Release of drugs from ointment bases II: In vitro release of benzocaine from suspension-type aqueous gels. 1977

F Bottari, and G Di Colo, and E Nannipieri, and M F Saettone, and M F Serafini

The in vitro release of benzocaine, suspended in an aqueous gel, through silicone rubber membranes was studied to test an extension of existing mathematical models. The theoretical treatment proposed is intended for experimental systems involving release, through a non-porous membrane, of a drug whose concentration is a few times (larger than or equal to 3) greater than its solubility in the vehicle. For either micronized (2micrometer) or macrosize (125 micrometer) drug, the Q (amount released) versus t1/2 (time1/2) plots were not linear until substantial time had elapsed. Excellent agreement was found between the experimental points and theoretical plots, generated by a computer fit to experimental data of an equation derived from a reported vehicle-boundary diffusion layer model. The values of the solubility and of the diffusion layer model. The values of the solubility and of the diffusion coefficient of benzocaine in the gel, calculated by the present mathematical treatment from release data, were in agreement with literature data. The particle size of released benzocaine did not influence the release pattern, thus confirming release in the present conditions to be diffusion rather than dissolution controlled. The present method is applicable for determining the solubility and diffusion coefficient of drugs in vehicles in cases not contemplated in current release theories.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008956 Models, Chemical Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment. Chemical Models,Chemical Model,Model, Chemical
D009823 Ointment Bases Various mixtures of fats, waxes, animal and plant oils and solid and liquid hydrocarbons; vehicles for medicinal substances intended for external application; there are four classes: hydrocarbon base, absorption base, water-removable base and water-soluble base; several are also emollients. Bases, Ointment
D010316 Particle Size Relating to the size of solids. Particle Sizes,Size, Particle,Sizes, Particle
D002626 Chemistry, Pharmaceutical Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use. Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D004058 Diffusion The tendency of a gas or solute to pass from a point of higher pressure or concentration to a point of lower pressure or concentration and to distribute itself throughout the available space. Diffusion, especially FACILITATED DIFFUSION, is a major mechanism of BIOLOGICAL TRANSPORT. Diffusions
D005782 Gels Colloids with a solid continuous phase and liquid as the dispersed phase; gels may be unstable when, due to temperature or other cause, the solid phase liquefies; the resulting colloid is called a sol.
D001566 Benzocaine A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS. Ethyl Aminobenzoate,4-Aminobenzoic Acid Ethyl Ester,Americaine,Anaesthesin,Anesthesin,Bensokain,Benzocaine Acetate,Benzocaine Formate,Benzocaine Hydrobromide,Benzocaine Hydrochloride,Benzocaine Methanesulfonate,Ethoform,Acetate, Benzocaine,Formate, Benzocaine,Hydrobromide, Benzocaine,Hydrochloride, Benzocaine,Methanesulfonate, Benzocaine
D012826 Silicone Elastomers Polymers of silicone that are formed by crosslinking and treatment with amorphous silica to increase strength. They have properties similar to vulcanized natural rubber, in that they stretch under tension, retract rapidly, and fully recover to their original dimensions upon release. They are used in the encapsulation of surgical membranes and implants. Elastomers, Silicone,Rubber Silicone,Silicone Rubber,Elastosil,Microfil,SE-30,Elastosils,Microfils,SE 30,SE30,Silicone Elastomer
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities

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