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Colchicine sublingual tablet, preparation method and application thereof

A technology of colchicine and sublingual tablet, applied in the field of colchicine, can solve the problem that the sublingual tablet does not have universal applicability and the like, and achieve the effects of avoiding liver first-pass effect, fast onset of action and reducing toxicity

Inactive Publication Date: 2016-03-23
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Currently, there is no report on sublingual tablets of colchicine. In view of the fact that the current sublingual tablets do not have universal applicability, how to successfully prepare an effective sublingual tablet of colchicine is the focus of research.

Method used

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  • Colchicine sublingual tablet, preparation method and application thereof
  • Colchicine sublingual tablet, preparation method and application thereof
  • Colchicine sublingual tablet, preparation method and application thereof

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preparation example Construction

[0048] The present invention provides a kind of preparation method of colchicine sublingual tablet described in above-mentioned technical scheme, comprises the following steps:

[0049] Inclusion of colchicine with cyclodextrin to obtain an inclusion compound;

[0050] Mixing the clathrate, mannitol, lactose and hydroxypropyl cellulose in an equal-volume ascending method to obtain a mixture;

[0051] mixing the mixture with hydroxypropylmethylcellulose and water, followed by granulation and drying in sequence to obtain an intermediate product;

[0052] The intermediate product is mixed with magnesium stearate and compressed into tablets to obtain colchicine sublingual tablets.

[0053] In the present invention, colchicine is clathrated with cyclodextrin to obtain clathrate; the specific steps of clathrate preferably include:

[0054] dissolving colchicine in an alcoholic solvent to obtain a colchicine solution;

[0055] The colchicine solution and cyclodextrin aqueous solut...

Embodiment 1

[0074] Embodiment 1: Colchicine relative bioavailability research

[0075] Test drug:

[0076] Name: Colchicine Sublingual Tablets, Specification: 0.5mg; Provider: Kunming Pharmaceutical Group Co., Ltd.; Batch Number: 20140616;

[0077] Reference preparation: colchicine tablets, specification: 1mg; provider: Kunming Pharmaceutical Group Co., Ltd.; batch number: 20140320;

[0078] animal:

[0079] Source, species, strain: Beagle, provided by the Experimental Animal Center of the Academy of Military Medical Sciences, body weight: 10-13kg, sex: ♂, total number of animals: 8.

[0080] Method and Results:

[0081] Chromatographic conditions:

[0082] Chromatographic column: Kromasil C 18 (200mm×4.6mm, 5μm);

[0083] Mobile phase: formic acid: 10mmol / L ammonium acetate: methanol (1:44:55, V:V:V);

[0084] Flow rate: 1.0mL / min;

[0085] Injection volume: 20μL;

[0086] Detection wavelength: 245nm;

[0087] Column temperature: 30°C;

[0088] Internal standard: carbamazepine...

Embodiment 2

[0101] Dissolve the prescribed amount of colchicine in the ratio of 1:1mL in ethanol with a mass fraction of 60%, and add a 20% mass fraction of hydroxypropyl-β-cyclodextrin aqueous solution, colchicine and hydroxypropyl-β - The mass ratio of cyclodextrin is 1:5, stir for 2 hours, heat the solution in a water bath to 60°C, remove the solvent under reduced pressure, scrape out the clathrate, and dry in an oven at 60±2°C At constant weight, the inclusion compound was passed through an 80-mesh sieve to obtain the colchicine hydroxypropyl-β-cyclodextrin inclusion compound;

[0102] Colchicine Sublingual Tablets 1000 Tablets Prescription Size:

[0103]

[0104] Note: 6.7g of colchicine hydroxypropyl-β-cyclodextrin inclusion compound contains 0.5g of colchicine;

[0105] Process: mix colchicine hydroxypropyl-β-cyclodextrin inclusion compound, mannitol, lactose and HPC in an equal-volume ascending method, and pass through a 20-mesh sieve for 3 times to obtain the mixture;

[010...

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Abstract

The invention provides a colchicine sublingual tablet, a preparation method and application thereof. The colchicine sublingual tablet is prepared from hydroxypropyl methyl cellulose, cyclodextrin, colchicine, mannitol, lactose, hydroxy propyl cellulose and magnesium stearate. The ratio of the total mass of the colchicine, the cyclodextrin, the mannitol, the lactose, the hydroxy propyl cellulose and the magnesium stearate to the mass of the hydroxypropyl methyl cellulose is (95-110):(0.4-0.6). The mass ratio of the colchicine to the cyclodextrin to the mannitol to the lactose to the hydroxy propyl cellulose to the magnesium stearate is (1.0-5.0):(1.0-40.0):(70.0-80.0):(8.0-10.0):(8.0-10.0):(0.5-1.5). Compared with the prior art, the colchicine sublingual tablet reduces a taken dosage, is quick in effect, avoids the liver first pass effect and improves bioavailability.

Description

technical field [0001] The invention relates to the technical field of colchicine, in particular to a colchicine sublingual tablet, a preparation method and application thereof. Background technique [0002] Colchicine is an alkaloid, named after it was first extracted from the liliaceous plant colchicine, also known as colchicine, molecular formula C 22 h 25 NO 6 , CAS No.: 64-86-8. The chemical name of colchicine is: (S)-N(5,6,7,9-tetraoxo-1,2,3,10-tetramethoxy-9-oxobenzo[α]-heptadene -7-base) acetamide; Its structural formula is shown in formula I: [0003] [0004] Colchicine can inhibit mitosis, destroy the spindle, and cause chromosomes to stagnate in metaphase. This abnormal division caused by colchicine is called colchicine mitosis; Without division, two daughter cells cannot be formed, thus doubling the chromosomes. Since American scholar Blakeslee (A.F.Blakeslee) succeeded in doubling the chromosomes of Datura and other plants with colchicine in 1937, colc...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/165A61K47/48A61K47/38A61P19/06A61P29/00
CPCA61K9/2054A61K9/006A61K9/2018A61K31/165
Inventor 高永良张伟杨兆祥
Owner KPC PHARM INC