Nefopam (N.F.) HCl is a non-narcotic centrally-acting, non-opioid benzoxazocine analgesic to relieve acute and chronic pain. It exhibits low bioavailability (about 36%) due to its first-pass degradation in the liver.
Intranasal administration has been used as a new route for targeting active brain sites and enhancing the bioavailability of N.F. HCl bypassing hepatic metabolism.
In situ gel of N.F. HCl was prepared by the cold method using different concentrations of Poloxamer 407, Poloxamer 188, HPMC K4M, Carbapol 934, and Hyaluronic acid polymers.
The results show that identification tests are superimposed with references, solubility study shows that N.F. HCl is suitable to be administered intranasally; Compatibi
... Show MoreThis study aims to develop a thermosensitive mucoadhesive periodontal in situ gel of secnidazole for local release of drug for treatment of periodontitis, in order to increase the drug residence time and to increase patient compliance while lowering the side effects of the drug.
Cold method was used to prepare 30 formulas of secnidazole periodontal in situ gel, using different concentrations of thermosensitive polymers (poloxamer407 alone or in combination with poloxamer 188) and methyl cellulose (MC ) or hydroxypropyl methylcellulose (HPMC K4M )in different concentrations used as mucoadhesive polymer and the resultant formulations were subjected to several tests such as gelation temperature GT, appearance and pH value. The fo
... Show MoreLasmiditan (LAS) was formulated as a nanoemulsion based in situ gel (NEIG)with the aim of improving its oral bioavailability via application intranasally. The solubility of LAS in oils, emulsifiers, and co-emulsifiers was determined to identify nanoemulsion (NE)components. Phase diagrams were constructed to identify the area of nanoemulsification. LAS NE was formulated using the spontaneous nanoemulsification method. Four NEs (F19, F24, F31, and F34) containing 7-15 % oleic acid (OA) as an oily phase, 40-55% labrasol (LR), and transcutol (TC) as emulsifier mixture at (1:1), (2:1), (3:1), and (1:2) ratio with 30-53 % (w/w) aqueous phase, having suitable optical transparency of 95–98%, globule size of 104-140 nm and polydisper
... Show MoreThe purpose of this study was to develop poloxamer-based in-situ gel of chloramphenicol aiming to increase bioavailability and prolong corneal contact time, controlling drug release, and enhancing ocular bioavailability. The in-situ gel was prepared using different concentrations of poloxamer 407 combined with hydroxypropyl methyl cellulose (HPMC) or carbapol 940 to achieve gelation temperature about physiological temperature and improve rheological behavior and gelling properties of poloxamer gel. The prepared formulations were evaluated for their appearance, pH, and sol-gel transition temperature. The formulations F2, F3, and F5 have a gelation temperature within the accepted range 35-370C an
... Show MoreThis study aimed to develop an oral drug delivery system for gastro-retentive sustained drug release of baclofen by using a 3D printed capsular device since baclofen has a short half-life of 2.5 to 4 hours and has a narrow absorption window. Firstly sustained-release tablets of baclofen were formulated through the hot-melt extrusion of various thermoplastic polymers and direct compression of the extrudate, then a capsular device was designed and 3D printed to contain two air pockets to enable floating of the device and has four windows for drug release.
3D printing of the capsular device was done by an FDM printer using biodegradable PLA filament, and the sustained release tablets were inserted into the device to allow the medici
... Show MoreThe aim of the present study is to formulate floating effervescent microsponge tablet of the narrow absorption window drug, Baclofen (BFN) for controlling drug release and thereby decrease the side effect of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablet. The prepared fl
... Show MoreItraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients.
The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles.
Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula wit
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