In the pharmaceutical industry, cryoprotectants are added to buffer formulations protect active ingredient from freeze- and thaw damage. We investigated freezing thawing of aqueous sodium citrate with various cryoprotectants, specifically amino acids (cysteine, histidine, arginine, proline lysine), disaccharides (trehalose sucrose), polyhydric alcohols (glycerol mannitol) surfactants (polysorba...

Recent studies have shown that drugs that are normally unable to cross the blood-brain barrier (BBB) following intravenous injection can be transported across this barrier by binding to poly(butyl cyanoacrylate) nanoparticles and coating with polysorbate 80. However, the mechanism of this transport so far was not known. In the present paper, the possible involvement of apolipoproteins in the tr...

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A multiple-unit oral floating system was prepared using the emulsification-solvent diffusion method to prolong the gastric emptying time of theophylline. For this purpose, theophylline, ethyl cellulose and dibutyl phthalate were dissolved in an ethanol/dichloromethane mixture, added to 0.1 M HCl containing NaCl (20%) or saturated theophylline and/or different concentrations of polysorbate 80 an...

The structures of micelles of the surfactant polysorbate 80 (Tween 80) in 0-50% aqueous dimethyl sulfoxide (DMSO) solutions (pH 7.2, ionic strength 2.44 mM) were investigated by means of small-angle X-ray scattering. At DMSO concentrations of 0-20%, core-shell cylinder micelles formed, and at 30-50% DMSO, core-shell discus micelles formed, that is, changing the hydrophobicity of the DMSO solven...

G. Ma, B. S. Levine, D. J. Lavrich Merck & Co., Inc. Purpose Amorphous solid dispersions have been increasingly used to enhance the bioavailability for poorly soluble drugs. Dissolution method development for these formulations has faced challenges due to their unstable super saturation state in aqueous media. Whether the dissolution sink condition should be based on API crystalline solubility ...

Its empirical formula is C24H28N2O5•HCl, and its molecular weight is 460.96. Benazeprilat, the active metabolite of benazepril, is a non-sulfhydryl angiotensin-converting enzyme inhibitor. Benazepril is converted to benazeprilat by hepatic cleavage of the ester group. Lotensin is supplied as tablets containing 5 mg, 10 mg, 20 mg, and 40 mg of benazepril hydrochloride for oral administration. Th...

BACKGROUND Polybutylcyanoacrylate (PBCA) nanoparticles coated with polysorbate-80 have been extensively proposed for delivering drugs into the animal brain and have shown great potential for therapeutic applications. In this study, we made an attempt to deliver the chemotherapeutic drug, temozolomide, into the brain by using PBCA nanoparticles. The physicochemical characteristics, in vitro rele...