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

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...

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.