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Pharmaceutical compositions comprising levodopa, a dopamine decarboxylase inhibitor and a COMT inhibitor and a method of administration thereof

A technology of dopamine decarboxylase and levodopa, applied in drug combination, drug delivery, pharmaceutical formulation, etc.

Inactive Publication Date: 2017-08-18
LOBSOR PHARM AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Administration of dopamine is ineffective since dopamine cannot cross the blood-brain barrier

Method used

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  • Pharmaceutical compositions comprising levodopa, a dopamine decarboxylase inhibitor and a COMT inhibitor and a method of administration thereof
  • Pharmaceutical compositions comprising levodopa, a dopamine decarboxylase inhibitor and a COMT inhibitor and a method of administration thereof
  • Pharmaceutical compositions comprising levodopa, a dopamine decarboxylase inhibitor and a COMT inhibitor and a method of administration thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0235] Example 1: Composition

[0236] Hereinafter, the use of the enteral gel composition (hereinafter referred to as "LECIGON" according to the present invention) will be described. TM ”) and commercially available levodopa / carbidopa enteral gels of the prior art (hereinafter referred to as "LCIG"), and the use of modified LECIGON TM Composition for stability testing. LCIG and LECIGON are given in Tables 2 and 3 below TM composition.

[0237] Table 2 Exemplary composition of LCIG

[0238]

[0239] Table 3 LECIGON TM Exemplary composition of

[0240]

[0241] Fifteen exemplary small scale batches as described in Table 4 were prepared as follows and filled into syringes for initial evaluation and stability evaluation under various storage and use conditions. Experimental batch sizes ranged from 100 g to 500 g. In Table 4, API is the active pharmaceutical ingredient, L is levodopa, C is carbidopa, and E is entacapone.

[0242] Table 4

[0243]

[0244]

Embodiment 2

[0245] Embodiment 2: preparation process

[0246] Exemplary preparations of intestinal gel samples to be tested are described below.

[0247] 1) Add sodium carboxymethylcellulose to purified water in a Pyrex beaker and homogenize for 1 to 2 minutes until a viscous solution without lumps is obtained.

[0248] 2) Add the active ingredients levodopa, carbidopa and entacapone and homogenize until a homogeneous suspension is obtained.

[0249] 3) Add additional excipients as described in Table 3 above and homogenize until dissolved.

[0250] 4) If necessary, during mixing, adjust the pH to the target pH by adding sodium hydroxide or hydrochloric acid solution.

[0251] 5) Manually fill the suspension into the syringe.

[0252] The process equipment used to prepare the experimental batches included: Silverson L5M homogenizer (Silverson Machines Ltd., Chesham, U.K.) and IKA Janke & Kunkel RW28W mixer (IKA Works GmbH, Staufen, Germany).

[0253] During preparation, the following...

Embodiment 3

[0257] Embodiment 3: stability test

[0258] This example demonstrates the stability of the enteric gel under various conditions.

[0259] 3.1. Unstable LECIGON TM Stability relative to LCIG

[0260] Unstabilized LECIGON TM The stability of carbidopa, especially the degradation product hydrazine (considered genotoxic) of carbidopa, was compared with that of LCIG. Hydrazine is formed equimolarly with 3,4-dihydroxyphenylacetone (DHPA), which is easier to measure, so in this experiment and others below, DHPA was used as the reference. Compare. The results are shown in Table 5 below.

[0261] table 5.

[0262]

[0263] As shown in Table 5, compared with the corresponding levodopa-carbidopa gel suspension (LCIG), in the three-component levodopa-carbidopa-entacapone gel suspension (LECIGON TM ) degrades about 50% faster in carbidopa.

[0264] 3.2. LECIGON TM stabilization of

[0265] Using LECIGON TM , for carbidopa, levodopa and entacapone, a 12-day stabilization ex...

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Abstract

A pharmaceutical gel composition for intra-intestinal administration is provided and comprises (i) a dopamine replacement agents, (ii) a dopamine decarboxylase inhibitor (DDI), and (iii) a COMT inhibitor.

Description

[0001] Cross References to Related Applications [0002] This application claims priority and benefit from Swedish Patent Application No. 1451034-1, filed September 4, 2014, and Swedish Patent Application No. 1550344-4, filed March 24, 2015, which are hereby incorporated by reference This article. Background technique [0003] Neurodegenerative diseases result when neurons fail to regenerate normally or replace themselves, thereby failing to replace damaged neurons. Progressive degeneration and / or death of neuronal cells often results in movement problems (eg, ataxia) or mental function problems (eg, dementia). Currently, many neurodegenerative diseases are considered incurable. Examples of neurodegenerative diseases include Parkinson's disease ("PD"), Alzheimer's disease ("AD"), and Huntington's disease ("HD"). [0004] Parkinson's disease is characterized by progressive degeneration of dopaminergic pathways, leading to decreased concentrations of the neurotransmitter dopa...

Claims

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Application Information

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IPC IPC(8): A61K31/195A61K9/06A61K31/198A61K31/277A61P25/16
CPCA61K9/06A61K31/277A61K9/0019A61K47/38A61K9/0024A61K45/06A61K31/198A61P25/16A61P25/28A61K31/165A61K2300/00A61K9/1652
Inventor 罗杰·伯索伊
Owner LOBSOR PHARM AB
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