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3. Preformulation evaluation of selumetinib for topical application: skin distribution and photodegradation analysis using MALDI imaging and LC-MS/MS.

Author

Nicol, Edith, Do, Bernard, Vignes, Marina, Annereau, Maxime, Paul, Muriel, Wolkenstein, Pierre, Touboul, David, and Secretan, Philippe-Henri

Subjects
LIQUID chromatography-mass spectrometry, TOPICAL drug administration, MASS spectrometry, NEUROFIBROMATOSIS 1, DESORPTION
Abstract

Understanding drug behavior within the skin, especially for photosensitive compounds, is crucial for developing effective and safe topical therapies. This study employs Matrix-Assisted Laser Desorption/Ionization Mass Spectrometry Imaging (MALDI-MSI) and Liquid Chromatography-Mass Spectrometry (LC-MS/MS) to investigate the skin permeation and photostability of selumetinib, a MEK inhibitor used in treating type 1 neurofibromatosis (NF1). The highest amounts of selumetinib in the skin sections were obtained when using the gel formulation, suggesting that it is to be preferred to cream formulations to achieve higher permeation of the drug. Our study also revealed that selumetinib is amenable to photodegradation in ex vivo skin explants, and yields one main degradation product, whose degradation is likely triggered by hydrogen abstraction. MALDI-MSI results showed selumetinib and its degradation product concentrate in skin appendages, indicating these structures might serve as drug reservoirs, potentially prolonging retention and efficacy. This study demonstrates that combining MALDI-MSI with LC/MS-MS can highly contribute to the characterization of the fate of photosensitive compounds in the skin, an essential prerequisite to the development of compound-specific photoprotective measures. It will also pave the way for innovative topical delivery strategies for NF1 treatment. [ABSTRACT FROM AUTHOR]

Published
2024
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4. Physicochemical Stability of Doravirine (Pifeltro ®): Characterization of Main Degradation Products and Assessment of Stability of Tablets Repackaged in Single-Dose Unit Containers.

Author

Houssen, Moïse, Secretan, Philippe-Henri, Nobilet, Loup, Jossot, Kilian, Guichard, Laura, Mwamba, Cédric, Ngy, David, Hassani, Lamia, Solgadi, Audrey, Antignac, Marie, Do, Bernard, Junot, Helga, and Sadou Yayé, Hassane

Subjects
MASS spectrometry, STRUCTURAL stability, ANTIVIRAL agents, BODY fluids, LIQUID chromatography-mass spectrometry
Abstract

Doravarine (DOR) is an antiviral drug with a marketed authorization for the management of occupational blood and body fluid exposure. The currently existing packaging, consisting of multiple unit bottles comprising 30 tablets, is not fully appropriate for daily nominative dispensing at the hospital. This study aims at assessing the impact of the change in packaging on the key attributes of the drug: assay, impurity profile, and dissolution. As the first step, which is not fully depicted in the literature, the main potential impurities that could appear during storage (i.e., degradation products (DPs) of DOR) were characterized using a forced degradation protocol followed by an LC-MS/MS analysis. These results paved the way for in silico toxicological assessment and targeted degradation product profiling. Based on this study, the assessment of the implication of repackaging on the formation of DOR's degradation products should be a primary focus. [ABSTRACT FROM AUTHOR]

Published
2024
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9. Fighting fake medicines: First quality evaluation of cardiac drugs in Africa

Author

Antignac, Marie, Diop, Bara Ibrahima, Macquart de Terline, Diane, Bernard, Melisande, Do, Bernard, Ikama, Stéphane Méo, N'Guetta, Roland, Balde, Dadhi M., Tchabi, Yessoufou, Sidi Aly, Abdallahi, Ali Toure, Ibrahim, Zabsonre, Patrick, Damorou, Jean Marie F., Takombe, Jean Laurent, Fernandez, Christine, Tafflet, Muriel, Empana, Jean Philippe, Plouin, Pierre François, Narayanan, Kumar, Marijon, Eloi, and Jouven, Xavier

Published
2017
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10. Identification of Degradation Products of the New Anticancer Drug Substance ONC201 by Liquid Chromatography–High-Resolution Multistage Mass Spectrometry

Author

Annereau, Maxime, primary, Vignes, Marina, additional, Bouchema, Tahar Sif Eddine, additional, Denis, Lucas, additional, Solgadi, Audrey, additional, Vieillard, Victoire, additional, Paul, Muriel, additional, Rieutord, André, additional, Grill, Jacques, additional, Secretan, Philippe-Henri, additional, and Do, Bernard, additional

Published
2023
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13. Identification of the Major Degradation Pathways of Selumetinib

Author

Bouchema, Tahar Sif eddine, primary, Annereau, Maxime, additional, Vieillard, Victoire, additional, Boquet, Raphael, additional, Coelho, Gisele Abreu, additional, Castelli, Florence, additional, Solgadi, Audrey, additional, Paul, Muriel, additional, Yagoubi, Najet, additional, Secretan, Philippe-Henri, additional, and Do, Bernard, additional

Published
2022
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14. Substandard drugs among five common antihypertensive generic medications: an analysis from 10 African countries

Author

Macquart de Terline, Diane, Diop, Bara I., Bernard, Melisande, Do, Bernard, Ikama, Méo S., N’guetta, Roland, Balde, Dadhi M., Tchabi, Yessoufou, Sidi Aly, Abdallahi, Ali Toure, Ibrahim, Zabsonre, Patrick, Damorou, Jean-Marc F., Takombe, Jean-Laurent, Narayanan, Kumar, Fernandez, Christine, Tafflet, Muriel, Plouin, Pierre-François, Empana, Jean-Philippe, Marijon, Eloi, Jouven, Xavier, and Antignac, Marie

Published
2018
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15. Unequal Behaviour between Hydrolysable Functions of Nirmatrelvir under Stress Conditions: Structural and Theoretical Approaches in Support of Preformulation Studies

Author

Secretan, Philippe-Henri, primary, Annereau, Maxime, additional, Kini-Matondo, Willy, additional, Prost, Bastien, additional, Prudhomme, Jade, additional, Bournane, Lina, additional, Paul, Muriel, additional, Yagoubi, Najet, additional, Sadou-Yayé, Hassane, additional, and Do, Bernard, additional

Published
2022
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19. Mixed Polymeric Micelles for Rapamycin Skin Delivery

Author

Le Guyader, Guillaume, primary, Do, Bernard, additional, Rietveld, Ivo B., additional, Coric, Pascale, additional, Bouaziz, Serge, additional, Guigner, Jean-Michel, additional, Secretan, Philippe-Henri, additional, Andrieux, Karine, additional, and Paul, Muriel, additional

Published
2022
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25. Comparative analysis of docetaxel: physical and chemical characterisation of Taxotère® and generics

Author

Da Costa Eloïse, Do Bernard, Solgadi Audrey, Lemare François, Le Guyader Guillaume, Delaloge Suzette, Annereau Maxime, Souquere Sylvie, Pierron Gérard, Paul Muriel, Viellard Victoire, Fleury Thomas, Roy Pétronille, Conq Jérôme, Unité de Technologies Chimiques et Biologiques pour la Santé (UTCBS - UM 4 (UMR 8258 / U1022)), Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Paris Cité (UPCité), Groupe matériaux et santé, Université Paris-Saclay, Service de pharmacologie clinique [Mondor], Assistance publique - Hôpitaux de Paris (AP-HP) (AP-HP)-Hôpital Henri Mondor-Université Paris-Est Créteil Val-de-Marne - Paris 12 (UPEC UP12), Hôpital Henri Mondor, Centre Hospitalier Intercommunal de Créteil (CHIC), Rétrovirus endogènes et éléments rétroïdes des eucaryotes supérieurs (UMR 9196), Université Paris-Sud - Paris 11 (UP11)-Institut Gustave Roussy (IGR)-Centre National de la Recherche Scientifique (CNRS), Analyse moléculaire, modélisation et imagerie de la maladie cancéreuse (AMMICa), Université Paris-Sud - Paris 11 (UP11)-Institut Gustave Roussy (IGR)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Ingénierie et Plateformes au Service de l'Innovation Thérapeutique (IPSIT), Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut de Chimie du CNRS (INC)-Université Paris-Saclay-Centre National de la Recherche Scientifique (CNRS), Institut Gustave Roussy (IGR), and Université Paris-Est Créteil Val-de-Marne - Paris 12 (UPEC UP12)

Subjects
0301 basic medicine, Cancer Research, Drug Compounding, Polysorbates, Antineoplastic Agents, Docetaxel, Pharmacology, Bioequivalence, Vial, Micelle, Risk Assessment, Excipients, 03 medical and health sciences, 0302 clinical medicine, medicine, Drugs, Generic, Humans, In patient, Particle Size, Adverse effect, Micelles, Ethanol, business.industry, Enterocolitis, [SDV.SP]Life Sciences [q-bio]/Pharmaceutical sciences, Drug Liberation, Kinetics, 030104 developmental biology, Oncology, Therapeutic Equivalency, 030220 oncology & carcinogenesis, Patient Safety, business, medicine.drug
Abstract

Several cases of fatal enterocolitis have been described in association with the use of docetaxel (DTX), and this increase in adverse events has been concomitant with a change in formulation. Indeed in 2010, a new DTX-based presentation has been introduced in the form of a single ready-to-use vial by Sanofi-Aventis, presentation also used for generics. In this study, different available formulations were compared (Sanofi 2 vials, Sanofi 1 vial, Accord Healthcare, Kabi, Hospira) in terms of composition compliance with control specifications and simulated micelle behaviour to try to determine what could be the potential causes of this problem. This work had permitted to show that all the tested products complied with specifications in terms of dosage and purity. Variations in the composition of polysorbate 80 (PS80) have been observed but are probably too small to be responsible for the toxicity found in patients. However, we identified a difference in micelle size and release kinetics probably because of doubling concentration of ethanol in new formulation. As a result, we emphasised the importance in the case of DTX of conducting bioequivalence studies as expected in European Medicines Agency (EMA) guidance to ensure patient safety, even though these formulation changes might seem minor. Therefore, further studies are needed to explore the potential role of ethanol, PS80 and the unbound fraction of DTX in the development of enterocolitis in patients treated with DTX.

Published
2020
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31. Post hoc study to investigate the potential causes of poor quality of cardiovascular medicines collected in sub-Saharan countries

Author

Secretan, Philippe-Henri, primary, Antignac, Marie, additional, Yagoubi, Najet, additional, Bernard, Mélisande, additional, Perier, Marie Cécile, additional, Takombe, Jean Laurent, additional, Balde, Dadhi, additional, N'Guetta, Roland, additional, Ikama, Méo Stéphane, additional, Zabsonre, Patrice, additional, Sidi Aly, Abdallahi, additional, Jouven, Xavier, additional, and Do, Bernard, additional

Published
2020
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33. Falsified and substandard cardiovascular drugs in Africa: a need for continued monitoring strategies

Author

Antignac, Marie, primary, Bara Diop, Ibrahima, additional, Macquart de Terline, Diane, additional, Bernard, Melisande, additional, Do, Bernard, additional, Ikama, Méo Stéphane, additional, N'Guetta, Roland, additional, Balde, Dadhi M, additional, Tchabi, Yessoufou, additional, Aly, Abdallahi Sidi, additional, Toure, Ibrahim Ali, additional, Zabsonre, Patrick, additional, F Damorou, Jean Marie, additional, Takombe, Jean Laurent, additional, Boyer Chatenet, Louise, additional, Narayanan, Kumar, additional, Marijon, Eloi, additional, Empana, Jean Philippe, additional, and Jouven, Xavier, additional

Published
2019
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35. Investigating therapeutic usage of combined Ticagrelor and Aspirin through solid-state and analytical studies

Author

Universitat Politècnica de Catalunya. Departament de Física, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Sadou Yayé, Hassane, Rietveld, Ivo B., Barrio Casado, María del, Secrétan, Philippe-Henri, Faucheron, Antoine, Karoui, Maher, Tilleul, Patrick, Yagoubi, Najet, Do, Bernard, Universitat Politècnica de Catalunya. Departament de Física, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Sadou Yayé, Hassane, Rietveld, Ivo B., Barrio Casado, María del, Secrétan, Philippe-Henri, Faucheron, Antoine, Karoui, Maher, Tilleul, Patrick, Yagoubi, Najet, and Do, Bernard

Abstract

The mainstay treatment for patients with acute coronary syndrome is an oral route dual antiplatelet therapy with a P2Y12-receptor antagonist and Aspirin (ASA). To improve patient adherence to such treatments, combination therapies (polypill) are envisioned. Physicochemical solid-state studies have been carried out to develop a preformulation strategy of ASA with the P2Y12-receptor antagonist Ticagrelor (TIC). The investigations were carried out using differential scanning calorimetry, liquid chromatography-high resolution-multistage mass spectrometry (LC-HR-MSn) and as complementary techniques Fourier transform infrared measurements and thermogravimetric analysis. A simple eutectic transition at 98 °C with a mole fraction for the eutectic liquid of 0.457 has been observed and the mixing of ASA and TIC molecules in each other's crystal structures appears to be limited. No cocrystals of TIC and ASA have been found. The appearance of the eutectic liquid was linked with a clear onset of chemical instability of the two pharmaceuticals. The decomposition mechanism in the liquid phase involves prior decomposition of ASA, whose residues react with well-identified TIC interaction sites. Seven interaction products were observed by LC-HR-MSn linked to corresponding degradation products. The most important degradation pathway is N-dealkylation. In conclusion, polypills of ASA and TIC are a viable approach, but the decomposition of ASA should be avoided by eliminating high temperatures and high humidity., Peer Reviewed, Preprint

Published
2017

37. Solid state stability and solubility of triethylenetetramine dihydrochloride

Author

Universitat Politècnica de Catalunya. Departament de Física, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Henriet, Theo, Gana, Inès, Ghaddar, Carine, Barrio Casado, María del, Cartigny, Yohann, Yagoubi, Najet, Do, Bernard, Tamarit Mur, José Luis, Rietveld, Ivo B., Universitat Politècnica de Catalunya. Departament de Física, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Henriet, Theo, Gana, Inès, Ghaddar, Carine, Barrio Casado, María del, Cartigny, Yohann, Yagoubi, Najet, Do, Bernard, Tamarit Mur, José Luis, and Rietveld, Ivo B.

Abstract

The API triethylenetetramine dihydrochloride used as an alternative treatment of Wilson¿s disease is sensitive to water and it exhibits polymorphism. As this may become an issue for the drug formulation, the physical stability has been studied by differential scanning calorimetry, high-pressure thermal analysis, dynamic vapor sorption, and X-ray diffraction as a function of temperature. In addition, high-pressure liquid chromatography and mass spectrometry have been used to study the purity and chemical stability of the API. A pressure-temperature phase diagram of the pure compound has been constructed and it can be concluded that form II is monotropic in relation to form I, which is the only stable solid. The solubilities of the different solid forms have been determined with the help of a temperature ¿ composition phase diagram. The API is very soluble, at 20° C about 10% of the saturated solution with respect to the dihydrate consists of API and the solubility of the pure form I is twice as high. Moreover, it has been shown that at 20 °C, a relative humidity above 40% induces the formation of the dihydrate and at 70% a saturated solution appears. At higher temperatures, the formation of the dihydrate appears at lower relative humidity values. A clear link has been established between the API¿s chemical stability, its physical stability and the relative humidity in the air. Humidity levels above 40% are detrimental to the quality of the API., Postprint (author's final draft)

Published
2016

43. An integrated view of theiInfluence of temperature, pressure, and humidity on the stability of trimorphic cysteamine hydrochloride

Author

Universitat Politècnica de Catalunya. Departament de Física, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Gana, Inès, Barrio Casado, María del, Ghaddar, Carine, Nicolai, Beatrice, Do, Bernard, Tamarit Mur, José Luis, Safta, Fathi, Rietveld, Ivo B., Universitat Politècnica de Catalunya. Departament de Física, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Gana, Inès, Barrio Casado, María del, Ghaddar, Carine, Nicolai, Beatrice, Do, Bernard, Tamarit Mur, José Luis, Safta, Fathi, and Rietveld, Ivo B.

Abstract

Understanding the phase behavior of pharmaceuticals is important for dosage form development and regulatory requirements, in particular after the incident with ritonavir. In the present paper, a comprehensive study of the solid-state phase behavior of cysteamine hydrochloride used in the treatment of nephropathic cystinosis and recently granted orphan designation by the European Commission is presented employing (high-pressure) calorimetry, water vapor sorption, and X-ray diffraction as a function of temperature. A new crystal form (I2/a, form III) has been discovered, and its structure has been solved by X-ray powder diffraction, while two other crystalline forms are already known. The relative thermodynamic stabilities of the commercial form I and of the newly discovered form III have been established; they possess an overall enantiotropic phase relationship, with form I stable at room temperature and form III stable above 37 degrees C. Its melting temperature was found at 67.3 +/- 0.5 degrees C. Cysteamine hydrochloride is hygroscopic and immediately forms a concentrated saturated solution in water with a surprisingly high concentration of 47.5 mol % above a relative humidity of 35%. No hydrate has been observed. A temperature composition phase diagram is presented that has been obtained with the unary pressure temperature phase diagram, measurements, and calculations. For development, form I would be the best form to use in any solid dosage form, which should be thoroughly protected against humidity., Postprint (author's final draft)

Published
2015

44. Triethylenetetramine dihydrochloride: interactions and conformations in two anhydrous structures and a hydrate

Author

Universitat Politècnica de Catalunya. Departament de Física i Enginyeria Nuclear, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Henriet, Theo, Nicolai, Beatrice, Ghaddar, Carine, Barrio Casado, María del, Do, Bernard, Yagoubi, Najet, Tamarit Mur, José Luis, Rietveld, Ivo B., Universitat Politècnica de Catalunya. Departament de Física i Enginyeria Nuclear, Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials, Henriet, Theo, Nicolai, Beatrice, Ghaddar, Carine, Barrio Casado, María del, Do, Bernard, Yagoubi, Najet, Tamarit Mur, José Luis, and Rietveld, Ivo B.

Abstract

Triethylenetetramine is a polyamine type chelating ligand for copper(II), which is currently used, mainly in its dihydrochloride form, as an alternative to d-penicillamine against Wilsons disease. Because knowledge about the solid-state behavior of pharmaceuticals is a prerequisite for the development of an effective dosage form, the crystal structures of two triethylenetetramine dihydrochloride polymorphs have been determined, and the infrared spectra and thermal expansion have been studied. No suitable crystals could be obtained of the two anhydrous forms, for which the structures have been solved from X-ray powder diffraction. Form I is monoclinic P2(1)/n with the cell parameters a = 11.0475(4) angstrom, b = 4.87475(16) angstrom, c = 11.1178(4) angstrom, and beta = 106.9826(13)degrees leading to V = 572.63(3) angstrom(3) with Z = 2. Form II is also monoclinic P2(1)/c with cell parameters a = 10.6734(6) angstrom, b = 12.3613(6) angstrom, c = 9.8479(7) angstrom, and beta = 115.985(3)degrees leading to a unit-cell volume of V = 1167.95(12) angstrom(3) with Z = 4. A recurring structural element is a ionic interaction between two chloride ions and two ammonium groups each organized in a diamond pattern present in the dihydrate (the salt is hygroscopic) and anhydrous form I. The molecular conformations are different in both anhydrous forms and in the dihydrate. Comparison of the thermal expansions demonstrates that form I has the smallest thermal expansion and thus possesses the strongest intermolecular interactions., Postprint (published version)

Published
2015

45. Substandard drugs among five common antihypertensive generic medications: an analysis from 10 African countries.

Author

de Terline, Diane Macquart, Diop, Bara I., Bernard, Melisande, Do, Bernard, Ikama, Méo S., N'guetta, Roland, Balde, Dadhi M., Tchabi, Yessoufou, Aly, Abdallahi Sidi, Toure, Ibrahim Ali, Zabsonre, Patrick, Damorou, Jean-Marc F., Takombe, Jean-Laurent, Narayanan, Kumar, Fernandez, Christine, Tafflet, Muriel, Plouin, Pierre-François, Empana, Jean-Philippe, Marijon, Eloi, and Jouven, Xavier

Published
2018
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46. Crystal structure and solid-state studies of aged samples of tienoxolol, an API designed against hypertension

Author

Teulon, Jean-Marie, Mahé, Nathalie, Do, Bernard, Nicolaï, Béatrice, Rietveld, Ivo B., Barrio Casado, María del, Tamarit Mur, José Luis, Céolin, René, Ghéchot, Christophe, Universitat Politècnica de Catalunya. Departament de Física i Enginyeria Nuclear, and Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials

Subjects
Ciències de la salut::Medicina::Farmacologia [Àrees temàtiques de la UPC], Hypertension Age factors, Física de l'estat sòlid, Física::Física de l'estat sòlid [Àrees temàtiques de la UPC], Indústria farmacèutica -- Investigació, X-ray diffractometer
Abstract

Aging of drug molecules is generally studied following regulatory procedures, i.e. under forced conditions and for relatively limited storage time; therefore naturally aged samples are rare and provide scientific reference data beyond regulatory considerations. Tienoxolol was studied after 25 years of storage in the dark under ambient conditions. About 86% of the samples still consisted of tienoxolol and the main impurity (13%) was caused by the hydrolysis of the ester moiety. Protection from humidity is therefore important. Other sensitive groups containing nitrogen and sulfur appear to be quite stable with less than 0.8% conversion over 25 years. In addition, the crystal structure has been solved. Tienoxolol orange needles were found to crystallize in the orthorhombic non-centrosymmetric space group Iba2, indicating that the crystal is a racemic compound. The unit cell parameters at room temperature are a = 10.069(5)A˚ , b = 45.831(10)A˚ , and c = 9.822(5) ˚A and the unit cell volume is 4533(3) ˚A3 with Z = 8. © 2011 Elsevier B.V.

Published
2012
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