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Composite preparations containing double phosphinic acid compounds and vitamin D clathrate and method of preparing the same

A bisphosphonic acid compound and compound preparation technology, which is applied in the field of medicine, can solve problems such as difficult large-scale production, cumbersome process, and vitamin D degradation, and achieve improved solubility, improved stability and dissolution rate, and high safety. Effect

Inactive Publication Date: 2008-09-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Japanese patent publication 78128,417 proposes an inclusion compound prepared from vitamin D3 and β-cyclodextrin, which improves the stability of vitamin D3 to light, heat and oxygen. The disadvantage is that the inclusion compound is difficult to dissolve in water
Patent CN1110275A discloses an inclusion compound of vitamin D and hydroxypropyl-β-cyclodextrin, which improves the stability and water solubility of vitamin D, but the process is cumbersome, including ethanol dissolution, rotary evaporation, and nitrogen blowing. Drying, ice water dissolution, filtration, freeze-drying and other steps may lead to vitamin D degradation, and it is not easy for large-scale production

Method used

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  • Composite preparations containing double phosphinic acid compounds and vitamin D clathrate and method of preparing the same
  • Composite preparations containing double phosphinic acid compounds and vitamin D clathrate and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Vitamin D 3 Study on Stability of Inclusion Complex of -Hydroxypropyl-β-cyclodextrin

[0025] Take an appropriate amount of inclusion compound and non-inclusion vitamin D powder and spread it into a thin layer of 2 mm thick, seal it in a glass ampoule, keep away from light, place it at 60°C, and place it under an illumination of (4500±500) 1x. Take samples at 5 and 10d, observe the appearance and detect the content. The results are attached figure 1 As shown, the clathrate significantly improved the stability of vitamin D to light and heat.

Embodiment 2

[0027] Alendronate Sodium Vitamin D3 Compound enteric-coated tablet

[0028] Vitamin D 3 Preparation of -Hydroxypropyl-β-cyclodextrin inclusion compound

[0029] Vitamin D 3 Feed with refined hydroxypropyl-β-cyclodextrin at a mass ratio of 1:1000. Weigh the HP-β-CD and vitamin D of the prescription ratio 3 ; Dissolve vitamin D3 with a small amount of 95% ethanol, and place it in a suitable container away from light; configure HP-β-CD and deionized water to form a 10% HP-β-CD aqueous solution, and mix HP-β-CD under stirring conditions Slowly add the aqueous solution to the vitamin D 3 In the container of the solution, sonicate for 20 minutes. Filtered through a 0.45 μm microporous membrane, the resulting clear solution was pre-frozen in a -70°C refrigerator for 12 hours, and then freeze-dried in a vacuum freeze dryer for 15 hours. The dry matter is pulverized and passed through a 80-mesh sieve.

[0030] tablet preparation

[0031] prescription:

[0032] Component Dosag...

Embodiment

[0044] Alendronate Sodium Vitamin D 3 Compound Capsules

[0045] Vitamin D 3 Preparation of -Hydroxypropyl-β-cyclodextrin inclusion compound

[0046] Vitamin D 3 Feed with refined hydroxypropyl-β-cyclodextrin at a mass ratio of 1:1000. Weigh the HP-β-CD and vitamin D of the prescription ratio 3 ; Dissolve vitamin D with a small amount of 95% ethanol 3 , placed in a suitable container away from light; HP-β-CD and deionized water were configured to form a 10% HP-β-CD aqueous solution, and the HP-β-CD aqueous solution was slowly added to vitamin D under stirring conditions. 3 In the container of the solution, sonicate for 20 minutes. Filtered through a 0.45 μm microporous membrane, the resulting clear solution was pre-frozen in a -70°C refrigerator for 12 hours, and then freeze-dried in a vacuum freeze dryer for 15 hours. The dry matter is pulverized and passed through a 80-mesh sieve.

[0047] Capsule preparation

[0048] prescription:

[0049] Component Dosage

[005...

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Abstract

The invention provides a compound preparation containing diphosphonic acid compound and vitamin clathrate and a preparation method thereof, and belongs to the technology field of medicines. The compound preparation comprises (wt%) diphosphonic acid compound 5-50 and vitamin D 0.005-0.5, wherein the vitamin D is prepared into clathrate derivative with cyclodextrin, and the weight ratio of vitamin D to clathrate derivative is 1:(100-2,000). The invention provides a simple and practical preparation method for a compound preparation containing alendronate and vitamin D with the improved solubility and stability of vitamin D. The inventive compound preparation has definite therapeutic effect and good safety; and has improved solubility and stability of vitamin D due to clathration of vitamin D with cyclodextrin or derivative thereof, thereby being helpful for controlling content uniformity in case of low dose preparation production and reducing the loss vitamin D raw material during batch charging.

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically, it relates to a compound preparation containing bisphosphonate and vitamin D clathrate, and further relates to the use and preparation method of the preparation. Background technique: [0002] Bisphosphonates are a class of artificially synthesized compounds that have been used clinically since the 1970s, with low side effects and definite curative effects, and have gradually replaced estrogens as commonly used drugs for the treatment of osteoporosis. These drugs are enzyme-resistant analogues of pyrophosphate. Pyrophosphate can inhibit bone mineralization under normal conditions. The P-O-P structure in pyrophosphate is replaced by P-C-P to become a bisphosphonate, which becomes more stable. Bisphosphonates mainly act on osteoclasts and inhibit bone resorption. There is also a certain effect of increasing bone mass, and will not cause hypercalcemia and hormone-like effects. [0...

Claims

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Application Information

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IPC IPC(8): A61K31/662A61K31/59A61K47/48A61K47/40A61P19/10A61K47/69
Inventor 何仲贵毕薇刘晓红孙进杨亚军
Owner SHENYANG PHARMA UNIVERSITY
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