Check patentability & draft patents in minutes with Patsnap Eureka AI!

Injectable, nonaqueous suspension with high concentration of therapeutic agent

Inactive Publication Date: 2009-01-22
DURECT CORP
View PDF10 Cites 37 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, formulation and delivery of these molecules are challenging due to solubility and viscosity limitations.
Commercialization strategies often involve lyophilized formulations that require reconstitution of the protein prior to being delivered by injection, which can add costs and time to the manufacturing process.
However, the requirement for a high concentration of the protein adds complexity to formulation design and promotes instability.
Typically, such volumes are administered only through intravenous (“IV”) infusion performed in a clinical or hospital setting, which leads to poor patient compliance.
However, achieving such highly concentrated mAb solutions is problematic due to solubility limitations and / or relatively high viscosities, which often results in protein aggregation and poor overall stability.

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
  • Injectable, nonaqueous suspension with high concentration of therapeutic agent
  • Injectable, nonaqueous suspension with high concentration of therapeutic agent
  • Injectable, nonaqueous suspension with high concentration of therapeutic agent

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Lysozyme Particles

[0035]A lysozyme solution was prepared by dissolving lysozyme (available from Sigma-Aldrich Corp. (St. Louis, Mo.)) in 6.5 mM sodium phosphate buffer, pH 6.0, at a protein concentration of 65 mg / mL. Sucrose and Tween 80 (or polysorbate 80) were optionally added to the lysozyme solution with the concentration of sucrose and Tween 80 in the final solution of 0%-5.5% and 0%-0.0065% weight / volume, respectively. The lysozyme solution was lyophilized according to the conditions shown in Table 1.

TABLE 1Lyophilization Conditions for the Preparation of Lysozyme Particles.HoldChamber PressureTimeProcess StepShelf Temperature(° C.)(mBar)(hours)Loading +5N / A2Freezing−50 (rate 0.50° C.)N / A2Freezing−50N / A2.5Vacuum on−50120 mT0.5Vacuum−50120 mT0.5hold1° Drying−10 (rate 1° C. / minute)120 mT0.751° Drying−10120 mT242° Drying   0 (rate 0.1° C. / minute) 80 mT1.72° Drying   0 80 mT22° Drying+35 (rate 0.25° C. /  80 mT2.3minute)2° Drying+35 80 mT102° Drying+20 (rate 1° C. / min...

example 2

Preparation of BSA Particles

[0037]BSA particles were produced according to the methods described in Example 1, except that BSA was used in place of lysozyme.

example 3

Preparation of CNTO 1275 Particles

[0038]Particles of a mAb were produced by dissolving CNTO 1275 in 6.5 mM sodium phosphate buffer with sucrose (concentration of 5.5% w / v), pH 6.0, with a protein concentration of 65 mg / mL. To the solution of CNTO 1275 was added 0.0065% w / v of Tween 80 (or polysorbate 80). The solution was lyophilized according to the conditions shown in Table 2.

TABLE 2Lyophilization Conditions for Preparation of CNTO 1275 Particles.HoldChamber PressureTimeProcess StepShelf Temperature(° C.)(mBar)(hours)Loading +5N / A2Freezing−50 (rate 0.50° C.)N / A2Freezing−50N / A2.5Vacuum on−50120 mT0.5Vacuum−50120 mT0.5hold1° Drying−10 (rate 1° C. / minute)120 mT0.751° Drying−10120 mT242° Drying   0 (rate 0.1° C. / minute) 80 mT1.72° Drying   0 80 mT22° Drying+35 (rate 0.25° C. /  80 mT2.3minute)2° Drying+35 80 mT102° Drying+20 (rate 1° C. / minute) 80 mT0.252° Drying+20 80 mT2Minimum Total time =50.5hours

[0039]CNTO 1275 particles having a particle size of less than approximately 125 μm were...

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
Percent by massaaaaaaaaaa
Percent by massaaaaaaaaaa
Forceaaaaaaaaaa
Login to View More

Abstract

An injectable, nonaqueous suspension including at least one therapeutic agent suspended in a single component vehicle. The single component vehicle is a single amphiphilic material, such as a polyethoxylated castor oil or derivative thereof, a polyoxyethylene alkyl ether, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene stearate, a block copolymer of polyethylene oxide-polypropylene oxide-polyethylene oxide, a block copolymer of polypropylene oxide-polyethylene oxide-polypropylene oxide, a tetra-functional block copolymer of polyethylene oxide-polypropylene oxide, or a tetra-functional block copolymer of polypropylene oxide-polyethylene oxide. A dosage kit that includes the injectable, nonaqueous suspension and a method of administering the injectable, nonaqueous suspension are also disclosed.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This application is a utility conversion and claims the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Patent Application No. 60 / 897,643 filed Jan. 26, 2007, entitled “INJECTABLE, NONAQUEOUS SUSPENSION WITH HIGH CONCENTRATION OF THERAPEUTIC AGENT.”TECHNICAL FIELD[0002]The present invention relates to an injectable suspension that includes a therapeutic agent. More specifically, the present invention relates to an injectable, nonaqueous suspension that includes the therapeutic agent suspended in a single component vehicle.BACKGROUND[0003]Proteins and peptides have become powerful therapeutic agents in the treatment of various diseases, such as cancer, inflammatory, cardiovascular, respiratory, and infectious diseases. However, formulation and delivery of these molecules are challenging due to solubility and viscosity limitations. Except for highly potent molecules, formulations of these molecules need to contain relatively high concen...

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): A61K39/395A61P35/00
CPCA61K9/0019C12Y302/01017A61K9/10A61K9/19A61K38/47A61K47/10A61K47/14A61K47/26A61K47/34A61K47/44C07K16/244A61K2039/505A61K39/3955A61K38/385C07K2317/94C07K2317/21A61K9/08A61P35/00C07K2317/31
Inventor HOUSTON, PAUL R.CHEN, GUOHUALUK, ANDREW SHEUNG-KING
Owner DURECT CORP
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com