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Microporous membrane-coated controlled-release diacerein pellet and preparation method thereof

A technology of diacerein and microporous membrane, which is applied in the field of microporous membrane controlled-release coated diacerein pellets and its preparation, and can solve problems affecting intestinal flora

Inactive Publication Date: 2017-05-24
FOSHAN TENGRUI MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Diacerein increases the likelihood of enterocolitis in patients taking antibiotics and / or chemotherapy, which affect the intestinal flora
Accidental or spontaneous overdose of diacerein can cause diarrhea

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of drug-containing pill core: take 10% diacerein, 20% microcrystalline cellulose, 5% sodium carboxymethyl starch, and 65% lactose and mix them uniformly in a mixer, and add an appropriate amount of 5% sodium hydroxypropylmethylcellulose solution as The adhesive is used to make a soft material, which is extruded through a 0.6-0.8mm sieve, rolled into a ball, and then boiled and dried to obtain a pill core.

[0031] Preparation of pellets with different coating weight gains:

[0032] Coating weight gain A prescription: Eudragit NE 30D aqueous dispersion 20kg, PVP 1kg, talcum powder 3kg, triethyl citrate 0.1kg.

[0033] Coating weight gain B prescription: Eudragit NE 30D aqueous dispersion 60kg, PVP 3kg, talcum powder 9kg.

[0034] Weigh 100kg of drug-containing pellet cores and put them in the fluidized bed, and spray the above-mentioned coating prescription A or B liquid through a spray gun in a fluidized state. Coating parameters: fan frequency 30, materia...

Embodiment 2

[0037] Preparation of drug-containing pill core: take 15% diacerein, 20% microcrystalline cellulose, 5% sodium carboxymethyl starch, and 60% lactose and mix them uniformly in a mixer, and add an appropriate amount of 5% sodium hydroxypropylmethylcellulose solution as The adhesive is used to make a soft material, which is extruded through a 0.6-0.8mm sieve, rolled into a ball, and then boiled and dried to obtain a pill core.

[0038] Preparation of pellets with different coating weight gains:

[0039] Coating weight gain A prescription: Eudragit NE 30D water dispersion 20kg, HPMC 1kg, talcum powder 3kg, triethyl citrate 0.1kg.

[0040] Coating weight gain B prescription: Eudragit NE 30D aqueous dispersion 60kg, HPMC 3kg, talcum powder 9kg, triethyl citrate 0.3kg.

[0041]Weigh 100kg of drug-containing pellet cores and put them in the fluidized bed, and spray the above-mentioned coating prescription A or B liquid through a spray gun in a fluidized state. Coating parameters: fa...

Embodiment 3

[0044] Preparation of drug-containing pill core: take 20% diacerein, 10% microcrystalline cellulose, 5% sodium carboxymethyl starch, and 65% starch and mix them uniformly in a mixer, and add an appropriate amount of 5% sodium hydroxypropyl methylcellulose solution as The adhesive is used to make a soft material, which is extruded through a 0.6-0.8mm sieve, rolled into a ball, and then boiled and dried to obtain a pill core.

[0045] Preparation of pellets with different coating weight gains:

[0046] Coating weight gain A prescription: Eudragit NE 30D aqueous dispersion 20kg, HPMC 1kg, titanium dioxide 1kg, magnesium stearate 2kg, triethyl citrate 0.1kg.

[0047] Coating weight gain B prescription: Eudragit NE 30D aqueous dispersion 60kg, HPMC 3kg, titanium dioxide 3kg, magnesium stearate 6kg, triethyl citrate 0.3kg.

[0048] Weigh 100kg of drug-containing pellet cores and put them in the fluidized bed, and spray the above-mentioned coating prescription A or B liquid through ...

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PUM

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Abstract

The invention discloses a microporous membrane-coated controlled-release trelagliptin succinate pellet and a preparation method thereof. The microporous membrane-coated controlled-release trelagliptin succinate pellet sequentially comprises a drug-containing pellet core and a controlled-release coating layer from inside to outside, wherein the drug-containing pellet core is prepared from a primary material and an auxiliary material at the ratio of (5%-20%):(80%-95%). According to the microporous membrane-coated controlled-release trelagliptin succinate pellet, a bitter taste can be coated, the effective ingredients can be dissolved out, constant long-acting plasma concentration is ensured, and the defect that a drug is discharged along with excrement before not completely released is avoided.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations for animals, more specifically, to a microporous membrane controlled-release coated diacerein pellet and a preparation method thereof. Background technique [0002] 1. Pharmacological and clinical effects [0003] Diacerelate is the primary inhibitor of IL-1 in osteoarthritis. It has been confirmed by cell experiments and animal experiments that the pharmacological effects of this product mainly include (1) this product can induce cartilage production, has analgesic, anti-inflammatory and antipyretic effects; (2) does not inhibit the synthesis of prostaglandins; (3) has the effect on bone Arthritis has the effect of delaying the progression of the disease. Pharmacokinetic studies have shown that in animals and humans, orally administered diacerein undergoes deacetylation into the active metabolite rhein before entering the systemic circulation. The peak time of a single oral administr...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/32A61K47/38A61K31/222A61P19/02A61P29/00
CPCA61K9/5026A61K9/0002A61K9/5089A61K31/222
Inventor 王雪峰
Owner FOSHAN TENGRUI MEDICINE TECH CO LTD
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