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Alfacalcidol oral liposome drug and preparation method and application thereof

An alfacalcidol and liposome technology, applied in liposome delivery, drug combination, drug delivery, etc., can solve many adverse reactions, poor stability of oral alfacalcidol, poor bioavailability, etc. To improve the therapeutic effect, increase oral absorption and bioavailability, and improve storage stability

Pending Publication Date: 2020-08-28
南通华山药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the development of new oral liposome formulations of alfacalcidol can solve the problems of poor stability, many adverse reactions, and poor bioavailability of oral alfacalcidol, thereby effectively improving the anti-osteoporosis effect of alfacalcidol. Therapeutic effect

Method used

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  • Alfacalcidol oral liposome drug and preparation method and application thereof
  • Alfacalcidol oral liposome drug and preparation method and application thereof
  • Alfacalcidol oral liposome drug and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Weigh 1 mg of alfacalcidol, 20 mg of soybean lecithin, 5 mg of cholesterol, and 2 mg of vitamin E in a round-bottomed flask, add 20 ml of dichloromethane and ultrasonically dissolve it in a short-term water bath. The round bottom flask was placed on a rotary evaporator, and dichloromethane was evaporated under reduced pressure at 40°C until a lipid film was formed on the inner wall of the round bottom flask, and the round bottom flask was placed in a desiccator to vacuum for 24 hours. Weigh 2mg of vitamin C and 1mg of EDTA-2Na and dissolve them in 20ml of 0.01M pH7.4 phosphate buffer, add the buffer into a round bottom flask to hydrate and elute the lipid film, and ultrasonically disperse it in a water bath for 30min to prepare lipid Coarse suspension of plastids. Subsequently, the liposome coarse suspension probe was sonicated at 200w for 30s to obtain a liposome suspension with a smaller particle size and uniform dispersion. 10 mg of trehalose is added to the liposom...

Embodiment 2

[0032] Weigh 1 mg of alfacalcidol, 50 mg of egg yolk lecithin, 10 mg of cholesterol, and 1 mg of dibutyl hydroxytoluene into a round bottom flask, add 20 ml of dichloromethane and ultrasonically dissolve it in a short-term water bath. The round bottom flask was placed on a rotary evaporator, and dichloromethane was evaporated under reduced pressure at 40°C until a lipid film was formed on the inner wall of the round bottom flask, and the round bottom flask was placed in a desiccator to vacuum for 24 hours. Weigh 2mg of sodium sulfite and 1mg of EDTA-2Na and dissolve them in 20ml of 0.01M pH7.4 phosphate buffer, add the buffer into a round bottom flask to hydrate and elute the lipid film, and ultrasonically disperse it in a water bath for 30 minutes to prepare lipid body suspension. Subsequently, the liposome coarse suspension probe was sonicated at 200w for 30s to obtain a liposome suspension with a smaller particle size and uniform dispersion. 10 mg of mannose is added into ...

Embodiment 3

[0034] Weigh 1 mg of alfacalcidol, 10 mg of hydrogenated soybean lecithin, 1 mg of cholesterol, and 1 mg of tert-butyl-4-hydroxyanisole into a round bottom flask, add 20 ml of dichloromethane and ultrasonically dissolve it in a water bath for a short time. The round bottom flask was placed on a rotary evaporator, and dichloromethane was evaporated under reduced pressure at 40°C until a lipid film was formed on the inner wall of the round bottom flask, and the round bottom flask was placed in a desiccator to vacuum for 24 hours. Weigh 2mg of sodium thiosulfate and 1mg of EDTA-2Na and dissolve in 20ml of 0.01M pH7.4 phosphate buffer, add the buffer into a round bottom flask to hydrate and elute the lipid film, and ultrasonically disperse it in a water bath for 30min to prepare A coarse suspension of liposomes was obtained. Subsequently, the liposome coarse suspension probe was sonicated at 200w for 30s to obtain a liposome suspension with a smaller particle size and uniform disp...

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Abstract

The invention discloses an alfacalcidol oral liposome drug and a preparation method and application thereof. The alfacalcidol oral liposome drug is prepared from the following raw materials in parts by weight: 1 part of alfacalcidol, 5-50 parts of phospholipid, 1-10 parts of cholesterol and 1-5 parts of an antioxidant. Alfacalcidol is encapsulated by liposome so that the chemical stability of alfacalcidol can be improved, the alfacalcidol can be protected from being damaged by gastric juice, bile, digestive enzymes and other substances through liposome, and the stability of the alfacalcidol ingastrointestinal tracts can be improved, so that absorption and bioavailability of the alfacalcidol in small intestines are improved; and compared with commercially available alfacalcidol tablets, the oral alfacalcidol lipidosome drug has high blood drug level and improved bioavailability, and the treatment effect on osteoporosis is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an oral liposome medicine of alfacalcidol and a preparation method and application thereof, and the method can be applied to industrial scale-up production. Background technique [0002] Alfacalcidol plays an important role in regulating calcium and phosphorus balance and bone metabolism, and it can be activated by 25-hydroxylase in the liver to become active 1α,25-(OH) 2 D3, and functions throughout the body and in osteoblasts. It can increase the reabsorption of calcium in the small intestine and renal tubules, inhibit the hyperplasia of parathyroid glands, reduce the synthesis and release of parathyroid hormone, and inhibit bone resorption; it can also increase the synthesis of transforming growth factors and insulin-like growth factors, and promote collagen and bone Matrix protein synthesis; in addition, the drug can also regulate muscle calcium metabol...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/593A61K47/22A61K47/18A61K47/10A61K47/02A61K47/14A61P19/10A61P19/08
CPCA61K9/127A61K9/0053A61K31/593A61K47/22A61K47/183A61K47/10A61K47/02A61K47/14A61P19/10A61P19/08
Inventor 施建飞钱建
Owner 南通华山药业有限公司
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