CN111939141A - Novel gel and preparation method and application thereof - Google Patents

Novel gel and preparation method and application thereof Download PDF

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Publication number
CN111939141A
CN111939141A CN202010666860.4A CN202010666860A CN111939141A CN 111939141 A CN111939141 A CN 111939141A CN 202010666860 A CN202010666860 A CN 202010666860A CN 111939141 A CN111939141 A CN 111939141A
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CN
China
Prior art keywords
gel
ethylparaben
povidone
sodium hydroxide
water
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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
CN202010666860.4A
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Chinese (zh)
Inventor
许海玉
肖学凤
李莹
徐刚
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Jiangsu Yinghua Biopharmaceutical Co ltd
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Jiangsu Yinghua Biopharmaceutical Co ltd
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Application filed by Jiangsu Yinghua Biopharmaceutical Co ltd filed Critical Jiangsu Yinghua Biopharmaceutical Co ltd
Priority to CN202010666860.4A priority Critical patent/CN111939141A/en
Publication of CN111939141A publication Critical patent/CN111939141A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/42Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention relates to a novel gel, which comprises the following components in percentage by mass: carbomer 9803-4%; 5-6% of Arabic gum; 4.5 to 5.2 percent of gelatin; 301.2-2% of povidone K; 3-4.2% of polyethylene glycol 400; 18-22% of glycerol; 1-1.5% of sodium hydroxide; 0.04 to 0.05 percent of ethylparaben; 1.2-1.4% of laurocapram; 55-65% of water. The gel provided by the invention has good suspension performance, the viscosity of the gel is sufficient, the medicine components are easy to uniformly mix, and the drug effect is favorably exerted. The gel preparation method of the invention can prepare the gel with the advantages.

Description

Novel gel and preparation method and application thereof
Technical Field
The invention relates to a novel gel, a preparation method thereof and application of the gel.
Background
The gel is applied to a plurality of ointments, such as treatment ointments for osteoarthritis, rheumatoid arthritis, hyperosteogeny, scapulohumeral periarthritis and the like, and other medicinal components are mixed into the gel to form the ointment which is convenient for patients to use.
However, the common gel has insufficient gel viscosity, difficult uniform mixing of the medicine components, poor medicine release performance and influence on the exertion of the medicine effect, or has poor biocompatibility with the skin and small medicine-loading rate.
Disclosure of Invention
In order to solve the technical problems, the invention provides a novel gel, which comprises the following components in percentage by mass:
carbomer 9803-4%; 5-6% of Arabic gum; 4.5 to 5.2 percent of gelatin; 301.2-2% of povidone K; 3-4.2% of polyethylene glycol 400; 18-22% of glycerol; 1-1.5% of sodium hydroxide; 0.04 to 0.05 percent of ethylparaben; 1.2-1.4% of laurocapram; 55-65% of water.
Preferably, the novel gel comprises the following components in percentage by mass:
980400 g of carbomer; 600g of Arabic gum; 500g of gelatin; povidone K30
150g of the total weight of the mixture; 400400 g of polyethylene glycol; 2000g of glycerol; 120g of sodium hydroxide; 5g of ethylparaben; 200g of silicon dioxide powder; 120g of laurocapram; 6000g of water.
The invention also provides a preparation method for preparing the novel gel, which comprises the following steps:
(1) adding ethylparaben into water, heating to dissolve ethylparaben to obtain ethylparaben water solution, and cooling;
(2) adding 1000mL of ethylparaben aqueous solution into glycerol and 400-polyethylene glycol, uniformly mixing, adding a mixture of carbomer 980 and Arabic gum, uniformly stirring, adding 2000mL of gelatin, a mixture of povidone K30 and ethylparaben aqueous solution into the mixed solution, rapidly and uniformly stirring, standing overnight, and reacting for 1 hour under stirring at 50-60 ℃ to prepare a mixed matrix for later use;
(3) adding 1000mL of sodium hydroxide into ethylparaben aqueous solution, stirring to dissolve the sodium hydroxide, adding the solution into the mixed matrix obtained in the step (2), uniformly stirring, and continuously stirring and reacting at 40-50 ℃ for 2 hours to obtain a blank matrix for later use;
(4) heating 2000mL of ethylparaben aqueous solution to 80 ℃, suspending, adding into the blank matrix in the step (3), adding laurocapram, mixing uniformly, drying the blank matrix, drying, and pressing into gel paste to obtain the product.
Preferably, the gel paste in step (4) is divided into 1000 pieces for use.
The invention also provides application of the novel gel in preparation of an ointment, and the novel gel is applied to the ointment as a matrix.
The gel of the invention has enough gel viscosity, easy and uniform mixing of the medicinal components, good medicament release performance and contribution to the exertion of the medicament effect. The gel is a hydrophilic matrix, has large drug-loading rate, and is particularly suitable for Chinese medicinal extracts; the biological compatibility with the skin is good, the stimulation to the skin is small, and allergy is not easy to cause; good ventilation, controllable viscosity and repeated uncovering and sticking. Because the matrix is hydrophilic, the plaster layer contains a certain amount of water, the horny layer of the skin is easy to soften after the plaster is pasted, the hydration effect is increased, and the transdermal absorption of the medicine is facilitated. The gel preparation method of the invention can prepare the gel with the advantages.
Detailed Description
The technical solutions in the embodiments of the present invention are clearly and completely described below, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all embodiments. All other embodiments, which can be obtained by a person skilled in the art without any inventive step based on the embodiments of the present invention, are within the scope of the present invention.
[ example 1 ]
A novel gel comprises the following components in percentage by mass:
carbomer 9804%; 6% of Arabic gum; 5% of gelatin; povidone K301.5%; 4004% of polyethylene glycol; 20% of glycerol; 1.5 percent of sodium hydroxide; 0.05 percent of ethylparaben; 1.4% of laurocapram; 60% of water.
Mixing the above materials, stirring, and drying to obtain the desired gel. Carbomer 980 is a polyacrylic acid crosspolymer which is capable of forming a high viscosity gel at very low concentrations. It has excellent thickening performance, high transparency, high viscosity, strong suspending capacity, excellent suspension stability and swelling property. The gel has good suspension property, sufficient viscosity, easy and uniform mixing of the medicinal components, good release property and contribution to the exertion of the medicinal effect. The gel is a hydrophilic matrix, has large drug-loading rate, and is particularly suitable for Chinese medicinal extracts; the biological compatibility with the skin is good, the stimulation to the skin is small, and allergy is not easy to cause; good ventilation, controllable viscosity and repeated uncovering and sticking. Because the matrix is hydrophilic, the plaster layer contains a certain amount of water, the horny layer of the skin is easy to soften after the plaster is pasted, the hydration effect is increased, and the transdermal absorption of the medicine is facilitated.
[ example 2 ]
Taking 980400 g of carbomer; 600g of Arabic gum; 500g of gelatin; povidone K30150 g; 400400 g of polyethylene glycol; 2000g of glycerol; 120g of sodium hydroxide; 5g of ethylparaben; 120g of laurocapram; 6000g of water. Mixing the above materials, stirring, and drying to obtain the desired gel.
[ example 3 ]
The invention also provides a preparation method for preparing the novel gel, which comprises the following steps:
(1) adding ethylparaben into water, heating to dissolve ethylparaben to obtain ethylparaben water solution, and cooling;
(2) adding 1000mL of ethylparaben aqueous solution into glycerol and polyethylene glycol 400, uniformly mixing, adding a mixture of carbomer 980 and Arabic gum, uniformly stirring, adding 2000mL of gelatin, povidone K30, povidone K90 and ethylparaben aqueous solution into the mixed solution, rapidly and uniformly stirring, standing overnight, and reacting for 1 hour under stirring at 50-60 ℃ to prepare a mixed matrix for later use;
(3) adding 1000mL of sodium hydroxide into ethylparaben aqueous solution, stirring to dissolve the sodium hydroxide, adding the solution into the mixed matrix obtained in the step (2), uniformly stirring, and continuously stirring and reacting at 40-50 ℃ for 2 hours to obtain a blank matrix for later use;
(4) heating 2000mL of ethylparaben aqueous solution to 80 ℃, suspending, adding into the blank matrix in the step (3), adding laurocapram, mixing uniformly, drying the blank matrix, drying, and pressing into gel paste to obtain the product.
Preferably, the gel paste in step (4) is divided into 1000 pieces for use.
The gel meeting the requirements can be prepared by the method, and the prepared gel is a hydrophilic matrix, has large drug-loading rate and is particularly suitable for Chinese medicinal extractum; the biological compatibility with the skin is good, the stimulation to the skin is small, and allergy is not easy to cause; good ventilation, controllable viscosity and repeated uncovering and sticking. Because the matrix is hydrophilic, the plaster layer contains a certain amount of water, the horny layer of the skin is easy to soften after the plaster is pasted, the hydration effect is increased, and the transdermal absorption of the medicine is facilitated.
The invention also provides application of the novel gel in preparation of an ointment, and the novel gel is applied to the ointment as a matrix. The medicinal components can be uniformly mixed in the gel, and the adhesiveness with the gel is good.
The foregoing description has disclosed fully preferred embodiments of the present invention. It should be noted that those skilled in the art can make modifications to the embodiments of the present invention without departing from the scope of the appended claims. Accordingly, the scope of the appended claims is not to be limited to the specific embodiments described above.

Claims (5)

1. The novel gel is characterized by comprising the following components in percentage by mass:
carbomer 9803-4%; 5-6% of Arabic gum; 4.5 to 5.2 percent of gelatin; 301.2-2% of povidone K; 3-4.2% of polyethylene glycol 400; 18-22% of glycerol; 1-1.5% of sodium hydroxide; 0.04 to 0.05 percent of ethylparaben; 1.2-1.4% of laurocapram; 55-65% of water.
2. The novel gel of claim 1, comprising: 980400 g of carbomer; 600g of Arabic gum; 500g of gelatin; povidone K30150 g; povidone K90400 g; 400400 g of polyethylene glycol; 2000g of glycerol; 120g of sodium hydroxide; 5g of ethylparaben; 200g of silicon dioxide powder; 120g of laurocapram; 6000g of water.
3. A process for the preparation of the novel gel of claim 1 or 2, comprising the steps of:
(1) adding ethylparaben into water, heating to dissolve ethylparaben to obtain ethylparaben water solution, and cooling;
(2) adding 1000mL of ethylparaben aqueous solution into glycerol and polyethylene glycol 400, uniformly mixing, adding a mixture of carbomer 980 and Arabic gum, uniformly stirring, adding 2000mL of gelatin, povidone K30, povidone K90 and ethylparaben aqueous solution into the mixed solution, rapidly and uniformly stirring, standing overnight, and reacting for 1 hour under stirring at 50-60 ℃ to prepare a mixed matrix for later use;
(3) adding 1000mL of sodium hydroxide into ethylparaben aqueous solution, stirring to dissolve the sodium hydroxide, adding the solution into the mixed matrix obtained in the step (2), uniformly stirring, and continuously stirring and reacting at 40-50 ℃ for 2 hours to obtain a blank matrix for later use;
(4) heating 2000mL of ethylparaben aqueous solution to 80 ℃, suspending, adding into the blank matrix in the step (3), adding laurocapram, mixing uniformly, drying the blank matrix, drying, and pressing into gel paste to obtain the product.
4. The process for preparing the novel gel of claim 3, wherein the gel paste of step (4) is divided into 1000 pieces for use.
5. Use of the novel gel of claim 1 or 2 in the preparation of an ointment wherein the novel gel is applied to the ointment as a base.
CN202010666860.4A 2020-07-13 2020-07-13 Novel gel and preparation method and application thereof Pending CN111939141A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202010666860.4A CN111939141A (en) 2020-07-13 2020-07-13 Novel gel and preparation method and application thereof

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Application Number Priority Date Filing Date Title
CN202010666860.4A CN111939141A (en) 2020-07-13 2020-07-13 Novel gel and preparation method and application thereof

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114796101A (en) * 2022-03-28 2022-07-29 江苏莹华生物制药有限公司 Sustained-release gel and preparation method and application thereof
CN114931548A (en) * 2022-05-19 2022-08-23 季华实验室 Preparation method of gendarussa wine gel paste

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102526349A (en) * 2010-12-31 2012-07-04 天津药物研究院 Gel ointment as well as preparation method and application thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102526349A (en) * 2010-12-31 2012-07-04 天津药物研究院 Gel ointment as well as preparation method and application thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114796101A (en) * 2022-03-28 2022-07-29 江苏莹华生物制药有限公司 Sustained-release gel and preparation method and application thereof
CN114931548A (en) * 2022-05-19 2022-08-23 季华实验室 Preparation method of gendarussa wine gel paste

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Application publication date: 20201117

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