News

We are proud to announce that our latest manuscript “Physico-chemical properties of two anhydrous azathioprine forms and their interaction with typical pharmaceutical excipients: highlighting new findings in drug formulation development” was accepted by Drug Development and Industrial Pharmacy. Preformulation studies, as a first and proactive step in rational drug formulation development, play an important role in anticipating formulation issues and identifying realistic paths in dosage form technology. In order to develop a stable, effective and safe dosage form, its investigations are designed to establish the physico-chemical, physico-mechanical properties of drug substances, excipients and packaging materials. As different types of polymorphs exhibit different physicochemical properties in terms of solubility, stability or therapeutic activity, the purpose of this paper is to present an evaluation of the physicochemical properties of two anhydrous AZA forms and their interaction with typical pharmaceutical excipients. Potential interactions between excipients and AZA can lead to alteration in physico-chemical stability of dosage form. Compared with the already known oral AZA tablet form (known as Imuran or Azasan), an alternative that sustained a prolonged gastric residence was studied, as such new capsule formulations were proposed and manufactured. Such modifications in the delivery system are needed to overcome the disadvantages associated with oral tablet form and to provide drugs of higher selectivity for medical treatment. In comparison with available Imuran or Azasan tablet composition, using lactose or lactose monohydrate as a major excipient, in the current work the stability of AZA forms I and II in the presence of another common excipient non-hygroscopic, chemically stable, with good flow properties and high compressibility is evaluated. Moreover, for those patients with lactose intolerance, another stable composition can be an exciting finding in AZA formulation development. On the other hand, considering the sensitivity of AZA Form II to humidity, different excipients combination and mixture compositions are tested in order to identify the suitable and stable drug formulation for both anhydrous AZA forms. The stability of AZA Form II in the presence of D-Mannitol is shown through experimental data consisting of the application of several techniques (such as, PXRD, TG/DSC, FT-IR, FT-Raman). The detailed results of the study can be read here: https://doi.org/10.1080/03639045.2022.2032131 and we hope you will find it interesting.

 

This work was supported by the Romanian grant POC 2014-2020, Priority axis 1 – A1.2.3-G, 4529/2017 (AMD-FARMA-MED-RO) carried out in collaboration with National Institute of Materials Physics.

We are proud to announce that our latest manuscript “Isomorphic Channel-Type Pseudopolymorphs of Azathioprine: From Structural Confirmations to a Rational Polymorph Screening Approach” was accepted by Crystal Growth & Design. The main goal of the study is to understand the isostructurality exhibited by the core molecule (immunosuppressant drug Azathioprine) in interaction with four organic strong polar solvents through its similarities in conformation and molecular packing. The structural characterization of the four isomorphic channel-type pseudopolymorphs, together with the so far-unknown crystal structure of all of them by SC-XRD analysis allows for a comparative study of the conformational flexibility of AZA, and it provides knowledge about the factors that govern the molecular organization within the crystal structures of the investigated AZA solvates series. Moreover, this study provides a viable strategy for enabling early new drug forms and aims to transform a systematic screen into a rational polymorph screening approach contributing to a better understanding of drug polymorphism landscape in the view of solubility data gathered out in the primary steps of the screening programs. The detailed results of the study can be read here: https://doi.org/10.1021/acs.cgd.0c01718 and we hope you will find it interesting.

Please allow us to introduce the beautiful Tanya, a senior lady bear adopted by SARA Pharm. Tanya was rescued at age 34 from an unmodernized Zoo and now she spends her golden years surrounded by trees and swimming pools in Libearty Zarnesti, Romania, the largest brown bears sanctuary in the world, a home for over 100 bears. Every bear located in this forest sanctuary of more than 170 acres was saved from inappropriate conditions, abused captivity or they were orphan bear cubs left vulnerable in the forest.

SARA Pharm’s activity is carried out in accordance with an implemented quality system that complies the ethical and research integrity principles. We care about nature and wildlife preservation and we hope to meet Tanya in person bear, after the current, well-known, situation ends. We think that will happen soon.

We are proud to announce that our latest manuscript, part as H2020-MSCA-RISE-2017 consortium (CLATHROPROBES project) was accepted by Molecules. In this paper, we report the in situ spectroelectrochemical cyclic voltammetric studies of the antimony-monocapped nickel(II) and iron(II) tris-pyridineoximates with a labile triethylantimony cross-linking group and Zr(IV)/Hf(IV) phthalocyaninate complexes in order to understand the nature of the redox events in the molecules of heterodinuclear zirconium(IV) and hafnium(IV) phthalocyaninate-capped derivatives. The investigated hybrid molecular systems that combine a transition metal (pseudo)clathrochelate and a Zr/Hf-phthalocyaninate moiety exhibit quite rich redox activity both in the cathodic and in the anodic region. The detailed studies of the abovementioned compounds can read it here: https://www.mdpi.com/1420-3049/26/2/336/htm

This work was supported by the European Commission H2020-MSCA-RISE-2017 Grant number, 778245, by the Slovak Grant Agencies APVV (contract Nos. APVV-15-0053, APVV-15-0079, APVV-19-0024 and DS-FR-19-0035) and VEGA (contracts No. 1/0139/20, 1/0718/19, 1/0504/20 and 1/0466/18), and by the Fundação para a Ciência e Tecnologia (FCT) and project UIDB/00100/2020 of Centro de Química Estrutural, Portugal.

We are pround that the patent application submitted by SARA Pharm Solutions and National Institute of Materials Physics “Procedee de preparare și utilizare ale noilor forme cristaline ale 6-(3-metil-5-nitroimidazol-4-il)sulfanil-9H-purinei.” – original title (in Romanian) (“Processes for the preparation and use of novel crystalline forms of 6-(3-methyl-5-nitroimidazol-4-yl) sulfanyl-9H-purine.”) was recently published with no. 133946 A0 from 30/03/2020:

The invention relates to novel crystalline forms of 6-(3-methyl-5-nitroimidazol-4-yl) sulfanyl-9H-purine used in medicine as an immunosuppressant, in the treatment and prevention of autoimmune diseases, and in organ transplantation in order to reject organ by the host. The present invention describes novel crystalline forms of 6-(3-methyl-5-nitroimidazol-4-yl) sulfanyl-9H-purine as five novel solvated forms (III, IV, V, VI, VII) obtained by simple steps and easy to control, characterization methods and their uses.

This work was supported by the Romanian grant POC 2014-2020, Priority axis 1 – A1.2.3-G, 4529/2017 (AMD-FARMA-MED-RO) carried out in collaboration with National Institute of Materials Physics.

We are proud to announce that our latest manuscript was accepted by Journal of Molecular Structure. The paper reveals the crystal structure of a new anhydrous solid-state form of Azathioprine, determined directly form powder X-Ray diffraction data, employing the direct-space genetic algorithm technique for structure solution, followed by Rietveld refinement, and you can read it here: https://www.sciencedirect.com/science/article/abs/pii/S0022286018312602.

Sara Pharm team congratulates our colleague Dumitru Samohvalov for his first paper published in Nature Chemistry : Formation of the layered conductive magnet CrCl2(pyrazine)2through redox-active coordination chemistry.

SARA Pharm Solutions will exhibit at Pharma ChemOutsourcing event on September 17-19, 2018 in Long Branch, NJ, USA.
Please feel free to stop by our stand or contact us in order to arrange a meeting.

Since January 2018 we have been working with our partner NIMP- National Institute of Materials Physics in the AMD-FARMA-MED-RO project (Physico-chemical analyzes, nanostructured materials and devices for pharmaceutical and medical applications in Romania). SARA Pharm has been awarded a grant for this project as a result of the POC competition – section G 1.2.3. -Partnership for knowledge transfer.

We are proud to announce that SARA Pharm has been awarded an Horizon 2020 grant (H2020-MSCA-RISE-2017 for the CLATHROPROBES project whose primary objective is to the design and development of novel, highly efficient chiroptical, luminescent probes for sensing and structural studies of biomolecules based on cage metal complexes as molecular reporters.

Our partners in the project are UNIVERSITAT WIEN (Austria), FRIEDRICH-ALEXANDER-UNIVERSITAET ERLANGEN NUERNBERG (Germany), UNIWERSYTET WROCLAWSKI (Poland) and SC Princeton Biomolecular Research Labs (Ukraine).