Vaginal fluconazole (FLZ) prolonged release tablets containing chitosan in physical blends with other bioadhesive polymers were designed. Chitosan was mixed with hydroxypropyl methylcellulose (HPMC), guar gum or sodium carboxymethyl cellulose (NaCMC) at different ratios and directly compressed into tablets. In-vitro release profiles of FLZ were monitored at pH 4.8. Compressing chitosan with HPMC at different ratios slowed FLZ release, however, time for 80% drug release (T) did not exceed 4.3 h for the slowest formulation (F11). Adding of chitosan to guar gum at 1:2 ratio (F3) showed delayed release with T 17.4 h while, in presence of PVP at 1:2:1 ratio (F5), T was 8.8 h. A blend of chitosan and NaCMC at 1:2 ratio (F15) showed prolonged drug release with T 11.16 h. Formulations F5 and F15 showed fair physical characteristics for the powder and tablets and were subjected to further studies. Fast swelling was observed for F15 that reached 1160.53 ± 13.02% in 4 h with 2 h bioadhesion time to mouse peritoneum membrane compared with 458.83 ± 7.09% swelling with bioadhesion time exceeding 24 h for F5. Extensive swelling of F15 could indicate possible dehydration effect on vaginal mucosa. Meanwhile, antifungal activity against s was significantly high for F5.
The aim of this work was to improve the in vitro dissolution of simvastatin through development of selfnanoemulsifying tablets. Various modified oils, surfactant and co-surfactant mixtures were used to prepare different self-nanoemulsifying drug delivery systems (SNEDDS) whose composition was optimized using drug-solubility, ternary phase diagram, system stability and droplet size distribution studies. Optimized SNEDDSs, with acceptable surfactant ratio, stability and particle size (nano-range) upon dilution with simulated gastric fluid (SGF, pH 1.2) under gentle agitation conditions, were loaded onto microcrystalline cellulose and nano-size colloidal silicon dioxide powders using loading factor (L f) = 0.2 and excipient ratio (R) = 20. Prepared powders were compressed into tablets and the in vitro performance of the prepared self-nanoemulsifying tablets was investigated. Results revealed that systems with 10% relatively polar oils (C 8), 60% Cremophore ® RH 40 (surfactant), and 30% Transcutol ® HP (co-surfactant), acquired good self-nanoemulsification properties either in liquid or tableted forms. Prepared self-nanoemulsifying tablets demonstrated significantly higher dissolution rates, compared to direct compression tablets (DCT) and marketed tablet (Zocor ®). In conclusion, self-nanoemulsifying tablets were able to introduce simvastatin successfully in a unique immediate-release solid dosage form.
In-situ polymerized methyl cyanoacrylate (MCA), ethyl cyanoacrylate (ECA), and butyl cyanoacrylate (BCA) were used to prepare nanocapsules of fluorescein or doxorubicin as markers by a w/o emulsion interfacial polymerization technique. Different concentrations of MCA were also used to show the effect of monomer concentration. The nanocapsules were characterized by electron microscopy, particle size analysis, holding capacity and in-vitro release of the marker substances. After selection of the polymerization solvent system, nearly spherical nanocapsules were obtained using each of the monomers. Most of the nanocapsules prepared were in the particle size range 500-1500 nm diameter. They were able to hold 55-74% of the marker initially present in aqueous solution. In-vitro dissolution studies showed that release of marker was retarded variably in an increasing order from nanocapsules containing MCA, ECA then BCA. Increasing the concentration of the monomer in the nanocapsules led to retardation of marker release.
The present investigation was designed to evaluate a psychoeducational intervention designed to increase understanding and awareness of adjustment and reintegration issues experienced by combat veterans following deployment. The specific issues addressed by this intervention are broader in scope than formal psychopathology or disorders experienced by a minority of combatants. Instead, the domain of difficulties covered pertains to many or most individuals returning from combat. Specifically, difficulties with emotion regulation, social functioning, planfulness and stress management among other concerns were delineated. Military and civilian attendees (N = 100) of two separate presentations of this model were asked to report on familiarity and understanding of reintegration difficulties incurred by homecoming combat veterans. Analyses indicated that relative to pre-intervention scores, attendees reported significantly greater understanding of numerous aspects of the post deployment experience and effect sizes were generally large (i.e., Cohen's d's were generally in excess of .8 at the item level and aggregate scale pre-post change = 1.04) [1]. Journal of Depression and Anxiety Jo urna l o f D e pr essio n a n d A nxiety
Diclofenac sodium (DS) a non-steroidal anti-inflammatory drug has a bitter taste and is a local stomach irritant. The aim of this study was to formulate taste masked DS orally dispersible tablets (ODTs) with targeted drug release in the intestine. Pellets of DS were designed using sugar sphere cores layered with DS followed by an enteric coat of Eudragit L100 and a second coat of Eudragit E100 for taste masking. The produced pellets had a high loading efficiency of 99.52% with diameters ranging from 493.7 to 638.9 µm. The prepared pellets were spherical with smooth surfaces on scanning electron microscopy examination. Pellets with the 12% enteric coat Eudragit L100 followed by 5% Eudragit E 100 resulted in 1.4 ± 0.5% DS release in simulated gastric fluid (SGF) and complete dissolution in simulated intestinal fluid (SIF). The pellets were then used to formulate ODTs. In vitro disintegration time of ODTs ranged from 20 ± 0.26 to 46 ± 0.27 s in simulated saliva fluid (SSF). Dissolution was less than 10% in SGF while complete drug release occurred in SIF. The release rate was higher for the optimized formulation (F12) in SIF than for the marketed product Voltaren® 25 mg tablets. The optimized ODTs formulation had a palatable highly acceptable taste.
The aim of this work was to develop self-nanoemulsifying liquisolid tablets (SNELT) to enhance the dissolution profile of poorly water-soluble simvastatin. SNELT present a unique technique of incorporating self-nanoemulsifying drug delivery systems (SNEDDS) into tablets. Optimized SNEDDS containing different oils, Cremophor RH 40 (surfactant) and Transcutol HP (co-surfactant), at different ratios, were used as liquid vehicles and loaded on carrier material, microcrystalline cellulose (MCC), and coating material, Cab-o-sil H-5 (nanosize colloidal silicon dioxide) powders at different loading factors (L ) and fixed excipient ratio (R = 20). The effect of using different carrier materials, granulated mannitol, crystalline mannitol, and maltodextrin with MCC at different ratios, and different coating materials, Aeroperl 300 (granulated silicon dioxide) at different excipient ratios (R), was also emphasized. Liquisolid powders with acceptable flowability, compressibility, and tablet weight were compressed into tablets. Results revealed that powders with L = 0.2 possessed the most preferable properties to be tableted. SNELT with MCC and Cab-o-sil H-5 were able to generate nanoemulsions and to enhance the cumulative percent of drug dissolved at 60 min significantly to reach up to 90%. Furthermore, using carrier material (granulated mannitol/MCC at ratio 3:1) enabled SNELT to disperse into nanoemulsion (Z-average = 25.7 nm) and improved the dissolution profile significantly to reach 99% at 60 min. Cab-o-sil H-5 proved to be a better coating material compared to Aeroperl 300. In conclusion, developed SNELT were promising in enhancing in vitro dissolution of simvastatin and excipients highly affect SNELT's performance.
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