Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Calcitriol injection and preparation method thereof

A technology for calcitriol and injections, which is applied in bone diseases, pharmaceutical formulations, medical preparations with non-active ingredients, etc., and can solve the problems of monotonous dosage forms, calcitriol sensitivity to light and air, soft capsules and gelatin The stability of pills is not good and other problems, and the effect of improving bioavailability is achieved.

Active Publication Date: 2013-06-12
CP PHARMA QINGDAO CO LTD
View PDF4 Cites 9 Cited by
  • 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 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Calcitriol injection and preparation method thereof
  • Calcitriol injection and preparation method thereof
  • Calcitriol injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 calcitriol injection

[0026] The prescription is:

[0027]

[0028] The preparation method is:

[0029] 1) Weigh 70% of the prescribed amount of distilled water, 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;

[0030] 2) Raise the temperature to 60°C, add the prescribed amount of calcitriol at a stirring speed of 500rpm, and continue stirring for 20 minutes until it is completely dissolved;

[0031] 3) Add the prescribed amount of sodium sulfite and appropriate amount of sodium chloride, stir to dissolve; then add 0.1% activated carbon of the total mass of the injection, stir evenly, let it stand, and filter to remove the carbon powder;

[0032] 4) After measuring and adjusting the pH value of the solution, add water for injection to the full amount; filter through 0.45 μm and 0.22 μm micr...

Embodiment 2

[0033] Embodiment 2 calcitriol injection

[0034] The prescription is:

[0035]

[0036] The preparation method is:

[0037] 1) Weigh 80% of the prescribed amount of distilled water, 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 15-25 minutes until completely dissolved;

[0038] 2) Raise the temperature to 70°C, add the prescribed amount of calcitriol at a stirring speed of 1000rpm, and continue stirring for 40 minutes until it is completely dissolved;

[0039] 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 total mass of the injection, stir evenly, let stand, and filter to remove the carbon powder;

[0040] 4) After measuring and adjusting the pH value of the solution, add water for injection to the full amount; filter through 0.45 μm and 0.22 μm microp...

Embodiment 3

[0041] Embodiment 3 calcitriol injection

[0042] The prescription is:

[0043]

[0044]

[0045] The preparation method is:

[0046] 1) Weigh 75% of the prescribed amount of distilled water, 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;

[0047] 2) Raise the temperature to 65°C, add the prescribed amount of calcitriol at a stirring speed of 800rpm, and continue stirring for 30 minutes until it is completely dissolved;

[0048] 3) Add the prescribed amount of sodium metabisulfite and appropriate amount of mannitol, stir to dissolve; then add 0.1% activated carbon of the total mass of the injection, stir evenly, let stand, and filter to remove the carbon powder;

[0049] 4) After measuring and adjusting the pH value of the solution, add water for injection to the full amount; filter through 0.45 μm and 0.22...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a calcitriol injection and a preparation method thereof. The injection is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 1.2-1.6% of meglumine, 18-24% of polyethylene glycol 400, 1.2-1.7% of polyethylene glycol 6000, 0.1% of antioxidant, an appropriate amount of isotonicity regulator and the balance of water for injection. According to the injection, 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 injection 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 ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/08A61K31/593A61K47/34A61K47/26A61P3/02A61P19/10A61P19/08A61P17/06A61K47/10
Inventor 王明刚陈阳生任莉
Owner CP PHARMA QINGDAO CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com