Floatable pharmaceutical microcapsule composition

A technology of microcapsules and drugs, applied in the direction of drug combination, microcapsules, and capsule delivery, which can solve problems such as drug-resistant TB

Inactive Publication Date: 2020-04-10
NANYANG TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A patient who does not receive his / her TB medications properly may also develop drug-resistant TB

Method used

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  • Floatable pharmaceutical microcapsule composition
  • Floatable pharmaceutical microcapsule composition
  • Floatable pharmaceutical microcapsule composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0207] Embodiment 1: the preparation procedure of microcapsule

[0208] Using water-oil-water (W 1 / O / W 2) double emulsification method to encapsulate the drug in casein-PLLA / PCL microcapsules. The amphiphile casein is capable of encapsulating both hydrophobic and hydrophilic drugs. Casein is the major protein in milk and has unique hydrophobic and hydrophilic domains (ie, amphipathic).

[0209] Aqueous casein solutions were prepared by dissolving 10, 30 or 50 mg of casein in distilled water, using 2 mg of sodium chloride (1 mL) as osmotic agent. Separately, a polymer solution was prepared by dissolving 0.3 g of PLLA and 0.1 g of PCL in 5 mL of DCM. Depending on the target disease (see table below), specific hydrophilic drugs were dissolved in the casein solution, while hydrophobic drugs were dissolved in the PLLA / PCL solution.

[0210]

[0211]

[0212] The resulting casein solution was then added dropwise to the polymer solution under magnetic stirring, and 10 μ...

Embodiment 2

[0235] Embodiment 2: the in vitro drug release profile of microcapsules

[0236] To test the hypothesis that microcapsules can provide better sustained and controlled release of multiple drugs, the release profiles of individual drugs from samples in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were studied.

[0237] method

[0238] In vitro release studies were performed in SGF for 48h. In some experiments, studies were conducted in SGF and then in SIF, where the total duration in SGF and SIF was 48h. Each microcapsule sample (20 mg) was added to a bottle containing SGF or SIF medium (20 mL). Both SGF and SIF bottles were placed in a 37°C rotary incubator. At various time points, half of the medium (10 mL) in each bottle was withdrawn and replaced with 10 mL of new medium. Time points include hourly intervals within 48 hours. By the procedure mentioned in Example 1, the drug content in the extracted medium was analyzed using RP-HPLC to determine t...

Embodiment 3

[0247] Embodiment 3: the in vivo drug release profile of microcapsules

[0248] Pharmacokinetic release of three different PD drugs (i.e., levodopa, carbidopa, and entacapone) from optimized casein (3% (w / v))-microparticles fed to healthy mice Kinetics were compared to a commercial formulation (ie control) with the same drug ratio as the microcapsules.

[0249] method

[0250] Experimental mice were divided into two groups (control group and F2), each consisting of five animals. Control preparations were freshly prepared (as solutions) in 0.6% methylcellulose diluted with saline solution on each experimental day. Then use a feeding syringe to administer 200ul (control) or 300μl (bolus) to mice by oral gavage at LD:CD:ENT=10:2.5:20mg.kg -1 (group 1, conventional preparation) and LD:CD:ENT=10:2.5:20mg.kg -1 (group 2, F2) a single dose of the drug solution. At defined time points of 0.25, 0.5, 1, 2, 4, 8, 12, 24 hr, mice were euthanized and blood was collected by cardiac p...

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Abstract

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 simulateddigestive 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.

Description

technical field [0001] The present invention relates to gastric floating microcapsules for trapping one or more, preferably multiple, drugs and methods for their manufacture. Background technique [0002] The listing or discussion in this specification of a document which is apparently prior published does not necessarily constitute an admission that the document is part of the prior art or is common general knowledge. [0003] Parkinson's disease (PD) is a degenerative disorder of the central nervous system that causes asymmetric episodes of bradykinesia, resting tremor, muscle rigidity, and postural instability. It is more common in older adults, with most cases occurring after the age of 50. Early signs and symptoms may be mild and may go unnoticed at first, but the symptoms of this motor degenerative disease stem from the death of dopamine-producing cells in the substantia nigra — an area of ​​the midbrain. [0004] Although the etiology of Parkinson's disease remains ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/58A61K47/34A61K47/42A61P25/16A61P3/10A61P31/06A61P9/10A61P31/18A61P25/00A61P35/00A61P25/28A61P3/00A61P9/12A61P13/12A61P29/00A61P3/04A61P1/04A61P1/16A61P19/02A61P37/02
CPCA61K47/42A61K9/5031A61P31/06A61P25/16A61P3/10A61K45/06A61K31/133A61K31/155A61K31/198A61K31/216A61K31/277A61K31/4409A61K31/496A61K2300/00A61K9/5084A61K9/5089A61K47/34A61K47/44
Inventor 吕世财琼苏普·贝克
Owner NANYANG TECH UNIV
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