Final published version
Research output: Contribution to Journal/Magazine › Journal article › peer-review
Research output: Contribution to Journal/Magazine › Journal article › peer-review
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TY - JOUR
T1 - Effect of pH, polymer concentration and molecular weight on the physical state properties of tolfenamic acid
AU - Sheraz, M.A.
AU - Ahmed, S.
AU - Rehman, I.U.
PY - 2015
Y1 - 2015
N2 - Tolfenamic acid (TA) has been transformed from crystalline to amorphous state through freeze-drying by using varying ratios of polyacrylic acid (PA) at various pH values. The characterization of the films has been carried out using X-ray diffraction, differential scanning calorimetry, Fourier transform infrared (FTIR) spectrometry and scanning electron microscopy. The results showed a gradual change in the solid state properties of TA and a complete transformation into its amorphous form in 1:8, 1:4, 1:2 and 1:1 ratios at pH 3, 4, 5 and 6, respectively. FTIR spectrometry reveals the formation of a yellow polymorphic form of TA. Polymer molecular weight has also been observed to affect the drug transformation and interaction as the low molecular weight PA (Mw ∼ 1800) was found to be most effective followed by its medium (Mv ∼ 450 000) and high molecular weight (Mv ∼ 3 000 000) forms. No signs of recrystallization in the TA-PA films were noted during the 12-week storage period. PA of low molecular weight has also been found more effective in inhibiting the recrystallization of the melt upon cooling thus proving a valuable polymer in producing stable amorphous solid dispersions of TA. © 2015 Informa Healthcare USA, Inc.
AB - Tolfenamic acid (TA) has been transformed from crystalline to amorphous state through freeze-drying by using varying ratios of polyacrylic acid (PA) at various pH values. The characterization of the films has been carried out using X-ray diffraction, differential scanning calorimetry, Fourier transform infrared (FTIR) spectrometry and scanning electron microscopy. The results showed a gradual change in the solid state properties of TA and a complete transformation into its amorphous form in 1:8, 1:4, 1:2 and 1:1 ratios at pH 3, 4, 5 and 6, respectively. FTIR spectrometry reveals the formation of a yellow polymorphic form of TA. Polymer molecular weight has also been observed to affect the drug transformation and interaction as the low molecular weight PA (Mw ∼ 1800) was found to be most effective followed by its medium (Mv ∼ 450 000) and high molecular weight (Mv ∼ 3 000 000) forms. No signs of recrystallization in the TA-PA films were noted during the 12-week storage period. PA of low molecular weight has also been found more effective in inhibiting the recrystallization of the melt upon cooling thus proving a valuable polymer in producing stable amorphous solid dispersions of TA. © 2015 Informa Healthcare USA, Inc.
KW - Amorphous
KW - Characterization
KW - Freeze-drying
KW - Polyacrylic acid
KW - Recrystallization
KW - polymer
KW - tolfenamic acid
KW - acrylic acid resin
KW - anthranilic acid derivative
KW - carbopol 940
KW - nonsteroid antiinflammatory agent
KW - Article
KW - crystallization
KW - differential scanning calorimetry
KW - drug solubility
KW - drug structure
KW - drug transformation
KW - freeze drying
KW - infrared spectroscopy
KW - molecular weight
KW - pH
KW - pH measurement
KW - physical chemistry
KW - priority journal
KW - scanning electron microscopy
KW - solid state
KW - X ray diffraction
KW - chemistry
KW - drug stability
KW - drug storage
KW - medicinal chemistry
KW - procedures
KW - Acrylic Resins
KW - Anti-Inflammatory Agents, Non-Steroidal
KW - Calorimetry, Differential Scanning
KW - Chemistry, Pharmaceutical
KW - Crystallization
KW - Drug Stability
KW - Drug Storage
KW - Freeze Drying
KW - Hydrogen-Ion Concentration
KW - Microscopy, Electron, Scanning
KW - Molecular Weight
KW - ortho-Aminobenzoates
KW - Polymers
KW - Spectroscopy, Fourier Transform Infrared
KW - X-Ray Diffraction
U2 - 10.3109/10837450.2013.871027
DO - 10.3109/10837450.2013.871027
M3 - Journal article
VL - 20
SP - 352
EP - 360
JO - Pharmaceutical Development and Technology
JF - Pharmaceutical Development and Technology
SN - 1083-7450
IS - 3
ER -