Sustained release formulation comprising octreotide and two or more polylactide-co-glycolide polymers

A technology of octreotide and glycolide, which is applied in the field of sustained-release preparations, can solve problems such as fluctuations in plasma levels, and achieve the effect of reducing fluctuations

Pending Publication Date: 2013-08-21
NOVARTIS AG
View PDF3 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A common disadvantage of using injectable depot formulations is fluctuations in plasma

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
  • Sustained release formulation comprising octreotide and two or more polylactide-co-glycolide polymers
  • Sustained release formulation comprising octreotide and two or more polylactide-co-glycolide polymers
  • Sustained release formulation comprising octreotide and two or more polylactide-co-glycolide polymers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1: Preparation of microparticles

[0059] An appropriate amount of PLGA polymer was dissolved in an appropriate amount of methylene chloride to yield an appropriate polymer concentration as specified in Table 2 in the "PLGA Concentration" column. An appropriate amount of drug is weighed, placed in a glass beaker, and the polymer solution is poured over the drug so that the resulting microparticles have a drug loading as specified in the "Drug Loading" column.

[0060] For example for microparticles with a drug loading of 20% and a polymer concentration of 20%, the quantities are as follows: 3.547g of PLGA polymer was dissolved in 17.7ml of dichloromethane, resulting in a 20% (w / v) polymer solution. Weigh 1.453g of octreotide pamoate (equivalent to 1.00g=20% octreotide free base), place it in a glass beaker, and pour the polymer solution on the drug.

[0061] The suspension was homogenized with an Ultra-Turrax rotor-stator stirrer at 20'000 rpm for 1 minute wh...

Embodiment 2

[0087] Example 2: Carrier Compositions A to G

[0088] Under vigorous stirring with a magnetic stirrer, CMC-Na, Mannitol and Pluronic F68 in the amounts as given in Table 3 were dissolved in about 15 ml of hot deionized water at a temperature of about 90°C. The resulting clear solution was cooled to 20 °C and made up to 20.0 ml with deionized water.

[0089] Table 3: Carriers suitable for microparticles (amounts given in g)

[0090]

Embodiment 3

[0091] Example 3: Microparticle Suspension

[0092] 170 mg of the microparticles of Examples 1-33 were suspended in 1.0 ml of vehicle of composition D (Table 3) in a 6R vial. The suspension was homogenized by hand shaking for about 30 seconds. The reconstituted suspension could be injected without any problem using a 20 gauge needle.

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
Intrinsic viscosityaaaaaaaaaa
Diameteraaaaaaaaaa
Login to view more

Abstract

The invention relates to a sustained release formulation comprising octreotide and two or more polylactide-co-glycolide polymers. In other words, the present invention relates to sustained release formulations comprising as active ingredient octreotide or a pharmaceutically-acceptable salt thereof and two or more different polylactide-co-glycolide polymers (PLGAs).

Description

[0001] related application [0002] This application is a PCT application filed on December 20, 2006 with the title of "Sustained-release formulation comprising octreotide and two or more polylactide-co-glycolide polymers" [0003] A divisional application of PCT / EP2006 / 012313, the date of entry of the PCT application into the Chinese national phase is June 23, 2008, and the application number is 200680048796.1. technical field [0004] The present invention relates to the field of pharmacy. In particular, the present invention relates to sustained release formulations comprising, as active ingredients, octreotide or a pharmaceutically acceptable salt thereof and two or more different polylactide-co-glycolide polymers (PLGA). [0005] These pharmaceutical compositions of the present invention are intended for the long-term maintenance treatment especially of acromegaly patients and the treatment of severe diarrhea and flushing associated with malignant carcinoid tumors and va...

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): A61K38/08A61K9/16A61K47/34A61P35/00A61P1/12A61P5/08
CPCA61K38/31A61K9/1647A61K9/0019A61K9/10A61K38/08A61K38/12A61P1/00A61P1/12A61P17/00A61P35/00A61P43/00A61P5/00A61P5/02A61P5/08A61K47/50A61K9/20A61K9/14A61K9/50A61K9/5015A61K9/5089A61K47/34A61K47/32
Inventor H·彼得森M·阿尔海姆
Owner NOVARTIS AG
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