Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.

Buccal, polar and non-polar spray or capsule

This invention relates to a solvent system for enhancing the solubility of an acidic, basic, or amphoteric pharmaceutical agent to produce a highly concentrated solution suitable for softgel filling or two piece encapsulation. The solvent system comprises polyethylene glycol containing 0.2-1.0 mole equivalents of an ionizing agent per mole equivalent pharmaceutical agent and 1-20% water. Glycerin or polyvinylpyrrolidone may be added to further enhance the solubility of certain drugs. The disclosed solvent system is capable of enhancing solubilities of pharmaceutical agents 40-400%. The ionizing agent functions by causing partial ionization (neutralization) of the free pharmaceutical agent. When the pharmaceutical agent is acidic, the ionizing agent is preferably a hydroxide ion species, whereas when the pharmaceutical agent is basic, the ionizing agent is preferably a hydrogen ion species. For amphoteric pharmaceutical agents, either hydroxide ion or hydrogen ion sources may be utilized to effect partial ionization. The disclosed solvent system is useful because it not only provides for the enhancement or improvement of bioavailability of acidic, basic and amphoteric pharmaceutical agents by delivering them already in solution, but it also provides for a highly concentrated solution capable of encapsulation in a small enough vessel to permit easy swallowing. The highly concentrated solid solutions of the present invention are also useful for conversion into tablets and as veterinary spot and pour on preparations.

Solvent system enhancing the solubility of pharmaceuticals for encapsulation

not available for EP1539106Abstract of corresponding document: WO2004035021Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compounds, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Buccal polar and non-polar spray or capsule containing drugs for treating disorders of the central nervous system

Disclosed is a propellant free buccal spray composition for transmucosal administration of a pharmacologically active compound comprising: an active compound in an amount of between 0.001 and 60 percent by weight of the total composition selected from the group consisting of anti-opioid agents, anti-migraine agents, pain control agents, anaesthetics, and mixtures thereof; and a polar solvent in an amount between 30 and 99 percent by weight of the total composition; wherein the anti-opioid agent is selected from the group consisting of nalmefene, cholecystokinin, nociceptin, neuropeptide FF, oxytocin, vasopressin, and mixtures thereof; the anti-migraine agent is selected from the group consisting of frovatriptan, zolmitriptan, rizatriptan, almotriptan, eletriptan, naratriptan, ergotamine, diethylergotamine, and mixtures thereof; and the pain control agent is selected from the group consisting of alfentanil, butorphanol, codeine, dezocine, fentanyl, hydrocodone, hydromorphone, levorphanol, meperidine, methadone, morphine, nalbuphine, oxycodone, oxymorphone, propoxyphene, pentazocine, sufentanil, tramadol, and mixtures thereof. Also disclosed are buccal aerosol sprays using polar and non-polar solvent which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The disclosed buccal polar compositions comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Buccal, polar and non-polar spray or capsule containing drugs for treating pain

Buccal, polar and non-polar spray or capsule containing drugs for treating metabolic disorders

The present invention relates to a coronary therapeutic agent in the form of soft gelatin capsules, which contain the active substance nifedipine in an organic solvent. In the prior art, there where problems regarding the capsule size and with respect to the low nifedipine active substance concentration. These problems are obviated by the invention, in that nifedipine with PVP, optionally as a coprecipitate and without glycerin, is dissolved in THFP and consequently permits a capsule weight of in all only e.g. 162 mg.

Coronary therapeutic agent in the form of soft gelatin capsules

1. Coronary therapeutic in the form of soft gelatine capsules consisting of a capsule casing which contains glycerol, one or several colourants with an absorption region which includes the spectral region which gives rise to the decomposition of the filler, as well as an opacifying agent, and a capsule filling which contains the active substance Nifedipin (1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-pyridine-3,5- dicarboxylic acid dimethyl ester) as well as polyvinylpyrrolidone (PVP), an organic solvent for Nifedipin and optionally further additives, characterised in that the capsule filling contains at least 4% by weight of Nifedipin as well as polyvinylpyrrolidone (PVP), both dissolved in a mixture of polyether alcohols of tetrahydrofurfuryl alcohols (THFP), glycerol being present exclusively as constituent in the capsule casing.

Hans Joss

Papers

Coronary therapeutic agent in the form of soft gelatin capsules

Therapeutic coronary composition in the form of soft gelatine capsules