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Objective: The goal behind of performing this study was to come out with an oroslippery buoyant ranitidine hydrochloride tablet to ease the swallowing process. Hence, the drug is released controllably in the stomach regardless of the effect on gastric emptying time.Materials and Methods: The core of the buoyant containing 150 mg of the drug was compressed directly, and sodium bicarbonate was employed as an effervescent agent, besides, hydroxyl propyl methyl cellulose (HPMC) polymer was utilized in different grades in the formulation process. The prepared core was immersed in the coating dispersion, which was formulated using xanthan gum (slipping agent) and Kollicoat instant release (IR) (for film formation). According to the variables in the formulation process, floating properties varies along with the release profile of the drug; therefore, investigation of the effects of variables was conducted, including polymer type and concentration in the core part, and the effect of Kollicoat IR amount as well as the level of coating.Results: According to this study, it was clearly obvious that T4 formulation, that consisted of HPMC K4M, after being dipped 2 times in dispersion of 0.3% xanthan gum and 14% Kollicoat IR, had provided an instant floating, moreover, the in vivo slipperiness was quite acceptable as well as the taste masking. Nevertheless, the percentage of drug release measured after 6 h was 90.15%.Conclusion: The resultant formulas is quite promising to take the lead as new approach to easy swallowing tablets without need of water especially for patients with swallowing problems as well as it is floating tablet that can retain the drug in gastric cavity to be continuously released to ensure its maximum absorption and may improve its bioavailability.

Different tablet dosage forms were prepared to be administered for patients with dysphagia (swallowing difficulties) like buccal, sublingual and orodispersible tablets, however, they possesses certain constrains like taste masking difficulties, limitations in drug and dose selection and friability. Hence, in an attempt to overcome these constrains, a new easily swallowed immediate release tablets containing (160mg) Valsartan were prepared, and designed to be slippery upon contact with saliva giving an easy swallowing of the intact tablet (without water) with efficient taste masking effect, thus, they called Oroslippery tablets (OSTs). Core tablets were prepared by direct compression using different superdisintegrants, followed by dipping in special coating dispersion containing different proportion of kollicoat IR (film former) and xanthan gum (slipperiness inducer) at different coating levels. These OSTs were optimized for their physical properties, in-vitro disintegration and release in addition to in-vivo slipperiness and taste masking effect. It was found that F12 containing 6% crosscarmellose sodium double coated with 15% kollicoat IR and 0.3% xanthan gum possessed a good mechanical strength (hardness=5.69±0.58 Kg/cm 2 , friability=0.09%±0.79), suitable in-vivo slipperiness and taste masking times (8±1.45 and 58±2.18 seconds) respectively, with longer disintegration time (5.57±1.36 minutes) but similar release profile to the commercial conventional tablet Diovan ® with similarity factor (f2= 68.4±1.07) and difference factor (f1= 1.39± 0.95). Therefore, this study developed a new easily swallowed tablet with an efficient taste masking property, high loading capacity and adequate mechanical strength that can be used as an alternative to buccal, sublingual and orodispersible tablets.

Objective: The aim of this study was to formulate a new developed solid dispersion (SD) containing fixed dose combination of nalidixic acid and cefdinir (500:300 mg) to improve dissolution rate of poorly soluble drugs via a new mechanism as well as the conventional mechanism of SD represented by the presence of hydrophilic carrier.Methods: Through this objective eight newly developed SD formulas of fixed dose combination of nalidixic acid and cefdinir (500:300 mg) and (polyethylene glycol 6000 and poloxamer 188) in different ratio were prepared, in addition to SD of each drug alone and simple mixture of individual SD (SMSD) prepared by means of fusion technique. Moreover, SDs beside pure drugs, simple mixture, and physical mixture (PM) were characterized by dissolution tests, solubility studies, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC), Fourier transform-infrared (FT-IR) spectroscopy and scanning electron microscopy (SEM). Results:From in vitro dissolution tests, PXRD, DSC, FT-IR, and SEM; it is indicated the presence of a physical complex between cefdinir and nalidixic acid in their SD containing combination of fixed dose of both drugs. This will affect the crystallinity of the second drug and their dissolution behavior in addition to the conventional mechanism owing to the presence of hydrophilic carrier (poloxamer 188). Conclusion:It was concluded that the newly prepared formula of SD containing fixed dose combination of nalidixic acid and cefdinir will be promising for higher dissolution profile than that from SD of each drug alone or SMSD of each drug.

Objective: The aim of this study was to formulate enteric coated oroslippery tablets (OSTs) of naproxen to overcome the common problems of stomach irritation and swallowing difficulties which accompanied the administration of naproxen tablets.Methods: Different formulas of enteric slippery tablets were prepared by direct compression method. Various parameters were investigated like the effect of eudragit L-100 (eud.) concentration (as an enteric polymer), coating level and effect of different concentrations of croscarmellose sodium CCS (as super disintegrant) on the physical properties. Finally, in an in vitro disintegration and release study was carried out. Results:The enteric slippery optimal formula (F8) was selected to consist of double coat (17.5% eudragit (eud.)) with core tablet containing (6% CCS). It was found that this optimal formula having an acceptable physical property (friability, hardness, thickness and weight variation). Besides, the best acid resistant potential represented by the protection of the OSTs for 2 h in 0.1 N HCl without any sign of disintegration and drug release. Moreover, it was found that (F8) has a disintegration time equal to (8±1.36 min) and release of 80% (20±0.18 min) in phosphate buffer pH 6.8. Conclusion:The result revealed the successful preparation of naproxen tablets using enteric slippery coating that can be easily swallowed and prevent direct irritation of the stomach with acceptable tablet weight.

Objective: Oral nanoemulsion (NE) represent one of the newest technology to enhance intestinal drug permeability, bioavailability and facilitate swallowing of the oral dosage form.Methods: In this study, montelukast sodium (MS) nanoemulsions (NEs) were formulated by ultra-sonication using different surfactants (tween 20, tween 60 and tween 80) in different surfactant: co-surfactant (ethanol) ratios (Smix). The prepared NEs were evaluated for different parameters including droplet size (DS) using zetasizer as a function of ultra-sonication time, dispersibility, phase separation, conductivity, percent transmittance, optical transparency, in vitro release in addition to morphology using transmission electron microscopic (TEM).Results: The results revealed that F3 was the optimum formula having an average DS 32.95±2.8 nm after 5 min ultra-sonication assured by zetasizer and TEM, furthermore, a clear to bluish NE was formed after aqueous dilution with high conductivity (59.2±1.76 μs/cm) which indicated the formation of O/W NE. In addition, an optically clear NE was formed with (88.6±2.1) % transmittance with no sedimentation, creaming or separation after centrifugation signifying the formation of a stable NE. Finally, F3 showed faster dissolution rate (92.45%±1.66) after 30 min compared to other formulas.Conclusion: The net result of this study is the formulation of a stable oral NE containing MS which presents new easily swallowed dosage form that may enhance drug permeability as well as it may reduce drug metabolism leading to improving bioavailability for asthmatic patients.

The present investigation was undertaken with the objective of developing fast dissolving film(s) of a tricyclic antidepressant drug amitriptyline hydrochloride in order to improve its bioavailability, optimize its therapeutic action especially when used to treat major depression and to enhance the compliance for the developmentally disable, mentally ill, elderly and pediatric patients. , the study based on cross over design using experimental animals (rabbits). The pharmacokinetic results revealed that the fast dissolving films has higher peak blood concentration (C max , 0.927µg/ml) within shorter time (T max, 2 hours), indicating rapid absorption and faster onset of action with acceptable bioavailability value. These findings suggest that the fast dissolving film containing amitriptyline hydrochloride is expected to become one of choices for the treatment of acute depression.

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