Melatonin tablet and methods of preparation and use
The present invention provides a pharmaceutical composition for sublingual or buccal administration of actives with low to poor aqueous solubility, e.g. the indole hormone melatonin, which contains a solution of the active in a pharmaceutically acceptable solvent adsorbed or absorbed onto particles of a pharmaceutically acceptable carrier and methods of preparing and using the pharmaceutical composition.
1. A tablet for sublingual or buccal administration of melatonin, said tablet comprising:
melatonin in a dissolved state;
a solvent which is polyethylene glycol (PEG) 200, 300, 400, and or 600; and
a pharmaceutically acceptable carrier to which the dissolved melatonin is adsorbed and which becomes a flowable powder, the carrier being silica or calcium silicate;
where in melatonin is in a dissolved state in the tablet, and
wherein the drug dissolution from the tablet is substantially complete within 15 minutes.
2. The tablet of claim 1 , in which the concentration of melatonin solubilized in the solvent is in the range of about 5% w/w to about 30% w/w.
3. The tablet of claim 1 , wherein the weight:weight ratio of carrier to melatonin solution is in the range of about 1:0.5 to about 1:4.
4. The tablet of claim 1 , further comprising a diluent, a disintegrant, and/or a lubricant.
5. A process for the preparation of the tablet of claim 1 , comprising the steps of:
dissolving melatonin in the PEG to form a drug solution; and
mixing the drug solution with the pharmaceutically acceptable carrier silica or calcium silicate to adsorb said solution to the carrier particles forming a flowable powder; and
compressing the solution-adsorbed carrier particles into a tablet.
6. The process of claim 5 , further comprising adding additional excipients to the solvated melatonin/adsorbent before compressing the solvated, adsorbed melatonin/adsorbent particles into the form of a tablet.