Soluble osthole clathrate, dispersing tablet and preparation method thereof
A technology of osthole and inclusion complex, which is applied in the directions of active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, drug combinations, etc., can solve the problems of low solubility of osthole, and achieve short disintegration time and film The effect of increased permeability and rapid dissolution
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Embodiment 1
[0037] One, the preparation of osthole inclusion compound:
[0038] Weigh 0.244 g of osthole, dissolve it in 20 mL of absolute ethanol, heat to 50°C, and stir to completely dissolve to obtain solution A;
[0039] Weigh 1.135 g of β-CD, place in 30 mL of distilled water, heat and stir until completely dissolved to obtain solution B;
[0040] Divide solution B into two parts on average, and add them to solution A in turn, with an interval of 15 minutes between the two additions; 6 hours later, the above mixed solution is rotary evaporated to remove ethanol, and concentrated to about 30 mL;
[0041] Refrigerate at a temperature of 4°C for 12 hours to obtain a white suspension, which was suction-filtered, and the precipitate was quickly washed with 50 mL of ethanol and appropriate amount of distilled water in turn, and vacuum-dried at 40°C to obtain a crude clathrate product, which was pulverized and passed through 80 Mesh sieve to obtain osthole inclusion compound.
[0042] Two...
Embodiment 2
[0061] The osthole β-cyclodextrin inclusion compound was prepared according to the technical scheme of Example 1.
[0062] Prepare the osthole inclusion compound dispersible tablet with the following components and ratios by weight:
[0063] Osthole β-cyclodextrin inclusion complex 72.5%
[0064] Thinner Microcrystalline Cellulose MCC 5%
[0065] Disintegrant cross-linked polyvinylpyrrolidone PVPP 16%
[0066] Disintegrant Low-substituted hydroxypropyl cellulose LPC 4%
[0067] Suspension micronized silica gel 1.5%
[0069] According to the preparation method of the osthole inclusion compound dispersible tablet of Example 1, after the disintegrating agent, diluent, suspending agent, corrective agent and the osthole inclusion compound are mixed uniformly by an equal amount incremental method, then add The glidant and lubricant are mixed evenly and tabletted to obtain osthole inclusion compound dispersible tablets.
Embodiment 3
[0071] The osthole β-cyclodextrin inclusion compound was prepared according to the technical scheme of Example 1.
[0072] Prepare the osthole inclusion compound dispersible tablet with the following components and ratios by weight:
[0073] Osthole β-cyclodextrin inclusion complex 60%
[0074] Thinner Microcrystalline Cellulose MCC 15%
[0075] Disintegrant cross-linked polyvinylpyrrolidone PVPP 16%
[0076] Disintegrant Low-substituted hydroxypropyl cellulose LPC 6%
[0077] Suspension micronized silica gel 2%
[0078] Lubricant Magnesium Stearate 1%
[0079] According to the preparation method of the osthole inclusion compound dispersible tablet of Example 1, after the disintegrating agent, diluent, suspending agent, corrective agent and the osthole inclusion compound are mixed uniformly by an equal amount incremental method, then add The glidant and lubricant are mixed evenly and tabletted to obtain osthole inclusion compound dispersible tablets.
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