Compositions and formulations for the treatment of thyroid eye disease

A pharmaceutical preparation, technology of use, applied in the field of compositions and preparations for the treatment of thyroid eye disease, capable of solving problems such as loss of vision and diplopia

Inactive Publication Date: 2014-08-06
尼奥特蒂克斯公司
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While some GO patients suffer only mild eye discomfort, 3-5% suffer from severe pain and inflammation with diplopia and even vision loss

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
  • Compositions and formulations for the treatment of thyroid eye disease
  • Compositions and formulations for the treatment of thyroid eye disease
  • Compositions and formulations for the treatment of thyroid eye disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Example 1: In vitro lipolysis experiment of rat adipocytes with β agonists and glucocorticoids

[0111] Glycerol was detected spectrophotometrically in cell culture media following chemical oxidation with hydrogen peroxide in bulk in vitro lipolysis experiments. Glycerol was assayed within 3 hours. Lipolysis levels were measured in cultured human adipocytes following one or more pre-incubation periods of exposure to beta agonists alone, glucocorticosteroids alone, or a combination of both, see below for more details . Preadipocytes are isolated and differentiated into adipocytes:

[0112] Human subcutaneous adipocytes were used in lipolysis experiments. Adipose tissue was collected by liposuction or lipectomy and preadipocytes were isolated as follows. Briefly, adipose tissue was minced and placed in a shaking chamber enriched with oxygen (5% CO 2 ; 75 times / min), incubate at 37°C for 1 hour in Krebs-Ringer bicarbonate buffer containing 1% bovine serum albumin an...

Embodiment 2

[0120] Example 2: Inhibition of lipogenesis by beta agonists and glucocorticoids

[0121] Non-limiting examples of such adipogenesis inhibition are as follows: Cell culture: 3T3-L1 preadipocyte cell line (ATCC, Manassas, VA) was divided into 4×10 5 Cells / T75ml flasks were inoculated into Dulbecco's Modified Eagle Medium (DMEM) containing 10% normal bovine serum and 1% penicillin / streptomycin antibiotics. Cells were incubated at 37°C, 5% CO 2 incubate. After 3 days, the cells were detached with trypsin, counted, and resuspended in a medium containing 6 × 10 5 Cells / well in 2 ml of medium in a 24-well plate. After 1-2 days, the cells are close to confluence and ready to initiate adipogenesis. Lipogenetic material: lipogenesis priming medium : DMEM / 10% fetal bovine serum / 0.5mM IBMX / 1μM dexamethasone adipogenesis medium : DMEM / 10% fetal bovine serum / 10μg / ml insulin lipogenesis maintenance medium : DMEM / 10% fetal bovine serum Negative Control Medium : DMEM / 10% normal ...

Embodiment 3

[0122] Example 3: Beta-2 Agonist Combination with Glucocorticosteroids Reduces Epididymal Fat Pad Mass

[0123] We sought to determine whether glucocorticosteroids reduce fat in vivo in a manner consistent with the in vitro lipolysis data described in Example 1. To this end, we measured epididymal fat pad mass in rats treated with the long-acting β-2 adrenergic agonist formoterol alone and in combination with budesonide.

[0124] Male Sprague Dawley rats (-500 g) were anesthetized in 4% isoflurane using a Matrx 3000 vaporizer. Then, inject 0.4 ml of vehicle (2% PEG) at the front 5 mm of the rear end of the fat pad to the animals listed in Table 2 below; formoterol in vehicle (3.48 μg / ml; dose=1.39 μg); or Formoterol (3.48 μg / ml) plus budesonide (10 μg / ml; dose = 1.39 μg formoterol, 4 μg budesonide). Each animal received drug treatment on one side and vehicle (2% PEG) on the opposite side; groups were balanced for drug and vehicle (see Table 2).

[0125] Injections 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
diameteraaaaaaaaaa
diameteraaaaaaaaaa
diameteraaaaaaaaaa
Login to view more

Abstract

Compositions, formulations, methods, and systems for treating regional fat deposits and fat-related conditions, dermal conditions, and muscular conditions. Methods comprise administering a composition comprising at least one compound that reduces desensitization of beta adrenergic receptors, for example a glucocorticosteroid, and / or at least one long-acting beta-2 adrenergic receptor agonist, for example, formoterol. Compositions to be administered include sustained release formulations comprising at least one long-acting beta-2 adrenergic receptor agonist, at least one compound that reduces desensitization of beta adrenergic receptors, or both in a sustained crystalline microparticle form.

Description

[0001] cross reference [0002] This application claims the benefit of U.S. Provisional Patent Application Serial Nos. 60 / 852,221, filed October 17, 2006, 60 / 898,009, filed January 29, 2007, and 60 / 919,011, filed April 13, 2007, which Incorporated herein by reference in its entirety. Background of the invention [0003] Graves' disease is a common disease with an incidence rate of 1 / 1000 women per year. In addition to hyperthyroidism, 25-50% of individuals with Graves' disease progress to clinically involving the eye, ie, thyroid eye disease. Graves' Ophthalmopathy (GO) is a typical form of thyroid eye disease. While some GO patients suffer only mild ocular discomfort, 3-5% suffer from severe pain and inflammation with diplopia and even vision loss. [0004] The clinical symptoms and signs of GO can be explained mechanistically as a marked increase in tissue volume within the bony orbit. Enlargement of the orbital tissue causes the globe to move forward, and outflow from 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 Patents(China)
IPC IPC(8): A61K31/135A61K31/167A61K31/575A61P3/04
Inventor J·D·多巴克
Owner 尼奥特蒂克斯公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap