The present work aimed to formulate azithromycin as amorphous solid dispersion for bitter taste masking, improving stability in an acid medium, and reducing the side effects. Solid dispersion with pH-dependent polymers (Eudragit L100, Eudragit S100) were prepared by the solvent evaporation method. The influence of polymer and drug-polymer ratio on production yields and loading% were evaluated. The F2 (AZI: L100 1:4) that gave the highest yield and loading (96 ± 0.3, 92.3 ± 0.07 respectively) was examined using Scanning electron microscopy (SEM), Fourier transform infrared (FT‑IR), Powder X‑ray diffraction (PXRD) and Differential scanning calorimetry (DSC). Taste masking evaluation was performed in vitro by two methods (in vitro drug release at saliva pH, and comparison of bitter taste threshold with the optimal formulation). (FT‑IR) study displayed that there was no interaction happen between azithromycin and Eudragit L100. DSC and PXRD emphasized the conversion of azithromycin from the crystalline to the amorphous form and entrapped inside the solid dispersion. In vitro, taste assessment detected no azithromycin release in salvia pH (6.8) within 5 min and minimal release in pH 1.2 which indicate this method might be a suitable approach to achieve taste masking of AZI and to improve stability in acid conditions.
The anatomy physiology and biochemistry of the eye render this organ impervious to foreign substances. Ocusert system was firstly developed in 1975 in the USA. It is a flat, flexible, solid and semisolid device which consists of drug reservoir by using various polymers. In the present study Timolol maleate loaded ocular inserts were prepared using different polymers (Methylcellulose, Hydroxypropyl methylcellulose, Eudragit, Ethyl cellulose, Polyvinyl pyrrolidone) by solvent casting method for the treatment of glaucoma. Glycerin, Polyethylene glycol and Dibutyl phthalate were used as plasticizers in different ratios. The prime objective of ocuserts formulating is to enhance therapeutic effect through continuous controlled delivery of ophthalmically active drug to the eye. The physiochemical parameters like thickness, weight, surface pH, folding endurance, % moisture absorption, % moisture loss and drug content were evaluated. In-vitro drug release studies were carried out using a Franz diffusion cell like model. Drug-polymer interactions were investigated by Fourier transform infrared (FTIR) spectroscopy. It was found that the higher the polymer percentage in the formula, the greater the weight and thickness of the film. The mechanical properties of the films reveal that the formulations (F2, F3, F4, F5, F6, F7 and F8) were strong, elastic with smooth surface and appropriate weight for ocular use. In addition to having surface pH that matches the requirements of the ocular dosage forms. It has also been shown that the formulas with hydrophobic polymers have low ability to absorb moisture as well as low moisture content. F4 (Eudragit RL 100 10%) gave sustained drug release with most of the drug being released after 8 hours (95.331%). The release profile of F4 followed the Korsmeyer-Peppas model and correlation coefficient (R2 = 0.992). FTIR studies did not show any evidence of interaction between the drug and the polymers.
Over exposure to sun radiation can cause a lot of skin disorders like erythema, hyperpigmentation, photoaging and cancers. In recent years, there has been an increasing interest in plants which are rich in bioactive compounds. These compounds have a lot of benefit toward cancers, cardiovascular diseases, aging etc. Among these compounds are polyphenols and their derivatives. This study showed several methods of extraction phenolic compounds from different cultivars of olive leaves using water or ethanol 80% (v/v) as solvents in different condition. The content of oleuropein compound was determined using HPLC method. Then using IR to emphasize the structure of the compounds in olive leaves. Ethanolic extract using Soxhlet apparatus was high in oleuropein. Oleuropein amount as a main phenolic compound in olive leaves was 2-7%. Then in vitro SPF number for olive leaves was determined according to the spectrophotometric method described by Mansur et al and the values were 14-29.9 in 1mg/ml.
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