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1. (WO2019027372) FLOATABLE PHARMACEUTICAL MICROCAPSULE COMPOSITION
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Pub. No.: WO/2019/027372 International Application No.: PCT/SG2018/050394
Publication Date: 07.02.2019 International Filing Date: 02.08.2018
IPC:
A61K 9/58 (2006.01) ,A61K 47/34 (2017.01) ,A61K 47/42 (2017.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
48
Preparations in capsules, e.g. of gelatin, of chocolate
52
Sustained or differential release type
54
containing discrete particles with coatings of different thicknesses or different materials
56
Organic coatings
58
containing solid synthetic polymers
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
42
Proteins; Polypeptides; Degradation products thereof; Derivatives thereof
Applicants:
NANYANG TECHNOLOGICAL UNIVERSITY [SG/SG]; 50 Nanyang Avenue Singapore 639798, SG
Inventors:
LOO, Say Chye Joachim; SG
BAEK, Jongsuep; SG
Agent:
KINNAIRD, James Welsh; SG
Priority Data:
10201706305X02.08.2017SG
Title (EN) FLOATABLE PHARMACEUTICAL MICROCAPSULE COMPOSITION
(FR) COMPOSITION DE MICROCAPSULE PHARMACEUTIQUE FLOTTABLE
Abstract:
(EN) Disclosed herein is a sustained release hollow core-shell microcapsule formulation for drug delivery comprising a hollow shell of one or more hydrophobic polymers, a drug containing hydrophilic or amphiphilic carrier matrix that is distributed over the inner surface of the hollow shell, a flotation agent, and an optional osmotic agent, wherein the microcapsule is capable of floating in a simulated digestive fluid for a period of from 24 to 96 hours. The microcapsules are prepared by a modified double emulsion (water/oil/water) solvent evaporation method. The microcapsule formulation may provide a sustained-release delivery system for treating chronic diseases such as Parkinson's disease, diabetes and tuberculosis, all of which require multiple drug combination therapies. The aim is to reduce dosing frequency and pill burden, thus improving patient medication compliance. In a specific embodiment, the hollow shell is formed from a mixture of Poly-L-lactide (PLLA) and poly(E-caprolactone) (PCL); and the amphiphilic carrier matrix is casein.
(FR) L'invention concerne une formulation de microcapsule à noyau-enveloppe creuse à libération prolongée pour l'administration de médicament comprenant une enveloppe creuse d'un ou de plusieurs polymères hydrophobes, un médicament contenant une matrice de support hydrophile ou amphiphile qui est distribuée sur la surface interne de l’enveloppe creuse, un agent de flottation, et un agent osmotique facultatif, la microcapsule étant capable de flotter dans un fluide digestif simulé pendant une période de 24 à 96 heures. Les microcapsules sont préparées par le procédé de double émulsion (eau/huile/eau)/évaporation de solvant modifié. La formulation de microcapsule peut fournir un système d'administration à libération prolongée pour traiter des maladies chroniques telles que la maladie de Parkinson, le diabète et la tuberculose, tous nécessitant de multiples thérapies de combinaison de médicaments. Le but est de réduire la fréquence de dosage et la charge de pilule, améliorant ainsi la conformité de médication du patient. Dans un mode de réalisation spécifique, l’enveloppe creuse est formée à partir d'un mélange de poly-L-lactide (PLLA) et de poly(E-caprolactone) (PCL); et la matrice de support amphiphile est la caséine.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)