Alfacalcidol injection and preparation method thereof

A technology for alfacalcidol and alcohol injection, which is applied in the field of alfacalcidol injection and its preparation, can solve the problems of low bioavailability, monotonous dosage form, and cannot exist stably for a long time, and achieves reduction in dosage and bioavailability. The effect of increasing the degree of

Inactive Publication Date: 2015-07-29
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the main preparation forms of alfacalcidol are soft capsules and capsules; the dosage form is relatively monotonous, and alfacalcidol is sensitive to light and air, and has low solubility for common organic solvents. Poor stability, extremely low content of active ingredients, low bioavailability
Alfacalcidol injection is not reported in the prior art, because it cannot exist stably for a long time, and its bioavailability is not high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Alfacalcidol Injection

[0038] The prescription is:

[0039] Alfacalcidol 0.5mg

[0040] Polyvinylpyrrolidone K30 1.2g

[0041] Hypromellose aqueous solution 18g

[0042] Sodium Lauryl Sulfate 1.2g

[0043] Sodium sulfite 0.1g

[0044] Sodium chloride appropriate amount

[0045] Add water for injection to 100g

[0046] The preparation method is:

[0047] 1) Weigh 70% of the prescribed amount of distilled water, add the prescribed amount of hypromellose aqueous solution, and stir well; continue to add the prescribed amount of polyvinylpyrrolidone K30 and sodium lauryl sulfate, and stir at 45°C for 15 minutes until completely dissolved ;

[0048] 2) Raise the temperature to 60°C, add the prescribed amount of alfacalcidol at a stirring speed of 500rpm, and continue stirring for 20 minutes until it is completely dissolved;

[0049] 3) Add the prescribed amount of sodium sulfite and appropriate amount of sodium chloride, stir to dissolve; then add 0.1% ac...

Embodiment 2

[0051] Example 2 Alfacalcidol Injection

[0052] The prescription is:

[0053] Alfacalcidol 0.5mg

[0054] Polyvinylpyrrolidone K30 1.6g

[0055] Hypromellose aqueous solution 24g

[0056] Sodium Lauryl Sulfate 1.7g

[0057] Sodium bisulfite 0.1g

[0058] Glucose Appropriate amount

[0059] Add water for injection to 100g

[0060] The preparation method is:

[0061] 1) Weigh 80% of the prescribed amount of distilled water, add the prescribed amount of hypromellose aqueous solution, and stir well; continue to add the prescribed amount of polyvinylpyrrolidone K30 and sodium lauryl sulfate, and stir at 55°C for 15-25min to all dissolved;

[0062] 2) Raise the temperature to 70°C, add the prescribed amount of alfacalcidol at a stirring speed of 1000rpm, and continue stirring for 40 minutes until it is completely dissolved;

[0063] 3) Add the prescribed amount of sodium bisulfite and an appropriate amount of glucose, stir to dissolve; then add 0.1% activated carbon of the t...

Embodiment 3

[0065] Example 3 Alfacalcidol Injection

[0066] The prescription is:

[0067] Alfacalcidol 0.5mg

[0068] Polyvinylpyrrolidone K30 1.4g

[0069] Hypromellose aqueous solution 20g

[0070] Sodium Lauryl Sulfate 1.5g

[0071] Sodium metabisulfite 0.1g

[0072] Moderate amount of mannitol

[0073] Add water for injection to 100g

[0074] The preparation method is:

[0075] 1) Weigh 75% of the prescribed amount of distilled water, add the prescribed amount of hypromellose aqueous solution, and stir evenly; continue to add the prescribed amount of polyvinylpyrrolidone K30 and sodium lauryl sulfate, and stir at 50°C for 20 minutes until completely dissolved ;

[0076] 2) Raise the temperature to 65°C, add the prescribed amount of alfacalcidol at a stirring speed of 800rpm, and continue stirring for 30 minutes until it is completely dissolved;

[0077] 3) Add the prescribed amount of sodium metabisulfite and an appropriate amount of mannitol, stir to dissolve; then add 0.1%...

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PUM

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Abstract

The invention relates to an alfacalcidol injection and a preparation method thereof. The injection is prepared from the following ingredients by weight percent: 0.0005 percent of alfacalcidol, 1.2-1.6 percent of polyvinylpyrrolidone K30, 18-24 percent of hydroxypropyl cellulose aqueous solution, 1.2-1.7 percent of sodium dodecyl sulfate, 0.1 percent of an antioxygen, a moderate amount of an isoosmotic adjusting agent, and the balance of water for injection. The content of alfacalcidol in the preparation is remarkably increased; the medicine dose is decreased; the stability of alfacalcidol for light and air is improved; the bioavailability of alfacalcidol is remarkably improved as well.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to an alfacalcidol injection and a preparation method thereof. Background technique [0002] Alfacalcidol (Alfacalcidol), its chemical name is 9,10-opening cholesteryl-5Z,7E,10(19)-triene-1α,3β-diol. It can regulate the balance of calcium and phosphorus in the body, increase the absorption of calcium and phosphorus in the intestine, reduce the level of parathyroid hormone in plasma, and improve women's menopause and osteoporosis caused by hormone drugs. It is suitable for osteoporosis and rickets and osteomalacia caused by various reasons. This product has the functions of promoting the absorption of calcium in the small intestine and regulating the transport of inorganic salts in the bone. In patients with obvious renal insufficiency, especially those who need long-term hemodialysis, the content of endogenous calcitriol is greatly reduced, and even the synthesis is almost stoppe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/593A61K47/38A61K47/32A61K47/20A61P19/10A61P19/08
Inventor 王明刚陈阳生任莉刘晓霞翟翠云金燕玲臧云龙
Owner CP PHARMA QINGDAO CO LTD
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