The present thesis project aims at designing and preparing a system that can serve as a prototype for a future anti-inflammatory oral pharmaceutical form. Specifically, the selected pharmaceutical form is a tablet, with the goal of achieving modified release. The active ingredient chosen for this formulation is Ibuprofen, a commonly used anti-inflammatory molecule in many formulations. Three fatty acids were used for the active ingredient's vehiculation in order to identify the most suitable one for obtaining a eutectic mixture. In the first phase, the physicochemical characterization of the raw materials used was performed. Analyses were conducted using scanning differential calorimetry, IR spectroscopy, X-ray diffractometry, and, only for pure Ibuprofen, thermogravimetric analysis. Physical mixtures of Ibuprofen and capric acid (C10), Ibuprofen and lauric acid (C12), and Ibuprofen and myristic acid (C14) were prepared and characterized. None of the mixtures proved suitable for achieving a eutectic. Therefore, solid dispersions of Ibuprofen and myristic acid were prepared, selected among the three fatty acids for being the most suitable based on its physicochemical characteristics, and the most promising dispersion was identified among them. In an attempt to further improve the formulation, additional mixtures were prepared between the selected solid dispersion and the fatty acids C10, C12, and C14, but none of them exhibited eutectic characteristics. The most promising dispersion was used for the preparation of tablets. Subsequently, reproducibility and release experiments of Ibuprofen from the prepared tablets were carried out. The release from two tablets, one in HCl and one in phosphate buffer, was evaluated after 30 minutes, 1 hour, 2 hours, 3 hours, and 24 hours. For the reproducibility experiment, six tablets were selected, with 3 placed in each beaker containing either HCl or phosphate buffer, and releases were evaluated after 30 minutes, 1 hour, 2 hours, 3 hours, and 4 hours. For this part of the research, a UV-visible spectrometer was used, and the unknown concentration was determined by constructing a calibration curve. A value of R^2 close to 1 was obtained, indicating a good linear correlation between the experimentally obtained values.
Il presente progetto di tesi si pone come obiettivo la progettazione e la preparazione di un sistema che possa fungere da prototipo per una futura forma farmaceutica ad azione antiinfiammatoria, mirata alla somministrazione orale. Nello specifico, la forma farmaceutica selezionata è la compressa e l’obiettivo è ottenere un rilascio modificato. Il principio attivo scelto per la realizzazione di tale formulazione è l’Ibuprofene, una molecola ad azione antiinfiammatoria comunemente utilizzata in molte formulazioni. Per la veicolazione dell’attivo sono stati utilizzati tre acidi grassi al fine di individuare il più idoneo per l’ottenimento di una miscela eutettica. In una prima fase, è stata eseguita la caratterizzazione chimico fisica delle materie prime utilizzate. Le analisi sono state effettuate mediante calorimetria differenziale a scansione, spettroscopia IR, diffrattometria ai raggi X e, solo per l’Ibuprofene puro, analisi termogravimetrica. In particolare, sono state preparate, e poi caratterizzate, le miscele fisiche di Ibuprofene e acido caprico (C10), Ibuprofene e acido laurico (C12) e Ibuprofene e acido miristico (C14). Nessuna miscela si è rivelata idonea al raggiungimento di un eutettico. Sono state dunque preparate delle dispersioni solide di ibuprofene e acido miristico, selezionato tra i tre acidi grassi perché più idoneo in base alle sue caratteristiche chimico-fisiche, e tra queste è stata individuata quella più promettente. Nel tentativo di migliorare ulteriormente la formulazione, si sono preparate ulteriori miscele tra la dispersione solida selezionata e gli acidi grassi C10, C12 e C14, ma nessuna di esse presentava caratteristiche di eutettico. La dispersione più promettente è stata utilizzata per la preparazione delle compresse. Successivamente sono stati eseguiti gli esperimenti di riproducibilità e di rilascio dell’Ibuprofene, da parte delle compresse preparate. Si è valutato il rilascio da due compresse, una in HCl e una in tampone fosfato, dopo 30 minuti, 1 ora, 2 ore, 3 ore e 24 ore. Nell’esperimento di riproducibilità sono state selezionate sei compresse di cui 3 poste in un becher ciascuno con HCl, e 3 in tampone fosfato e sono stati valutati i rilasci dopo 30 minuti, 1 ora, 2 ore, 3 ore e 4 ore. Per questa parte della ricerca, lo strumento utilizzato è stato uno spettrometro UV-visibile e la concentrazione incognita è stata ricavata mediante la costruzione di una retta di taratura. È stato ottenuto un valore di R^2 vicino ad 1, e quindi una buona correlazione lineare tra i valori ottenuti sperimentalmente.
Sistemi a rilascio modificato Ibuprofene-acidi grassi: preparazione e caratterizzazione chimico-fisica
GAMBUZZA, MARTINA
2022/2023
Abstract
The present thesis project aims at designing and preparing a system that can serve as a prototype for a future anti-inflammatory oral pharmaceutical form. Specifically, the selected pharmaceutical form is a tablet, with the goal of achieving modified release. The active ingredient chosen for this formulation is Ibuprofen, a commonly used anti-inflammatory molecule in many formulations. Three fatty acids were used for the active ingredient's vehiculation in order to identify the most suitable one for obtaining a eutectic mixture. In the first phase, the physicochemical characterization of the raw materials used was performed. Analyses were conducted using scanning differential calorimetry, IR spectroscopy, X-ray diffractometry, and, only for pure Ibuprofen, thermogravimetric analysis. Physical mixtures of Ibuprofen and capric acid (C10), Ibuprofen and lauric acid (C12), and Ibuprofen and myristic acid (C14) were prepared and characterized. None of the mixtures proved suitable for achieving a eutectic. Therefore, solid dispersions of Ibuprofen and myristic acid were prepared, selected among the three fatty acids for being the most suitable based on its physicochemical characteristics, and the most promising dispersion was identified among them. In an attempt to further improve the formulation, additional mixtures were prepared between the selected solid dispersion and the fatty acids C10, C12, and C14, but none of them exhibited eutectic characteristics. The most promising dispersion was used for the preparation of tablets. Subsequently, reproducibility and release experiments of Ibuprofen from the prepared tablets were carried out. The release from two tablets, one in HCl and one in phosphate buffer, was evaluated after 30 minutes, 1 hour, 2 hours, 3 hours, and 24 hours. For the reproducibility experiment, six tablets were selected, with 3 placed in each beaker containing either HCl or phosphate buffer, and releases were evaluated after 30 minutes, 1 hour, 2 hours, 3 hours, and 4 hours. For this part of the research, a UV-visible spectrometer was used, and the unknown concentration was determined by constructing a calibration curve. A value of R^2 close to 1 was obtained, indicating a good linear correlation between the experimentally obtained values.È consentito all'utente scaricare e condividere i documenti disponibili a testo pieno in UNITESI UNIPV nel rispetto della licenza Creative Commons del tipo CC BY NC ND.
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https://hdl.handle.net/20.500.14239/17464