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Complex formulation for preventing or treating osteoporosis which comprises solid dispersion of vitamin d or its derivative and bisphosphonate

A technology of solid dispersion and composite preparation, applied in the field of preparation of the composite preparation, prevention or treatment of osteoporosis

Inactive Publication Date: 2009-09-16
HANMI SCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, these complex preparations have a problem of rapid decomposition due to the high reactivity of vitamin D

Method used

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  • Complex formulation for preventing or treating osteoporosis which comprises solid dispersion of vitamin d or its derivative and bisphosphonate
  • Complex formulation for preventing or treating osteoporosis which comprises solid dispersion of vitamin d or its derivative and bisphosphonate
  • Complex formulation for preventing or treating osteoporosis which comprises solid dispersion of vitamin d or its derivative and bisphosphonate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] According to the amount described in Table 1, add 2-hydroxypropyl-β-cyclodextrin (Aldrich) to the ethanol / water mixture and stir until the solution becomes clear, then add it to it Cholecalciferol (Fluka, Chemie GmbH, Buchs). The resulting mixture was spray-dried with a spray dryer (Buchi, MiniSpray Dryer, B-191, Switzerland) to obtain a solid dispersion. The spray drying was performed at an inlet temperature of 50°C and a pump speed of 30 rpm, followed by drying the solid dispersion at 50°C for 2 hours after spraying.

Embodiment 2

[0070] The steps of Example 1 were repeated to prepare a solid dispersion of vitamin D or its derivatives, except that 0.02 mg of d,l-α-tocopherol (BASF) was further added.

Embodiment 3

[0072] The steps of Example 1 were repeated to prepare a solid dispersion of vitamin D or its derivatives, except that 0.05 mg of ascorbic acid (BASF) was further added.

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PUM

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Abstract

The present invention relates to a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which comprises said solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation of the present invention comprising vitamin D or a derivative thereof and a bisphosphonate can maintain a constant therapeutic level of vitamin D or a derivative thereof through its improved drug stability, while enhancing the patient compliance by minimizing inconvenience and adverse effects when administered to patients. Therefore, the complex formulation of the present invention can be advantageously used for preventing and treating osteophorosis.

Description

Technical field [0001] The present invention relates to a solid dispersion comprising vitamin D or a derivative thereof and cyclodextrin, a composite preparation for preventing or treating osteoporosis comprising the solid dispersion and a bisphosphonate, and the preparation of the composite preparation Methods. Background technique [0002] Osteoporosis is a metabolic bone disease in which bone mineral density (BMD) is reduced and bone microstructure is destroyed, leading to an increased risk of fractures. Osteoporosis can be caused by some congenital factors, menopause, hyperthyroidism, hyperparathyroidism, chronic renal failure, or administration of glucocorticoid drugs, and it is most common in postmenopausal women with estrogen deficiency. The increase in osteoclast resorption far exceeds the bone formation of osteoblasts and reduces intestinal calcium absorption, which leads to a rapid decrease in BMD. [0003] In the treatment of osteoporosis, bisphosphonates that reduce b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/592A61K9/16
CPCA61K9/5042A61K9/1652C08B37/0015A61K9/2054A61K9/2866A61K9/205C08L5/16A61K31/592A61K9/1611B82Y5/00A61K47/48969A61K9/1629A61K47/6951A61P19/10A61P3/02A61P3/14A61K9/10A61K31/59
Inventor 禹钟守李鸿基陈周男
Owner HANMI SCI CO LTD
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