sustained release tablets were confirmed by x-ray powder diffraction. The techniques including differential scanning calorimetry and infrared spectroscopy, x-ray powder diffraction were used for assessing the compatibility between clarithromycin and several excipients as magnesium stearate, lactose, sodium carboxymethyl cellulose, polyvinyl-pyrrolidone K-30 and microcrystalline cellulose. All of these methods showed compatibilities between clarithromycin and the selected excipients. Alcohol prescription simulation was also done, which showed incompatibility between clarithromycin and concentration alcohol. Conclusion: It was confirmed that the reason for the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.

Development and Certification of Formononetin Reference Material for Quality Control of Functional Foods and Botanical Supplements

2019 ◽  
Vol 15 (5) ◽  
pp. 553-559
Author(s):  
Ningbo Gong ◽  
Baoxi Zhang ◽  
Kun Hu ◽  
Zhaolin Gao ◽  
Guanhua Du ◽  
...  
Keyword(s):  
Quality Control ◽  
Reference Material ◽  
Functional Foods ◽  
Certified Reference Materials ◽  
Coulometric Titration ◽  
Pharmaceutical Formulations ◽  
Uncertainty Estimation ◽  
Expanded Uncertainty ◽  
Scanning Calorimetry ◽  
Botanical Supplements

Background: Formononetin is a common soy isoflavonoid that can be found abundantly in many natural plants. Previous studies have shown that formononetin possesses a variety of activities which can be applied for various medicinal purposes. Certified Reference Materials (CRMs) play a fundamental role in the food, traditional medicine and dietary supplement fields, and can be used for method validation, uncertainty estimation, as well as quality control. Methods: The purity of formononetin was determined by Differential Scanning Calorimetry (DSC), Coulometric Titration (CT) and Mass Balance (MB) methods. Results: This paper reports the sample preparation methodology, homogeneity and stability studies, value assignment, and uncertainty estimation of a new certified reference material of formononetin. DSC, CT and MB methods proved to be sufficiently reliable and accurate for the certification purpose. The purity of the formononetin CRM was therefore found to be 99.40% ± 0.24 % (k = 2) based on the combined value assignments and the expanded uncertainty. Conclusion: This CRM will be a reliable standard for the validation of the analytical methods and for quality assurance/quality control of formononetin and formononetin-related traditional herbs, food products, dietary supplements and pharmaceutical formulations.

scholarly journals Calorimetric analysis of ice onset temperature during cryoablation: a model approach to identify early predictors of effective applications

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Elena Campagnoli ◽  
Andrea Ballatore ◽  
Valter Giaretto ◽  
Matteo Anselmino
Keyword(s):  
Cooling Rate ◽  
Latent Heat ◽  
Bovine Liver ◽  
Onset Temperature ◽  
Ice Formation ◽  
Scanning Calorimetry ◽  
Calorimetric Analysis ◽  
Early Predictors ◽  
Latent Heat Capacity ◽  
Model Approach

AbstractAim of the present study is to analyze thermal events occurring during cryoablation. Different bovine liver samples underwent freezing cycles at different cooling rate (from 0.0075 to 25 K/min). Ice onset temperature and specific latent heat capacity of the ice formation process were measured according to differential scanning calorimetry signals. A computational model of the thermal events occurring during cryoablation was compiled using Neumann’s analytical solution. Latent heat (#1 = 139.8 ± 7.4 J/g, #2 = 147.8 ± 7.9 J/g, #3 = 159.0 ± 4.1 J/g) of all liver samples was independent of the ice onset temperature, but linearly dependent on the water content. Ice onset temperature was proportional to the logarithm of the cooling rate in the range 5 ÷ 25 K/min (#3a = − 12.2 °C, #3b = − 16.2 °C, #3c = − 6.6 °C at 5K/min; #3a = − 16.5 °C, #3b = − 19.3 °C, #3c = − 11.6 °C at 25 K/min). Ice onset temperature was associated with both the way in which the heat involved into the phase transition was delivered and with the thermal gradient inside the tissue. Ice onset temperature should be evaluated in the early phase of the ablation to tailor cryoenergy delivery. In order to obtain low ice trigger temperatures and consequent low ablation temperatures a high cooling rate is necessary.

scholarly journals Difference in the Dissolution Behaviors of Tablets Containing Polyvinylpolypyrrolidone (PVPP) Depending on Pharmaceutical Formulation After Storage Under High Temperature and Humid Conditions

2016 ◽  
Vol 19 (4) ◽  
pp. 511 ◽  
Author(s):  
Yoh Takekuma ◽  
Haruka Ishizaka ◽  
Masato Sumi ◽  
Yuki Sato ◽  
Mitsuru Sugawara
Keyword(s):  
High Temperature ◽  
Benzoic Acid ◽  
Dissolution Rate ◽  
Simple Structure ◽  
Pharmaceutical Formulations ◽  
Magnesium Stearate ◽  
Principal Agent ◽  
Amino Groups ◽  
Dissolution Tests ◽  
Rosuvastatin Calcium

PURPOSE. Storage under high temperature and humid conditions has been reported to decrease the dissolution rate for some kinds of tablets containing polyvinylpolypyrrolidone (PVPP) as a disintegrant. The aim of this study was to elucidate the properties of pharmaceutical formulations with PVPP that cause a decrease in the dissolution rate after storage under high temperature and humid conditions by using model tablets with a simple composition. METHODS. Model tablets, which consisted of rosuvastatin calcium or 5 simple structure compounds, salicylic acid, 2-aminodiphenylmethane, 2-aminobiphenyl, 2-(p-tolyl)benzoic acid or 4.4’-biphenol as principal agents, cellulose, lactose hydrate, PVPP and magnesium stearate as additives, were made by direct compression. The model tables were wrapped in paraffin papers and stored for 2 weeks at 40°C/75% relative humidity (RH). Dissolution tests were carried out by the paddle method in the Japanese Pharmacopoeia 16th edition. RESULTS. Model tablets with a simple composition were able to reproduce a decreased dissolution rate after storage at 40°C/75% RH. These tablets showed significantly decreased water absorption activities after storage. In the case of tablets without lactose hydrate by replacing with cellulose, a decreased dissolution rate was not observed. Carboxyl and amino groups in the structure of the principal agent were not directly involved in the decreased dissolution. 2-Benzylaniline tablets showed a remarkably decreased dissolution rate and 2-aminobiphenyl and 2-(p-tolyl)benzoic acid tablets showed slightly decreased dissolution rates, though 4,4’-biphenol tablets did not show a decrease dissolution rate. CONCLUSIONS. We demonstrated that additives and structure of the principal agent were involved in the decreased in dissolution rate for tablets with PVPP. The results suggested that one of the reasons for a decreased dissolution rate was the inclusion of lactose hydrate in tablets. The results also indicated that compounds as principal agents with low affinity for PVPP may be easily affected by airborne water under high temperature and humid conditions. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals CHARACTERISATION OF INCLUSION COMPLEXES BETWEEN BIFONAZOLE AND DIFFERENT CYCLODEXTRINS IN SOLID AND SOLUTION STATE

2017 ◽  
Vol 36 (1) ◽  
pp. 81 ◽  
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Gabriel Hancu ◽  
Blanka Székely-Szentmiklósi ◽  
Ibolya Fülöp ◽  
...  
Keyword(s):  
Inclusion Complexes ◽  
Binary Systems ◽  
Pharmaceutical Formulations ◽  
2D Nmr ◽  
Local Drug Delivery ◽  
Stable Complex ◽  
Resonance Spectroscopy ◽  
Scanning Calorimetry ◽  
2D Nmr Spectroscopy ◽  
Major Drawback

The aim of this study is to confirm the formation of inclusion complexes between bifonazole (BFZ) and different cyclodextrin (CD) derivatives. Bifonazole, an imidazole antifungal derivative,is a very hydrophobic compound, which is a major drawback in obtaining topical pharmaceutical formulations with optimal bioavailability. Cyclodextrins may increase local drug delivery by enhancing the drug release and/or permeation. The binary systems between bifonazole and cyclodextrins were prepared in two molar ratios by physical-mixture methods.The physicochemical properties of these complexes were studied by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance spectroscopy (NMR) methods. Results showed favourable molecular interaction between the components, in solid state and in solution. 1H NMR -CD titrations and molecular modelling study showed that the most stable complex was obtained when using γ-CD. The Job’s method and 2D NMR spectroscopy sustain the 2:1 stoichiometry of the BFZ:γ-CD complex.

scholarly journals Formulation development and evaluation of Silybum marianum tablets

Rodriguésia ◽  
2020 ◽  
Vol 71 ◽  
Author(s):  
Valeria Andrea Cianchino ◽  
Laura Silvina Favier ◽  
Claudia Alicia Ortega ◽  
Cecilia Peralta ◽  
Diego Alberto Cifuente
Keyword(s):  
Ethanolic Extract ◽  
Soxhlet Extraction ◽  
Pharmaceutical Formulations ◽  
Magnesium Stearate ◽  
Major Constituent ◽  
Active Principle ◽  
Formulation Development ◽  
Silybum Marianum ◽  
Disintegration Time ◽  
Popular Medicine

Abstract In popular medicine Silybum marianum is used as a hepatoprotective agent. Silymarin is the major constituent. The present work deals with the formulation and evaluation of S. marianum tablets from ethanolic extract by direct compression. The ethanolic extract was obtained from seeds by soxhlet extraction. Two pharmaceutical formulations were prepared using fluid extract as an active principle, and Aeroperl® 300 Pharma as a carrier. In order to improve flow ability and compressibility, co-processed excipients MicroceLac® 100 and FlowLac® 90 were employed. Pre-compression and post-compression parameters were evaluated according to USP 34-NF 29. Besides, silymarin was determined by NMR spectral data. Both formulations showed excellent rheological properties and the best biopharmaceutical parameters were observed in F2 (S. marianum ethanolic extract, aeroperl® 300 Pharma, flowLac® 90, glycolate starch and magnesium stearate) in terms of the friability (0.82 %) and the disintegration time (8.05 min).

scholarly journals Compatibility Studies of Valsartan with Different Pharmaceutical Excipients

2019 ◽  
Vol 70 (7) ◽  
pp. 2590-2600
Author(s):  
Ioana Cristina Tita ◽  
Lavinia Lupa ◽  
Bogdan Tita ◽  
Roxana Liana Stan ◽  
Laura Vicas
Keyword(s):  
Magnesium Stearate ◽  
Dosage Forms ◽  
Compatibility Studies ◽  
Scanning Calorimetry ◽  
Pharmaceutical Dosage Forms ◽  
Lactose Monohydrate ◽  
Pharmaceutical Excipients ◽  
Solid Dosage ◽  
Fourier Transformed Infrared Spectroscopy ◽  
Ft Ir

Compatibility studies between active drugs and excipients are substantial in the pharmaceutical technology. Thermal analysis has been extensively used to obtain information about drug-excipient interactions and to perform pre-formulation studies of pharmaceutical dosage forms. The objective of the present study was to evaluate the compatibility of the valsartan (VALS) with pharmaceutical excipients of common use including diluents, binders, disintegrants, lubricants and solubilising agents. Thermogravimetry (TG), derivative thermogravimetry (DTG), but especially differential scanning calorimetry (DSC) were used for a first screening to find small variations in peak temperature and/or their associated enthalpy for six drug/excipient mixtures (starch, cross caramelose sodique, microcrystalline cellulose 102, povidone K30, lactose monohydrate and magnesium stearate), which indicate some degree of interaction. Additional methods using Fourier transformed infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRPD) confirmed the incompatibility of VALS with starch, povidone K30, lactose monohydrate and magnesium stearate. Those excipients should be avoided in the development of solid dosage forms.

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