阅读说明：本技术 一种治疗关节积液的外敷制剂及其制备方法 (External application preparation for treating hydrarthrosis and preparation method thereof ) 是由 刘国英 于 2020-07-24 设计创作，主要内容包括：本发明涉及中药外敷制剂技术领域,具体涉及一种治疗关节积液的外敷制剂及其制备方法,所述治疗关节积液的外敷制剂,由活性成分和辅料组成,所述活性成分由以下重量份的药物制成：炙黄芪9-12重量份、柴胡3-15重量份、骨碎补6-15重量份、透骨草6-15重量份、茯苓6-15重量份、鸡血藤10-20重量份、牛膝10-20重量份、红花1-5重量份、羌活3-12重量份、川芎3-12重量份、当归3-12重量份、杜仲10-18重量份、党参10-18重量份、芒硝3-9重量份、冰片1-3重量份、薄荷醇0.1-0.8重量份。本发明提供的外敷制剂通过药物间的相互配伍,能够缓解关节疼痛,消除积液,对治疗膝关节炎等有显著疗效,且避免口服带来对肠胃肝肾等脏器的损伤影响,毒副作用小。(The invention relates to the technical field of traditional Chinese medicine external application preparations, in particular to an external application preparation for treating hydrarthrosis and a preparation method thereof, wherein the external application preparation for treating hydrarthrosis comprises active ingredients and auxiliary materials, and the active ingredients are prepared from the following medicines in parts by weight: 9-12 parts of roasted astragalus membranaceus, 3-15 parts of radix bupleuri, 6-15 parts of rhizoma drynariae, 6-15 parts of garden balsam stem, 6-15 parts of poria cocos, 10-20 parts of caulis spatholobi, 10-20 parts of radix achyranthis bidentatae, 1-5 parts of safflower carthamus, 3-12 parts of notopterygium root, 3-12 parts of ligusticum wallichii, 3-12 parts of angelica sinensis, 10-18 parts of eucommia ulmoides, 10-18 parts of codonopsis pilosula, 3-9 parts of mirabilite, 1-3 parts of borneol and 0.1-0.8 part of menthol. The external application preparation provided by the invention can relieve arthralgia and eliminate hydrops through mutual compatibility of medicines, has a remarkable curative effect on treating gonarthritis and the like, avoids the damage influence on organs such as intestines, stomachs, livers and the like caused by oral administration, and has small toxic and side effects.)

1. The externally applied preparation for treating hydrarthrosis is characterized by comprising active ingredients and auxiliary materials, wherein the active ingredients are prepared from the following medicines in parts by weight:

9-12 parts of roasted astragalus membranaceus, 3-15 parts of radix bupleuri, 6-15 parts of rhizoma drynariae, 6-15 parts of garden balsam stem, 6-15 parts of poria cocos, 10-20 parts of caulis spatholobi, 10-20 parts of radix achyranthis bidentatae, 1-5 parts of safflower carthamus, 3-12 parts of notopterygium root, 3-12 parts of ligusticum wallichii, 3-12 parts of angelica sinensis, 10-18 parts of eucommia ulmoides, 10-18 parts of codonopsis pilosula, 3-9 parts of mirabilite, 1-3 parts of borneol and 0.1-0.8 part of menthol.

2. The external preparation according to claim 1, wherein the active ingredient is prepared from the following drugs in parts by weight:

10 parts of radix astragali preparata, 12 parts of radix bupleuri, 9 parts of rhizoma drynariae, 9 parts of garden balsam stem, 9 parts of poria cocos, 15 parts of caulis spatholobi, 15 parts of radix achyranthis bidentatae, 3 parts of safflower, 8 parts of notopterygium root, 8 parts of ligusticum wallichii, 8 parts of angelica sinensis, 12 parts of eucommia ulmoides, 12 parts of codonopsis pilosula, 6 parts of mirabilite, 2 parts of borneol and 0.2 part of menthol.

3. The formulation for external application according to claim 1, wherein the adjuvant comprises: 50-80 parts of polyethylene glycol, 10-20 parts of glycerol, 5-8 parts of vegetable oil, 3-15 parts of a filler and 8-30 parts of modified chitosan.

4. The formulation for external application according to claim 3, wherein the polyethylene glycol is at least one selected from the group consisting of PEG200, PEG400, PEG800 and PEG 2000.

5. The external preparation according to claim 4, wherein the polyethylene glycol consists of PEG400 and PEG2000 in a weight ratio of 1: 0.3-0.8.

6. The formulation for external application according to claim 3, wherein the filler is selected from at least one of methylcellulose, sodium carboxymethylcellulose, sodium alginate, agar, gum arabic, xanthan gum, pectin, bentonite; and/or

The vegetable oil is at least one selected from tea oil, olive oil, cottonseed oil and castor oil.

7. A process for preparing the formulation for external application of any one of claims 1 to 6, comprising the steps of:

(1) cleaning radix astragali Preparata, bupleuri radix, rhizoma Drynariae, caulis et folium Gaultheriae Yunnanensis, Poria, caulis Spatholobi, Achyranthis radix, Carthami flos, Notopterygii rhizoma, rhizoma Ligustici Chuanxiong, radix Angelicae sinensis, Eucommiae cortex, and radix Codonopsis, grinding into Chinese medicinal powder, soaking the Chinese medicinal powder in 2-3 times volume of water at 40-60 deg.C for 1-2 hr, decocting at 100-120 deg.C for 0.5-2 hr, and cooling to obtain Chinese medicinal composition;

(2) stirring and dissolving chitosan and acid anhydride in ethyl acetate, then adjusting the pH value of the system to 4-5, then carrying out ultrasonic dispersion treatment for 1-2h at the temperature of 40-50 ℃, wherein the ultrasonic frequency is 22-30KHz, adding elementary iodine into the solution, heating to 120-130 ℃, and carrying out reflux reaction for 3-5h to obtain an intermediate;

uniformly dispersing the intermediate, alkyl glycoside and silane coupling agent in ethanol, and then performing ultrasonic dispersion for 2-3h at the temperature of 100-150 ℃ in an inert gas atmosphere to obtain modified chitosan;

(3) mixing the modified chitosan and the Chinese medicinal composition, adding Natrii sulfas, Borneolum Syntheticum and menthol, mixing, and adding polyethylene glycol, glycerol, vegetable oil, filler and modified chitosan to obtain topical preparation for treating hydrarthrosis.

8. The process of claim 7, wherein the anhydride is selected from at least one of maleic anhydride and acetic anhydride.

9. The method according to claim 7, wherein the alkyl glycoside is at least one member selected from the group consisting of C8-C16 alkyl glycosides.

Technical Field

The invention relates to the technical field of traditional Chinese medicine external application preparations, in particular to an external application preparation for treating hydrarthrosis and a preparation method thereof.

Background

Knee osteoarthritis refers to chronic and degenerative joint diseases caused by degeneration and hyperosteogeny of knee cartilage. Statistics have shown that 80% of people over the age of 50 have proliferative changes in the knee joint, and about 90% of people over the age of 60 have proliferative changes in the knee joint. Joint effusion is characterized in that when a joint is diseased or has certain systemic diseases, factors such as osteophyte and detached cartilage fragments stimulate to induce synovial inflammatory change, promote synovial hyperplasia and exudation, form joint effusion and secrete media directly or indirectly causing cartilage degradation into joint fluid, and the joint effusion further enables chondrocytes immersed in the joint effusion to swell, necrose and fall off, aggravate primary diseases and form vicious circle.

At present, NSAIDS medicines are commonly adopted to diminish inflammation and relieve pain in the prevention and treatment of knee osteoarthritis and secondary joint effusion thereof in clinical practice, or chondroitin sulfate and glucosamine are adopted to protect articular cartilage medicines, or joint puncture liquid drawing is performed, or transparent sodium hyaluronate, glucocorticoid and the like are injected into joints to improve synovial secretion, however, clinical practice shows that the NSAIDS medicines taken for a long time can cause adverse reactions such as gastrointestinal tract and the like; joint puncture injection belongs to invasive treatment, and repeated injection can increase the probability of joint infection.

In addition, the external application preparation in the prior art has short action time on affected parts and low drug effect.

Disclosure of Invention

The invention aims to overcome the problems in the prior art, and provides an external preparation for treating hydrarthrosis and a preparation method thereof.

In order to achieve the purpose, the invention provides an external application preparation for treating hydrarthrosis, which consists of an active ingredient and auxiliary materials, wherein the active ingredient is prepared from the following medicines in parts by weight:

9-12 parts of roasted astragalus membranaceus, 3-15 parts of radix bupleuri, 6-15 parts of rhizoma drynariae, 6-15 parts of garden balsam stem, 6-15 parts of poria cocos, 10-20 parts of caulis spatholobi, 10-20 parts of radix achyranthis bidentatae, 1-5 parts of safflower carthamus, 3-12 parts of notopterygium root, 3-12 parts of ligusticum wallichii, 3-12 parts of angelica sinensis, 10-18 parts of eucommia ulmoides, 10-18 parts of codonopsis pilosula, 3-9 parts of mirabilite, 1-3 parts of borneol and 0.1-0.8 part of menthol.

The external application preparation provided by the invention is applied to the affected part to implement the drug effect, has the effects of promoting diuresis and excreting dampness, promoting blood circulation and removing blood stasis, dredging channels and collaterals, removing dampness and dredging arthralgia, tonifying kidney and strengthening tendons by mutual compatibility of the medicines, can diminish inflammation, relieve pain, promote blood circulation and remove blood stasis, open orifices and penetrate bones and promote local blood circulation when being applied to the affected part, thereby relieving arthralgia, eliminating hydrops, having remarkable curative effect on treating gonarthritis and the like, avoiding the injury influence on organs such as intestines, stomach, liver and kidney and the like caused by oral administration, and having small toxic and side effects.

Preferably, the active ingredients are prepared from the following medicines in parts by weight:

10 parts of radix astragali preparata, 12 parts of radix bupleuri, 9 parts of rhizoma drynariae, 9 parts of garden balsam stem, 9 parts of poria cocos, 15 parts of caulis spatholobi, 15 parts of radix achyranthis bidentatae, 3 parts of safflower, 8 parts of notopterygium root, 8 parts of ligusticum wallichii, 8 parts of angelica sinensis, 12 parts of eucommia ulmoides, 12 parts of codonopsis pilosula, 6 parts of mirabilite, 2 parts of borneol and 0.2 part of menthol.

In order to prolong the drug effect, the auxiliary materials preferably comprise: 50-80 parts of polyethylene glycol, 10-20 parts of glycerol, 5-8 parts of vegetable oil, 3-15 parts of a filler and 8-30 parts of modified chitosan.

The polyethylene glycol in the auxiliary materials is mixed with the glycerol to form a gelatinous medicine at a lesion part, and the gelatinous medicine can cover the lesion part for a long time and treat the lesion part; in addition, the polyethylene glycol can also slowly release the active ingredients, so that discomfort caused by overhigh drug concentration of a lesion part during initial dropping of the nasal drops can be avoided, and the drug can be released for a long time to achieve the effect of long-acting treatment.

In order to further improve the sustained release effect of the drug and prolong the drug effect, the polyethylene glycol is preferably selected from at least one of PEG200, PEG400, PEG800 and PEG2000, and more preferably, the polyethylene glycol consists of PEG400 and PEG2000 in a weight ratio of 1: 0.3-0.8.

In order to further improve the slow release effect of the medicament and prolong the medicament effect, the filling agent is at least one selected from methylcellulose, sodium carboxymethylcellulose, sodium alginate, agar, Arabic gum, xanthan gum, pectin and bentonite.

In order to promote drug absorption, it is preferable that the vegetable oil is at least one selected from the group consisting of tea oil, olive oil, cottonseed oil, and castor oil.

The invention also provides a method for preparing the external application preparation, which comprises the following steps:

(1) cleaning radix astragali Preparata, bupleuri radix, rhizoma Drynariae, caulis et folium Gaultheriae Yunnanensis, Poria, caulis Spatholobi, Achyranthis radix, Carthami flos, Notopterygii rhizoma, rhizoma Ligustici Chuanxiong, radix Angelicae sinensis, Eucommiae cortex, and radix Codonopsis, grinding into Chinese medicinal powder, soaking the Chinese medicinal powder in 2-3 times volume of water at 40-60 deg.C for 1-2 hr, decocting at 100-120 deg.C for 0.5-2 hr, and cooling to obtain Chinese medicinal composition;

(2) stirring and dissolving chitosan and acid anhydride in ethyl acetate, then adjusting the pH value of the system to 4-5, then carrying out ultrasonic dispersion treatment for 1-2h at the temperature of 40-50 ℃, wherein the ultrasonic frequency is 22-30KHz, adding elementary iodine into the solution, heating to 120-130 ℃, and carrying out reflux reaction for 3-5h to obtain an intermediate;

uniformly dispersing the intermediate, alkyl glycoside and silane coupling agent in ethanol, and then performing ultrasonic dispersion for 2-3h at the temperature of 100-150 ℃ in an inert gas atmosphere to obtain modified chitosan;

(3) mixing the modified chitosan and the Chinese medicinal composition, adding Natrii sulfas, Borneolum Syntheticum and menthol, mixing, and adding polyethylene glycol, glycerol, vegetable oil, filler and modified chitosan to obtain topical preparation for treating hydrarthrosis.

The long-chain branch of the chitosan and the molecular chain of the alkyl glycoside are mutually crosslinked, so that the effective components in the medicament can be locked in the molecular chain to achieve the effect of slowly releasing the medicament, and the action time of the medicament is prolonged. By modifying chitosan, hydrophilic groups and hydrophobic groups are introduced on chitosan molecules, so that molecular bonds can be fully formed with various active ingredients in the traditional Chinese medicine compound, active ingredients are adsorbed as much as possible, and the medicine is slowly released in the later use process, thereby prolonging the action time of the medicine. In addition, the alkyl glycoside in the molecular chain can promote the absorption of the medicine, thereby improving the medicine effect.

Preferably, the acid anhydride is at least one selected from maleic anhydride and acetic anhydride.

Preferably, the alkyl glycoside is at least one selected from the group consisting of C8-C16 alkyl glycosides.

Through the technical scheme, the invention has the following technical effects:

the external application preparation provided by the invention is applied to the affected part to implement the drug effect, has the effects of promoting diuresis and excreting dampness, promoting blood circulation and removing blood stasis, dredging channels and collaterals, removing dampness and dredging arthralgia, tonifying kidney and strengthening tendons by mutual compatibility of the medicines, can diminish inflammation, relieve pain, promote blood circulation and remove blood stasis, open orifices and penetrate bones and promote local blood circulation when being applied to the affected part, thereby relieving arthralgia, eliminating hydrops, having remarkable curative effect on treating gonarthritis and the like, avoiding the injury influence on organs such as intestines, stomach, liver and kidney and the like caused by oral administration, and having small toxic and side effects.

Detailed Description

The endpoints of the ranges and any values disclosed herein are not limited to the precise range or value, and such ranges or values should be understood to encompass values close to those ranges or values. For ranges of values, between the endpoints of each of the ranges and the individual points, and between the individual points may be combined with each other to give one or more new ranges of values, and these ranges of values should be considered as specifically disclosed herein.