CN101352544A - Carrier gel for treating gout - Google Patents

Carrier gel for treating gout Download PDF

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Publication number
CN101352544A
CN101352544A CNA2008100132058A CN200810013205A CN101352544A CN 101352544 A CN101352544 A CN 101352544A CN A2008100132058 A CNA2008100132058 A CN A2008100132058A CN 200810013205 A CN200810013205 A CN 200810013205A CN 101352544 A CN101352544 A CN 101352544A
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China
Prior art keywords
gel
gout
carrier
transdermal
colchicine
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CNA2008100132058A
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Chinese (zh)
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王悦
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Individual
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Individual
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Abstract

The invention provides an externally applied gel for treating gout, which is an externally applied medicine made from traditional Chinese medicine components such as nidus vespae, colchicine, a gel matrix, and the like., and by taking a coupling medium as transdermal carrier. The anti-gout gel can quickly eliminate redness, swelling, pain and fever symptoms of gouty arthritis, inhibit granulocyte infiltration and formation of lactic acid, reduce synthesis of uric acid, shorten and stop the acute attack of the gouty arthritis, prevent gout complications that threaten life, suspend tissue and organ damage caused by deposition of the uric acid, thus ensure that the illness of a patient is stabilized and can not deteriorate anymore for a long time. With the coupling medium adopted as the transdermal carrier of the medicine, the gel is characterized in that: a dermal hydration gradient can be naturally formed in the skin permeation course of the coupling medium, the gradient is independent of concentration when driving osmotic pressure difference, the gel has high deformability, can keep the components thereof unchanged after the skin permeation course and can permeate corneum of mammals through a plurality of transformation. The gel also has high transdermal efficiency, and full dermal permeabilities are not different between species and different parts. The gel avoids the deficiencies of injections and oral liquid medicines, is safe owing to the external use, and has no toxicity and side effects. The gel has simple components, low cost, requires no special devices and production conditions, and is available for large-scale industrialized production.

Description

A kind of carrier gel for the treatment of gout
Technical field:
The present invention relates to a kind of carrier gel for the treatment of gout and preparation method thereof, belong to the technical field of medicine and preparation method thereof.
Background technology:
Gout is a kind of than ancient disease.B.C. 5th century medical science father Xi Bo carat at the bottom of (Hippocrates) just relevant for the record of gout clinical manifestation.11st century are human represents gout with Guta one speech, thinks that at that time gout is that vivotoxin causes, and the meaning of Guta is exactly that drop by drop toxin enters the joint and causes disease.13rd century Guta derives and is Gout, and uses so far always.Ancient times, people did not know that gout is that what reason causes, so there is not good Therapeutic Method, can only attempt treating with sexual repression, acupuncture, blood-letting, have a shower water or cathartic yet, and significant effect is surely not arranged.The Leeuwenhoek of Holland in 1679 is with the bar-shaped crystallization to uric acid sodium of microscope first observed, but he and do not know crystalline chemical constituent.Sweden chemist Seheele had found uric acid in 1776.Wollaston analyzed the uric acid sodium salt in 1797, and attempted explaining the relation of gout and uric acid.The Garrod doctor of Britain in 1848 has measured the existence that uric acid is arranged in the blood.German Freudweiler in 1899 confirms that injection uric acid sodium crystallization meeting causes acute arthritis.German EmilFischer in 1907 propose the complete metabolic pathway of purine.Nineteen twenty-nine Thannhauser proposes the drainage theory of uric acid.Up to Benedict in 1949 and Sorenson with radioactive substance research body in the generation of uric acid and excretion and every day volume of the circular flow.Just use micropolariscope to observe directly uric acid sodium salt crystal in the tophus up to McCarty in 1961 and Hollander, from then on the relation of gout and uric acid has been had further and understood.
Modern medicine thinks, gout (gout) be one group because the disease due to the purine metabolic disturbance.Its clinical characters is a hyperuricemia, and the gouty acute arthritis that causes is therefrom shown effect repeatedly, tophus deposition, tophus chronic arthritis and joint deformity.Often involve kidney and cause that chronic interstitial nephritis and uric acid renal calculus form.Primary disease increases reason according to uric acid in the blood can be divided into constitutional and Secondary cases two big classes.The cause of disease of primary gout, owing to belong to the hereditary due to the congenital purine metabolic disturbance, great majority are not illustrated as yet except that minority.The cause of disease of secondary gout can be caused by multiple reasons such as nephropathy, leukemia, medicines.Primary disease is sent out well in male and menopausal women, and the male is more than the women, and men and women's ratio is about 20: 1., pain repeatedly outbreak red, swollen, hot with the joint according to primary disease, joint motion is dumb to be main clinical manifestation, Chinese medicine belongs to " arthromyodynia " category.
The sickness rate of gout is in rising trend in China at present.The outbreak repeatedly of acute gout or chronic gout, the easiest initiation metabolism disorder gout complication, for example hyperlipemia, hypertension, diabetes, obesity, arteriosclerosis and coronary heart disease etc., serious threat people's health and life.To the medicine of goat, injection and oral drugs are arranged at present.Injection can bring treatment painful to patient, and there is untoward reaction in the oral drugs majority, and also there is certain limitation in therapeutic effect.With the natural drug is main component, is aided with the exterior-applied gel of carrier transdermal drag delivery preparation, does not see launch and bibliographical information.
Summary of the invention:
The present invention aims to provide a kind of local topical carrier gel for the treatment of acute gout, is the clinical newtype drug that a kind of safe and effective percutaneous dosing is provided.
One of the object of the invention: a kind of carrier gel product for the treatment of acute gout is provided.
Two of the object of the invention: the industrialized process for preparing that this external carrier gel is provided.
Three of the object of the invention: the main uses of illustrating this external carrier gel.
Technical solution of the present invention is achieved in that a kind of local topical gel for the treatment of acute gout.It is by Chinese medicinal components such as Nidus Vespae, colchicine, gel-type vehicle and adopt carrier to form as the transdermal carrier, the external used medicine for preparing through special process.
Described Chinese medicinal components comprises what Nidus Vespae, Rhizoma Paridis, Caulis Trachelospermi, Flos Lonicerae, Gypsum Fibrosum, Semen Coicis, Radix Cyathulae, Radix Scrophulariae, Rhizoma Atractylodis, Cortex Phellodendri, Radix Paeoniae Rubra, Scolopendra, Spina Gleditsiae, Rhizoma Corydalis and colchicine were formed according to a certain ratio.Wherein colchicine can be a Chinese medicine extract, also can be chemical compound.We make a distinction between the important and the lesser one, and compatibility is rigorous.Acute gouty arthritis is produced effect significantly, after the medication a few hours can make arthritic red, swollen, bitterly, the heat symptom-complex shape rapidly disappears.It does not influence uric acid metabolism and drainage.It mainly act as antiinflammatory, suppresses granulocyte infiltration and lactic acid formation.
Described gel-type vehicle is polyacrylic material or medical macromolecular materials.Preferred carbomer, Polycarbophil, CBP, Polyethylene Glycol, sodium carboxymethyl cellulose etc., or one or more combination wherein.
Said cutaneous permeable agent is to adopt the transdermal carrier of carrier as medicine.Carrier is meant to have the high deformation ability, and can be power with skin hydration pressure, and the lipoid aggregation in the duct of the efficient little several times of penetration ratio self also is called the flexible nano liposome.Be in the phospholipid composition of liposome, to add surfactant such as sodium cholate etc., make its lipid membrane have the deformability of height.But carrier topical targeting skin, and but prolong drug is in the action time of skin, see through horny layer and enter skin corium, major part is eliminated by lymphatic capillary, all the other can be with muscle, the joint diffusion of Concentraton gradient under skin, compare with other exterior-applied formulations, have good medication amount one effect relationship.Constitute the ingredient of the transdermal carrier of carrier, comprise that pharmaceutics allows the cutaneous permeable agent that uses.Preferred composition is one or more combination in phosphatidylcholine (SPc), sodium cholate (BS), ethanol, propylene glycol, triethanolamine, the azone.
Concrete medicine of the present invention is formed:
Nidus Vespae 1-50 part, Rhizoma Paridis 1-50 part, Caulis Trachelospermi 1-50 part, Flos Lonicerae 1-100 part, Gypsum Fibrosum 1-100 part, Semen Coicis 1-100 part, Radix Cyathulae 1-100 part, Radix Scrophulariae 1-100 part, Rhizoma Atractylodis 1-100 part, Cortex Phellodendri 1-100 part, Radix Paeoniae Rubra 1-100 part, Scolopendra 1-100 part, Spina Gleditsiae 1-20 part, Rhizoma Corydalis 1-20 part, colchicine 1-20 part, carbomer 5-25 part, S-PC (SPc) 100-250 part, sodium cholate (BS) 5-20 part, ethanol 30-80 part, triethanolamine 5-20 part.
Concrete preparation technology of the present invention:
With 14 flavor Chinese medicine decoctings such as Nidus Vespae 2 times, merge decocting liquid, precipitation is filtered, and concentrates 1: 2, adds the colchicine stirring and dissolving; Carbomer is added injection water expansion dissolving; S-PC (SPc) alcoholic solution is mixed with an amount of BS, and add lipophilic drugs, the solution that obtains is 8.7%SPC, 1.3%BS and 8.5% ethanol.This solution and triethanolamine-Ha buffer (pH6.2 wherein can add water soluble drug) mixes, and the lipoid total concentration is 10%.The suspension that obtains is through ultrasonic, lyophilization, at last with in press dispersing emulsification machine or supersound process to obtain ideal particle diameter.Filtering with microporous membrane with 0.2um.With the said components mixing,, promptly obtain product of the present invention through packing, check.
Main uses of the present invention is, it is a kind of anti-gout drugs, can eliminate rapidly gouty arthritis red, swollen, bitterly, the heat symptom-complex shape, suppress that granulocyte soaks into and lactic acid forms, reduce uric acid and synthesize, promote urate excretion, shorten and the acute attack of ending gouty arthritis, prevent the formation of gouty arthritis,chronic, prevent that life-threatening gout complication from taking place, end uric acid and deposit caused histoorgan infringement, make patient's long-term stability and no longer development.Total effective rate reaches 95%.
The present invention has overcome the deficiency of injection, oral drugs, avoids the first pass effect of medicine at gastrointestinal, liver, drug safety, and it is painful not have treatment, has no side effect.The present invention constitutes simply, and cost is lower, and equipment that need not be special and working condition are easy to realize industrialized great production.
The specific embodiment:
In order to help those skilled in the art more fully to understand the present invention,, be described in detail the specific embodiment of the present invention in conjunction with experimental data.But the right that cited embodiment does not limit the present invention in any way.
Embodiment 1:
Prescription is formed:
A: Nidus Vespae 25g, Rhizoma Paridis 25g, Caulis Trachelospermi 25g, Flos Lonicerae 45g, Gypsum Fibrosum 45g, Semen Coicis 45g, Radix Cyathulae 45g, Radix Scrophulariae 35g, Rhizoma Atractylodis 35g, Cortex Phellodendri 35g, Radix Paeoniae Rubra 35g, 3 of Scolopendras, Spina Gleditsiae 20g, Rhizoma Corydalis 20g
B: Acritamer 940 10g, colchicine 1.5g, Borneolum Syntheticum 2g, Mentholum 2g
C: S-PC 100g, sodium cholate 5g, ethanol 50ml, triethanolamine 10g
Make 1000g
Preparation method:
1. A group 14 flavor medicines are added 7-8 times of water gaging decocting 2 times, 2 hours for the first time, 1 hour for the second time, twice decocting liquid merged, 3 times of amount ethanol precipitations, filtering and concentrating to 1: 2.
2. carbomer is added deionized water dissolving 10 hours, be added in A group extracting solution, colchicine, abundant stirring and dissolving, left standstill 10-20 hour.
3. S-PC (SPc) is used dissolve with ethanol, add sodium cholate (BS) and mix, and add lipophilic drugs, the solution that obtains is 8.7%SPC, 1.3%BS and 8.5% ethanol.This solution and triethanolamine _ Ha buffer (pH6.2 wherein can add water soluble drug) mixes, and the lipoid total concentration is 10%.The suspension that obtains is through ultrasonic, lyophilization, at last with in press dispersing emulsification machine or supersound process to obtain ideal particle diameter, with the microporous filter membrane degerming of 0.2um.
4. step 3 solution is joined in step 2 medicinal liquid stir, packing gets final product.
Embodiment 2:
Prescription is formed:
A: Nidus Vespae 35g, Rhizoma Paridis 35g, Caulis Trachelospermi 35g, Flos Lonicerae 50g, Gypsum Fibrosum 50g, Semen Coicis 55g, Radix Cyathulae 50g, Radix Scrophulariae 50g, Rhizoma Atractylodis 45g, Cortex Phellodendri 50g, Radix Paeoniae Rubra 55g, 8 of Scolopendras, Spina Gleditsiae 40g, Rhizoma Corydalis 20g
B: Acritamer 940 10g colchicine 2g, Borneolum Syntheticum 5g, Mentholum 5g
C: S-PC 150g, sodium cholate 10g, ethanol 50ml, triethanolamine 10g.
Make 1000g
Preparation method:
Its preparation method is with embodiment 1.

Claims (7)

1. exterior-applied gel for the treatment of gout.It is characterized in that: the external used medicine that it is formed, makes through special process as the transdermal carrier by Chinese medicinal components such as Nidus Vespae, colchicine, gel-type vehicle and employing carrier.
2. the described Chinese medicinal components of claim 1, it is characterized in that: it is made of according to a certain ratio Nidus Vespae, Rhizoma Paridis, Caulis Trachelospermi, Flos Lonicerae, Gypsum Fibrosum, Semen Coicis, Radix Cyathulae, Radix Scrophulariae, Rhizoma Atractylodis, Cortex Phellodendri, Radix Paeoniae Rubra, Scolopendra, Spina Gleditsiae, Rhizoma Corydalis and colchicine, wherein colchicine can be a Chinese medicine extract, also can be chemical compound.
3. the described gel-type vehicle of claim 1, it is characterized in that: described gel-type vehicle is polyacrylic material or medical macromolecular materials.One or more combination wherein such as preferred carbomer, Polycarbophil, CBP, Polyethylene Glycol, sodium carboxymethyl cellulose etc.
4. the described employing carrier of claim 1 is as the transdermal carrier of medicine, it is characterized in that: form the skin hydration gradient in the carrier transdermal process naturally, this gradient-driven permeable pressure head and concentration are irrelevant, component is constant after having high deformation and transdermal, can repeatedly be out of shape by mammiferous horny layer, transdermal efficient height, whole bark permeability do not have to reach between kind the difference of different parts.Constitute the ingredient of the transdermal carrier of carrier, comprise that pharmaceutics allows the cutaneous permeable agent that uses.Preferred composition is one or more combination in phosphatidylcholine (SPc), sodium cholate (BS), ethanol, propylene glycol, triethanolamine, the azone.
5. the prescription of the described exterior-applied gel of claim 1: it is characterized in that: Nidus Vespae 1-50 part, Rhizoma Paridis 1-50 part, Caulis Trachelospermi 1-50 part, Flos Lonicerae 1-100 part, Gypsum Fibrosum 1-100 part, Semen Coicis 1-100 part, Radix Cyathulae 1-100 part, Radix Scrophulariae 1-100 part, Rhizoma Atractylodis 1-100 part, Cortex Phellodendri 1-100 part, Radix Paeoniae Rubra 1-100 part, Scolopendra 1-100 part, Spina Gleditsiae 1-20 part, Rhizoma Corydalis 1-20 part, colchicine 1-20 part, carbomer 5-25 part, S-PC (SPc) 100-250 part, sodium cholate (BS) 5-20 part, ethanol 30-80 part, triethanolamine 5-20 part.
6. the preparation method of the described exterior-applied gel of claim 1 is characterized in that: with 14 flavor Chinese medicine decoctings such as Nidus Vespae 2 times, merge decocting liquid, precipitation is filtered, and concentrates 1:2, adds the colchicine stirring and dissolving; Carbomer is added injection water expansion dissolving; S-PC (SPc) alcoholic solution is mixed with an amount of BS, and add lipophilic drugs, the solution that obtains is 8.7%SPC, 1.3%BS and 8.5% ethanol.This solution and triethanolamine-Ha buffer (pH6.2 wherein can add people's water soluble drug) mixes, and the lipoid total concentration is 10%.The suspension that obtains is through ultrasonic, lyophilization, at last with in press dispersing emulsification machine or supersound process to obtain ideal particle diameter.Filtering with microporous membrane with 0.2um.With the said components mixing,, promptly obtain product of the present invention through packing, check.
7. the purposes of the described exterior-applied gel of claim 1, it is characterized in that: it is a kind of anti-gout drugs, can eliminate rapidly gouty arthritis red, swollen, bitterly, the heat symptom-complex shape, suppressing granulocyte infiltration and lactic acid forms, it is synthetic to reduce uric acid, promote urate excretion, shorten and end the acute attack of gouty arthritis, prevent the formation of gouty arthritis,chronic, prevent that life-threatening gout complication from taking place, end uric acid and deposit caused histoorgan infringement, make long-term nonprogressor and no longer development.
CNA2008100132058A 2008-09-16 2008-09-16 Carrier gel for treating gout Pending CN101352544A (en)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021506967A (en) * 2017-12-15 2021-02-22 マーク、フーパーMark Hooper Dissolution of monosodium urate to treat gout
CN112791158A (en) * 2021-01-12 2021-05-14 李果 Miao medicine composition for treating gout and preparation method thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021506967A (en) * 2017-12-15 2021-02-22 マーク、フーパーMark Hooper Dissolution of monosodium urate to treat gout
CN112791158A (en) * 2021-01-12 2021-05-14 李果 Miao medicine composition for treating gout and preparation method thereof

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Open date: 20090128