Leech colon targeted oral preparation and preparation method thereof
A technology for colon-targeted and oral preparations, which is applied in the direction of pill delivery, pharmaceutical formulations, and medical preparations of non-active ingredients. It can solve the problems of high cost, high equipment requirements, and low operability, achieving excellent release, Excellent bioavailability
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[0044] The preparation method of the leech colon targeting micropill of the present invention is: starch or dextrin (preferred starch powder and dextrin are mixed in a mass ratio of 2:3) is made into a blank micropill core; the active ingredient is dissolved and sprayed on the blank micropill On the center of the pill; prepare the inner coating layer solution, coat until the weight gain is 5-7%; mix the film-forming agent and porogen in an appropriate proportion, add ethanol to dissolve (you can also add a plasticizer to mix), and adjust the content percentage According to the weight gain ratio of the coating, the coating is done until the weight gain is 8-12%.
[0045] The preparation method of leech colon targeting tablet of the present invention is: A, get active component and filler, tabletting is made into tablet core (can adopt ethanol to press with wet granulation); B, preparation inner coating layer solution, coating To increase the weight by 4-6%; C, take film-forming...
Embodiment 1
[0070] prescription:
[0071]
[0072] Preparation:
[0073] 1. After mixing the recombinant hirudin and starch evenly, add ethanol as a wetting agent, make a soft material, granulate, dry at 50-60°C, mix evenly with magnesium stearate, granulate, and compress into tablets.
[0074] 2. Put the plain tablets obtained in step 1 into the coating pan with an inclination angle of 45°, adjust the rotation speed to 65-75r / m, blow in hot air with a temperature of 30-40°C, preheat, and adjust the atomization pressure to 1.2-1.8 kg / cm 2 , spray the coating solution of the mixture of guar gum, sodium alginate and inulin at a flow rate of 10-15 mL / min·kg, and coat until the weight gain is 5%.
[0075] 3. Mix cellulose acetate, PVP (K30) and Eudragit S in proportion, dissolve in ethanol, make it fully swell, let it stand overnight, add plasticizer after it is completely dissolved, mix well, and set aside. Coat the inner-coated tablet with the method in step 2, increase the weight to ...
Embodiment 2
[0077] prescription:
[0078]
[0079] Preparation:
[0080] 1. Mix natural hirudin and dextrin evenly, add ethanol as a wetting agent, make soft material, granulate, dry at 50-60°C, mix evenly with magnesium stearate, granulate, and tablet
[0081] 2. Put the plain tablets obtained in step 1 into the coating pan with an inclination angle of 45°, adjust the rotation speed to 65-75r / m, blow in hot air with a temperature of 30-40°C, preheat, and adjust the atomization pressure to 1.2-1.8 kg / cm 2 , spray the mixed coating solution of guar gum, inulin and sodium alginate at a flow rate of 10-15 mL / min·kg, and coat until the weight gain is 5%.
[0082] 3. Dissolve ethyl cellulose, cellulose acetate, Eudragit S, and Eudragit L in ethanol to make them fully swell, and place them overnight. After they are completely dissolved, add plasticizer TEC, mix well, and set aside. Coat the inner coated tablet with the method in step 2 to a weight gain of 7%, and dry at 40°C to obtain
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