CN110638795A - Inhalable medicine and preparation method thereof - Google Patents

Inhalable medicine and preparation method thereof Download PDF

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Publication number
CN110638795A
CN110638795A CN201911081437.1A CN201911081437A CN110638795A CN 110638795 A CN110638795 A CN 110638795A CN 201911081437 A CN201911081437 A CN 201911081437A CN 110638795 A CN110638795 A CN 110638795A
Authority
CN
China
Prior art keywords
inhalable
polyamino acid
medicine
inhalable medicament
coating layer
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201911081437.1A
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Chinese (zh)
Inventor
何松繁
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Huisheng Medical Science And Technology (xuzhou) Co Ltd
Original Assignee
Huisheng Medical Science And Technology (xuzhou) Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Huisheng Medical Science And Technology (xuzhou) Co Ltd filed Critical Huisheng Medical Science And Technology (xuzhou) Co Ltd
Priority to CN201911081437.1A priority Critical patent/CN110638795A/en
Publication of CN110638795A publication Critical patent/CN110638795A/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles

Abstract

An inhalable medicine comprises liquid active medicine, carrier substance, and coating layer. The preparation method comprises the following steps: (1) grinding carrier material to 500-3000 nm, adding liquid active medicine for full absorption; (2) dissolving polyamino acid in glycol to obtain polyamino acid solution; (3) and (3) respectively and simultaneously spraying the mixture in the step (1) and the mixed solution in the step (2) into a freeze dryer to realize coating, so as to obtain the inhalable medicament. The beneficial effect is that the problem that the existing liquid medicine is difficult to realize the absorbability is solved.

Description

Inhalable medicine and preparation method thereof
Technical Field
The invention belongs to the field of biological medicine, and particularly relates to an inhalable medicine.
Background
Currently, drug delivery via inhalation has been used for the treatment of certain respiratory disease states, such as infection, inflammation, or bronchoconstriction, and has also proven to be the preferred approach to achieve sufficiently high drug levels. In some cases, certain medicaments delivered via inhalation may produce fewer systemic side effects when inhaled. In another aspect, drugs for systemic activity can be delivered via inhalation to take advantage of the high surface area of the lungs, providing rapid drug absorption into the systemic circulation without the first pass metabolic effects associated with oral administration. In some cases, delivery of the agent to the lung may be for the convenience of the patient or healthcare provider. The usual way of using the drug is to grind the drug and the hydrophobic substance together to a certain particle size, thereby achieving inhalation of the drug. However, many medicaments are liquids, easily form large droplets, are easily absorbed in the nostrils, and are difficult to achieve effective inhalation.
Disclosure of Invention
The invention mainly aims to provide an inhalable medicament and a preparation method thereof, and solves the problem that the existing liquid medicament is difficult to realize inhalable.
In order to achieve the technical effects, the invention adopts the following technical scheme:
an inhalable medicine comprises liquid active medicine, carrier substance, and coating layer.
The liquid active drug is a liquid which is non-reactive with the carrier substance and the coating layer.
The carrier substance is at least one of galactose, lactose, sucrose, raffinose, maltose and sorbose.
The coating layer is a copolymer of two of proline, lysine and phenylalanine which are used as the polyamino acid, and the molecular weight is 12000-15000;
the preparation method of the inhalable medicine comprises the following steps:
(1) grinding carrier material to 500-3000 nm, adding liquid active medicine for full absorption;
(2) dissolving polyamino acid in glycol to obtain polyamino acid solution;
(3) and (3) respectively and simultaneously spraying the mixture in the step (1) and the mixed solution in the step (2) into a freeze dryer to realize coating, so as to obtain the inhalable medicament.
The viscosity of the polyamino acid solution is 9-10 poise.
The particle size of the inhalable medicine is 2-5 microns.
The invention has the beneficial effects that: (1) the coating layer has hydrophobicity, can not easily agglomerate and can be effectively absorbed.
(2) The coating layer has degradability, and can gradually release the drug and reduce the drug toxicity.
Detailed Description
For further understanding of the present invention, the following embodiments are provided to illustrate the technical solutions of the present invention in detail, and the scope of the present invention is not limited by the following embodiments.
An inhalable medicine comprises liquid active medicine, carrier substance, and coating layer.
The liquid active drug is a liquid which is non-reactive with the carrier substance and the coating layer.
The carrier substance is at least one of galactose, lactose, sucrose, raffinose, maltose and sorbose, can be absorbed by human body, and has no adverse effect on human body.
The coating layer is a copolymer of the two of proline, lysine and phenylalanine as the polyamino acid, has the molecular weight of 12000-15000, has hydrophobicity and degradability, can avoid agglomeration, and slows down the toxicity caused by quick release of the medicament; the preparation method of the inhalable medicine comprises the following steps:
(1) grinding carrier material to 500-3000 nm, adding liquid active medicine for full absorption;
(2) dissolving polyamino acid in glycol to obtain polyamino acid solution;
(3) and (3) respectively and simultaneously spraying the mixture in the step (1) and the mixed solution in the step (2) into a freeze dryer to realize coating, so as to obtain the inhalable medicament.
The viscosity of the polyamino acid solution is 9-10 poise, the viscosity is proper, and good coating can be formed.
The particle size of the inhalable medicine is 2-5 microns, the particle size distribution range is small, and the inhalable can be realized.
Example 1
An inhalable medicine comprises liquid active medicine, carrier substance, and coating layer.
The liquid active drug is ambroxol hydrochloride.
The carrier material is galactose.
The coating layer is a copolymer of proline and lysine as the polyamino acid, and the molecular weight is 15000;
the preparation method of the inhalable medicine comprises the following steps:
(1) grinding carrier material to 500 nm, adding liquid active medicine for full absorption;
(2) dissolving polyamino acid in glycol to obtain polyamino acid solution;
(3) and (3) respectively and simultaneously spraying the mixture in the step (1) and the mixed solution in the step (2) into a freeze dryer to realize coating, so as to obtain the inhalable medicament.
The viscosity of the polyamino acid solution is 10 poise.
The particle size of the inhalable medicine is 2-5 microns.
Example 2
An inhalable medicine comprises liquid active medicine, carrier substance, and coating layer.
The liquid active drug is ambroxol hydrochloride.
The carrier substance is at least one of galactose, lactose, sucrose, raffinose, maltose and sorbose.
The coating layer is a copolymer of two of proline, lysine and phenylalanine as the polyamino acid, and the molecular weight is 12000; the preparation method of the inhalable medicine comprises the following steps:
(1) grinding carrier material to 3000 nm, adding liquid active medicine for full absorption;
(2) dissolving polyamino acid in glycol to obtain polyamino acid solution;
(3) and (3) respectively and simultaneously spraying the mixture in the step (1) and the mixed solution in the step (2) into a freeze dryer to realize coating, so as to obtain the inhalable medicament.
The viscosity of the polyamino acid solution is 9 poise.
The particle size of the inhalable medicine is 2-5 microns.
The foregoing illustrates and describes the principles, general features, and advantages of the present invention. It should be understood by those skilled in the art that the above embodiments do not limit the scope of the present invention in any way, and all technical solutions obtained by using equivalent substitution methods fall within the scope of the present invention.

Claims (7)

1. An inhalable medicament, comprising: comprises liquid active medicine, carrier substance and coating layer.
2. An inhalable medicament as claimed in claim 1, characterised in that: the liquid active drug is a liquid which is non-reactive with the carrier substance and the coating layer.
3. An inhalable medicament as claimed in claim 1, characterised in that: the carrier substance is at least one of galactose, lactose, sucrose, raffinose, maltose and sorbose.
4. An inhalable medicament as claimed in claim 1, characterised in that: the coating layer is a copolymer of two of proline, lysine and phenylalanine which are used as the polyamino acid, and the molecular weight is 12000-15000.
5. A process for the preparation of an inhalable medicament as claimed in claim 1, wherein: the method comprises the following steps:
(1) grinding carrier material to 500-3000 nm, adding liquid active medicine for full absorption;
(2) dissolving polyamino acid in glycol to obtain polyamino acid solution;
(3) and (3) respectively and simultaneously spraying the mixture in the step (1) and the mixed solution in the step (2) into a freeze dryer to realize coating, so as to obtain the inhalable medicament.
6. An inhalable medicament as claimed in any one of claims 1 to 5, characterised in that: the viscosity of the polyamino acid solution is 9-10 poise.
7. An inhalable medicament as claimed in any one of claims 1 to 5, characterised in that: the particle size of the inhalable medicine is 2-5 microns.
CN201911081437.1A 2019-11-07 2019-11-07 Inhalable medicine and preparation method thereof Pending CN110638795A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201911081437.1A CN110638795A (en) 2019-11-07 2019-11-07 Inhalable medicine and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201911081437.1A CN110638795A (en) 2019-11-07 2019-11-07 Inhalable medicine and preparation method thereof

Publications (1)

Publication Number Publication Date
CN110638795A true CN110638795A (en) 2020-01-03

Family

ID=68995636

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201911081437.1A Pending CN110638795A (en) 2019-11-07 2019-11-07 Inhalable medicine and preparation method thereof

Country Status (1)

Country Link
CN (1) CN110638795A (en)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101325945A (en) * 2005-12-12 2008-12-17 雅戈泰克股份公司 Powder compositions for inhalation

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101325945A (en) * 2005-12-12 2008-12-17 雅戈泰克股份公司 Powder compositions for inhalation

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Application publication date: 20200103

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