Unlock instant, AI-driven research and patent intelligence for your innovation.

Potassium ion binding polymers for pharmaceutical compositions

A kind of technology of acrylic polymer, copolymer

Inactive Publication Date: 2011-07-27
RELYPSA INC
View PDF17 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although generally safe from a toxicological point of view, the inconvenience of high doses and the use of resins in large quantities (for example, Renagel doses can reach up to 15 g / d, while sodium-bound resins require significantly higher doses) require further investigation. Improve resin binding capacity

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
  • Potassium ion binding polymers for pharmaceutical compositions
  • Potassium ion binding polymers for pharmaceutical compositions
  • Potassium ion binding polymers for pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0151] Synthesis of Core-Shell Crosslinked Polyallylamine Particles

[0152] In this process, spherical particles are formed by the reverse suspension method, in which the prepolymer (polyallylamine) is crosslinked with epichlorohydrin. Block copolymers can be used to increase the mechanical stability of the droplets during the crosslinking reaction and can provide an outer shell membrane that is chemically immobilized on the core particle.

[0153] General method for synthesizing block copolymers

[0154] Block copolymers are prepared by the RAFT living radical polymerization method. Use dithiocarbazide compound as reversible chain transfer agent (CTA) and diazonitrile radical initiator (AMVN) in the reaction, represent respectively as follows:

[0155]

[0156] Synthesis of the first block of poly(n-butyl acrylate-co-tert-butyl acrylate)

[0157] n-Butyl acrylate (25 g, 195 mmol) and tert-butyl acrylate (25 g, 195 mmol) were mixed with CTA (173:1 monomer:CTA, 616 mg, 2...

Embodiment 2

[0206] Synthesis of 1,3 Diaminopropane / Epichlorohydrin Crosslinked Particles (Denoted as: Particle-Pi-4-s)

[0207] The reactor used was a 3 L volume baffled three neck round bottom flask equipped with oil bath heating, a water cooled reflux condenser and a mechanical stirrer with a 3 inch propeller. First, a solution of 1,3-diaminopropane (90.2g, 1.21mole) dissolved in 90.2g of water, a surfactant (6.4g of branched chain sodium dodecylbenzenesulfonate dissolved in 100g of water) and 1kg of toluene were added to the in this reactor. The initial batch was stirred at 600 rpm for 2 minutes and then at 300 rpm for 10 minutes before the addition of epichlorohydrin. During the remainder of the test, the same stirring speed was maintained throughout. The reaction solution was heated to 80°C and maintained at this temperature throughout the test period.

[0208] In another container, a solution of 40% by mass of epichlorohydrin in toluene was prepared. 1.2 equivalents of epichlo...

Embodiment 3

[0214] Preparation of Ethylcellulose Shell / 1,3-Diaminopropane Epichlorohydrin Crosslinked Core Particles prepare

[0215] The granules obtained in Example 2 were spray coated with a shell of ethylcellulose polymer using a Wurster fluid bed coater 2""-4"" / 6"" portable unit. The fluidized bed unit was run using a 30% by weight solids aqueous emulsion ( ECD, FMC Corporation), deposited on the core particles to form a coating with an average thickness of 5 microns.

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

PropertyMeasurementUnit
The average diameteraaaaaaaaaa
The average diameteraaaaaaaaaa
The average diameteraaaaaaaaaa
Login to View More

Abstract

The invention provides pharmaceutical compositions comprising potassium binding polymers. The potassium binding polymer is a crosslinked cation exchange polymer, and comprises a cationic counter-ion to potassium and acid groups, wherein the acid groups are selected from carboxylic groups and phosphonic groups. The fraction of ionization of the acid groups is greater than about 75% at the physiological pH in the colon. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and / or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and / or the use of hyperkalemia causing drugs.

Description

[0001] This application is a divisional application of the invention patent application (application date March 30, 2005) with application number 200580010529.0. [0002] cross reference [0003] This application is a continuation-in-part of US Application Serial No. 10 / 965,274, filed October 13,2004. This application is a continuation-in-part of: U.S. Application Serial No. 10 / 814,527, filed March 30, 2004; U.S. Application Serial No. 10 / 814,749, filed March 30, 2004; and U.S. Application Serial No. 10 / 813,872, filed March 30, 2004. These applications are incorporated by reference in their entirety. Background technique [0004] Selective ion absorbers have been used to correct electrolyte balance disturbances in human diseases such as hyperphosphatemia, hyperoxaluria, hypercalcemia, and hyperkalemia. Hyperphosphatemia occurs in patients with renal failure, whose kidneys cannot excrete enough phosphate ions to offset the intake of exogenous phosphate in the diet. This r...

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): A61K9/16A61K31/78A61P1/16A61P3/00A61P3/12A61P3/14A61P5/16A61P9/04A61P9/12A61P13/12A61K9/14A61K9/32A61K9/50A61K31/74A61K45/06A61K47/30
CPCA61K45/06A61K9/5031A61K31/74A61K9/5026A61K47/32A61K9/1635A61K31/78A61K31/785A61K31/795A61K31/80A61P1/16A61P13/12A61P3/00A61P3/12A61P3/14A61P39/02A61P39/04A61P43/00A61P5/16A61P7/00A61P7/08A61P9/00A61P9/04A61P9/10A61P9/12A61K47/52A61K9/2027A61K9/2031A61K47/34A61K9/2846A61K9/14A61K47/50A61K9/28C08F120/06C08F128/02
Inventor 多米尼克·沙尔莫约翰·福德特兰张汉廷埃里克·康纳刘明军格里特·克莱纳
Owner RELYPSA INC