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Extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt thereof

Inactive Publication Date: 2006-03-09
BOEHRINGER INGELHEIM INT GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0036] The extended release formulations (a) and (b) according to the present invention intended for oral administration allow to select and estimate which in vitro release characteristic and timing of a formulation is most suitable to achieve the desired in vivo plasma profiles preferably with a once daily application. Therefore, two different formulation principles have been developed for pellets. The two formulation principles have different release rate types and a different pH dependency is available. These alternative formulations are beneficial to patients as the extended release drug delivery will allow patients to treat their symptoms with a single daily dose, thereby increasing patient convenience and compliance.
[0079] Therefore, the presence of a pore-forming component provides the further advantage that the release characteristic is accelerated and occurs more rapid, i.e., the effects of the second layer are enhanced significantly.

Problems solved by technology

However, it has proved difficult to formulate a dosage form having a suitable combination of modified, extended, or sustained-release and handling properties, where the drug is one having relatively high solubility, as in the case of pramipexole dihydrochloride.
However, in practical use, it appears that any formulation having a modified or controlled release profile designed for a once daily application would meet the above requirements for which a general teaching how to adjust such a profile is missing.

Method used

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  • Extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt thereof
  • Extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt thereof
  • Extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt thereof

Examples

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example 1

[0134] One embodiment of the qualitative and quantitative composition of pramipexole extended 10 release pellets according to the present invention (Formulation D) is shown in Table 1.

TABLE 1Qualitative and Quantitative Composition ofPramipexole Extended Release (ER) Capsule (Formulation D)mg permg per0.75 mg0.75 mgReference toIngredientcapsulecapsuleFunctionStandardsER Pellets consisting of:88.458Pramipexole dihydrochloride0.750Active ingredientCompanymonohydratestandardMicrocrystalline cellulose pellets73.980Non-pareille carrierPh.Eur. / NF(Cellets 700)pelletHydroxypropyl cellulose0.150Wet binderPh.Eur. / NF(KLUCEL ® EF)Talc0.495GlidantPh.Eur. / USPMethacrylic acid copolymer,7.500Functional coatingPh.Eur. / NFType B (EUDRAGIT ® S 100)Ammonio methacrylate3.750Functional coatingPh.Eur. / NFcopolymer, Type B(EUDRAGIT ® RS 100)Triacetin1.833PlasticizerPh.Eur. / USPEthanol (96%)173.333*SolventPh.Eur.Purified water30.000*SolventPh.Eur. / USPHPMC capsule, size 346.000ShellCompanyStandardTotal134.458...

example 2

[0135] One embodiment of the qualitative and quantitative composition of pramipexole extended release pellets according to the present invention (Formulation E) is shown in Table 2.

TABLE 2Qualitative and Quantitative Composition ofPramipexole ER Capsule (Formulation E)mg permg per0.75 mg0.75 mgReference toIngredientcapsulecapsuleFunctionStandardsER Pellets consisting of:91.600Pramipexole dihydrochloride0.750Active ingredientCorporatemonohydratestandardMicrocrystalline cellulose pellets73.980Non-pareille carrierPh.Eur / NF(Cellets 700)pelletHydroxypropyl cellulose0.150Wet binderPh.Eur. / NF(KLUCEL ® EF)Talc0.578GlidantPh.Eur. / USPMethacrylic acid copolymer,9.250Functional coatingPh.Eur. / NFType B (EUDRAGIT ® S 100)Ammonio methacrylate4.625Functional coatingPh.Eur. / NFcopolymer, Type B(EUDRAGIT ® RS 100)Triacetin2.267PlasticizerPh.Eur. / USPEthanol (96%)214.167*SolventPh.Eur.Purified water30.000*SolventPh.Eur. / USPHPMC capsule, size 346.000ShellCompanyStandardTotal137.60091.600

*removed during...

example 3

[0136] One embodiment of the qualitative and quantitative composition of pramipexole extended release pellets according to the present invention (Formulation F) is shown in Table 3.

TABLE 3Qualitative and Quantitative Composition ofPramipexole ER Capsule (Formulation F)mg permg per0.75 mg0.75 mgReference toIngredientcapsulecapsuleFunctionStandardsER Pellets consisting of:80.063Pramipexole dihydrochloride0.750Active ingredientCorporatemonohydratestandardMicrocrystalline cellulose pellets73.980Non-pareille carrierPh.Eur / NF(Cellets 700)pelletHydroxypropyl cellulose0.150Wet binderPh.Eur. / NF(KLUCEL ® EF)Talc0.495GlidantPh.Eur. / USPEthyl cellulose (N14)3.750Functional coatingPh.Eur. / NFMacrogol 60000.938PlasticizerPh.Eur. / USPEthanol (96%)49.167*SolventPh.Eur.Purified water32.583*SolventPh.Eur. / USPHPMC capsule, size 346.000ShellCompanyStandardTotal126.06380.063

*removed during processing (does not appear in the final product)

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Abstract

An extended release pellet comprising an active ingredient selected from pramipexole and the pharmaceutically acceptable salts thereof, and at least one release-modifying excipient.

Description

RELATED APPLICATIONS [0001] This application claims priority to European Application No. 04019249.4 filed Aug. 13, 2004, which is hereby incorporated by reference in its entirety. FIELD OF THE INVENTION [0002] The present invention is directed to an extended release pellet formulation containing pramipexole or a pharmaceutically acceptable salt thereof, method for manufacturing the same and use thereof. BACKGROUND OF THE INVENTION [0003] Pramipexole is a known dopamine D2 receptor agonist. It is structurally different from the ergot-derived drugs, e.g., bromocriptine or pergolide. It is also pharmacologically unique in that it is a full agonist and has receptor selectivity for the dopamine D2 family of dopamine receptors. [0004] Pramipexole is designated chemically as (S)-2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and has the molecular formula C10H17N3S and a relative molecular mass of 211.33. The chemical formula is as follows: [0005] The salt form commonly used is pr...

Claims

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Application Information

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IPC IPC(8): A61K9/26A61K9/50A61K31/428
CPCA61K9/5078A61P25/00A61P25/16A61K9/50A61K31/428
Inventor FRIEDL, THOMASBRICKL, ROLF-STEFAN
Owner BOEHRINGER INGELHEIM INT GMBH
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