Agomelatine suspension nasal spray and application thereof
A technology of agomelatine and nasal spray, which is applied in the field of pharmaceutical preparations, can solve problems such as liver toxicity and elevated transaminases, and achieve the effects of promoting transmembrane absorption, solving liver toxicity and side effects, and overcoming poor water solubility
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0039] Embodiment 1 investigates the impact of different surfactants on the nasal spray bioavailability of the present invention
[0040] Preparation:
[0041] 1. Agomelatine is finely pulverized until D90 is 10 μm
[0042] 2. Drug suspension: stir and dissolve the prescribed amount of surfactant with an appropriate amount of water, then add agomelatine and stir to disperse to obtain a drug suspension.
[0043] 3. Suspension base: Add appropriate amount of water to microcrystalline cellulose and sodium carboxymethyl cellulose to obtain a suspension base.
[0044] 4. Isotonic solution: Dissolve anhydrous glucose with an appropriate amount of purified water to obtain a glucose solution.
[0045] 5. Mix the drug suspension, suspending matrix, glucose solution and preservative solution, add purified water to the weight. Adjust the pH, and disperse with a high-shear dispersing emulsifier at 10,000 rpm and shear for 30 minutes. The obtained nasal spray suspension is filled into ...
Embodiment 2
[0054] Embodiment 2 investigates the impact of different micropowder particle sizes on the nasal spray bioavailability of the present invention
[0055] According to the research results of Example 1, with the following prescription, the suspension nasal spray of different particle diameters is prepared with reference to the method of Example 1, (1000 bottles).
[0056] table 3
[0057]
[0058] Pharmacokinetic test in rats:
[0059] Select 18 adult rats, 12 males and 6 females (non-perifeeding period), and divide them into three groups, 6 in each group (the ratio of male to female is 2:1), and administer them at a dose of 20 mg / kg. Determination of the main pharmacokinetic parameters of each test animal: half-life, peak time, maximum plasma concentration and AUC 0～t , and the measurement results are shown in Table 4 below.
[0060] Table 4
[0061]
[0062]
[0063] As shown in Table 4 above, as the particle size of agomelatine micropowder decreases, the bioavail...
Embodiment 3
[0064] Embodiment 3 investigates the impact of different pH on the bioavailability of nasal spray of the present invention
[0065] The research on the pH solubility of agomelatine raw material was studied. Under the condition of 37 ℃, the saturation concentration of the raw material drug in different pH solutions was determined by the shake flask dissolution method for 24 hours. The pH-solubility curve is shown in figure 1 , the results showed that agomelatine had little pH dependence.
[0066] According to the research result of embodiment 1 and implementation 2, with following prescription, the suspension nasal spray of different pH is prepared with reference to the method for embodiment 1, (1000 bottles).
[0067] table 5
[0068]
[0069] Pharmacokinetic test in rats:
[0070] Select 18 adult rats, 12 males and 6 females (non-peri-feeding period), divide them into three groups, 6 rats in each group (the ratio of male to female is 2:1), and administer them at a dose o...
PUM
| Property | Measurement | Unit |
|---|---|---|
| surface area | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
Login to View More