Physico-chemical characterization of omeprazole and its salts

U razvoju lijekova važno je izabrati najprimjereniju kristalnu formu aktivne tvari. Tvari, koje su stabilne samo u određenom pH području, predstavljaju izazov za razvoj formulacije. Istraživana molekula omeprazol spada u skupinu prazola; lijekova koji su inhibitori protonske pumpe u ljudskom organizmu, a njihovo je glavno obilježje snažno i dugotrajno smanjenje stvaranja želučane kiseline. Za prazole je poznato, da su osjetljivi na degradaciju u kiselom okruženju. Zato se u formulaciji stabiliziraju alkalnim dodacima ili se daju u obliku bazičnih soli. Priprava i karakterizacija bazičnih soli je potrebna u slučaju izravne uporabe u formulaciji, odnosno i za praćenje mogućeg zasoljavanja slobodne molekule. Za potrebe istraživanja sintetizirane su soli omeprazola iz skupine alkalijskih (Li, Na, K) i zemnoalkalijskih metala (Mg, Ca). Istražena su i fizikalno-kemijska svojstva pet soli, koristeći neke analitičke metode (Ramanovu i Fourier-transformiranu infracrvenu mikroskopiju, analizu na termopostolju, dinamičku sorpciju vlage, nuklearnu magnetsku rezonanciju, difrakciju rentgenskih zraka na polikristalnom uzorku, termogravimetriju, diferencijalnu pretražnu kalorimetriju te teorijski izračun vibracijskih frekvencija). Zaključeno je, da je vibracijska spektroskopija prikladna spektroskopska metoda, koja na točan, brz i nedestruktivan način određuje fizikalno-kemijske karakteristike omeprazola i njegovih soli.In drug development, it is important to have a suitable crystalline form of the active substance. Substances that are stable only within a certain pH range are a challenge for the formulation developement. Omeprazole molecule belongs to the group of prazoles; drugs which are proton pump inhibitors in the human body, but their main characteristic is a strong and long-lasting reduction of gastric acid formation. For the prazoles, it is known to be sensitive to degradation in an acid environment. The formulation is then stabilized with alkaline additives or is used in the form of basic salts. Preparation and characterization of basic salts is needed in the case of use in the formulation and to monitor any possible salinization of free molecule. For purposes of this study, the salts of omeprazole from the group of alkali metal (Li, Na, K) and alkaline earth metals (Mg, Ca) were synthesized. Also the physicochemical properties of five salts were probed, using Fourier-transform infrared and Raman microscopy, hot stage, dynamic vapour sorption, nuclear magnetic resonance, thermogravimetry, diffferenctial scanning calorimetry and theoretical calculation of vibrational frequencies. It was found, that vibrational spectroscopy serves as appropriate spectroscopic tool which in accurate, quick and non-destructive way determines the physicochemical characteristics of omeprazole and its salts

Solubilization of ibuprofen for freeze dried parenteral dosage forms

Ibuprofen, a weakly acidic non-steroidal anti-inflammatory drug having poor aqueous solubility, is a challenging drug for the development of pharmaceutical formulations, resulting in numerous research attempts focusing on improvement of its solubility and consequently bioavailability. Most studies have been done for solid dosage forms, with very little attention paid to parenterals. Hence, the main purpose of the present study was to enhance ibuprofen solubility as a result of formulation composition and the freeze drying process. Moreover, the purpose was to prepare a freeze dried dosage form with improved ibuprofen solubility that could, after simple reconstitution with water for injection, result in an isotonic parenteral solution. Solubility of ibuprofen was modified by various excipients suitable for parenteral application. Drug interactions with selected excipients in the final product/lyophilisate were studied by a combined use of XRPD, DSC, Raman and ssNMR. Analyses of lyophilized samples showed solubility enhancement of ibuprofen and in situ formation of an ibuprofen salt with the alkaline excipients used

Spectroscopic Characterization of Omeprazole and Its Salts

During drug development, it is important to have a suitable crystalline form of the active pharmaceutical ingredient (API). Mostly, the basic options originate in the form of free base, acid, or salt. Substances that are stable only within a certain pH range are a challenge for the formulation. For the prazoles, which are known to be sensitive to degradation in an acid environment, the formulation is stabilized with alkaline additives or with the application of API formulated as basic salts. Therefore, preparation and characterization of basic salts are needed to monitor any possible salinization of free molecules. We synthesized salts of omeprazole from the group of alkali metals (Li, Na, and K) and alkaline earth metals (Mg, Ca). The purpose of the presented work is to demonstrate the applicability of vibrational spectroscopy to discriminate between the OMP and OMP-salt molecules. For this reason, the physicochemical properties of 5 salts were probed using infrared and Raman spectroscopy, NMR, TG, DSC, and theoretical calculation of vibrational frequencies. We found out that vibrational spectroscopy serves as an applicable spectroscopic tool which enables an accurate, quick, and nondestructive way to determine the characteristic of OMP and its salts

Solubilization of ibuprofen for freeze dried parenteral dosage forms

Ibuprofen, a weakly acidic non-steroidal anti-inflammatory drug having poor aqueous solubility, is a challenging drug for the development of pharmaceutical formulations, resulting in numerous research attempts focusing on improvement of its solubility and consequently bioavailability. Most studies have been done for solid dosage forms, with very little attention paid to parenterals. Hence, the main purpose of the present study was to enhance ibuprofen solubility as a result of formulation composition and the freeze drying process. Moreover, the purpose was to prepare a freeze dried dosage form with improved ibuprofen solubility that could, after simple reconstitution with water for injection, result in an isotonic parenteral solution. Solubility of ibuprofen was modified by various excipients suitable for parenteral application. Drug interactions with selected excipients in the final product/lyophilisate were studied by a combined use of XRPD, DSC, Raman and ss-NMR. Analyses of lyophilized samples showed solubility enhancement of ibuprofen and in situ formation of an ibuprofen salt with the alkaline excipients used

AROME-ESO Oncology Consensus Conference: access to cancer care innovations in countries with limited resources. Association of Radiotherapy and Oncology of the Mediterranean Area (AROME-Paris) and European School of Oncology (ESO - Milan)

Purpose: Cancer is a leading cause of mortality worldwide. Its incidence is still increasing, particularly in developing countries. Recent progresses further strengthen the differences between low/middle and high-income countries. This situation calls for joint action to reduce inequities in cancer outcomes among the patients. The Association of Radiotherapy and Oncology of the Mediterranean Area (AROME) and the European School of Oncology (ESO), have initiated joint conferences devoted to access to innovations in oncology in the Mediterranean area. The heterogeneity of the economic, political and cultural situations of the different participating countries, offers the opportunity to develop consensus conference

Ružička days : International conference 18th Ružička Days “Today Science – Tomorrow Industry” : Proceedings

Proceedings contains articles presented at Conference divided into sections: chemical analysis and synthesis, chemical and biochemical engineering, food technology and biotechnology, medical chemistry and pharmacy, environmental protection and meeting of young chemists