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Journal of Pharmacy Research
ISSN NO: 0974-6943
The Journal of Pharmacy Research is an online Journal, publishing of correct version and document can be modified when, we/or author get comments from any readers. The journal is devoted to the promotion of Pharmaceutical sciences and related disciplines (including Pharmacy, medical, Biotech, Botany, organic and medicinal chemistry,  Nursing, Paramedical, prescription etc  fields).



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Journal: Journal of Pharmacy Research , Volume: 6, Issue: May
Article Id: JPRS-PCS-00001294
Title: Utility of plasticised polymer in solid dispersions for solubility enhancement of thermosensitive and poorly soluble API
Category: Pharmaceutics
Section: Research Article
Author Affiliation: Department of Pharmaceutics, Institute of Pharmacy, National Institute of Medical Sciences University, Shobha Nagar, Jaipur 303121, Rajasthan, India
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Background/objective: Despite sophisticated technique as hot melt extrusion has established its place in formation of amorphous molecular dispersions, the advantage of which can’t be extrapolated to thermosensitive poorly soluble API, like Acetazolamide, because of inherent formulation problems such as degradation and/or browning following melting, residual crystallinity if processed at lower temperature than its melting point and processing problems such as poor extrudability. Thus the present study interestingly explores a stepwise approach to obtain solubility enhanced, thermodynamically stable amorphous molecular dispersions of thermosensitive drugs by hot melt extrusion technique. Methods: Solid dispersions of Acetazolamide with a polymethacrylate solubiliser in 1:1 and 1:2 weight ratios and with a solubiliser and a plasticiser in 1:2:0.15 and 1:2:0.30 weight ratios were prepared by hot melt extrusion and studied for drug content, thermal degradation, molecular interactions, solid state characterisation, solubility characteristics and subsequently accelerated stability study. Results: The formulation and the processing problems associated with solid dispersions of Acetazolamide with a solubiliser were overcome by coprocessing their optimised proportion with appropriate proportion of plasticiser, giving completely amorphous, molecular dispersions of Acetazolamide with markedly enhanced solubility characteristics. During stability study, the optimised proportion of solid dispersions reported only an insignificant change in solubility characteristics and amorphous nature of the drug. Conclusion: Thus, the study provided formulation strategies in a stepwise manner to enhance solubility characteristics of a poorly soluble API showing thermal degradation when processed by hot melt extrusion.

Journal: Journal of Pharmacy Research , Volume: 6, Issue: May
Article Id: JPRS-PC-00001295
Title: Synthesis, spectral analysis and biological screening of some new N-(un)substituted N-(5-chloro-2-methoxyphenyl)-aryl sulfonamides
Category: Pharmaceutical Chemistry
Section: Research Article
Author Affiliation: Department of Chemistry, Government College University, Lahore 54000, Pakistan
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Objectives: Due to various biological activities of sulfonamides, a series of new N-(5-chloro- 2-methoxyphenyl)-aryl sulfonamides (3aee) and their N-benzyl/ethyl substituted derivatives (6a-e & 7a-e) were synthesized followed by antibacterial activity evaluation. Methods: A facile and environmentally benign series of N-(5-chloro-2-methoxyphenyl)-aryl sulfonamide (3aee) was synthesized in basic aq. medium by coupling of 5-chloro-2- methoxyaniline (1) and various aryl sulfonyl chlorides (2aee). Further N-benzyl/ethyl substituted derivatives (6aee & 7aee) were synthesized by stirring 3aee with the electrophiles 4 & 5 at room temperature (RT). The structure elucidation of the synthesized compounds was processed through spectral data. Results: All the newer synthesized aryl sulfonamide derivatives were obtained in moderate to good yields in the range of 74e85%. Out of fifteen synthesized derivatives, six compounds 3b, 3c, 3e, 6a, 7d & 7e were active against the both bacterial strains of Grampositive bacteria relative to ciprofloxacin, the reference standard. The significant activity of compound 6a against all bacterial strains might be due to ethyl and ter-butyl groups in the molecule. Conclusion: The synthesized compounds exhibited moderate to good activity against the applied bacterial strains and so the structural changes in the substituents altered the inhibitory properties significantly.