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1.
Molecules ; 28(9)2023 May 03.
Article in English | MEDLINE | ID: mdl-37175270

ABSTRACT

The low water solubility of an active pharmaceutical ingredient (aripiprazole) is one of the most critical challenges in pharmaceutical research and development. This antipsychotic drug has an inadequate therapeutic impact because of its minimal and idiosyncratic oral bioavailability to treat schizophrenia. The main objective of this study was to improve the solubility and stability of the antipsychotic drug aripiprazole (ARP) via forming binary as well as ternary inclusion complexes with hydroxypropyl-ß-cyclodextrin (HPßCD) and L-Arginine (LA) as solubility enhancers. Physical mixing and lyophilization were used in different molar ratios. The developed formulations were analyzed by saturation solubility analysis, and dissolution studies were performed using the pedal method. The formulations were characterized by FTIR, XRD, DSC, SEM, and TGA. The results showcased that the addition of HPßCD and LA inclusion complexes enhanced the stability, in contrast to the binary formulations and ternary formulations prepared by physical mixing and solvent evaporation. Ternary formulation HLY47 improved dissolution rates by six times in simulated gastric fluid (SGF). However, the effect of LA on the solubility enhancement was concentration-dependent and showed optimal enhancement at the ratio of 1:1:0.27. FTIR spectra showed the bond shifting, which confirmed the formation of new complexes. The surface morphology of complexes in SEM studies showed the rough surface of lyophilization and solvent evaporation products, while physical mixing revealed a comparatively crystalline surface. The exothermic peaks in DSC diffractograms showed diminished peaks previously observed in the diffractogram of pure drug and LA. Lyophilized ternary complexes displayed significantly enhanced thermal stability, as observed from the thermograms of TGA. In conclusion, it was observed that the preparation method and a specific drug-to-polymer and amino acid ratio are critical for achieving high drug solubility and stability. These complexes seem to be promising candidates for novel drug delivery systems development.


Subject(s)
Antipsychotic Agents , beta-Cyclodextrins , 2-Hydroxypropyl-beta-cyclodextrin , Solubility , Aripiprazole , beta-Cyclodextrins/chemistry , Solvents , Arginine/chemistry , Pharmaceutical Preparations , Calorimetry, Differential Scanning , Spectroscopy, Fourier Transform Infrared
2.
Clin Med Res ; 14(3-4): 159-162, 2016 Dec.
Article in English | MEDLINE | ID: mdl-28188140

ABSTRACT

Angioimmunoblastic T-cell lymphoma (AITL) is a rare subtype of peripheral T-cell lymphoma (PTCL). AITL typically presents with lymphadenopathy, fever, rash, hepatosplenomegaly, and rarely polyarthritis. We report the case of a 50-year-old female who presented with lymphadenopathy, rash, and symmetric polyarthritis. She was later diagnosed with AITL and was treated with chemotherapy with resolution of arthritis. AITL should be suspected in paitents presenting with rheumatoid-like arthritis and diffuse lymphadenopathy.


Subject(s)
Arthritis/complications , Immunoblastic Lymphadenopathy/complications , Lymphoma, T-Cell/complications , Lymphoma, T-Cell/diagnosis , Antineoplastic Agents/therapeutic use , Arthritis/diagnosis , Arthritis, Rheumatoid/complications , Arthritis, Rheumatoid/diagnosis , Cartilage , Diagnosis, Differential , Exanthema/complications , Female , Humans , Immunoblastic Lymphadenopathy/diagnosis , Immunohistochemistry , Lymphadenopathy/complications , Lymphoma, T-Cell/drug therapy , Middle Aged , Treatment Outcome
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