Controlled release formulation for treating sleep disorders

Example 1

Controlled-Release Tablet Comprising Sustained Release Zolpidem as a Core Coating with Immediate Release Zaleplon

[0050]The materials PVP-K30, Zolpidem tartrate, lactose monohydrate, HPMC K100 LV, A vicel PH101 and tartaric acid in the below table were mixed together, granulated with water, dried and calibrated. The granules were then mixed with magnesium stearate and compressed to a tablet to obtain sustained release Zolpidem.

PVP-K 301.47%(w / w)Zolpidem tartrate2.88%(w / w)Zaleplon2.30%(w / w)Lactose monohydrate49.29%(w / w)HPMC K100 LV15.67%(w / w)Avicel PH10114.75%(w / w)Tartaric acid7.37%(w / w)Mg Stearate0.74%(w / w)Eudragit E1005.12%(w / w)Titanium Dioxide0.39%(w / w)Iron oxide Red0.02%(w / w)Total100(w / w)

[0051]The sustained release Zolpidem is coated with the immediate release Zaleplon (containing Zaleplon, Eudragit E100, titanium dioxide and iron oxide Red) to obtain the title controlled-release tablet.

[0052]The in vitro dissolution profiles of the tablets were established using the Appa...

Controlled-Release Double Layer Tablet Comprising Sustained Release Zolpidem and Immediate Release Zaleplon

[0053]The formulation of the controlled-release tablet in a double-layer form is listed in the below table. Sustained release entity of the tablet comprising 6.25 mg of Zolpidem was produced as follows. The materials PVP-K 30, Zolpidem tartrate, lactose monohydrate, HPMC K100 LV, Avicel PH101 and tartaric acid were mixed together, granulated with water, dried and calibrated. The resulting granules were mixed with magnesium stearate and then pre-compressed to a sustained release Zolpidem.

PVP-K 301.61%(w / w)Zolpidem tartrate2.88%(w / w)Zaleplon2.30%(w / w)Lactose monohydrate68.07%(w / w)HPMC K100 LV8.30%(w / w)Avicel PH1016.45%(w / w)Tartaric acid4.61%(w / w)Croscarmellose sodium1.38%(w / w)Sodium lauryl sulfate0.21%(w / w)Mg Stearate0.97%(w / w)Eudragit E1002.81%(w / w)Titanium Dioxide0.39%(w / w)Iron oxide Red0.02%(w / w)Total100(w / w)

Immediate release entity of the tablet was produced by mixing Zaleplo...

Controlled-Release Capsule Comprising Pellets Comprising Sustained Release Zolpidem as a Core Coating with Immediate Release Zaleplon

[0055]Zolpidem, tartaric acid and PVP K30 were dissolved in 95% alcohol and then meshed with #100 mesh. CF granulator was used to coat the above mentioned mixture to sugar sphere #25-30 to get pellet 1. Pellet 1 was cured at 40° C. for 8 hours to reduce water content to less than 1%.

[0056]Ethycellulose N10F, PVP K30 and Triethylcitrate were dissolved in 95% alcohol and then meshed with #100 mesh. CF granulator was used to coat the mixture onto the above-mentioned pellet 1 to get pellet 2. Pellet 2 was cured at 40° C. for 8 hours to reduce water content to less than 1%.

[0057]Zaleplon and Eudragit E100 were dissolved in 95% alcohol and dichromethane and then meshed with #100 mesh. CF granulator was used to coat the above mentioned mixture onto pellet 2 to get pellet 3. Pellet 3 was cured at 40° C. for 8 hours to reduce water content to less than 1% and t...