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THE POSSIBILITY OF USING X-RAY POWDER DIFFRACTION, INFRARED AND RAMAN SPECTROSCOPY IN THE STUDY OF THE IDENTIFICATION OF STRUCTURAL POLYMORPHS OF ACETAMINOPHEN

100%

Stasiłowicz A., Mizera M., Tykarska E., Lewandowska K., Miklaszewski A., Cielecka-Piontek J.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 6

997-1004

Paracetamol (acetaminophen), a pain-killer with antipyretic properties, shows structural polymorphism. It occurs in three polymorphic forms: monoclinic, orthorhombic, and unstable form III. In the study, the commercially available samples of paracetamol (P1 and P2) were examined using X-ray powder diffraction, infrared, and Raman spectroscopy. Results demonstrated that all of the methods defined polymorphic forms of paracetamol in the samples. However, only Raman spectroscopy and PXRD methods detected impurities in the sample P1. These methods transpired to be more sensitive than the FT-IR method, which identified samples of paracetamol as one structural form (monoclinic polymorph). Moreover, the Raman spectroscopy identified impurities in the form P1 as changes in the crystalline form.

Synthesis, immunosuppressive properties, mechanism of action and X-ray analysis of a new class of isoxazole derivatives

84%

Bąchor U., Ryng S., Mączyński M., Artym J., Kocięba M., Zaczyńska E., Kochanowska I., Tykarska E., Zimecki M.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 2

251-263

In the search for potential therapeutics, isoxazole derivatives are still objects of interest. Previously described immunoregulatory properties of 5-amino-3-methyl-4-isoxazolecarboxylic acid (AC) benzylamides prompted us to synthesize a new class of compounds of immunotropic activity. A series of new compounds containing the isoxazole moiety were synthesized using Passerini three-component reaction. The effects on phytohemagglutinin A (PHA)-induced proliferation of human peripheral blood mononuclear cells (PBMC), production of tumor necrosis factor alpha (TNF α) in human whole blood cultures stimulated with lipopolysaccharide (LPS) and two-way mixed lymphocyte reaction (MLR) of PBMC, were investigated. Also, the effect of 1-(cyclohexylcarbamoyl)cyclohexyl 5-amino-3-methylisoxazole-4-carboxylate (PUB1) on the expression of signaling molecules associated with cell apoptosis in Jurkat cells was also determined. The results showed that the compounds inhibited to various degree mitogen-induced PBMC proliferation in a dose-dependent manner and TNF α production at 10 μg/ml. PUB1 compound, selected on the basis of its strongest antiproliferative activity, was also shown to inhibit MLR. The molecular data suggest that immunosuppressive action of PUB1 depended on induction of Fas and elevation of caspase 8 expression. In summary, we revealed immunosuppressive properties of a new class of isoxazoles and established the mechanism of action of a representative PUB1 compound.

The radiolytic studies of panipenem in the solid state

84%

Zalewski P., Rosiak N., Kilińska K., Skibiński R., Szymanowska D., Tykarska E., Piekara-Sady L., Lewandowska K., Miklaszewski A., Piontek J. C.

Acta Poloniae Pharmaceutica - Drug Research

2020

vol. 77

issue 2

241-250

The influence of ionizing radiation on the physicochemical properties of panipenem in solid state was studied. In the first part of our studies, we evaluated the possibility of applying radiosterilization to obtain sterile panipenem. Spectroscopic (FT-IR, Raman), chromatography (HPLC and HPLC-MS) and X-ray powder diffraction (XRPD) studies have shown that irradiation of ertapenem with the 25 kGy, the dose required to achieve sterility, does not change the physicochemical properties of the studied compound. The antimicrobial activity of panipenem irradiated with the dose of 25 kGy was reduced for three species. It was confirmed that the decrease in antimicrobial activity might be related to isomerization of panipenem.

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3 Acta Poloniae Pharmaceutica - Drug Research

1 2020

2 2019

3 Tykarska E.

2 Lewandowska K.

2 Miklaszewski A.

1 Artym J.

1 Bąchor U.

1 Cielecka-Piontek J.

1 Kilińska K.

1 Kochanowska I.

1 Kocięba M.

1 Mizera M.

1 Mączyński M.

1 Piekara-Sady L.

1 Piontek J. C.

1 Rosiak N.

1 Ryng S.

1 Skibiński R.

1 Stasiłowicz A.

1 Szymanowska D.

1 Zaczyńska E.

1 Zalewski P.

1 Zimecki M.

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THE POSSIBILITY OF USING X-RAY POWDER DIFFRACTION, INFRARED AND RAMAN SPECTROSCOPY IN THE STUDY OF THE IDENTIFICATION OF STRUCTURAL POLYMORPHS OF ACETAMINOPHEN

Synthesis, immunosuppressive properties, mechanism of action and X-ray analysis of a new class of isoxazole derivatives

The radiolytic studies of panipenem in the solid state