Biomaterial Database

[The solubility of drugs in molten suppository bases]. 1990

P Pflegel, and H Schöbel, and T Klaus, and U Raguse

Sektion Pharmazie, Ernst-Moritz-Arndt-Universität Greifswald.

Solubility of 18 drugs used in rectal therapy in molten suppository base, (Massa suppositoriorum 15, Pharmacopeia of the G.D.R. Rosupol U, 37 degrees C) is determined. Separation of drug-saturated base from drug cristals is carried out in an air-heated centrifuge followed by a partition step between petroleum ether and an aqueous medium and photometrical determination of drug concentration. The procedure leads to results with relative standard deviation of 2% (medium value of 18 drugs). The investigation gave solubility values in the range between 0.002% (theobromine) and 26% (lidocaine), whereas benzoate, phenobarbital sodium and procaine hydrochloride are completely insoluble. Sodium salicylate has an unexpected high solubility (0.48%). The solubility is temperature depended and thus the solubility enthalpy can be determined. Relations between structure and solubility are discussed for pyrazolin-5-ones and purines. A correlation between solubilities in the base and in aqueous buffer (phosphate, pH 7.4) does not exist in the series studied.

UI	MeSH Term	Description	Entries
D010783	Photometry	Measurement of the various properties of light.	Photometries
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
D004364	Pharmaceutical Preparations	Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form.	Drug,Drugs,Pharmaceutical,Pharmaceutical Preparation,Pharmaceutical Product,Pharmaceutic Preparations,Pharmaceutical Products,Pharmaceuticals,Preparations, Pharmaceutical,Preparation, Pharmaceutical,Preparations, Pharmaceutic,Product, Pharmaceutical,Products, Pharmaceutical
D005079	Excipients	Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc.	Excipient,Stabilizing Agent,Stabilizing Agents,Suspending Agent,Suspending Agents,Agent, Stabilizing,Agent, Suspending,Agents, Stabilizing,Agents, Suspending
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
D013488	Suppositories	Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature.	Rectal Suppositories,Vaginal Suppositories,Vaginal Suppository,Suppositories, Rectal,Suppositories, Vaginal,Suppository, Vaginal
D013696	Temperature	The property of objects that determines the direction of heat flow when they are placed in direct thermal contact. The temperature is the energy of microscopic motions (vibrational and translational) of the particles of atoms.	Temperatures
D013816	Thermodynamics	A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)	Thermodynamic