Zolpimist™: insomnia

ZolpiMist is a US approved, patented, cherry-flavoured, oro-mucosal spray formulation of zolpidem tartrate (marketed under the brand name of Ambien® or Stilnox®), a non-benzodiazepine prescribed for the short-term treatment of insomnia characterised by difficulties with sleep initiation, as per Ambien®’s approved indication.

It provides a convenient and easy-to-use alternative route of administration, by delivering a therapeutic dose with one or two actuations of the spray into the oral cavity. The ZolpiMist device comprises a child-proof two-part packaging system consisting of a base and a cap designed to prevent manual disassembly. The base is designed to hold a multi-dose, Type 1 amber glass bottle, fitted with a non-pressurised metered spray pump assembly delivering 100µL of solution containing 5mg of zolpidem tartrate and mimicking the reference drug Ambien® (or Stilnox®), which is available in 5mg and 10mg tablets.

The pharmaceutical development of ZolpiMist was designed and implemented to ensure pharmacokinetic and therapeutic equivalence to Ambien® in terms of Cmax and the overall systemic drug exposure (AUC) following its administration.

The pivotal studies demonstrated bioequivalence of ZolpiMist 5mg and 10mg doses with the respective Ambien® tablets. The time to detectable levels of both ZolpiMist doses were significantly shorter than the corresponding Ambien® tablets. Also, there was a significantly greater decrease in Digit Symbol Substitution Test (DSST) scores (a measure of attention, perceptual speed, motor speed, visual scanning and memory) for both ZolpiMist doses when compared to Ambien® at 13 minutes post-dose. Hence, ZolpiMist induced sleepiness significantly faster than Ambien®.

Sleep disorders, especially insomnia, are common in elderly people. The pivotal study which involved individuals’ ≥65 years old, demonstrated the therapeutic equivalency of ZolpiMist 5mg with Ambien® 5mg.  Higher plasma concentrations were achieved earlier with ZolpiMist 5mg when compared to the reference drug, which was manifested by significantly earlier detectable level up to 20 minutes.

The safety and tolerability was similar for both drugs and ZolpiMist appears to be a safe agent for both the elderly and non-elderly patients for the treatment of insomnia.

ZolpiMist advantages include reduced sleep latency, patient convenience, and ease of use as it is administered without the need of water, unlike conventional tablets. Additionally, it can be used in patient populations experiencing difficulties in swallowing and/or suffering with gastrointestinal (GI) disorders that restrict the absorption of drugs via the GI mucosa.

If you are interested to learn more about ZolpiMistplease email  This email address is being protected from spambots. You need JavaScript enabled to view it.  (Chief Business Officer)