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

Stable and efficient dephosphorization composition

A composition and high-efficiency technology, applied in the direction of drug combination, active ingredients of anhydride/acid/halide, metabolic diseases, etc., can solve the problems of limitation, phosphorus reduction ability, pH environment change, etc., and achieve reduced dosage and comprehensive utilization efficiency High, less involved effect

Inactive Publication Date: 2013-06-05
尹颖
View PDF2 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, lanthanum carbonate is an extremely water-insoluble inorganic salt, and its solubility in water is only 2.38×10 -7 mol / L, therefore, after oral administration, such as commercially available lanthanum carbonate chewable tablets (trade name: Fosrenol), it is difficult to quickly disperse in the gastrointestinal tract, and further dissociate the trivalent lanthanum ion that exerts the effect of reducing phosphorus , and its phosphorus-lowering ability is also susceptible to changes in the pH environment in the body. Therefore, it is undoubtedly that the inherent physical and chemical properties of lanthanum carbonate limit the effective phosphorus-binding ability of trivalent lanthanum ions. It is a fact that people are extremely reluctant to see in clinical applications
[0007] In summary, for hyperphosphatemia, the development and application of new phosphorus binders is undoubtedly an effective means. The ideal phosphorus binder should have high affinity for phosphorus, stable and rapid phosphorus binding ability, less systemic absorption, no Toxic and side effects, can be used for a long time, easy to accept, and low in price, but unfortunately, there is no phosphorus binder that meets the conditions of an ideal phosphorus binder

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
  • Stable and efficient dephosphorization composition
  • Stable and efficient dephosphorization composition
  • Stable and efficient dephosphorization composition

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0051] The present embodiment illustrates the preparation method of lanthanum lactate trihydrate of the present invention, and concrete steps are as follows:

[0052] a) Weigh 1.0 kg of lanthanum carbonate and fully pulverize it through an 80-mesh sieve, and evenly disperse it in an appropriate amount of water at 65-70°C;

[0053] b) Add 0.9kg of lactic acid to the above a), mix evenly under stirring conditions, and react completely under airtight conditions at 65-70°C;

[0054] c) Evaporate and dry the above obtained solution at 75-80°C to constant weight, dissolve it in 10.0L of water and filter, take the filtrate and evaporate and dry it to constant weight at 75-85°C to obtain crude lanthanum lactate;

[0055] d) The crude lanthanum lactate obtained above was washed with 5.0 L of water, concentrated, air-dried and pulverized, and then vacuum-dried at 90-100°C for 7.5 hours to obtain lanthanum lactate trihydrate, weighing 1.72 kg;

preparation Embodiment 2

[0057] This embodiment illustrates the preparation method of lanthanum lactate hydrate containing different crystal water structures according to the present invention, and the specific steps are as follows:

[0058] a) Weigh 1.2kg of lanthanum carbonate and fully pulverize it through an 80-mesh sieve, and evenly disperse it in an appropriate amount of water at 65-70°C;

[0059] b) Add 1.3kg of lactic acid to the above a), mix evenly under stirring conditions, and react completely under airtight conditions at 65-70°C;

[0060] c) Evaporate and dry the above obtained solution at 75-80°C to constant weight, dissolve it with 12.0L of water and filter, take the filtrate and evaporate and dry it at 75-85°C to constant weight to obtain crude lanthanum lactate;

[0061] d) The crude lanthanum lactate obtained above was washed with 10.0 L of water, concentrated, blast-dried, pulverized, and then vacuum-dried at 100-110°C for 5.5 hours to obtain lanthanum lactate tetrahydrate, weighing...

preparation Embodiment 3

[0067] The preparation of the stable and high-efficiency phosphorus-reducing composition tablet of the present invention:

[0068] Prescription composition:

[0069]

[0070] Preparation process: 1) After pulverizing an appropriate amount of lanthanum lactate hydrate, microcrystalline cellulose, lactose, crospovidone, and sodium carboxymethyl starch through an 80-mesh sieve, weigh the recipe quantity for later use; 2) Prepare 3.0% hydroxy The propyl methylcellulose solution is ready for use; 3) Put the weighed components in 1) into the mixer and mix them evenly; 4) Add the prescription amount 2) to the mixture to make soft materials, and granulate them with a high-efficiency wet granulator , dried below 60°C; 5) pass the dried granules through a 16-mesh sieve for granulation, add magnesium stearate, mix well, and then compress on a tablet machine to obtain the product.

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 provides a stable and efficient composition for dephosphorization. The composition comprises lanthanum lactate hydrate and pharmaceutically acceptable proper auxiliary materials, wherein the average value of crystalline water in the lanthanum lactate hydrate is 0.5-6.0. The composition is applied in the form of oral administration, and the clinical daily dosage on the basis of anhydrous lanthanum lactate is 0.05-2.0g. The composition provided by the invention is free of aluminum and calcium, thereby avoiding the side effect of aluminosis, angiosteosis or the like of the patient due to taking of aluminum and calcium. The active component of the composition exists in the form of lanthanum lactate hydrate, so the solubility is high, and thus, the consistent high-level phosphorus combining capacity in vivo and in vitro can be always kept without being dependent on pH. The composition solves the problems of high consumption, high cost, poor mouthfeel and severe adverse reactions, including nausea, emesis and the like, in other lanthanum-containing dephosphorization medicines. The invention also provides a method for preparing the lanthanum lactate hydrate in the composition.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a stable and efficient phosphorus-reducing composition, belonging to the technical field of medicine. Background technique [0002] Hyperphosphatemia is a disease in which blood phosphate levels exceed normal levels (normal blood phosphorus levels are about 37.2-43.4mg / L), also known as hyperphosphatemia. Hyperphosphatemia can be caused by increased phosphate intake, decreased excretion, or disturbance in redistribution: ①Increased intake, such as excessive oral or intravenous phosphate; ②Reduced excretion, such as in patients with renal failure, glomerular filtration 3) Phosphate redistribution disorder, when acidosis, tissue destruction or massive hemolysis, phosphate redistribution occurs disorder. [0003] Clinically, hyperphosphatemia can cause hyperparathyroidism and osteodystrophy and other phenomena that seriously endanger people's health. It should be pointed out that hy...

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): A61K31/19A61P3/12
Inventor 尹颖
Owner 尹颖
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