Objective: Ultraviolet Visible spectrophotometric was adopted to identify and quantify any adulteration with PDE-5 inhibitors (Sildenafil and Tadalafil) in selected dietary supplements used for sexual enhancement in the Lebanese market
Methods: Nine dietary supplements, randomly collected from Lebanese pharmacies, were screened for Sildenafil and Tadalafil using UV-spectrophotometry for both qualitative and quantitative detection.
Results: Tadalafil was detected in one sample at a dose of 59 mg/dosage unit, with the maximal recommended dose being 20 mg. Sildenafil was detected in five samples at doses ranging from 11.7 to 188.2 mg/dosage unit, with the maximal recommended dose being 100 mg.
Conclusion: This study demonstrates that regular analysis of supposed dietary supplements is needed for more effective quality control and health promotion. The method described for the extraction, identification and quantification of Tadalafil and Sildenafil would be useful for regulatory detection of adulterations.
Purpose: To design and prepare effervescent floating gastroretentive tablets for controlled fexofenadine hydrochloride (HCl) release and enhanced oral bioavailability. Method: Various tablet formulations of the drug were prepared by direct compression. A systematic approach in the design of the formulations was adopted, where, first, formulations consisting of single polymers with a high polymer : sodium bicarbonate ratio were investigated for its physicochemical properties (in-vitro floating behaviour, drug release profile, etc). Next, improvement of tablets' properties was achieved by decreasing polymer : sodium bicarbonate ratio. Subsequently, a final optimization step involved blending polymers at different polymer : polymer ratios. The formulations were evaluated in vitro and in vivo in albino rabbits Results: The formulation consisting of hydroxypropyl methylcellulose K15M/hydroxypropyl methylcellulose K100LV at 1 : 2 ratio (F8) showed good floating properties (14 s floating lag time) with nearly zero order controlled drug release for 24 h (R 2 = 0.9876). In-vivo bioavailability studies of F8 in albino rabbits showed a significant increase in area under the curve (AUC, 134 %, p < 0.05) and hence an improvement in its oral bioavailability, compared to a commercial conventional product. Conclusion: The good quality of the effervescent floating gastroretentive tablets of fexofenadine HCl developed is an indication that the approach used is suitable for the formulation of the drug for controlled drug release and enhanced oral bioavailabiliy. This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest
Purpose: Diabetic somatic neuropathy is one of the most prevalent complications in type 1 diabetes mellitus. Many treatments were investigated to alleviate the pain associated with this condition. Capsaicin is a naturally occurring lipophilic alkaloid that proved to be an effective and safe treatment of chronic painful disorders. Despite the known therapeutic benefits of capsaicin, the conventional topical formulations have limited bioavailability. Therefore, the current study aims to develop capsaicin nanoemulgel to increase skin permeation and enhance its activity against neuropathic pain. Methods: Low-energy emulsification method was used to prepare nanoemulsions, using eucalyptus oil as the oily phase, tween 80 as a surfactant, propylene glycol, ethanol and isopropyl alcohol as co-surfactants. Pseudo-ternary phase diagrams were constructed to investigate and optimize the formulation. Subsequently, the optimum formulation was formulated as a nanoemulgel and investigated for, skin permeation using Franz diffusion cell, and diabetic neuropathy management using alloxan-induced diabetic mice. Results: The selected nanoemulsion containing 0.05% capsaicin is composed of 8 % oil, 24 % Smix (Tween 80: isopropyl alcohol 2:1 w/w) and 68 % water. It is characterized by nanosized globules (28.15±0.24 nm) with a relatively low polydispersity index (0.27±0.05). The nanoemulgel revealed circa 4-fold increase in capsaicin cumulative permeation when compared to the conventional gel, and an improvement in its antinociceptive properties was observed in the treated diabetic mice (p<0.05). Conclusion: The selected capsaicin nanoemulgel would be a promising transdermal formulation that may alleviate diabetic neuropathy in type 1 diabetes mellitus patients.
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