Dispersion preparation containing colloidal bismuth pectin and preparing method therefor

Abstract

A dispersion preparation containing colloidal bismuth pectin is provided. 1 g is adopted as a unit for the preparation. Each unit of the preparation includes: 44.0 to 900.0 mg of colloidal bismuth pectin, 1.0-500 mg of a penetration enhancer, 2.0-312.5 mg of acid-source pore forming agent, 2.0-250.0 mg of alkali-source pore forming agent and 1.0-400.0 mg of a disintegrating agent.

Claims

1. A dispersion preparation containing colloidal bismuth pectin, wherein each unit of the preparation comprises: 44.0-900.0 mg of colloidal bismuth pectin; 1.0-500 mg of a penetration enhancer; 2.0-312.5 mg of acid-source pore forming agent; 2.0-250.0 mg of alkali-source pore forming agent; and 1.0-400.0 mg of a disintegrating agent; wherein the penetration enhancer comprises at least one member selected from calcium sulphate dehydrate and calcium bicarbonate; the acid resource pore-forming agent is selected from at least one member from anhydrous citric acid, monohydrate citric acid, tartaric acid, fumaric acid, monopotassium phosphate, sodium dihydrogen phosphate, glycine and EDTA; and the alkali resource pore-forming agent is sodium bicarbonate.

2. The dispersion preparation containing colloidal bismuth pectin, as recited in claim 1, wherein each gram of the dispersion preparation containing colloidal bismuth pectin further comprises 5.0-50.0 mg lubricant, and the lubricant is at least one member selected from glyceryl behenate, poloxamerl 88, sodium dodecyl sulfate, PEG6000, silicon dioxide and talcum powder.

3. The dispersion preparation containing colloidal bismuth pectin, as recited in claim 1 or 2, wherein the dispersion preparation comprises filler.

4. The dispersion preparation containing colloidal bismuth pectin, as recited in claim 3, wherein an addition amount of the filler is 1.0-375.0 mg in each gram of the dispersion preparation.

5. The dispersion preparation containing colloidal bismuth pectin, as recited in claim 3, wherein the filler is at least one member selected from lactose, microcrystalline cellulose, mannitol, sucrose and pregelled starch.

6. The dispersion preparation containing colloidal bismuth pectin, as recited in claim 1, wherein the disintegrating is at least one member selected from low substituted hydroxypropy cellulose, crospovidone, croscarmellose sodium or sodium carboxymethyl starch.

7. The dispersion preparation containing colloidal bismuth pectin, as recited in claim 1 or 2, wherein the dispersion preparation is dispersed tablet.

8. A method for preparing the dispersion preparation containing colloidal bismuth pectin, as recited in claim 7, comprising steps of: mixing a required quantity of the crude material and the auxiliary material by drying mix and tablet compressing.

9. A method for preparing the dispersion preparation containing colloidal bismuth pectin, as recited in claim 7, comprising steps of: adding adhesive into a required quantity of the crude material and the auxiliary material, pelleting by a wet process and then tablet compressing.

10. The method for preparing the dispersion preparation containing colloidal bismuth pectin, as recited in claim 9, wherein the adhesive is at least one member selected from a group consisting of water, 30 vol %-80 vol % ethyl alcohol, 30 vol%-80 vol % ethanol solution containing 3wt %-5wt % polyvinylpyrrolidone, and 0.2wt % tween-80 aqueous solution, wherein an additive amount of the adhesive is 160800 l/g for each gram of the dispersion preparation.

Description

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT

[0042] Colloidal bismuth pectin adopted in preferred embodiments of the present invention comprises 14-16% (mass percent) metallic bismuth.

Example 1

[0043] Formulation: 324.7 g of colloidal bismuth pectin, 25.0 g of low substituted hydroxypropy cellulose, 80.8 g of microcrystalline cellulose, 15.0 g of calcium sulphate dehydrate, 27.5 g monohydrate citric acid, 22.0 g of sodium bicarbonate, 5.0 g of talcum powder, and 80.0-400.0 ml ethyl alcohol with a concentration of 50%. 1000 tablets are made, and each tablet weighs 500 mg.

[0044] A preparation process of the dispersion preparation comprises steps of:

[0045] grinding a crude material and an auxiliary material;

[0046] screening by a 100 mesh screen;

[0047] weighing a formula dosage of colloidal bismuth pectin, low substituted hydroxypropy cellulose, microcrystalline cellulose, calcium sulphate dehydrate and sodium bicarbonate and mixing uniformly;

[0048] adding a formula dosage of soft material made by 50% ethanol, screening by 24 mesh screen, granulating, drying for 2 hours under 60 C., and screening whole grains by 24 meshes, adding monohydrate citric acid and talcum powder, mixing uniformly; and

[0049] testing drug contents, tabletting, coating a film, testing and packaging.

[0050] Testing indicators: hardness 3.00.5kg, dispersal uniformity 135 s, dissolution rate 80.19%, and a weight difference meets requirements.

Example 2

[0051] Formulation:324.7 g of colloidal bismuth pectin, 26.5 g of low substituted hydroxypropy cellulose, 98.0 g of microcrystalline cellulose, 15.9 g of calcium sulphate dehydrate, 33.1 g monohydrate citric acid, 26.5 g of sodium bicarbonate, 5.3 g of talcum powder. 1000 tablets are made, and each tablet weighs 500 mg.

[0052] A preparation process of the dispersion preparation comprises steps of:

[0053] grinding a crude material and an auxiliary material;

[0054] screening by a 100 mesh screen;

[0055] weighing a formula dosage of colloidal bismuth pectin, low substituted hydroxypropy cellulose, microcrystalline cellulose, calcium sulphate dehydrate, sodium bicarbonate, anhydrous citric acid and talcum powder and mixing uniformly;

[0056] testing drug contents, tabletting, testing and packaging.

[0057] Testing indicators: hardness 3.00.5 kg, dispersal uniformity 135 s, dissolution rate 80.19%, and a weight difference meets requirements.

Examples 3-9

[0058]

TABLE-US-00005 Crude material and auxiliary Example Example Example Example Example Example Example material 3 4 5 6 7 8 9 Colloidal bismuth 17.6 324.7 324.7 259.7 324.7 324.7 324.7 pectin, mg lactose, mg 50.0 25.0 25.0 microcrystalline 103.0 48.7 80.8 177.2 7.7 92.0 18.5 cellulose, mg hydroxypropy 25.0 25.0 25.0 26.5 26.5 26.5 cellulose, mg calcium sulphate 0.4 15.0 15.0 12.5 70.4 15.9 47.7 dehydrate, mg sodium 100.0 25.0 22.0 20.0 42.4 29.2 47.7 bicarbonate, mg anhydrous citric 125.0 27.5 59.6 acid, mg monohydrate citric 31.3 25.0 acid, mg fumaric acid, mg 36.4 tartaric acid, mg 53.0 poloxamer 188, mg 5.0 sodium dodecyl 4.0 sulfate, mg PEG6000, mg 5.0 silicon dioxide, mg 4.8 magnesium 1.0 stearate, mg talcum powder, mg 5.3 5.3 5.3 50% 400.0 400.0 ethanol, l/tablet 3% 100.0 polyvinylpyrrolidone 50% ethanol solution, l/tablet 0.2% tween-80, l/ 80.0 100.0 100.0 100.0 tablet tablet weight, mg 400 499.7 500 550.2 530 530 530 dispersible 78 120 125 132 136 125 118 uniformity, s dissolution rate, % 98.8 81.6 80.2 85.6 91.6 85.4 96.8 Colloidal stability conforms conforms conforms conforms conforms conforms conforms with with with with with with with regulations regulations regulations regulations regulations regulations regulations

Examples 10-15

[0059]

TABLE-US-00006 Crude material and Example Example Example1 Example1 Example1 Example auxiliary material 10 11 2 3 4 15 Colloidal bismuth 324.7 974.0 324.7 73.0 173.7 211.2 pectin, mg lactose, mg 50.0 50.0 microcrystalline 52.9 200.0 75.0 100.0 cellulose, mg hydroxypropy 25.0 cellulose, mg saccharose, mg 20.0 37.5 pregelatinized starch, 5.0 mg hydroxypropyl 26.5 65.0 25.0 100.0 25.0 cellulose, mg crospovidone, mg 50.0 croscarmellose 45.0 50.0 sodium, mg carboxyl methyl 5.0 starch sodium, mg calcium sulphate 25.2 40.0 15.0 250.0 15.0 15.0 dihydrate, mg sodium 42.4 74.0 15.0 1.0 25.0 25.0 bicarbonate, mg anhydrous citric 90.0 1.0 31.3 acid, mg monohydrate citric 15.0 acid, mg fumaric acid, mg 53.0 tartaric acid, mg 31.3 Glyceryl Behenate, 15.0 mg silicon dioxide, mg 25.0 talcum powder, mg 5.3 5.0 5.0 5.0 50% ethanol 100.0 solution, l/tablet 3% 200.0 polyvinylpyrrolidone 50% ethanol solution, l/tablet 0.2% tween-80, l/ 100.0 100.0 tablet tablet weight, mg 530 1508 374.7 500 500 500 dispersible 120 143 110 123 136 105 uniformity, s dissolution rate, % 98.8 85.0 85.3 88.9 85.1 86.6 Colloidal stability Conforms Conforms Conforms Conforms Conforms Conforms with with with with with with regulations regulations regulations regulations regulations regulations