Compound alendronate sodium vitamin D3 enteric-coated tablet and preparation method thereof

A technology of compound alendronate sodium and alendronate sodium, which is applied in the direction of pharmaceutical formula, medical preparations containing active ingredients, and pill delivery, which can solve low bioavailability, reduce patient compliance, and increase dosage To achieve good patient compliance, avoid adverse reactions, and increase stability

Inactive Publication Date: 2010-01-27
WUXI DINGFU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the two hydrogen atoms connected to a carbon atom in the structure of alendronate sodium are replaced by two phosphonic acid groups, more H can be released. + , which is highly corrosive
When the patient takes it, part of the alendronate sodium dissolves, producing a higher concentration of H on the surface of the esophageal mucosa. + , resulting in damage to the epithelium and mucosa of the upper gastrointestinal tract, patients oft

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Prepare raw materials according to the following formula: (1000 tablets)

[0038] Tablet core: weight % by weight

[0039] Main ingredient: Alendronate sodium: 6.525g 5.99%

[0040] (Contains Alendronate 5g)

[0041] Beta-ring of Vitamin D3 2g 1.83%

[0042] Dextrin inclusion complex: (contains vitamin D3 200000 IU)

[0043] Diluent: Microcrystalline Cellulose: 50g 45.87%

[0044] Starch: 28g 25.69%

[0045] Disintegrant: Crospovidone: 5g 4.59%

[0046] Binder: Povidone: 5g 4.59%

[0047] Lubricant: Magnesium Stearate: 0.5g 0.46%

[0048] Enteric coating solution: weight weight percent

[0049] Enteric coating material: polyacrylic acid resin: 6g 5.50%

[0050]Plasticizer: Triethyl citrate: 0.6g 0.55%

[0051] Antisticking agent: Talc: 3g 2.75%

[0052] Weigh alendronate sodium, microcrystalline cellulose, starch, and 1 / 3 amount of crospovidone according to the above formula, mix we...

Embodiment 2

[0056] Prepare raw materials according to the following formula: (1000 tablets)

[0057] Tablet core: weight % by weight

[0058] Main drug: Alendronate sodium: 13.05g 11.45%

[0059] (Containing Alendronate 10g)

[0060] Beta-Ring of Vitamin D3 4g 3.51%

[0061] Dextrin inclusion complex: (contains vitamin D3 400000 IU)

[0062] Diluent: Microcrystalline Cellulose: 50g 43.86%

[0063] Lactose: 23.5g 20.61%

[0064] Disintegrant: Croscarmellose 5g 4.39%

[0065] sodium:

[0066] Binder: Povidone: 5g 4.39%

[0067] Lubricant: Stearic Acid: 1g 0.88%

[0068] Enteric coating solution: weight weight percent

[0069] Enteric coating material: polyacrylic acid resin: 6g 5.26%

[0070] Plasticizer: Triethyl citrate: 0.6g 0.53%

[0071] Antisticking agent: Talc powder: 3g 2.63%

[0072] Weigh alendronate sodium, microcrystalline cellulose, lactose, and 1 / 4 amount o...

Embodiment 3

[0076] Prepare raw materials according to the following formula: (1000 tablets)

[0077] Tablet core: weight % by weight

[0078] Main drug: Alendronate sodium: 26.10g 12.99%

[0079] (Contains Alendronate 20g)

[0080] Beta-ring of Vitamin D3 8g 3.98%

[0081] Dextrin inclusion complex: (containing vitamin D3 800000 IU)

[0082] Diluent: Microcrystalline Cellulose: 100g 49.75%

[0083] Pregelatinized starch: 30g 14.92%

[0084] Disintegrant: Hydroxypropylcellulose: 10g 4.98%

[0085] Lubricant: Magnesium Stearate: 1g 0.50%

[0086] Micronized silica gel: 1g 0.50%

[0087] Enteric coating solution: weight weight percent

[0088] Enteric coating material: polyacrylic acid resin: 12g 5.97%

[0089] Plasticizer: Triethyl citrate: 1.2g 0.60%

[0090] Anti-sticking agent: Talc powder: 6g 2.99%

[0091] Weigh alendronate sodium, microcrystalline cellulose, pregelatinized ...

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PUM

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Abstract

The invention discloses a compound alendronate sodium vitamin D3 enteric-coated tablet and a preparation method thereof. The preparation is an enteric-coated tablet consisting of alendronate sodium, beta-cyclodextrin inclusion compound of vitamin D3, an enteric-coating material and other pharmaceutical excipients. The invention has simple process and good stability, is insoluble in stomach and can rapidly release in intestine, thereby avoiding adverse reactions stimulating upper gastrointestinal and having good patient compliance.

Description

technical field [0001] The invention relates to a combined preparation of alendronate sodium and vitamin D3, more specifically, a compound alendronate sodium vitamin D3 enteric-coated tablet and a preparation method thereof. Background technique [0002] Alendronate sodium is a third-generation new bisphosphonate drug, which has a strong inhibitory effect on osteoclasts and a certain effect on increasing bone mass, and will not cause hypercalcemia and hormone-like symptoms. There is no long-term use of the first-generation bisphosphonate drugs, which can cause bone mineralization inhibition and lead to osteomalacia side effects. It is currently a highly evaluated osteoporosis prevention and treatment drug in the international clinical community and has been widely used. Treatment of primary or secondary osteoporosis, hypercalcemia, osteitis deformans, bone pain caused by tumor bone metastasis and other diseases. [0003] Vitamin D3, a fat-soluble vitamin, can promote intest...

Claims

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Application Information

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IPC IPC(8): A61K31/663A61K31/593A61K9/28A61K9/30A61K47/40A61P19/10
Inventor 沈立新梁晓晖刘福双邹济高李燕春
Owner WUXI DINGFU PHARMA
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