Palatable ibuprofen aqueous base solutions are described which contain dissolved therein ibuprofen and hydroxypropyl beta cyclodextrin, which form an inclusion complex, and sweeteners to mask the sour taste common to organic acids.
A pharmaceutical composition for oral consumption in liquid form is provided, characterized in that the composition contains a drug, preferably a lipophilic NSAID, complexed to .beta.-cyclodextrin in a formulation also containing an acid-base couple, preferably an effervescent acid-base couple. The weight of the acid-base couple is greater than 1% of the weight of water in which the composition is to be dissolved, and provides an acid or neutral pH.
The dissolution of lipophilic compounds in aqueous solutions of hydroxypropylcyclodextrins can be accelerated by the addition of co-solubilizers, such as ethanol or ammonia, which again can be removed, together with water, by evaporation or by freeze-drying leaving lipophile: hydroxypropylcyclodextrin complexes as a residue. The co-solubilizer method was used successfully with steroid drugs (5-androstene-3.beta.,17.beta.-diol, 4-androstene-3,17-dione, dehydroepiandrosterone, dexamethasone, 5-.alpha.-dihydro-testosterone, 6-methylprednisolone, and testosterone), peptides (gramicidin S) and a macrocyclic antibiotic (amphotericin B). The complexes prepared in this manner were amorphous and possessed satisfactory stability.
A composition comprising an isothiazolone compound mixed with a branched cyclodextrine, wherein the isothiazolone compound can be stabilized to water, so that it is possible to provide an aqueous solution comprising an isothiazolone compound which is excellent in storage stability and aqueous solution stability.
Cyclodextrin derivatives and inclusion complexes having increased solubility and stability are provided. Cyclodextrin derivatives include amino and other modified cyclodextrins, and linked cyclodextrins. Inclusion complexes comprising the foregoing cyclodextrins, and processes for making the cyclodextrin derivatives are disclosed. Also disclosed are cyclodextrin derivatives comprising otherwise substituted or unsubstituted cyclodextrins covalently bonded to agents such as pharmaceuticals. The covalent bond, when broken, yields the agent in active form. Pharmaceutical compositions and methods of treating an animal host are also described, as well as chromatographic compositions and a method for separating racemic mixtures.
