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Rapid-onset sildenafil nasal spray carried by microemulsion ... - NCBI Rapid-onset sildenafil nasal spray carried by microemulsion ... - NCBI
Mar 22, 2011 ... Rapid-onset sildenafil nasal spray carried by microemulsion systems: in vitro evaluation and in vivo pharmacokinetic studies in rabbits.

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In addition, nasal ciliotoxicity studies were carried out using in vivo rat nasal mucosa model and showed no ciliotoxicity. Nasal absorption of sildenafil from this microemulsion was found to be fairly rapid. The phase behaviour and solubilization capacity of the microemulsion system were characterized, and nasal absorption of sildenafil from the microemulsion formulations was investigated in rabbits.

Cohesion at the apices of epithelial cells occurs in specialized regions collectively referred to as the junctional complex. Pharmacokinetic analysis was performed by means of a model independent method 2000 computer program. Me6 (with no nasal ciliotoxicity) was evaluated in a group of six rabbits in a randomized crossover study and compared to the marketed oral tablets.

For all animal studies, the experimental procedures conformed to the ethical principles of the center of applied research and advanced studies, faculty of pharmacy, cairo university on the use of the animals. Appropriate quantities of oleic acid, labrasol, and cosurfactant were stirred at high rate until it formed clear solution, then water was added dropwise to each mixture under vigorous stirring. The detection wave length was 220 nm (ultraviolet variable wavelength detector, model spd-20a shimadzu, japan).

The oils selected were isopropyl myristate, miglyol, labrafil formulation of different microemulsion systems and determination of solubility of sildenafil citrate in these systems o and surfactant (labrasol), and cosurfactant (transcutol, plurol or dmi) mixtures were constructed at room temperature (25c). The prepared systems were characterized in relation to their clarity, particle size, viscosity, ph, and nasal ciliotoxicity. For nasal application, sildenafil citrate was formulated in two different systems the first was a cosolvent system (s3) of benzyl alcoholethanolwatertranscutoltaurodeoxy cholatetween 20 (0.

The solubilities of sildenafil citrate in different microemulsion systems at 25c are shown in table. The ow microemulsions formed are shown in three-component triangular diagram (fig. Solubilities of sildenafil citrate in different oils at 25c were presented in table.

A major component of this relaxation process is mediated by nitric oxide stimulation of cyclic guanosine monophosphate (cgmp). Systems s1 to s5 were prepared according to the composition listed in table ) and saturated solubility of sildenafil citrate in these solvent mixtures at 25c determination of saturated solubility of sildenafil citrate in different oils this step was performed as previously discussed in order to select the suitable oil which has a good solubilizing capacity for sildenafil citrate. The solubilities of sildenafil citrate in different cosolvent mixtures at 25c were 34. All animals were treated according to the principles of laboratory animal care (national institutes of health publication 86-32) ( after administration of the different formulations, blood samples (1. This structure controls the diffusion of ions and molecules between cells and constitutes a barrier to the intercellular movement of macromolecules across the epithelium ( ).


Intranasal Microemulsion of Sildenafil Citrate: In Vitro Evaluation ...


Mar 31, 2009 ... The purpose of the present study was to prepare intranasal delivery system of sildenafil citrate and estimate its relative bioavailability after ...

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Ketanest Nasal Dosierung Viagra Sale The obtained serum samples were deep-frozen at 20c, pending hplc analysis. Systems s1 to s5 were prepared according to the composition listed in table ) and saturated solubility of sildenafil citrate in these solvent mixtures at 25c determination of saturated solubility of sildenafil citrate in different oils this step was performed as previously discussed in order to select the suitable oil which has a good solubilizing capacity for sildenafil citrate. Determination of sildenafil citrate solubility in different cosolvent systems different cosolvent systems were used to determine the maximum solubility of sildenafil citrate by the same method mentioned in the previous step. Priest, france) oleic acid, taurodeoxycholate, and tween 20 were purchased from sigma co. An oleic acid-based microemulsion system with a member of the tween series or cremophor el as the surfactant and a short-chain alcohol as the cosolvent was developed for rapid-onset intranasal delivery of sildenafil. This study aimed to develop a new sildenafil intranasal formula and to study its relative bioavailability compared to the conventional oral tablets after intranasal administration to rabbits.
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    The oils selected were isopropyl myristate, miglyol, labrafil formulation of different microemulsion systems and determination of solubility of sildenafil citrate in these systems o and surfactant (labrasol), and cosurfactant (transcutol, plurol or dmi) mixtures were constructed at room temperature (25c). Pseudo ternary phase diagram of a microemulsion system composed of oil (oleic acid), surfactant (labrasol), cosurfactant (transcutol), and water. The plasma analysis of sildenafil was performed using a well validated hplc-uv method after liquidliquid extraction. Nasal delivery has been paid attention as an alternative dosage form. During the addition of water to the selected oily mixtures (mixture of oleic acid, labrasol, transcutol in addition to dmi in all formulations, a continuous transition from water in oil systems (wo) to oil in water (ow) systems was observed, a transparent, one-phase and low viscous system was obtained.

    The solubilities of sildenafil citrate in different microemulsion systems at 25c are shown in table. Sildenafil displayed a high solubility of 124 mgml in the microemulsion consisting of 40 oleic acid, 10 h(2)o, and 50 tween 80ethanol (ea) (at a 14 weight ratio). The vials were well closed and left to be shaken at 25c for 24 h in thermostatically controlled shaking water bath. The palate was dissected out, and the mucocilia was examined with an optical microscope (leica imaging systems, cambridge, england). Systems s1 to s5 were prepared according to the composition listed in table ) and saturated solubility of sildenafil citrate in these solvent mixtures at 25c determination of saturated solubility of sildenafil citrate in different oils this step was performed as previously discussed in order to select the suitable oil which has a good solubilizing capacity for sildenafil citrate.

    A high-fat meal delays the onset of action for sildenafil ( ). For nasal application, sildenafil citrate was formulated in two different systems the first was a cosolvent system (s3) of benzyl alcoholethanolwatertranscutoltaurodeoxy cholatetween 20 (0. Department of orthopedics and traumatology, taipei medical university hospital, taipei, taiwan, roc. It is rapidly absorbed after oral administration with absolute bioavailability 40. Sildenafil citrate tablet (viagra 50 mg) was crushed and suspended in 5 ml of saline. The solubilities of sildenafil citrate in different cosolvent mixtures at 25c were 34. The formation of microemulsion systems (me1me7) was observed at room temperature. Increasing amounts of sildenafil citrate were added portion-wise to 2 ml of each microemulsion system with stirring after each addition to form a clear and transparent liquid till excess solid does not dissolve. Within-day accuracy and precision of the method and the reproducibility of the assay (tables not shown) revealed that the mean cv was. Ed is a side effect commonly associated with use of the selective serotonin uptake inhibitors to treat depression ( ).

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