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Pharmaceutical composition containing surface-coated microparticles

A technology of surface coating and composition, which is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., can solve the problems of low loading capacity, compound is difficult to encapsulate nanoparticles, and nanoparticles are not easy to realize, and achieve high The effect of stability

Inactive Publication Date: 2011-06-01
NITTO DENKO CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the case of peptide and protein drugs, it has been shown that unless the drug is encapsulated within a nanoparticle matrix, their stability is low
However, due to the large size of these compounds and the often hydrophobic environment in the nanoparticle matrix, these compounds are difficult to encapsulate within nanoparticles, and this often results in very low loading capacity and thus requires the administration of large quantities of nanoparticles to mucosal surfaces.
Moreover, it has been clarified in publications that the delivery of nanoparticles across mucous membranes is not easily achieved (Non-Patent Document 6)

Method used

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  • Pharmaceutical composition containing surface-coated microparticles
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  • Pharmaceutical composition containing surface-coated microparticles

Examples

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preparation example Construction

[0103] The invention also provides a method for preparing the above-mentioned pharmaceutical composition. The method of the present invention includes mixing a drug, a surface-coated polymer, and microparticles in a solution having a suitable pH, optionally changing the pH to cause electrostatic interaction between the drug and the surface-coating polymer, and the surface coating The non-covalent bond interaction between the polymer and the microparticles. This method does not require heat treatment or the like and is therefore convenient.

[0104] In this method, the combination of the drug, the surface-coated polymer, and the microparticles, and the pH (predetermined pH) of the composition of the present invention are determined in advance. These factors can be determined as mentioned above in the explanation about the composition of the present invention. The microparticles are usually prepared by the above-mentioned method before mixing the drug, the surface coating polymer...

preparation example 1

[0123] Preparation Example 1: Preparation of poly(lactic-co-glycolic acid) (PLGA) particles of various particle sizes

[0124] PLGA microparticles were prepared using PLGA (RESOMER RG 502H, Bohringer Ingelheim) with a lactide:glycolide ratio of 50:50. The PLGA was dissolved in HPLC grade acetone at the desired concentration. Under continuous stirring, the PLGA / acetone solution was added dropwise to purified water at a ratio of 1:3. The mixture was stirred until all the acetone had evaporated (about 4 hours).

[0125] The particle size distribution of the obtained particles was measured by a dynamic light scattering measuring device (DLS 802, Viscotek). Table 1 shows the relationship between the PLGA concentration and the diameter of the obtained particles. Obviously, by reducing the polymer concentration in the initial organic solvent solution, smaller particles can be obtained easily and reproducibly.

[0126] Table 1

[0127] Influence of PLGA concentration on particle size

[0...

Embodiment 1

[0129] Example 1: Preparation of a microparticle system coated with a drug-surface-coated polymer complex in two different buffer systems

[0130] Insulin (pI about 5.3) was used as a protein drug, and chitosan was used as a positively charged surface coating polymer.

[0131] Add 1.5 ml of bovine insulin (Sigma, 160 μg / ml) in 0.5 mM citric acid solution (pH 4.5) to 1.5 ml of chitosan (Bioneer 143 kDa, 0.72 mg) in 0.5 mM citric acid solution (pH 4.5) / ml), and leave the mixture at room temperature for at least 30 min. Suspend 3 ml of PLGA particles (about 100 nm in diameter; hereinafter also referred to as "PLGA 100") (pH 4.5; PLGA particle concentration: 500 μg / ml) prepared as described in Preparation Example 1 in 0.5 mM citric acid solution The chitosan / insulin solution is added to the chitosan / insulin solution, and the mixture is left at room temperature for at least 1 hour. The pH was increased to 6.0 with NaOH (0.1-2.5N), and salts and supplements were added thereto to prov...

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Abstract

Disclosed is a pharmaceutical composition which can be used for the administration of a low-molecular-weight substance or a high-molecular-weight substance such as a peptide and a protein by a means other than injection with high efficiency. Also disclosed is a method for producing the composition. Specifically disclosed is a pharmaceutical composition for transmucosal administration, which comprises (a) a substance which can carry a positive or negative electrical charge at a given pH value, (b) pharmaceutically acceptable microparticles, and (c) a pharmaceutically acceptable surface-coating polymer which can be electrically charged at the above-mentioned pH value. In the composition, the surface-coating polymer coats the surfaces of the microparticles, and the substance is immobilized on the surfaces of the microparticles through the surface-coating polymer. In the composition, the microparticles interact non-covalently with the surface-coating polymer and, at the same time, the surface-coating polymer interacts electrostatically with the substance, thereby forming a complex.

Description

Technical field [0001] The invention relates to a medicinal composition for transmucosal administration and a preparation method thereof. More specifically, the present invention relates to a novel transmucosal drug composition comprising a complex composed of a drug, microparticles, and a surface coating polymer, wherein the surface coating polymer coats the surface of the microparticles, and the drug passes through the The surface-coated polymer is fixed on the surface of the microparticle, and the composite is formed by the non-covalent bond interaction between the microparticle and the surface-coated polymer and the concurrent electrostatic interaction between the surface-coated polymer and the drug 物; and its preparation method. Background technique [0002] Advances in biotechnology have led to the discovery of a large number of therapeutic compounds, such as peptides, proteins, polysaccharides, polynucleic acids, siRNA, RNA, antibodies, antigens, low molecular weight drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/137A61K31/4045A61K31/715A61K38/00A61K38/28A61K39/00A61K45/00A61K47/30A61K47/32A61K47/36A61K47/42A61K48/00A61P3/10A61P11/10A61P25/06
CPCA61K47/34A61K47/32A61K31/715A61K9/0043A61K47/42A61K31/195A61K9/1676A61K31/137A61K31/4045A61K9/19A61P11/10A61P25/06A61P37/04A61P3/10A61K9/16
Inventor 大久保胜之北浦千枝子味吞宪二郎E.皮尔森C.J.罗伯特斯M.C.戴维斯S.斯托尼克-特伦基L.伊鲁姆
Owner NITTO DENKO CORP
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