Multi-unit bowel dissolvable preparation of compound alendronate sodium and vitamin D3 and preparation method thereof

A technology for compound alendronate sodium and alendronate sodium, which can be applied to medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., and can solve problems such as increased dose, low bioavailability, pain, etc. , to avoid irritation, increase contact area, and improve bioavailability

Inactive Publication Date: 2010-01-13
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 often feel pain when swallowing, esophageal burning, heartburn, etc., and severe peptic ulcers may occur; at the same time, the bioavailability of alendronate sodium is low, It is only 0.7% to 1%. In order to achieve an effective therapeutic concentration, the dosage must be increased when taking it, which just increases the adverse reactions of the digestive tract, greatly reduces the patient's compliance, and the drug effect cannot be fully exerted.

Method used

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  • Multi-unit bowel dissolvable preparation of compound alendronate sodium and vitamin D3 and preparation method thereof
  • Multi-unit bowel dissolvable preparation of compound alendronate sodium and vitamin D3 and preparation method thereof
  • Multi-unit bowel dissolvable preparation of compound alendronate sodium and vitamin D3 and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prepare materials according to the following formula: (1000 capsules)

[0033]

[0034] Weigh alendronate sodium, vitamin D3, diluent, and disintegrant through a 100-mesh sieve according to the above formula, mix well, add an appropriate amount of hydroxypropyl methylcellulose solution, prepare pellets and dry them;

[0035] Dissolve the enteric-coated material in an appropriate amount of ethanol, and add a plasticizer to adjust the film-forming properties of the enteric-coated solution;

[0036] The prepared drug-containing pellets are placed in a fluidized bed or other coating equipment, and the coating liquid is sprayed while blowing hot air to obtain enteric-coated pellets.

Embodiment 2

[0038] Prepare materials according to the following formula: (1000 capsules)

[0039]

[0040] According to the above formula, take alendronate sodium, microencapsulated vitamin D3 powder, diluent, and disintegrant through a 100-mesh sieve, mix well, add an appropriate amount of povidone solution, prepare granules and dry them;

[0041] Disperse the enteric material in an appropriate amount of water, add a plasticizer to adjust the film-forming properties of the enteric coating solution, and add an anti-adhesive agent to adjust the viscosity of the enteric coating solution;

[0042] The prepared drug-containing granules are placed in a fluidized bed or other coating equipment, and the coating liquid is sprayed while blowing hot air to obtain enteric-coated granules.

Embodiment 3

[0044] Prepare materials according to the following formula: (1000 capsules)

[0045]

[0046] Weigh alendronate sodium, vitamin D3, diluent, and disintegrant through a 100-mesh sieve according to the above formula, mix well, add an appropriate amount of water, prepare pellets and dry them;

[0047] Dissolving the enteric material in an appropriate amount of ammonia water with a pH of 9, adding a plasticizer to adjust the film-forming properties of the enteric coating solution, and adding an anti-adhesive agent to adjust the viscosity of the enteric coating solution;

[0048] The prepared drug-containing pellets are placed in a fluidized bed or other coating equipment, and the coating liquid is sprayed while blowing hot air to obtain enteric-coated pellets.

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Abstract

The invention discloses a multi-unit bowel dissolvable preparation of compound alendronate sodium and vitamin D3 and a preparation method thereof. The preparation is bowel dissolvable micro-pills or bowel dissolvable granules comprising the alendronate sodium, the vitamin D3, one or a plurality of bowel dissolvable coating materials and other medicinal auxiliary materials; and the preparation is undissolvable in the stomach, is evenly released in the bowel and has the characteristics of high bioavailability, light adverse reaction, convenient taking and the like.

Description

technical field [0001] The invention relates to a combined preparation of sodium alendronate and vitamin D3, more specifically, a multi-unit enteric-coated preparation of compound sodium alendronate and vitamin D3 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 side effect of etidronate, the first generation of bisphosphonates, which can inhibit bone mineralization and lead to osteomalacia after long-term administration. It is a highly evaluated osteoporosis prevention and treatment drug in the international clinical circle. It has been widely used in the treatment of various diseases such as primary or secondary osteoporosis, hypercalcemia, osteitis deformans, and bone pain caused by tumor bone metastasis. [0003] Fosamax Pl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/663A61K31/593A61K9/34A61K9/36A61K9/32A61K9/40A61K9/16A61P19/10A61P19/08
Inventor 沈立新梁晓晖刘福双邹济高
Owner WUXI DINGFU PHARMA
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