CN112043788A - A topical pharmaceutical composition for treating gout and preparation method thereof - Google Patents

A topical pharmaceutical composition for treating gout and preparation method thereof Download PDF

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CN112043788A
CN112043788A CN202011084696.2A CN202011084696A CN112043788A CN 112043788 A CN112043788 A CN 112043788A CN 202011084696 A CN202011084696 A CN 202011084696A CN 112043788 A CN112043788 A CN 112043788A
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parts
root
treating gout
mixture
pharmaceutical composition
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李智民
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Jilin Shurun Pharmaceutical Co ltd
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Jilin Shurun Pharmaceutical Co ltd
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
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    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/30Extraction of the material
    • A61K2236/33Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
    • A61K2236/331Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using water, e.g. cold water, infusion, tea, steam distillation, decoction
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    • A61K2236/30Extraction of the material
    • A61K2236/39Complex extraction schemes, e.g. fractionation or repeated extraction steps
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • A61K2236/50Methods involving additional extraction steps
    • A61K2236/51Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying

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Abstract

The invention discloses an external pharmaceutical composition for treating gout and a preparation method thereof, relating to the technical field of external pharmaceutical compositions, wherein the external pharmaceutical composition for treating gout comprises the following raw material components: lily, Chinese pulsatilla root, divaricate saposhnikovia root, dahurian angelica root, Mongolian snakegourd root, menthol, borneol, azone, 1, 3-butanediol, 1, 2-pentanediol, carbomer, diethanolamine, dipotassium glycyrrhizinate, methyl paraben, glycerol and water. The external medicine composition for treating gout provided by the invention adopts lily, Chinese pulsatilla root, divaricate saposhnikovia root, dahurian angelica root, mongolian snakegourd root, menthol and borneol as the raw material components of the traditional Chinese medicine, is green and natural, does not contain hormone, can be used for a long time, and can efficiently relieve pain by the effective components; the menthol, the borneol, the azone, the 1, 3-butanediol and the 1, 2-pentanediol are used as the raw material components of the transdermal agent, so that the active ingredients of the traditional Chinese medicine can be quickly transdermally penetrated, the drug effect is exerted, and the effect of quickly curing and relieving pain is achieved.

Description

A topical pharmaceutical composition for treating gout and preparation method thereof
Technical Field
The invention relates to the technical field of external pharmaceutical compositions, in particular to an external pharmaceutical composition for treating gout and a preparation method thereof.
Background
Gout is a common and complex type of arthritis that can develop in all ages. Patients with gout often have sudden joint pain at night, the joint is in urgent attack, severe pain, edema, red swelling and inflammation appear at the joint, and the pain is slowly relieved until the pain disappears for days or weeks.
At present, no external medicine and health care product batch taking gout as a main treatment function exists in the market. Only other analgesic topical products: the western medicine analgesic external product is mainly a non-steroidal anti-inflammatory product, mainly has anti-inflammatory effect, has a certain analgesic effect, but has an undesirable analgesic effect on gout and cannot be used for a long time. The traditional Chinese medicine pain-relieving external product mainly takes rheumatic bone pain as main material, and the pain-relieving effect on gout can not meet the clinical requirement.
The pain in acute stage of gout is severe, rapid pain relief is needed, the transdermal speed of the product is high, and the existing ointment product basically takes azone as a main transdermal agent and has poor transdermal auxiliary effect with traditional Chinese medicine macromolecules.
Disclosure of Invention
Aiming at the defects in the prior art, the invention provides an external pharmaceutical composition for treating gout and a preparation method thereof.
The external medicine composition for treating gout comprises the following raw material components: lily, Chinese pulsatilla root, divaricate saposhnikovia root, dahurian angelica root, Mongolian snakegourd root, menthol, borneol, azone, 1, 3-butanediol, 1, 2-pentanediol, carbomer, diethanolamine, dipotassium glycyrrhizinate, methyl paraben, glycerol and water.
Preferably, the external pharmaceutical composition for treating gout comprises the following raw material components in parts by weight: 5-40 parts of lily, 10-40 parts of Chinese pulsatilla root, 5-30 parts of divaricate saposhnikovia root, 5-20 parts of angelica dahurica, 10-30 parts of trichosanthes root, 3-10 parts of menthol, 4-20 parts of borneol, 0.5-2 parts of azone, 1-5 parts of 1, 3-butanediol, 1, 2-pentanediol, 0.8-1.2 parts of carbomer, 0.02-0.04 part of diethanolamine, 0.08-0.12 part of dipotassium glycyrrhizinate, 0.5-2 parts of methylparaben, 2.5-3.5 parts of glycerol and 50-80 parts of water.
Further preferably, the external pharmaceutical composition for treating gout comprises the following raw materials in parts by weight: 35 parts of lily, 25 parts of Chinese pulsatilla root, 10 parts of divaricate saposhnikovia root, 10 parts of angelica dahurica, 13 parts of trichosanthes root, 3 parts of menthol, 4 parts of borneol, 1 part of azone, 4 parts of 1, 3-butanediol, 2 parts of 1, 2-pentanediol, 1 part of carbomer, 0.03 part of diethanolamine, 0.1 part of dipotassium glycyrrhizinate, 1.25 parts of methyl hydroxybenzoate, 3 parts of glycerol and 70 parts of water.
In the raw material components, lily, Chinese pulsatilla root, divaricate saposhnikovia root, dahurian angelica root, Mongolian snakegourd root, menthol and borneol are used as traditional Chinese medicine components to provide effective components for treating gout; menthol, borneol, azone, 1, 3-butanediol and 1, 2-pentanediol are components of the transdermal agent, wherein the menthol and the borneol in the traditional Chinese medicine components have the transdermal effect at the same time; carbomer, diethanol amine, dipotassium glycyrrhizinate, methyl hydroxybenzoate, glycerol and water are taken as auxiliary components.
The preparation method of the external pharmaceutical composition for treating gout comprises the following steps:
s1, mixing lily and Chinese pulsatilla root to obtain a mixture A, and extracting the mixture A with water to obtain an extracting solution A for later use;
s2, preparing a mixture B from the divaricate saposhnikovia root, the dahurian angelica root and the Mongolian snakegourd root, and extracting the mixture B with water to obtain an extracting solution B for later use;
s3, mixing menthol and borneol, and grinding the mixture into semi-liquid state to obtain a mixture C for later use;
s4, mixing the extracting solution A and the extracting solution B, and concentrating to obtain a concentrated solution;
s5, adding the mixture C, glycerol, half of 1, 3-butanediol, half of 1, 2-pentanediol, glycerol and the balance of water into the concentrated solution, uniformly mixing, heating, emulsifying, cooling, adding azone, half of 1, 3-butanediol, half of 1, 2-pentanediol, dipotassium glycyrrhizinate and methyl paraben, uniformly mixing, adding triethanolamine to adjust the pH value, and preparing a mixture D;
s6, filling or pasting the mixture D to obtain the external medicine composition for treating gout;
in step S1, the weight ratio of the mixture a to water is 1: 6; in step S2, the weight ratio of the mixture B to water is 1: 5.
preferably, in step S1, the extraction is performed at 100 ℃ for 5 hours each time for 2 times.
Preferably, in step S2, the extraction is performed 2 times at 100 ℃ for 2 hours each time.
Preferably, in step S4, the concentration is performed to a density of 1.1g/cm3
Preferably, in step S5, the PH is adjusted to 6.6-7.
The invention has the beneficial effects that:
(1) the external medicine composition for treating gout provided by the invention adopts lily, Chinese pulsatilla root, divaricate saposhnikovia root, dahurian angelica root, mongolian snakegourd root, menthol and borneol as the raw material components of the traditional Chinese medicine, is green and natural, does not contain hormone, can be used for a long time, and can efficiently relieve pain by the effective components; the menthol, the borneol, the azone, the 1, 3-butanediol and the 1, 2-pentanediol are used as the raw material components of the transdermal agent, so that the active ingredients of the traditional Chinese medicine can be quickly transdermally penetrated, the drug effect is exerted, and the effect of quickly curing and relieving pain is achieved.
(2) The external medicine composition for treating gout provided by the invention meets the prescription requirements of medicines and health care products specified by the state, fills the gap of external medicines for treating gout, and has great commercial value.
(3) The preparation method of the external pharmaceutical composition for treating gout provided by the invention is simple to operate, stable in process, easily available in raw materials and strong in operability, active ingredients of the raw materials can be retained to the maximum extent, and the prepared external pharmaceutical composition for treating gout is rapidly released, so that the effect is remarkable.
Detailed Description
Hereinafter, embodiments of the present invention will be described in detail. The following examples are only for illustrating the technical solutions of the present invention more clearly, and therefore are only examples, and the protection scope of the present invention is not limited thereby.
It is to be noted that, unless otherwise specified, technical or scientific terms used herein shall have the ordinary meaning as understood by those skilled in the art to which the invention pertains.
Example 1
The external pharmaceutical composition for treating gout comprises the following raw materials in parts by weight: 35 parts of lily, 25 parts of Chinese pulsatilla root, 10 parts of divaricate saposhnikovia root, 10 parts of angelica dahurica, 13 parts of trichosanthes root, 3 parts of menthol, 4 parts of borneol, 1 part of azone, 4 parts of 1, 3-butanediol, 2 parts of 1, 2-pentanediol, 1 part of carbomer, 0.03 part of diethanolamine, 0.1 part of dipotassium glycyrrhizinate, 1.25 parts of methyl hydroxybenzoate, 3 parts of glycerol and 70 parts of water.
The preparation method of the external pharmaceutical composition for treating gout comprises the following steps:
s1, mixing lily and Chinese pulsatilla root to obtain a mixture A, and extracting the mixture A with water to obtain an extracting solution A for later use;
s2, preparing a mixture B from the divaricate saposhnikovia root, the dahurian angelica root and the Mongolian snakegourd root, and extracting the mixture B with water to obtain an extracting solution B for later use;
s3, mixing menthol and borneol, and grinding the mixture into semi-liquid state to obtain a mixture C for later use;
s4, mixing the extracting solution A and the extracting solution B, and concentrating to obtain a concentrated solution;
s5, adding the mixture C, glycerol, half of 1, 3-butanediol, half of 1, 2-pentanediol, glycerol and the balance of water into the concentrated solution, uniformly mixing, heating, emulsifying, cooling, adding azone, half of 1, 3-butanediol, half of 1, 2-pentanediol, dipotassium glycyrrhizinate and methyl paraben, uniformly mixing, adding triethanolamine to adjust the pH value, and preparing a mixture D;
s6, filling or pasting the mixture D to obtain the external medicine composition for treating gout;
in step S1, the weight ratio of the mixture a to water is 1: 6; in step S2, the weight ratio of the mixture B to water is 1: 5.
in step S1, the extraction is performed at 100 ℃ for 2 times, each time for 5 hours.
In step S2, the extraction is performed 2 times at 100 ℃ for 2 hours each time.
In step S4, the concentration is carried out until the density is 1.1g/cm3
In step S5, the PH is adjusted to 7.
Test example 1
The raw material components of the external pharmaceutical composition for treating gout are screened according to the mixture ratio
Firstly, the sources of the raw material components are shown in Table 1
TABLE 1
Figure BDA0002719974120000051
Second, test contents
1.1 Positive: diclofenac diethylamine emulsion agent, specification: 20 grams/tube, 1 tube/box, lot number: VJ4M, produced by GSK Consumer Healthcare Schweiz AG.
1.2 animal, feed and rearing Environment
Animals: ICR mice, SPF grade, male, body weight 19-20g, liening biotechnology, ltd, production license number: SCXK (jeao) 2015 + 0001, quality certification number: 211002300049396, respectively;
feed: rat and mouse maintenance feed, batch number 19073211, Beijing Ke's Australian cooperative feed Co., Ltd., license number: kyo feeding certificate (2014) 06054;
a breeding environment: barrier environment animal observation room, temperature: 21-25 ℃, relative humidity: 40-70%, the license number used by experimental animals: SYXK (Ji) 2015-0009.
1.3 Main instruments and reagents
Counter, model: i30, Shenzhen, Hai Tian Di science and technology Limited; electronic balance, model: DT100, well-known double jie test instrument factory; glacial acetic acid (analytical grade), batch number: 20181025, Beijing chemical plant; weiting depilatory cream, batch number: 2022050401x, product of Lijie time chemical (China) Co.
1.4 test methods
30 mice were obtained by the writhing method, and the abdomen was depilated in the range of 2.6cm x 3 cm. Mice were randomly divided into 3 groups of 10 mice each, namely a blank control group, a positive control group and a test substance group. After 24 hours of depilation, 0.6% acetic acid was intraperitoneally injected at 0.1ml/10g BW into each mouse in the blank control group, and the number of writhing of each mouse within 15min after administration of the analgesic agent was recorded by a counter; uniformly coating a test object on parchment paper according to the dose of 0.5 g/mouse, then pasting the parchment paper on the abdomen of a tested mouse, and fixing the test object by using a non-irritant adhesive plaster; treating the positive substance according to the same dosage and method of the test substance; after 30min, the covering is respectively uncovered, acetic acid is injected according to the method of a blank control group, and the times of writhing of the mice are recorded.
1.5 data statistics
Data analysis was performed using SPSS statistical software. The two sets of mean comparisons were performed using a t-test in sets.
(1) Screening of Chinese medicine raw material components in proportion
TABLE 2
Figure BDA0002719974120000071
(2) Proportioning screening of raw material components of transdermal agent
TABLE 3
Figure BDA0002719974120000072
Test example 2
Pain-relieving effect test of the pharmaceutical composition for external use for treating gout prepared in example 1
Test site: jilin leads to ventilation in east Chang district.
The test method comprises the following steps: in 2019, 120 patients with local gout acute attack are randomly selected, the patients are divided into three groups, the external pharmaceutical composition for treating gout, the rheumatic ostealgia ointment and the non-steroidal anti-inflammatory cream which are prepared in the embodiment 1 are respectively externally applied and smeared once every 4 hours and 3 times, and the pain relieving effect is tested for 12 hours.
TABLE 4
Example 1 Rheumatism ostealgia plaster Non-steroidal anti-inflammatory cream
12-hour pain relief ratio (%) 77.5% 35.0% 57.5%
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; such modifications and substitutions do not depart from the spirit and scope of the present invention, and they should be construed as being included in the following claims and description.

Claims (8)

1. A topical pharmaceutical composition for treating gout, comprising: the external medicine composition for treating gout comprises the following raw material components: lily, Chinese pulsatilla root, divaricate saposhnikovia root, dahurian angelica root, Mongolian snakegourd root, menthol, borneol, azone, 1, 3-butanediol, 1, 2-pentanediol, carbomer, diethanolamine, dipotassium glycyrrhizinate, methyl paraben, glycerol and water.
2. The topical pharmaceutical composition for the treatment of gout according to claim 1, wherein: the external medicine composition for treating gout comprises the following raw material components in parts by weight: 5-40 parts of lily, 10-40 parts of Chinese pulsatilla root, 5-30 parts of divaricate saposhnikovia root, 5-20 parts of angelica dahurica, 10-30 parts of trichosanthes root, 3-10 parts of menthol, 4-20 parts of borneol, 0.5-2 parts of azone, 1-5 parts of 1, 3-butanediol, 1, 2-pentanediol, 0.8-1.2 parts of carbomer, 0.02-0.04 part of diethanolamine, 0.08-0.12 part of dipotassium glycyrrhizinate, 0.5-2 parts of methylparaben, 2.5-3.5 parts of glycerol and 50-80 parts of water.
3. The topical pharmaceutical composition for the treatment of gout according to claim 1, wherein: the external medicine composition for treating gout comprises the following raw material components in parts by weight: 35 parts of lily, 25 parts of Chinese pulsatilla root, 10 parts of divaricate saposhnikovia root, 10 parts of angelica dahurica, 13 parts of trichosanthes root, 3 parts of menthol, 4 parts of borneol, 1 part of azone, 4 parts of 1, 3-butanediol, 2 parts of 1, 2-pentanediol, 1 part of carbomer, 0.03 part of diethanolamine, 0.1 part of dipotassium glycyrrhizinate, 1.25 parts of methyl hydroxybenzoate, 3 parts of glycerol and 70 parts of water.
4. The method for preparing a pharmaceutical composition for external use for treating gout according to any one of claims 1 to 3, wherein: the preparation method of the external pharmaceutical composition for treating gout comprises the following steps:
s1, mixing lily and Chinese pulsatilla root to obtain a mixture A, and extracting the mixture A with water to obtain an extracting solution A for later use;
s2, preparing a mixture B from the divaricate saposhnikovia root, the dahurian angelica root and the Mongolian snakegourd root, and extracting the mixture B with water to obtain an extracting solution B for later use;
s3, mixing menthol and borneol, and grinding the mixture into semi-liquid state to obtain a mixture C for later use;
s4, mixing the extracting solution A and the extracting solution B, and concentrating to obtain a concentrated solution;
s5, adding the mixture C, glycerol, half of 1, 3-butanediol, half of 1, 2-pentanediol, glycerol and the balance of water into the concentrated solution, uniformly mixing, heating, emulsifying, cooling, adding azone, half of 1, 3-butanediol, half of 1, 2-pentanediol, dipotassium glycyrrhizinate and methyl paraben, uniformly mixing, adding triethanolamine to adjust the pH value, and preparing a mixture D;
s6, filling or pasting the mixture D to obtain the external medicine composition for treating gout;
in step S1, the weight ratio of the mixture a to water is 1: 6; in step S2, the weight ratio of the mixture B to water is 1: 5.
5. the method for preparing a pharmaceutical composition for external use for treating gout according to claim 4, wherein: in step S1, the extraction is performed at 100 ℃ for 2 times, each time for 5 hours.
6. The method for preparing a pharmaceutical composition for external use for treating gout according to claim 4, wherein: in step S2, the extraction is performed 2 times at 100 ℃ for 2 hours each time.
7. The method for preparing a pharmaceutical composition for external use for treating gout according to claim 4, wherein: in step S4, the concentration is carried out until the density is 1.1g/cm3
8. The method for preparing a pharmaceutical composition for external use for treating gout according to claim 4, wherein: in step S5, the PH is adjusted to 6.6-7.
CN202011084696.2A 2020-10-12 2020-10-12 A topical pharmaceutical composition for treating gout and preparation method thereof Pending CN112043788A (en)

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