Calcitriol emulsion and preparation method thereof

A technology of calcitriol emulsion and emulsifier, which is applied in bone diseases, pharmaceutical formulations, emulsion delivery, etc. It can solve problems such as monotonous dosage forms, low content of active ingredients, poor stability of soft capsules and capsules, etc. To achieve the effect of increasing bioavailability

Active Publication Date: 2013-06-12
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 calcitriol are soft capsules and capsules; the dosage form is relatively monotonous, and calcitriol is sensitive to light and air, and has low solubility in common organic solvents. The stability of soft capsules and capsules Not good, extremely low content of active ingredients, low bioavailability
Calcitriol emulsion has not been 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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  • Calcitriol emulsion and preparation method thereof
  • Calcitriol emulsion and preparation method thereof
  • Calcitriol emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1 calcitriol emulsion

[0025] The prescription is:

[0026]

[0027] The preparation method is:

[0028] 1) Take the prescribed amount of castor oil, add the prescribed amount of calcitriol, gum arabic and methylcellulose, and stir evenly at 500rpm to obtain the oil phase;

[0029] 2) Take the prescribed amount of water for injection, add the prescribed amount of polyethylene glycol 400, and stir evenly; continue to add the prescribed amount of meglumine and polyethylene glycol 6000, and stir at 45°C for 15 minutes until completely dissolved to obtain a solution;

[0030] 3) Slowly add the above oil phase into the obtained solution along the same direction at a stirring speed of 500 rpm, emulsify twice in a high-pressure homogenizer, filter and fill, and sterilize at 115°C for 30 minutes to obtain the product.

Embodiment 2

[0031] Embodiment 2 calcitriol emulsion

[0032] The prescription is:

[0033]

[0034] The preparation method is:

[0035] 1) Take the prescribed amount of peanut oil, add the prescribed amount of calcitriol, tragacanth gum and hydroxypropyl cellulose, and stir evenly at 1000 rpm to obtain the oil phase;

[0036] 2) Take the prescribed amount of water for injection, add the prescribed amount of polyethylene glycol 400, and stir evenly; continue to add the prescribed amount of meglumine and polyethylene glycol 6000, and stir at 55°C for 25 minutes until completely dissolved to obtain a solution;

[0037] 3) Slowly add the above oil phase into the obtained solution along the same direction at a stirring speed of 1000 rpm, emulsify 4 times in a high-pressure homogenizer, filter and fill, and sterilize at 115°C for 30 minutes to obtain the product.

Embodiment 3

[0038] Embodiment 3 calcitriol emulsion

[0039] The prescription is:

[0040]

[0041]

[0042] The preparation method is:

[0043] 1) Take the prescribed amount of corn oil, add the prescribed amount of calcitriol, poloxamer and sodium alginate, and stir evenly at 800 rpm to obtain the oil phase;

[0044] 2) Take the prescribed amount of water for injection, add the prescribed amount of polyethylene glycol 400, and stir evenly; continue to add the prescribed amount of meglumine and polyethylene glycol 6000, and stir at 50°C for 20 minutes until completely dissolved to obtain a solution;

[0045] 3) Slowly add the above oil phase into the obtained solution along the same direction at a stirring speed of 800 rpm, emulsify in a high-pressure homogenizer for 3 times, filter and fill, and sterilize at 115°C for 30 minutes to obtain the product.

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Abstract

The invention relates to a calcitriol emulsion and a preparation method thereof. The emulsion is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 0.7-1.2% of meglumine, 12-18% of polyethylene glycol 400, 1.5-2.5% of polyethylene glycol 6000, 0.5-30% of vegetable oil, 4.0% of emulsifying agent, 1.0% of coemulsifier and the balance of water for injection. According to the emulsion, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a calcitriol emulsion and a preparation method thereof. Background technique [0002] Calcitriol is a white crystalline powder that is sensitive to light and air. Slightly soluble in methanol, ethanol, ethyl acetate. Tm is 111-115°C. It is one of the most important metabolic active products of vitamin D3 in the human body. It can promote the absorption of calcium in the small intestine and regulate the transport of inorganic salts in the bone. It is mainly used for osteoporosis and renal osteodystrophy in patients with chronic renal failure. , especially in patients requiring long-term hemodialysis; postoperative spontaneous and pseudohypoparathyroidism; vitamin D3-dependent rickets and hypophosphatemic vitamin D-resistant rickets; skin diseases such as psoriasis; and other vitamins D deficiency. Oral absorption of calcitriol is fast, peaking in 3 to 6 hours, t1 / 2 is about 3...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/593A61K47/34A61K47/26A61P3/02A61P19/10A61P19/08A61P17/06
Inventor 王明刚陈阳生任莉
Owner CP PHARMA QINGDAO CO LTD
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