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Peptide slow-release formulations

A technology of pre-formulation and active agent, applied in the field of preparation precursors, can solve the problems of inability to filter sterilization, inability to heat sterilization, difficulty in preparing PLGA microbeads, etc.

Active Publication Date: 2013-12-18
CAMURUS AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] In addition, it is quite difficult to prepare PLGA microbeads using the existing somatostatin analog depot system
In particular, since the beads are granules, they cannot be filter sterilized, and because the PLGA copolymer melts at about 40°C, they cannot be heat sterilized
Therefore, the complex preparation process must all be carried out under highly sterile conditions

Method used

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  • Peptide slow-release formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0191] Availability of Multiple Liquid Crystal Phases in Depot Formulations for Choice of Composition

[0192] Injectable formulations containing various ratios of phosphatidylcholine ("PC" - Epikuron 200) and glyceryl dioleate (GDO) and ethanol as solvent were prepared to illustrate the accessibility of the depot precursor formulation after equilibration with excess water Various liquid crystal phases.

[0193] Weigh an appropriate amount of PC and ethanol in a glass vial, and place the mixture on a shaker until the PC is completely dissolved to form a clear liquid solution. GDO is then added to form an injectable homogeneous solution.

[0194] Each formulation was injected into vials and equilibrated with excess water. Phase properties were evaluated visually and between cross-polarizations at 25 °C. The results are listed in Table 1.

[0195] Table 1

[0196]

[0197] L 2 = reverse micellar phase; I 2 = anti-cubic liquid crystal phase; H II = inverse hexagonal li...

Embodiment 2

[0199] Viscosity in PC / GDO (5:5) or PC / GDO (4:6) with added solvents (ethanol, PG, and NMP)

[0200] A mixture of about 25% ethanol and PC / GDO / EtOH was prepared according to the method in Example 1. Use a rotary evaporator (vacuum, 1 hour at 40°C, then 2 hours at 50°C) to remove all or almost all of the ethanol in the mixture, weigh the resulting mixture in a glass vial, and then add 1, 3, 5, 10 Or 20% solvent (ethanol, propylene glycol (PG) or n-methylpyrrolidone (NMP)). The samples were allowed to equilibrate for several days, then the viscosity was measured with a CarriMed CSL 100 viscometer equipped with automatic notch setting.

[0201] This example clearly illustrates the need for solvents for some depot formulation precursors in order to obtain injectable formulations (see figure 1 ). The viscosity of solvent-free PC / GDO mixtures increases with increasing PC ratio. Systems with low PC / GDO ratios (more GDO) with low concentrations of solvent are injectable.

Embodiment 3

[0202] Example 3: Preparation of depot compositions containing the peptide octreotide

[0203] Octreotide acetate (24 mg or 60 mg) was dissolved in 0.1 g of ethanol. 0.36 g of PC and 0.54 g of GDO were sequentially dissolved in this solution to obtain a depot preparation precursor. The formulation precursor was injected into excess aqueous phase (syringe 23G, 0.6mm x 30mm) to obtain bulk liquid crystalline phase (I 2 structure). That is, octreotide (2.4% or 6.0%) did not change the overall composition and phase properties after exposure to an aqueous environment.

[0204] The octreotide depot precursor formulation in this example was tested for stability to crystallization during storage. Each formulation was stable for at least two weeks at 4-8°C.

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Abstract

A composition for the delayed delivery of a peptide active agent comprising; i) a salt of said peptide active agent comprising at least one positively charged peptide ion and at least one negatively charged counter-ion ii) a sustained-release delivery vehicle. Wherein said at least one negatively charged counter-ion is a halide ion, preferably a chloride or bromide ion.

Description

technical field [0001] The present invention relates to formulation precursors (preformulations) for the in situ generation of compositions of salts of controlled release peptide active agents, especially somatostatin analogues. In particular, the invention relates to a preformulation of at least one salt of an amphiphilic component and a peptide active agent (eg a somatostatin analogue) for parenteral administration. technical background [0002] Many bioactive agents including drugs, nutrients, vitamins, etc. have a "window of function". That is to say there is a concentration range within which these substances are observed to provide certain biological effects. When the concentration in a suitable part of the body (eg locally or eg serum concentration) falls below a certain level, the substance no longer produces a beneficial effect. Similarly, there is generally an upper concentration level above which increasing the concentration yields no further benefit. In some c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K9/00A61K38/00A61K47/10A61K47/14A61K47/24
CPCA61K9/0019A61K38/31A61K47/14A61K47/24A61K9/08A61K47/10A61P1/12A61P1/18A61P27/02A61P35/00A61P3/04A61P5/06A61P5/48A61P9/14A61K47/08A61K47/34
Inventor 马库斯·约翰松弗雷德里克·约阿布松卡塔林·尼斯托尔克里斯特·图勒松弗雷德里克·蒂贝里
Owner CAMURUS AB
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