Leech colon targeted oral preparation and preparation method thereof

A technology for colon-targeted and oral preparations, applied in pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of high cost, high equipment requirements, low operability, etc., and achieve excellent release, Excellent bioavailability

Active Publication Date: 2012-11-07
CHONGQING DUOPUTAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A patent similar to the present invention is CN01176785A, which discloses a special oral preparation of recombinant bifunctional hirudin and its preparation method, and also mentions the colon targeting preparation of hirudin, but the preparation method requires high equipment and is expensive. Low operability in industrial mass production

Method used

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  • Leech colon targeted oral preparation and preparation method thereof
  • Leech colon targeted oral preparation and preparation method thereof
  • Leech colon targeted oral preparation and preparation method thereof

Examples

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preparation example Construction

[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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Abstract

The invention relates to the field of preparation, in particular to a leech colon targeted oral preparation prepared by taking leech extract, natural hirudin and recombinant hirudin as active ingredients and a preparation method thereof. The invention aims at solving the technical problems that a leech colon targeted oral preparation which is released and absorbed and gives curative effect to be played at a colon part is provided and bioavailability of oral administration is improved. The preparation method comprises the following steps of: preparing the active ingredients into a coating front midbody, then applying a colon targeted coating system onto the coating front midbody, wherein the coating system comprises an inner coating layer and an outer coating layer; the inner coating layeris mixture of 1 part of guar gum, 1-3 parts of sodium alginate and 1-3 parts of inulin, the mixture is dissolved with water and is prepared into coating solution with the concentration of 2-5%, and weight of the coating is increased by 3-9%; and the outer coating layer is mixture of a film forming agent and a porogenic agent, the outer coating layer is in a weight proportion relation that 6-8 parts of the film forming agent and 2-4 parts of the porogenic agent are adopted, and the weight of the coating is increased by 3-15%. The oral preparation provided by the invention can be released and absorbed at the colon part, and the bioavailability can be improved.

Description

technical field [0001] The invention relates to the field of preparations, in particular to a leech colon-targeted oral preparation made from leech extract, natural hirudin and recombinant hirudin as active ingredients and a preparation method thereof. Background technique [0002] Leech is a traditional Chinese medicine, which is recorded in "Shen Nong's Materia Medica", and has been recorded in successive dynasties of herbal medicines. Traditional Chinese medicine believes that it has the functions of breaking blood, removing blood stasis and dredging menstruation. It has always been used to treat lumps in the abdomen, lumps, blood stasis, amenorrhea, and bruises. The Chinese Pharmacopoeia 2000 edition records that this product is the dried whole body of the leech WhitmaniapigraWhitman, the leech Hirudoniponicawhitman or the willow leaf leech WhitmaniaacranulataWhitman. Hirudin is an acidic polypeptide secreted by the salivary glands of leeches. It is a single-chain polyp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K35/62A61K38/58A61K9/36A61K9/16A61K9/20A61K47/36A61K47/38A61P7/02
Inventor 甘奇志曾新张海燕
Owner CHONGQING DUOPUTAI PHARMA
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