Extended release formulations of rasagiline and uses thereof
A technology of delayed release and active agent, which can be used in medical preparations containing active ingredients, cardiovascular system diseases, organic active ingredients, etc., and can solve problems such as low efficacy
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Embodiment 9
[0067] Example 9 describes the preparation of a third type of rasagiline mesylate ER coated pellet comprising a drug layer coating an inert pellet, a subcoat layer and a higher percentage (27%) of ER coating For the outer functional layer of the coating, the pellets were dry blended with silica instead of the Aerosil 200 used in Examples 7-8. The dissolution profiles of these pellets were evaluated using IFS (pH 6.8) in USP Apparatus 1 at 100 rpm and a temperature of 37°C, and as shown, the release profile in this case was slower than for the pellets of Examples 7-8 The observed release pattern is due to the difference in functional layer thickness.
[0068] Additional rasagiline mesylate ER pellets with or without subcoating designed for different release profiles of the drug are described in Example 10.
[0069] When designing a 24 hour delayed release product for oral administration, it is desired that the drug be absorbed throughout the entire release time, ie from all pa...
Embodiment 1
[0128] Example 1. In vivo study of rasagiline-pramipexole combination in MPTP mouse model of PD
[0129] The study consisted of 10 groups of approximately 7-9 mice each, which were treated according to Table 1. Specifically, mice were administered IPTP intraperitoneally (IP) to induce a Parkinson's disease (PD) model, and treated with a constant dose of pramipexole, a non-ergoline dopamine agonist indicated for the treatment of early PD, and varying doses of pramipexole. Sagiline is a drug combination for treatment. During the initial 5 days (days 0-4), MPTP was injected daily and on days 0-11 IP or using an ALZET pump (ALZET micro-osmotic pump, model 1002, at a rate of 0.25 μl / hr, DUREECT Corporation, Cupertino , USA) administered the drug combination to simulate sustained release. Every day during the initial five days (Day 0-4), Groups 5-7 were administered the drug combination 30 min prior to MPTP application, and on subsequent Days 5-11, on each dosing day, at approxima...
Embodiment 2
[0136] Example 2. In vivo study of rasagiline metabolite aminoindan in the MPTP mouse model of PD
[0137] Female C57B1 / 6 mice weighing 20 + / - 1 g were used for all experiments (10 mice per group). MPTP was administered by IP injection at a dose of 40 mg / Kg per day for 5 days. Controls were naive untreated mice injected with saline, and MPTP-administered mice injected with saline. Aminoindan was applied for 12 days by daily IP injection or by sustained release of IP implanted using the ALZET pump. The effect of the treatment was assessed by measuring dopamine and its metabolites (dihydroxyphenylacetic acid and homovanillic acid) in the left and right striatum taken from the mice at the end of the experiment. Striatal tissue samples were prepared for HPLC as described in the experiments.
[0138] like figure 2 As shown, MPTP treatment resulted in a greater than 90% reduction in dopamine levels relative to control, ie naive mice. Treatment with the rasagiline metabolite am...
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