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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
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  • 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 levels throughout the release, such as high peak levels and close to zero plasma levels

Method used

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  • 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.

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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

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Application Information

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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
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