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Alfacalcidol solution and preparation method thereof

An alfacalcidol and solution technology, which is used in bone diseases, pharmaceutical formulations, medical preparations with inactive ingredients, etc. The effect of dose and bioavailability improvement

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 solution 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

[0035] Embodiment 1 Alfacalcidol solution

[0036] The prescription is:

[0037] Alfacalcidol 0.5mg

[0038] Polyvinylpyrrolidone K30 0.9g

[0039] Hypromellose aqueous solution 27g

[0040] Sodium Lauryl Sulfate 12g

[0041] Sodium sulfite 0.2g

[0042] Aspartame 0.5g

[0043] Distilled water up to 100g

[0044] The preparation method is:

[0045] 1) Weigh 80% 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 55°C for 25 minutes to complete dissolve;

[0046] 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;

[0047] 3) Add distilled water to the full amount, add the prescribed amount of sodium sulfite and aspartame, stir to dissolve; test at room temperature, after...

Embodiment 2

[0048] Embodiment 2 Alfacalcidol solution

[0049] The prescription is:

[0050] Alfacalcidol 0.5mg

[0051] Polyvinylpyrrolidone K30 1.2g

[0052] Hypromellose aqueous solution 30g

[0053] Sodium Lauryl Sulfate 14g

[0054] Sodium bisulfite 0.2g

[0055] Sucrose 0.5g

[0056] Distilled water up to 100g

[0057] The preparation method is:

[0058] 1) Weigh 70% 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 45°C for 15 minutes to complete dissolve;

[0059] 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;

[0060] 3) Add distilled water to the full amount, add the prescribed amount of sodium bisulfite and sucrose, stir to dissolve; test at room temperature, after pas...

Embodiment 3

[0061] Embodiment 3 Alfacalcidol solution

[0062] The prescription is:

[0063] Alfacalcidol 0.5mg

[0064] Polyvinylpyrrolidone K30 1.1g

[0065] Hypromellose aqueous solution 28g

[0066] Sodium Lauryl Sulfate 13g

[0067] Sodium metabisulfite 0.2g

[0068] Stevioside 0.5g

[0069] Distilled water up to 100g

[0070] The preparation method is:

[0071] 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 to complete dissolve;

[0072] 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;

[0073] 3) Add distilled water to the full amount, add the prescribed amount of sodium metabisulfite and stevioside, stir to dissolve; test at room temper...

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PUM

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Abstract

The invention relates to an alfacalcidol solution and a preparation method thereof. The solution is prepared from the following ingredients by weight percent: 0.0005 percent of alfacalcidol, 0.9-1.2 percent of polyvinylpyrrolidone K30, 27-30 percent of hydroxypropyl methylcellulose water solution, 12-14 percent of lauryl sodium sulfate, 0.2 percent of an antioxygen, 0.5 percent of a corrigent, and the balance of distilled water. Compared with the prior art, the content of alfacalcidol in the solution is remarkably increased; the medicine dose is reduced; 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 solution 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 stopped...

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孙桂玉王清亭汪泓
Owner CP PHARMA QINGDAO CO LTD
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