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Intestine and stomach administration bioadhesive microsphere preparation and preparation method of intestine and stomach administration bioadhesive microsphere preparation

A bioadhesion and gastrointestinal technology, applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, non-effective ingredients of polymer compounds, etc., can solve the problem of increased viscosity of raw and auxiliary materials and soft materials, and it is difficult to simultaneously take into account slow release, adhesion, Problems such as ball formation, to achieve high drug loading, enhance hydrophobic interaction and electrostatic interaction, and enhance bioadhesion performance

Inactive Publication Date: 2018-01-16
雷笑天
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The technical problem to be solved by the present invention: for the addition of adhesive materials, the viscosity of raw and auxiliary soft materials is greatly increased, and the traditional industrial microsphere / pellet production method is difficult to simultaneously meet the requirements of slow release, adhesion, and ball formation. , providing a bioadhesive microsphere preparation for gastrointestinal administration and a preparation method thereof

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0027] Take 0.1g of lactose and 0.1g of pectin, add them to 10mL of absolute ethanol, stir at 300r / min for 20min, then add 0.4g of gastrointestinal absorption drug, add absolute ethanol to 100mL, and continue stirring for 1h to obtain the drug-loading solution. Add 0.2g of hydroxypropyl methylcellulose and 0.2g of hydrophobin to 100mL of absolute ethanol, stir at 300r / min for 20min, then add 0.4g of soybean lecithin, and continue to stir for 20min to obtain an adhesion solution. Add it into the adhesive solution, stir at 600r / min for 30min at 0°C to obtain a dispersion, take 32g of Span-80, add it to 1.6L of liquid paraffin, stir at 600r / min for 20min, and then at 0°C, Add the dispersion liquid dropwise at 1mL / min, heat to 20°C after the dropwise addition, and stir at 300r / min for 8h, filter to obtain the filter residue, wash the filter residue with petroleum ether for 3 times, place in a drying oven, and dry at 25°C for 25h. Gastrointestinal administration of bioadhesive micr...

example 2

[0029] Take 0.1g of lactose and 0.1g of pectin, add them to 15mL of absolute ethanol, stir at 350r / min for 25min, then add 0.7g of gastrointestinal absorption drug, add absolute ethanol to 150mL, and continue stirring for 1.5h to obtain the drug-loading solution. Take 0.3g of hydroxypropyl methylcellulose and 0.3g of hydrophobin, add them to 150mL of absolute ethanol, stir at 350r / min for 25min, then add 0.7g of soybean lecithin, and continue to stir for 25min to obtain an adhesive liquid, and the drug-loaded Add the liquid into the adhesive liquid, stir at 700r / min for 35min at 5°C to obtain a dispersion, take 49g of Span-80, add it to 2.5L of liquid paraffin, stir at 700r / min for 25min, and then at 5°C, Add the dispersion liquid dropwise at 1mL / min, heat to 25°C after the dropwise addition, and stir at 350r / min for 9h, filter the filter residue, wash the filter residue 4 times with petroleum ether, place in a drying oven, and dry at 30°C for 28h , to obtain bioadhesive micro...

example 3

[0031] Take 0.2g of lactose and 0.2g of pectin, add them to 20mL of absolute ethanol, stir at 400r / min for 30min, then add 1.0g of gastrointestinal absorption drug, add absolute ethanol to 200mL, and continue to stir for 2h to obtain the drug-loading solution. Add 0.5g of hydroxypropyl methylcellulose and 0.5g of hydrophobin into 200mL of absolute ethanol, stir at 400r / min for 30min, then add 1.0g of soybean lecithin, and continue to stir for 30min to obtain an adhesion solution. Add it into the adhesive solution, stir at 800r / min for 40min at 10°C to obtain a dispersion, take 64g of Span-80, add it to 3.2L of liquid paraffin, stir at 800r / min for 30min, and then at 10°C, Add the dispersion liquid dropwise at 2mL / min, heat to 30°C after the dropwise addition, and stir at 400r / min for 10h, filter to obtain the filter residue, wash the filter residue with petroleum ether for 3 to 5 times, place in a drying oven, and dry at 35°C After 30 hours, the bioadhesive microspheres for ga...

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Abstract

The invention relates to an intestine and stomach administration bioadhesive microsphere preparation and a preparation method of the intestine and stomach administration bioadhesive microsphere preparation, and belongs to the technical field of medical preparations. A natural polymeric amylose compound is prepared from lactose and pectin to serve as a drug-loaded material, and is quite excellent in biocompatibility, high in drug loading capacity, good in spheronization and slow release feature; and the side effect of a drug reaches the lowest level. Soybean lecithin is used to improve the lipid solubility of the drug and strengthens the membrane permeability, the retention time on an absorption part in vivo is prolonged, the drug release and the membrane permeation absorption are promoted,the drug availability is improved, meanwhile, the soybean lecithin and hydrophobin produces a synergistic effect, the hydrophobin molecule is folded, a hydrophobic group and a sulfydryl embedded in the hydrophobin are exposed, so that the hydrophobic interaction of the hydrophobin is strengthened, the hydrophobic effect and the mutual electrostatic interaction between an amino acid residue on thehydrophobin and a mucosa protein are strengthened, the disulfide bond formed by a cysteine residue on the hydrophobin and a thiol group of a glycoprotein in a mucus is increased, and the bioadhesiveperformance is strengthened.

Description

technical field [0001] The invention relates to a bioadhesive microsphere preparation for gastrointestinal administration and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Since the 1990s, bioadhesive sustained-release microparticle preparations have a large specific surface area, can easily enter the mucous layer and have a strong adhesion to the mucous membrane, and at the same time have a good The advantages of slow and controlled release drugs have once become a hot spot in the research of new drug dosage forms. Nevertheless, there are still several obstacles to the practical translational application of bioadhesive microparticle formulations. [0003] Bioadhesive drug delivery system is a kind of natural or synthetic polymer material, through which it has a long-term close contact with the surface of the mucous membrane of the body tissue, thereby prolonging the residence time of the drug in...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/24A61K47/38A61K47/42A61K47/26A61K47/36
Inventor 雷笑天王之霖陈倩
Owner 雷笑天
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