Full
Outline
To prepare lasmiditan tablets and study the in vitro dissolution and pharmacokinetics.
Literature and patents were investigated for designing and optimizing the formulation composition and preparation process. Based on the wet granulation preparation process, taking Reyow® as the reference preparation, the optimal excipient ratios of pregelatinized starch, croscarmellose sodium and magnesium stearate were screened out by Box-Behnken experiment. The particle size and tableting hardness of the API before granulation were determined by single factor experiment. The relevant permeation parameters and pharmacokinetic characteristics of the self-developed tablets and reference preparation in the PAMPA (parallel artificial membrane permeability assay) and the pharmacokinetic characteristics in Beagle dogs were further studied.
The particle size of the API was determined to be 220 μm, and the hardness of the tablet was 80 N. The content of pregelatinized starch was 8.77%, and the content of croscarmelase sodium was 4.58%. The magnesium stearate content was 2.67%. The membrane permeability of the self-developed tablets and the reference preparation were 1.125×10-4 and 1.117×10-4 cm·s-1, respectively, and the permeability rates were 0.846 804 and 0.847 113 μg·min-1·cm-2, respectively. The in vivo experiments showed that the Cmax of the self-made tablets and Reyow® were 189 and 188 ng·L-1, the Tmax was 3 h. The oral relative bioavailability of homemade tablets was 93.32%.
The PAMPA permeation and release behavior in Beagle dogs were basically the same between the self-developed tablets and the reference tablets. The self-developed preparation is preliminary bioequivalent to the original product. The process is suitable for the preparation of lasmiditan tablets.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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