Preparation and Evaluation of Mouth Dissolving Films for the Delivery of Almotriptan

Abstract

The aim of the present investigation is to prepare and evaluate mouth dissolving films (MDFs) of Almotriptan (ALMO) and to find out the effect of various formulation variables like film thickness, plasticizers, polymer viscosities and solubilizing agents on physico-mechanical and drug release properties of ALMO. Hydroxyl propyl methyl cellulose (HPMC E3, E5, E15) of different viscosity grades were used as film forming agents, poly ethylene glycol (PEG-400) and glycerol as plasticizers. The developed MDFs were characterized for film thickness, disintegration time, FTIR, DSC, XRD and drug release behavior. The films were homogenous, elegant, transparent and smooth in texture. Photomicrographs, along with DSC and XRD studies confirm no recrystallization of ALMO with in MDFs. In-vitro dug release studies indicate that HPMC E15 films attributed to their higher viscosity showed slower ALMO release compared to other formulations. Addition of solubilizing agents (PVP K30 and SLS) to HPMC E3 formulations brought a significant increase in ALMO release rates compared to formulations without them. The formulation F5 showed quicker disintegration (within 8.66sec) and ALMO release rates (complete release was obtained in 80sec) along with good physico-mechanical properties. Accelerated stability studies revealed no significant change in appearance and ALMO content in MDFs indicating that ALMO was stable in MDFs.

Novel quinoline derivatives carrying nitrones/oximes nitric oxide donors: Design, synthesis, antiproliferative and caspase-3 activation activities

“…The 2-alkylthioquinoline-3-carbaldhyde derivatives 4a-h were prepared by stirring of compounds 1a or 1b with sodium sulfide in DMF, further alkylation in the same reaction with different alkyl halides afforded the intermediates 4a-h. [49] The structure of the new derivatives 4d-f was confirmed by 1 H NMR, mass spectroscopy, and elemental analysis. 1 H NMR spectra of compounds 4d-f exhibited a common singlet signal at δ 10.18-10.16 ppm related to −CHO. The aldehydic carbon appeared at δ 191.9-191.6 ppm in 13 C NMR spectrum.…”

“…Additionally, quinolines are considered as an interesting group of compounds, many of which have widespread pharmacologicalactions such as anti-microbial, [1][2][3][4] anti-inflammatory, [5][6][7][8] antitubercular, [9][10][11][12] anti-convulsant, [13] antihypertensive, [14,15] antioxidant, [16][17][18][19] and anticancer [20] activities. Nitrones can release nitric oxide in larger amounts compared to corresponding oximes.…”

“…actions such as anti-microbial, [1][2][3][4] anti-inflammatory, [5][6][7][8] antitubercular, [9][10][11][12] anti-convulsant, [13] antihypertensive, [14,15] antioxidant, [16][17][18][19] and anticancer [20] activities. Several mechanisms can explain the anticancer effect of quinoline derivatives including: topoisomerase inhibition, [21][22][23] DNA intercalation, [24] protein kinases inhibition, [25][26][27] tubulin polymerase inhibition, [28][29][30][31] and induction of apoptosis.…”