Compositions comprising alprazolam for treating primary insomnia and insomnia associated with anxiety states and process for preparing them

摘要

Disclosed is a composition comprising alprazolam for treating primary insomnia and insomnia associated with anxiety states and the corresponding use and method comprising the administration of alprazolam sublingual tablets having a disintegration time lower than 30 seconds and having the alprazolam preferably in non-crystalline or partially crystalline form according to the X-ray diffraction crystallography expanded for the position delta 9-12.5 (2 theta), to a patient suffering from said disorder. There is also disclosed a method for preparing a composition according to the invention, where the alprazolam is solved in a pharmaceutical acceptable solvent and a binder, preferably polyvinylpyrrolidone, is incorporated to the solution. A pre-made mixture of part of the cross-linked carboxymethyl-cellulose and the rest of the ingredients of the composition is impregnated with the solution and is dried and grinded, and is added to the rest of the cross-linked carboxymethyl-cellulose and the flavoring additives, being then mixed and compressed.

主权项

1. A pharmaceutical composition in the form of sublingual tablets characterised by:
comprising combination of alprazolam and a binder having mucoadhesive properties; wherein the ratio of alprazolam to the binder is in the range between 0.3:1 and 3:1; and, wherein said composition has a disintegration time lower than 30 seconds, in vitro when measured in a standard USP apparatus in medium water without discs according to the United States Pharmacopoeia; and wherein the degree of crystallinity of the alprazolam is less than 10%.