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

Calcitriol pellet and preparation method thereof

A technology of calcitriol pellets and calcitriol, which is applied in bone diseases, pharmaceutical formulas, medical preparations of non-active ingredients, etc., and can solve problems such as monotonous dosage forms, low bioavailability, and inability to exist stably for a long time , to achieve the effect of improving bioavailability and reducing dosage

Active Publication Date: 2013-06-12
CP PHARMA QINGDAO CO LTD
View PDF5 Cites 5 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 pellets are not reported in the prior art because they cannot exist stably for a long time and their 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 pellet and preparation method thereof
  • Calcitriol pellet and preparation method thereof
  • Calcitriol pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 calcitriol pellets

[0040] The prescription is:

[0041] Calcitriol 1.5mg

[0042] Meglumine 6.0g

[0043] Macrogol 400 3.6g

[0044] Macrogol 6000 45g

[0045] Starch 210g

[0046] Sodium carboxymethyl starch 15g

[0047] Appropriate amount of pregelatinized starch.

[0048] The preparation method is:

[0049] 1) Weigh the raw and auxiliary materials of the prescription amount, pass through 80-mesh sieve respectively;

[0050] 2) Take the sieved pregelatinized starch and add distilled water to make a binder solution;

[0051] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, starch and sodium carboxymethyl starch evenly in equal increments, and add the above binder solution to prepare into soft material;

[0052] 4) Prepare pellets by extrusion spheronization technology, dry at 50°C for 20 minutes, sieve and pack.

Embodiment 2

[0053] Embodiment 2 calcitriol pellets

[0054] The prescription is:

[0055] Calcitriol 1.5mg

[0056] Meglumine 12g

[0057] Macrogol 400 5.4g

[0058] Macrogol 6000 75g

[0059] Lactose 150g

[0060] Low-substituted hydroxypropyl cellulose 30g

[0061] Hydroxypropyl Cellulose Appropriate amount.

[0062] The preparation method is:

[0063] 1) Weigh the raw and auxiliary materials of the prescription amount, and pass through a 120-mesh sieve for later use;

[0064] 2) Take the sieved hydroxypropyl cellulose and add distilled water to make a binder solution;

[0065] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, lactose and low-substituted hydroxypropyl cellulose in equal increments, and add the above binder The solution is made into a soft material;

[0066] 4) Prepare pellets by extrusion spheronization technology, dry at 70°C for 40 minutes, sieve and pack.

Embodiment 3

[0067] Embodiment 3 calcitriol pellets

[0068] The prescription is:

[0069] Calcitriol 1.5mg

[0070] Meglumine 9.0g

[0071] Macrogol 400 4.5g

[0072] Macrogol 6000 60g

[0073] Dextrin 180g

[0074] Microcrystalline Cellulose 24.0g

[0075] Proper amount of povidone.

[0076] The preparation method is:

[0077] 1) Weigh the raw and auxiliary materials of the prescription amount, pass through a 100-mesh sieve for later use;

[0078] 2) Take the sieved povidone and add distilled water to make a binder solution;

[0079] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, dextrin and microcrystalline cellulose evenly in an equal increment method, and add the above binder solution to prepare into soft material;

[0080] 4) Prepare pellets by extrusion spheronization technology, dry at 60°C for 30 minutes, sieve and pack.

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 pellet and a preparation method thereof. The pellet is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 2.0-4.0% of meglumine, 1.2-1.8% of polyethylene glycol 400, 15-25% of polyethylene glycol 6000, 50.0-70.0% of filler, 5.0-10.0% of disintegrant and an appropriate amount of binder. According to the pellet, 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 pellet 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 t...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/593A61K47/34A61K47/18A61P3/02A61P3/14A61P19/10A61P19/08A61P17/06
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