CN115463098A - Arbidol-containing particles, preparation method and application thereof, and arbidol dry suspension - Google Patents

Arbidol-containing particles, preparation method and application thereof, and arbidol dry suspension Download PDF

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Publication number
CN115463098A
CN115463098A CN202210753035.7A CN202210753035A CN115463098A CN 115463098 A CN115463098 A CN 115463098A CN 202210753035 A CN202210753035 A CN 202210753035A CN 115463098 A CN115463098 A CN 115463098A
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arbidol
sweetener
preparation
type
suspension
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秦杰子
姚燕
贺敦伟
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Zezheng Shanghai Biotechnology Co ltd
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Zezheng Shanghai Biotechnology Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1611—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses

Abstract

The invention relates to the technical field of pharmacy, in particular to an arbidol-containing granule, a preparation method and application thereof, and an arbidol dry suspension. According to the preparation method, silicon dioxide is not used as a flow aid in the preparation process of the abiduoir granules, acetylated distarch adipate and the like are used as a suspending agent to be matched with dry granulation, the flowability of the abiduoir granules is guaranteed, sucrose is not contained in a first sweetening agent added in the dry granulation process, and a second sweetening agent is added after the dry granulation is finished, so that the influence of the contact of the sucrose and the abiduoir on the stability of the abiduoir is avoided, and the technical effect of improving the stability of the abiduoir is realized on the premise of guaranteeing the flowability of the abiduoir granules.

Description

Arbidol-containing particles, preparation method and application thereof, and arbidol dry suspension
Technical Field
The invention relates to the technical field of pharmacy, in particular to an arbidol-containing particle, a preparation method and application thereof, and an arbidol dry suspension.
Background
Arbidol (Arbidol) is a new antiviral drug and an immune stimulant, is a new non-nucleoside antiviral drug with the chemical name of 6-bromo-4- (dimethylaminomethyl) -5-hydroxy-1-methyl-2- (phenylthiomethyl) -1H-indole-3-carboxylic acid ethyl ester hydrate. The main indications are influenza caused by influenza A and B viruses, and the influenza virus also has antiviral activity on other respiratory virus infections. It can prevent the contact, adhesion and fusion of influenza virus coat and host cell membrane, and its action is related to the activation of 2, 5-oligoadenylate synthetase, and it can specifically inhibit the fusion of virus cyst membrane and host cell membrane by activating 2, 5-oligoadenylate synthetase, so as to block the replication of virus. On the other hand, it also induces interferon production by host cells and stimulates humoral responses and phagocytosis by macrophages.
The existing common formulation of the dry arbidol is a suspension, which is usually a direct mixing process or a wet granulation process, and in order to meet the filling requirement, silicon dioxide is generally added in the prescription to improve the fluidity of the material. Meanwhile, a sweetener is added in the preparation process of the suspension. However, the abidol is poorly compatible with the glidants, silicon dioxide, and the sweetener, sucrose, and the addition of silicon dioxide and sweetener can seriously affect the stability of the abidol.
In view of this, the invention is particularly proposed.
Disclosure of Invention
The invention aims to improve the stability of the arbidol in the arbidol particles from the aspect of improving the preparation method of the arbidol particles, and further apply the obtained arbidol particles to the preparation of medicaments taking the arbidol as a main effective component so as to solve the technical problem of poor stability of the arbidol in the medicaments.
In order to solve the technical problems and achieve the purpose, the invention provides the following technical scheme:
in a first aspect, the invention provides a method for preparing granule containing arbidol, which comprises mixing arbidol or its derivatives with a first type of auxiliary material and then dry granulating to obtain granule containing arbidol;
the arbidol derivatives include arbidol hydrochloride;
the first type of auxiliary material is an auxiliary material which does not influence the chemical stability of the arbidol;
the first type of adjunct does not comprise silica.
In an optional embodiment, the mass ratio of the arbidol or the derivative thereof to the first type of excipients is 1:15 to 40.
In alternative embodiments, the first type of adjuvant comprises at least one of a suspending agent, a first sweetener, or a flocculating agent;
the suspending agent is selected from at least one of acetylated distarch adipate, xanthan gum or microcrystalline cellulose-sodium carboxymethylcellulose or a composition thereof;
the first sweetener is at least one of maltodextrin, glucose, sucralose or aspartame or a combination thereof;
the flocculating agent is at least one of sodium chloride, sodium citrate or aluminum chloride or a composition thereof.
In alternative embodiments, the suspending agent is acetylated distarch adipate; the first sweetener is maltodextrin and sucralose; the flocculant is sodium chloride;
in an optional embodiment, the mass ratio of the abidotol or the derivative thereof to the first type of auxiliary material is 1:15 to 35.
In an alternative embodiment, the mass ratio of arbidol or its derivatives to acetylated distarch adipate, maltodextrin, sodium chloride and sucralose is 1:3 to 7:10 to 30:0.5 to 2:0.1 to 1.
In a second aspect, the present invention provides an abiduole-containing particle prepared by the method of any one of the preceding embodiments.
In a third aspect, the present invention provides the use of the abidol-containing particles described in the previous embodiments in (a) or (b):
(a) Preparing a medicament for treating viral upper respiratory tract infection;
(b) Preparing the medicine for preventing or treating influenza.
In alternative embodiments, the pharmaceutical dosage form comprises a suspension, tablet, or capsule.
Preferably, the suspension is a dry suspension.
In a fourth aspect, the invention provides a preparation method of an aristol dry suspension, wherein the aristol-containing granules described in the foregoing embodiment are mixed with a second type of auxiliary material to obtain the aristol dry suspension.
Preferably, the second type of adjuvant comprises at least one of a second sweetener or a flavoring agent.
Preferably, the second sweetener is selected from at least one of sucrose, glucose or maltose or a combination thereof.
Preferably, the flavoring agent is selected from at least one of fruit powder essence, vanilla essence or mint essence or a combination thereof.
Preferably, the mass ratio of the abiduoir-containing particles to the second sweetener and flavoring agent is 1:10 to 35:0.1 to 1.
According to the invention, silicon dioxide is not used as a flow aid in the preparation process of the abiduole granules, and acetylated distarch adipate and the like are used as a suspending agent to be matched with dry granulation, so that the flowability of the abiduole granules is ensured, sucrose is not contained in the first sweetener added in the dry granulation process, and the second sweetener is added after the dry granulation is completed, so that the influence of the contact of the sucrose and the abiduole on the stability of the abiduole is avoided, and the technical effect of improving the stability of the abiduole is realized on the premise of ensuring the flowability of the abiduole granules.
Detailed Description
In order to make the objects, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the embodiments of the present invention, and it is obvious that the described embodiments are some embodiments of the present invention, but not all embodiments. Thus, the following detailed description of the embodiments of the present invention is not intended to limit the scope of the invention as claimed, but is merely representative of selected embodiments of the invention. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
In a certain embodiment, in a first aspect, the present invention provides a method for preparing a granule containing abidol, comprising mixing the abidol or a derivative thereof with a first type of excipient and dry granulating to obtain a granule containing abidol;
the arbidol derivatives include arbidol hydrochloride;
the first type of auxiliary material is an auxiliary material which does not influence the chemical stability of the arbidol;
the first type of adjuvant does not include silica.
In an optional embodiment, the mass ratio of the abidotol or the derivative thereof to the first type of auxiliary material is 1:15 to 40.
In alternative embodiments, the first type of adjuvant comprises at least one of a suspending agent, a first sweetener, or a flocculating agent;
the suspending agent is selected from at least one of acetylated distarch adipate, xanthan gum or microcrystalline cellulose-sodium carboxymethylcellulose or a composition thereof;
the first sweetener is at least one of maltodextrin, glucose, sucralose or aspartame or a combination thereof;
the flocculating agent is at least one selected from sodium chloride, sodium citrate or aluminum chloride or a composition thereof.
In alternative embodiments, the suspending agent is acetylated distarch adipate; the first sweetener is maltodextrin and sucralose; the flocculant is sodium chloride.
In an optional embodiment, the mass ratio of the arbidol or the derivative thereof to the first type of excipients is 1:15 to 35.
In an alternative embodiment, the mass ratio of arbidol or derivative thereof to acetylated distarch adipate, maltodextrin, sodium chloride and sucralose is 1:3 to 7:10 to 30:0.5 to 2:0.1 to 1.
In a second aspect, the present invention provides an abiduole-containing particle prepared by the method of any one of the preceding embodiments.
In a third aspect, the present invention provides the use of the abidol-containing particles described in the previous embodiments in (a) or (b):
(a) Preparing a medicament for treating viral upper respiratory tract infection;
(b) Preparing the medicine for preventing or treating influenza.
In alternative embodiments, the pharmaceutical dosage form comprises a suspension, tablet, or capsule.
Preferably, the suspension is a dry suspension.
In a fourth aspect, the present invention provides a method for preparing an abiduoir dry suspension, wherein the ariduoir-containing particles described in the foregoing embodiment are mixed with a second type of excipients to obtain the ariduoir dry suspension.
Preferably, the second type of adjuvant comprises at least one of a second sweetener or a flavoring agent.
Preferably, the second sweetener is selected from at least one of sucrose, glucose or maltose or a combination thereof.
Preferably, the flavoring agent is selected from at least one of fruit powder essence, vanilla essence or mint essence or a combination thereof.
Preferably, the mass ratio of the abidopol-containing particles to the second sweetener and flavoring agent is 1:10 to 35:0.1 to 1.
Some embodiments of the invention are described in detail below. The embodiments described below and the features of the embodiments can be combined with each other without conflict.
Example 1
This example provides a preparation method of an abiduol hydrochloride dry suspension, which includes the following components:
name (R) mg/bag Function of
Arbidol hydrochloride 51.8 API
Acetylated distarch adipate 259 Suspending aid
Maltodextrin 1500 First sweetener
Sucrose 1690.4 A second sweetener
Sodium chloride 53.7 Flocculating agent
Sucralose 8.1 First sweetener
Banana powder essence 24.8 Flavoring agent
Cherry powder essence 12.2 Flavoring agent
Total up to 3600 N/A
The preparation method comprises the following steps:
according to the use amounts of the components in the table above, abiduol hydrochloride, acetylated distarch adipate, maltodextrin, sodium chloride and sucralose are weighed, after mixing, dry granulation is carried out by using a 120G dry press to obtain abiduol hydrochloride particles, then the abiduol hydrochloride particles are mixed with sucrose, banana powder essence and cherry powder essence, and finally, the abiduol hydrochloride suspension is obtained by packaging with a double-aluminum composite film.
Example 2
This example differs from example 1 in that the actual amounts used are shown in the following table:
Figure BDA0003718957530000061
Figure BDA0003718957530000071
example 3
This example differs from example 1 in that the actual amounts used are shown in the following table:
name (R) mg/bag Function of
Arbidol hydrochloride 51.8 API
Acetylated distarch adipate 362.6 Suspending aid
Maltodextrin 1558 A first sweetener
Sucrose 1813 A second sweetener
Sodium chloride 103.6 Flocculating agent
Sucralose 51.8 A first sweetener
Banana powder essence 31.8 Flavoring agent
Cherry powder essence 20 Flavoring agent
Total up to 3992.6 N/A
Comparative example 1
Figure BDA0003718957530000072
Figure BDA0003718957530000081
The preparation method comprises the following steps:
according to the using amount of the components in the table, the abiduol hydrochloride, the acetylated distarch adipate, the maltodextrin, the sucrose, the sodium chloride, the sucralose and the titanium dioxide are weighed, after mixing, a 120G dry press is used for dry granulation to obtain the abiduol hydrochloride particles, then the abiduol hydrochloride particles are mixed with the banana powder essence and the cherry powder essence, and finally the abiduol hydrochloride suspension is obtained by packaging with a double-aluminum composite film.
Comparative example 2
Name(s) mg/bag Action
Arbidol hydrochloride 51.8 API
Acetylated distarch adipate 259 Suspending agent
Maltodextrin 1500 First sweetener
Sucrose 1690.4 First sweetener
Sodium chloride 53.7 Flocculating agent
Sucralose 8.1 A first sweetener
Titanium dioxide 50 Light-shading agent
Banana powder essence 24.8 Flavoring agent
Cherry powder essence 12.2 Flavoring agent
Total up to 3650 N/A
The preparation method comprises the following steps:
according to the using amounts of the components in the table, abidopol hydrochloride, acetylated distarch adipate, maltodextrin, sucrose, sodium chloride, sucralose and titanium dioxide are weighed, mixed, dry-granulated by using a 120G dry press to obtain abidopol hydrochloride particles, then the abidopol hydrochloride particles are mixed with banana powder essence and cherry powder essence, dried, and finally packaged by adopting a double-aluminum composite film to obtain the abidopol hydrochloride suspension.
Comparative example 3
The comparative example provides a preparation method of an arbidol hydrochloride dry suspension, and the components of the arbidol hydrochloride dry suspension are as follows:
name (R) mg/bag
Abidol hydrochloride 51.8
Acetylated distarch adipate 259
Maltodextrin 1500
Sucrose 1690.4
Silicon dioxide 50
Sodium chloride 53.7
Sucralose 8.1
Banana powder essence 24.8
Cherry powder essence 12.2
The preparation method comprises the following steps:
weighing all the components according to the using amounts of the components in the table, uniformly mixing, and finally packaging by adopting a double-aluminum composite film to obtain the arbidol hydrochloride suspension.
Comparative example 4
Figure BDA0003718957530000091
Figure BDA0003718957530000101
The preparation method comprises the following steps:
according to the using amount of the components in the table, the abiduol hydrochloride, the acetylated distarch adipate, the maltodextrin, the sucrose, the sodium chloride, the sucralose and the titanium dioxide are weighed, after mixing, a 120G dry press is used for dry granulation to obtain the abiduol hydrochloride particles, then the abiduol hydrochloride particles are mixed with the banana powder essence and the cherry powder essence, and finally the abiduol hydrochloride suspension is obtained by packaging with a double-aluminum composite film.
Comparative example 5
Figure BDA0003718957530000102
Figure BDA0003718957530000111
The preparation method comprises the following steps:
according to the using amounts of the components in the table, abidopol hydrochloride, acetylated distarch adipate, maltodextrin, sucrose sodium chloride, sucralose and titanium dioxide are weighed, mixed, dry granulation is carried out by using a 120G dry press to obtain the abidopol hydrochloride particles, then the abidopol hydrochloride particles are mixed with banana powder essence and cherry powder essence, drying is carried out, and finally double aluminum composite films are adopted for packaging to obtain the abidopol hydrochloride suspension.
Examples of the experiments
The chemical stability of the abiduol hydrochloride suspensions prepared in example 1 and comparative examples 1-5 above was compared and the experimental procedure was as follows:
diluent agent: ethanol-0.1 mol/L hydrochloric acid solution (volume ratio 30.
Test solution: taking 1 bag of the Arbidol hydrochloride suspension, quantitatively transferring the content into a 200ml measuring flask, adding about 100ml of diluent, carrying out ultrasonic treatment for 15 minutes to dissolve, cooling, diluting to a scale with the diluent, shaking up, taking a proper amount, centrifuging (15000rpm, 10 minutes) and taking a supernatant.
Control solution: precisely measuring 1ml of the test solution, placing the test solution into a 200ml measuring flask, diluting the test solution to a scale with a diluent, and shaking up.
Chromatographic conditions are as follows: octadecylsilane bonded silica was used as a packing (Welch Utimate LP-C18, 4.6 mm. Times.150mm, 5 μm or equivalent performance column); dissolving sodium heptanesulfonate solution (1.1 g of sodium heptanesulfonate and 5.9g of ammonium perchlorate) in a proper amount of water, adding 13.2ml of triethylamine, uniformly mixing, diluting with water to 1000ml, and adjusting the pH value to 3.0 by using phosphoric acid) -methanol (volume ratio of 30; the detection wavelength is 255nm; the column temperature is 30 ℃; the flow rate was 1.0ml per minute; the injection volume was 20. Mu.l.
The determination method comprises the following steps: precisely measuring the test solution and the reference solution, respectively injecting into a liquid chromatograph, and recording the chromatogram.
Limitation: if an impurity peak exists in a chromatogram of the test solution, the peak area of a single impurity is not more than the main peak area (0.5%) of the control solution, the sum of the peak areas of the impurities is not more than 3 times (1.5%) of the main peak area of the control solution, and less than 0.1% of the impurities are ignored.
The auxiliary material which does not influence the chemical stability of the Abadol in the invention means that after a certain auxiliary material is added, the peak area of a single impurity obtained by the chemical stability detection method can directly fail to meet the condition.
Accelerated conditions for the standing stability were 40 ℃ and humidity 75% RH, and the results of detection of substances related to each embodiment after acceleration were as follows:
example 1 Day 0 Accelerated condition of 1 month
RRT1.8(％) 0.1 0.3
RRT2.1(％) <0.05 0.1
Total impurities (%) 0.2 0.6
Comparative example 1 Day 0 Accelerated condition of 1 month
RRT1.8(％) 0.1 0.2
RRT2.1(％) <0.05 0.3
Total hetero (%) 0.2 0.7
Figure BDA0003718957530000121
Figure BDA0003718957530000131
Comparative example 3 Day 0 Accelerated condition of 1 month
RRT1.8(％) 0.1 0.9
RRT2.1(％) <0.05 1.6
Total impurities (%) 0.2 3.0
Comparative example 4 Day 0 Accelerated conditions for 10 days
RRT1.8(％) 0.1 1.2
RRT2.1(％) <0.05 0.2
Total impurities (%) 0.4 1.8
Comparative example 5 Day 0 Accelerated conditions for 10 days
RRT1.8(％) 0.2 1.6
RRT2.1(％) <0.05 0.2
Total impurities (%) 0.4％ 2.2
By comparing the results of the above examples and comparative examples, it can be found that the arbidol-containing granules, the preparation method and the application thereof, and the arbidol dry suspension provided by the invention are prepared by dry granulation, so that the flowability of the arbidol granules is ensured, meanwhile, the sweetener is added, the condition that the stability of arbidol is influenced by the direct contact of sucrose and arbidol is avoided, the conventional glidant silicon dioxide is removed in the examples, and the flowability of the arbidol granules is not influenced, so that the technical effect of improving the stability of arbidol is realized on the premise of ensuring the flowability of the arbidol granules.
Finally, it should be noted that: the above embodiments are only used to illustrate the technical solution of the present invention, and not to limit the same; while the invention has been described in detail and with reference to the foregoing embodiments, it will be understood by those skilled in the art that: the technical solutions described in the foregoing embodiments may still be modified, or some or all of the technical features may be equivalently replaced; and the modifications or the substitutions do not make the essence of the corresponding technical solutions depart from the scope of the technical solutions of the embodiments of the present invention.

Claims (10)

1. The preparation method of the granule containing the abiduole is characterized by comprising the following steps of mixing the abiduole or the derivatives thereof with a first type of auxiliary materials, and performing dry granulation to obtain the granule containing the abiduole;
the arbidol derivatives include arbidol hydrochloride;
the first type of auxiliary material is an auxiliary material which does not influence the chemical stability of the arbidol;
the first type of adjunct does not comprise silica.
2. The preparation method according to claim 1, wherein the mass ratio of the arbidol or the derivative thereof to the first type of auxiliary material is 1:15 to 40.
3. The method of claim 1, wherein the first type of excipient comprises at least one of a suspending agent, a first sweetener, or a flocculating agent;
the suspending agent is selected from at least one of acetylated distarch adipate, xanthan gum or microcrystalline cellulose-sodium carboxymethyl cellulose or a composition thereof;
the first sweetener is at least one of maltodextrin, glucose, sucralose or aspartame or a combination thereof;
the flocculating agent is at least one selected from sodium chloride, sodium citrate or aluminum chloride or a composition thereof.
4. The method of claim 3, wherein the suspending agent is acetylated distarch adipate; the first sweetener is maltodextrin and sucralose; the flocculant is sodium chloride.
5. The preparation method according to claim 4, wherein the mass ratio of the arbidol or the derivative thereof to the first auxiliary material is 1:15 to 35.
6. The method according to claim 4, wherein the mass ratio of the arbidol or the derivative thereof to the acetylated distarch adipate, the maltodextrin, the sodium chloride and the sucralose is 1:3 to 7:10 to 30:0.5 to 2:0.1 to 1.
7. Arbidol-containing particles prepared by the method of any one of claims 1 to 6.
8. Use of the abidopol-containing particles as claimed in claim 7 in (a) or (b):
(a) Preparing a medicament for treating viral upper respiratory tract infection;
(b) Preparing the medicine for preventing or treating influenza.
9. The use of claim 8, wherein the pharmaceutical dosage form comprises a suspension, a tablet or a capsule;
preferably, the suspension is a dry suspension.
10. A preparation method of the aridol dry suspension is characterized in that the aridol-containing particles as claimed in claim 7 are mixed with a second type of auxiliary materials to obtain the aridol dry suspension;
preferably, the second type of adjuvant comprises at least one of a second sweetener or flavoring agent;
preferably, the second sweetener is selected from at least one of sucrose, glucose or maltose or a combination thereof;
preferably, the flavoring agent is selected from at least one of fruit powder essence, vanilla essence or mint essence or a combination thereof;
preferably, the mass ratio of the abidopol-containing particles to the second sweetener and flavoring agent is 1:10 to 35:0.1 to 1.
CN202210753035.7A 2022-06-28 2022-06-28 Arbidol-containing particles, preparation method and application thereof, and arbidol dry suspension Pending CN115463098A (en)

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