CN111053735A - Cold compress gel for treating insomnia - Google Patents

Cold compress gel for treating insomnia Download PDF

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Publication number
CN111053735A
CN111053735A CN202010117232.0A CN202010117232A CN111053735A CN 111053735 A CN111053735 A CN 111053735A CN 202010117232 A CN202010117232 A CN 202010117232A CN 111053735 A CN111053735 A CN 111053735A
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CN
China
Prior art keywords
weight
parts
cold compress
mirtazapine
compress gel
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
CN202010117232.0A
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Chinese (zh)
Inventor
陈济世
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.)
Shanghai Jieping Hospital Management Co Ltd
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Shanghai Jieping Hospital Management 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 Shanghai Jieping Hospital Management Co Ltd filed Critical Shanghai Jieping Hospital Management Co Ltd
Priority to CN202010117232.0A priority Critical patent/CN111053735A/en
Publication of CN111053735A publication Critical patent/CN111053735A/en
Pending legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives

Abstract

The invention relates to a cold compress gel for treating insomnia, which consists of 0.5-3 parts by weight of mirtazapine, 1-5 parts by weight of melatonin, 0.1-1 part by weight of carbomer and 80-95 parts by weight of water. Mirtazapine has proven to be a safe, well tolerated and effective antidepressant. The mirtazapine and melatonin of the invention have synergistic effect in improving sleep by external application. In particular, the side effects of mirtazapine can be reduced.

Description

Cold compress gel for treating insomnia
Technical Field
The invention relates to a cold compress gel for treating insomnia.
Background
Mirtazapine, a class of antidepressants, is known as a noradrenergic and specific 5-hydroxytryptamine antidepressant (NaSSA) which enhances both noradrenergic and 5-hydroxytryptamine neurotransmission by antagonizing the presynaptic α 2-adrenergic receptor, while blocking the postsynaptic 5-hydroxytryptamine (5-HT2 and 5-HT3) receptors.
Dosage units for oral administration of mirtazapine are generally considered to be in the form of conventional tablets. The concentration of the pharmaceutically active ingredient may range up to 15 to 45 mg mirtazapine. These known tablets are generally acceptable in terms of their pharmaceutical activity, and mirtazapine has proven to be a safe, well-tolerated and effective antidepressant. Nevertheless, as seems unavoidable in the field of antidepressant drugs, mirtazapine also needs improvement. In particular, improvements are needed in reducing side effects. For mirtazapine, these side effects mainly include appetite enhancement, weight gain, daytime sleepiness, sexual dysfunction, gastrointestinal side effects, edema, restless legs, dry mouth, excessive sedation.
More specifically, mirtazapine is also needed to further enhance its beneficial effects on cold compress.
Disclosure of Invention
Aiming at the defects in the prior art, the invention aims to provide a cold compress gel for treating insomnia, wherein the cold compress gel consists of 0.5-3 parts by weight of mirtazapine, 1-5 parts by weight of melatonin, 0.1-1 part by weight of carbomer and 80-95 parts by weight of water.
The mass ratio of the mirtazapine to the melatonin is 1: 1-4.
The cold compress gel further comprises 0.1-1 weight part of silicon dioxide.
The cold compress gel also comprises 0.1-1 weight part of ethanol.
The cold compress gel also comprises 0.1-1 weight part of preservative.
The cold compress gel also comprises 0.1-1 weight part of emulsifier.
The emulsifier is one or two of oleic acid polyoxyethylene ether and polyethylene glycol fatty acid ester. A preparation method of a cold compress gel for treating insomnia comprises the following steps:
adding 0.1-1 part by weight of carbomer into 80-95 parts by weight of water, and stirring at high speed until the carbomer is uniformly mixed;
adding 0.5-3 parts by weight of mirtazapine and 1-5 parts by weight of melatonin, and stirring at high speed until the mixture is uniformly mixed;
packaging to obtain the cold compress gel.
The mass ratio of the mirtazapine to the melatonin is 1: 1-4.
A method for preparing cold compress gel for treating insomnia comprises adding 0.1-1 weight part of emulsifier into 80-95 weight parts of water, and stirring at high speed to obtain paste;
adding 0.1-1 weight part of silicon dioxide, 0.1-1 weight part of preservative and 0.1-1 weight part of carbomer, and stirring at high speed until the mixture is uniformly mixed;
adding 0.5-3 parts by weight of mirtazapine and 1-5 parts by weight of melatonin, and stirring at high speed until the mixture is uniformly mixed;
adding 0.1-1 weight part of ethanol, stirring, and grinding with a grinder;
vacuumizing and degassing;
and (5) packaging to obtain the finished product.
Mirtazapine has proven to be a safe, well tolerated and effective antidepressant. Nevertheless, as seems unavoidable in the field of antidepressant drugs, mirtazapine also needs improvement. In particular, improvements are needed in reducing side effects. These side effects mainly include appetite enhancement, weight gain, edema, restless legs, dry mouth, excessive sedation.
The mirtazapine and melatonin of the invention have synergistic effect in improving sleep by external application. In particular, the side effects of mirtazapine can be reduced. Mirtazapine has unexpected technical effects when used together with melatonin.
The above-described and other features, aspects, and advantages of the present application will become more apparent with reference to the following detailed description.
Detailed Description
In order to make the objects, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions of the embodiments of the present invention will be clearly and completely described below. It is to be understood that the embodiments described are only a few embodiments of the present invention, and not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the described embodiments of the invention without any inventive step, are within the scope of protection of the invention.
Unless defined otherwise, technical or scientific terms used herein shall have the ordinary meaning as understood by one of ordinary skill in the art to which this invention belongs. The use of "first," "second," and similar terms in the description and claims of the present application do not denote any order, quantity, or importance, but rather the terms are used to distinguish one element from another. Also, the use of the terms "a" or "an" and the like do not denote a limitation of quantity, but rather denote the presence of at least one.
A cold compress gel for treating insomnia, which consists of 0.5-3 parts by weight of mirtazapine, 1-5 parts by weight of melatonin, 0.1-1 part by weight of carbomer and 80-95 parts by weight of water.
The mass ratio of the mirtazapine to the melatonin is 1: 1-4.
The cold compress gel further comprises 0.1-1 weight part of silicon dioxide.
The cold compress gel also comprises 0.1-1 weight part of ethanol.
The cold compress gel also comprises 0.1-1 weight part of preservative.
The cold compress gel also comprises 0.1-1 weight part of emulsifier.
The emulsifier is one or two of oleic acid polyoxyethylene ether and polyethylene glycol fatty acid ester. A preparation method of a cold compress gel for treating insomnia comprises the following steps:
adding 0.1-1 part by weight of carbomer into 80-95 parts by weight of water, and stirring at high speed until the carbomer is uniformly mixed;
adding 0.5-3 parts by weight of mirtazapine and 1-5 parts by weight of melatonin, and stirring at high speed until the mixture is uniformly mixed;
packaging to obtain the cold compress gel.
The mass ratio of the mirtazapine to the melatonin is 1: 1-4.
DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION
Preparation of cold compress gel 1:
adding 0.5 part by weight of carbomer into 90 parts by weight of water, and stirring at high speed until the carbomer is uniformly mixed; adding 1 weight part of mirtazapine and 3 weight parts of melatonin, and stirring at a high speed until the mixture is uniformly mixed to obtain the cold compress gel.
Preparation of cold compress gel 2:
adding 0.5 part by weight of carbomer into 90 parts by weight of water, and stirring at high speed until the carbomer is uniformly mixed; adding 3 parts by weight of mirtazapine and 1.5 parts by weight of melatonin, and stirring at high speed until the mixture is uniformly mixed to obtain the cold compress gel.
Preparation of cold compress gel 3:
adding 0.5 part by weight of carbomer into 90 parts by weight of water, and stirring at high speed until the carbomer is uniformly mixed; adding 0.5 weight part of mirtazapine and 3 weight parts of melatonin, and stirring at a high speed until the mixture is uniformly mixed to obtain the cold compress gel.
Test objects: each group had 20 subjects to be treated (10 males and 10 females), and all subjects completed the trial. The cold compress gel of the invention is used before sleeping every day (the mass ratio of mirtazapine to melatonin is 1: 0.5, 1: 3 and 1: 6 respectively, and the amount of mirtazapine in the cold compress gel is 60 mg). The duration of treatment was 90 days, and the 90-day weight change and sleep-aiding effect of the test subjects were measured. If a subject is not therapeutically effective, the two single doses are administered to the subject at least two weeks apart. Through experiments, the mass ratio of mirtazapine to melatonin is 1: the subject of 3 had similar weight changes as placebo at 0.5% and 0.8%, respectively, while the other mass ratios had larger changes at 8.3% and 9.4%, respectively, which are closer to the data of about 10% for mirtazapine disclosed. According to the data fed back by the test subjects, as with the mirtazapine tablets, the mass ratio of mirtazapine to melatonin of the invention is 1: 0.5, 1: 3, 1: 6 has good curative effect on helping sleep.
While there have been shown and described what are at present considered the fundamental principles and essential features of the invention and its advantages, it will be apparent to those skilled in the art that the invention is not limited to the details of the foregoing exemplary embodiments, but is capable of other specific forms without departing from the spirit or essential characteristics thereof. The present embodiments are therefore to be considered in all respects as illustrative and not restrictive, the scope of the invention being indicated by the appended claims rather than by the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein.
Furthermore, it should be understood that although the present description refers to embodiments, not every embodiment may contain only a single embodiment, and the description is given here only for clarity, and those skilled in the art should integrate the description, and the embodiments may be combined appropriately to form other embodiments understood by those skilled in the art.

Claims (10)

1. The cold compress gel for treating insomnia is characterized by comprising 0.5-3 parts by weight of mirtazapine, 1-5 parts by weight of melatonin, 0.1-1 part by weight of carbomer and 80-95 parts by weight of water.
2. The cold compress gel for treating insomnia according to claim 1, wherein the mass ratio of mirtazapine to melatonin is 1: 1-4.
3. The cold compress gel for treating insomnia according to claim 1, further comprising 0.1-1 parts by weight of silicon dioxide.
4. The cold compress gel for treating insomnia according to claim 1, further comprising 0.1-1 parts by weight of ethanol.
5. The cold compress gel for treating insomnia according to claim 1, further comprising 0.1-1 parts by weight of a preservative.
6. The cold compress gel for treating insomnia according to claim 1, further comprising 0.1-1 parts by weight of an emulsifier.
7. The cold compress gel for treating insomnia according to claim 6, wherein said emulsifier is one or two selected from polyoxyethylene oleate, polyethylene glycol fatty acid ester.
8. A preparation method of cold compress gel for treating insomnia is characterized by comprising the following steps:
adding 0.1-1 part by weight of carbomer into 80-95 parts by weight of water, and stirring at high speed until the carbomer is uniformly mixed;
adding 0.5-3 parts by weight of mirtazapine and 1-5 parts by weight of melatonin, and stirring at high speed until the mixture is uniformly mixed;
packaging to obtain the cold compress gel.
9. The preparation method of the cold compress gel for treating insomnia as claimed in claim 8, wherein the mass ratio of mirtazapine to melatonin is 1: 1-4.
10. A preparation method of cold compress gel for treating insomnia is characterized by comprising the following steps:
adding 0.1-1 weight part of emulsifier into 80-95 weight parts of water, and stirring at high speed to form paste;
adding 0.1-1 weight part of silicon dioxide, 0.1-1 weight part of preservative and 0.1-1 weight part of carbomer, and stirring at high speed until the mixture is uniformly mixed;
adding 0.5-3 parts by weight of mirtazapine and 1-5 parts by weight of melatonin, and stirring at high speed until the mixture is uniformly mixed;
adding 0.1-1 weight part of ethanol, stirring, and grinding with a grinder;
vacuumizing and degassing;
packaging to obtain the cold compress gel.
CN202010117232.0A 2020-02-25 2020-02-25 Cold compress gel for treating insomnia Pending CN111053735A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202010117232.0A CN111053735A (en) 2020-02-25 2020-02-25 Cold compress gel for treating insomnia

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN202010117232.0A CN111053735A (en) 2020-02-25 2020-02-25 Cold compress gel for treating insomnia

Publications (1)

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CN111053735A true CN111053735A (en) 2020-04-24

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113262260A (en) * 2021-06-05 2021-08-17 亳州益智健康产业有限公司 Cold compress gel for treating insomnia
CN116139070A (en) * 2022-12-23 2023-05-23 杭州健崃生物科技有限公司 Sleep-aiding cold compress gel and preparation method thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5552428A (en) * 1992-06-24 1996-09-03 Instituto Farmacologico Lombardo-Iflo, S.A.S. Compounds effective in the treatment of circadian rhythms and related disorders, the novel pharmaceutical preparations and novel method of application
US5891903A (en) * 1996-12-06 1999-04-06 Societe L'oreal S.A. Use of melatonin in a composition for stabilizing hydrophilic gelling polymers
CN1395487A (en) * 2000-02-11 2003-02-05 阿克佐诺贝尔公司 The use of mirtazapine for treatment of sleep disorders
CN1942191A (en) * 2004-04-21 2007-04-04 奥尔加侬股份有限公司 Pharmaceutical composition comprising a salt of mirtazapine
US20130253449A1 (en) * 2010-12-07 2013-09-26 Yutoku Pharmaceutical Industries Co., Ltd. Noradrenergic and specific serotonergic antidepressant-containing transdermal patch

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5552428A (en) * 1992-06-24 1996-09-03 Instituto Farmacologico Lombardo-Iflo, S.A.S. Compounds effective in the treatment of circadian rhythms and related disorders, the novel pharmaceutical preparations and novel method of application
US5891903A (en) * 1996-12-06 1999-04-06 Societe L'oreal S.A. Use of melatonin in a composition for stabilizing hydrophilic gelling polymers
CN1395487A (en) * 2000-02-11 2003-02-05 阿克佐诺贝尔公司 The use of mirtazapine for treatment of sleep disorders
CN1942191A (en) * 2004-04-21 2007-04-04 奥尔加侬股份有限公司 Pharmaceutical composition comprising a salt of mirtazapine
US20130253449A1 (en) * 2010-12-07 2013-09-26 Yutoku Pharmaceutical Industries Co., Ltd. Noradrenergic and specific serotonergic antidepressant-containing transdermal patch

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
刘绍贵: "《中成药购药用药指南》", 31 July 2007, 湖南科学技术出版社 , pages: 191 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113262260A (en) * 2021-06-05 2021-08-17 亳州益智健康产业有限公司 Cold compress gel for treating insomnia
CN116139070A (en) * 2022-12-23 2023-05-23 杭州健崃生物科技有限公司 Sleep-aiding cold compress gel and preparation method thereof

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