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Tablets of mosapride citrate and preparation method thereof

A technology of mosapride citrate and dispersible tablets, which is applied in the field of medicine and can solve problems such as difficulty in fully mixing, low bioavailability, and low dissolution rate

Active Publication Date: 2012-10-10
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because mosapride citrate is an insoluble drug, it is almost insoluble in water, often encounters the problem that the dissolution rate is low or even unqualified in the actual production of mosapride citrate oral solid preparation; and because citric acid The content of mosapride in the preparation is low, and it is difficult to fully mix during preparation. When performing dissolution testing, there are often problems of high and low, and large differences in dissolution between tablets
When there is an urgent need for quick-acting and high-efficiency preparations in clinical practice, solving the problem of low bioavailability of insoluble drugs due to low solubility and slow dissolution has always been a major problem in the pharmaceutical industry
[0007] Chinese patent application CN1359680A discloses a pharmaceutical formulation of mosapride citrate suitable for preparing dispersible tablets by wet granulation and tabletting method, wherein besides the active ingredient mosapride citrate, it also contains disintegrant solution, diluent, lubricant, glidant, binding agent, the formula is suitable for the preparation of dispersible tablets, but the dissolution rate of mosapride citrate dispersible tablets prepared by the prescription and preparation process disclosed in this document The effect is still unsatisfactory, affecting the bioavailability of the drug in the body
[0008] Chinese patent application CN1911233A discloses a pharmaceutical composition containing mosapride and an antioxidant, which inhibits the degradation of mosapride by adding an oxygen free radical scavenger (blocker) antioxidant to the composition , however it does not disclose mosapride citrate dispersible tablets

Method used

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  • Tablets of mosapride citrate and preparation method thereof
  • Tablets of mosapride citrate and preparation method thereof
  • Tablets of mosapride citrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053]Mosapride Citrate Dispersible Tablets

[0054] Mosapride Citrate 6g

[0055] Povidone K15 12g

[0056] Lactose 150g

[0057] Starch 150g

[0058] Low-substituted hydroxypropyl cellulose 6g

[0059] 5% povidone K30 aqueous solution appropriate amount

[0060] Micronized silica gel 1.5g

[0061] Magnesium Stearate 1.5g

[0062] Made into 3000 pieces

[0063] Preparation method: each raw and auxiliary material is weighed according to the prescription amount. Add mosapride citrate to 600ml of absolute ethanol, heat in a water bath at 60°C until completely dissolved, then add povidone K15 and stir to dissolve; transfer to a rotary evaporator, evaporate ethanol under reduced pressure at 60°C, Make a solid dispersion; dry the solid dispersion at 60°C for 3 hours under reduced pressure, take it out, crush it, and pass it through a 100-mesh sieve for later use; pass lactose, starch and low-substituted hydroxypropyl cellulose through a 80-mesh sieve, and then add the solid...

Embodiment 2

[0065] Mosapride Citrate Dispersible Tablets

[0066] Mosapride Citrate 7.5g

[0067] Povidone K30 30g

[0068] Lactose 210g

[0069] Starch 60g

[0070] Low-substituted hydroxypropyl cellulose 15g

[0071] 5% povidone K30 aqueous solution appropriate amount

[0072] Micronized silica gel 1.5g

[0073] Magnesium Stearate 1.5g

[0074] Made into 3000 pieces

[0075] Preparation method: each raw and auxiliary material is weighed according to the prescription amount. Add mosapride citrate to 1500ml of absolute ethanol, heat in a water bath at 60°C until completely dissolved, then add povidone K30 and stir to dissolve; transfer to a rotary evaporator, evaporate ethanol under reduced pressure at 60°C, and prepare into a solid dispersion; dry the solid dispersion at 60°C for 4 hours, take it out, crush it, and pass it through a 100-mesh sieve for later use; pass lactose, starch and low-substituted hydroxypropyl cellulose through a 80-mesh sieve, and then add the solid disper...

Embodiment 3

[0076] Embodiment 3 mosapride citrate dispersible tablet

[0077] Mosapride Citrate 15g

[0078] Macrogol 4000 75g

[0079] Lactose 90g

[0080] Starch 150g

[0081] Low-substituted hydroxypropyl cellulose 8g

[0082] 5% povidone K30 aqueous solution appropriate amount

[0083] Micronized silica gel 3g

[0084] Magnesium Stearate 3g

[0085] Made into 3000 pieces

[0086] Preparation method: each raw and auxiliary material is weighed according to the prescription amount. Add mosapride citrate to 2500ml of absolute ethanol, heat in a water bath at 60°C until completely dissolved, then add polyethylene glycol 4000 and stir to dissolve; transfer to a rotary evaporator, evaporate ethanol under reduced pressure at 60°C, Make a solid dispersion; dry the solid dispersion at 60°C for 4 hours, take it out, crush it, and pass it through a 100-mesh sieve for later use; pass lactose, starch and low-substituted hydroxypropyl cellulose through a 80-mesh sieve, and then add the solid...

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Abstract

The invention belongs to the field of medicaments and in particular relates to tablets containing mosapride citrate and a preparation method thereof. Because the mosapride citrate is almost insoluble, defects of slow dissolution and low in-vitro and in-vivo bioavailability are present in the mosapride citrate tablets prepared by the common method. In order to improve the dissolution and bioavailability of the mosapride citrate, the invention provides dispersible tablets containing the mosapride citrate and a preparation method thereof. The prepared mosapride citrate dispersible tablets have high dissolution speed and low dissolution difference. The accumulated dissolution in five minutes is close to 100 percent, and the dispersible tablets are almost dissolved completely.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a tablet containing mosapride citrate and a preparation method thereof. Background technique [0002] Mosapride Citrate (Mosapride Citrate), the chemical name is 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methanol Base] benzamide citrate, white or off-white crystalline powder, odorless, slightly bitter. The melting point is 143-145°C. Soluble in dimethylformamide and pyridine, slightly soluble in methanol, insoluble in 95% ethanol, insoluble in water or ether. [0003] Mosapride citrate is a new third-generation gastric motility drug, mainly used for functional dyspepsia with heartburn, belching, nausea, vomiting, early satiety, upper abdominal distension and other gastrointestinal symptoms. The drug can enhance gastrointestinal motility, but does not affect gastric acid secretion, and has no side effects such as extrapyramidal reaction and diarrhea, and is well tol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/136A61K47/38A61P1/14A61P1/08
Inventor 赵志全强红刚牛桂云
Owner LUNAN PHARMA GROUP CORPORATION
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