CN101066455B - Medicine carrying aquogel matrix for preparing plaster and its preparation process - Google Patents
Medicine carrying aquogel matrix for preparing plaster and its preparation process Download PDFInfo
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- CN101066455B CN101066455B CN2007100270689A CN200710027068A CN101066455B CN 101066455 B CN101066455 B CN 101066455B CN 2007100270689 A CN2007100270689 A CN 2007100270689A CN 200710027068 A CN200710027068 A CN 200710027068A CN 101066455 B CN101066455 B CN 101066455B
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Abstract
The present invention discloses one kind of medicine carrying aquogel matrix for preparing plaster and its preparation process. The medicine carrying aquogel matrix has the recipe comprising deionizedwater 60-80 weight portions, carbomer-940 resin 1-3 weight portions, carbomer-941 resin 10-20 weight portions, Tween-80 0.01-0.03 weight portions, EDTA-2-Na 0.001-0.004 weight portions, and alcohol 1-3 weight portions, and is prepared through stirring, dispersing and kneading. The present invention has facile materials, high biocompatibility, no toxicity and irritation, excellent medicine compatibility and other advantages.
Description
Technical field
The present invention relates to a kind of transdermal administration novel form preparation, particularly a kind of high-moisture hydrophilic gel plaster substrate.
Background technology
After transdermal delivery system (being called for short TTS) is meant medicine and pharmaceutic adjuvant combination, be affixed on skin surface and realize the special preparation of treatment whole body and local disease, it is the new formulation technology that has just developed rapidly in the world since the nineties in 20th century, has the distinct advantages that other dosage form does not possess, drug safety, convenience; The most suitable to producing the medicine that stimulates or cause decomposing through the intestines and stomach; Long action time, medication number of times are few; No liver first-pass effect; Be fit to child, old people's use etc.Whole world transdermal delivery system product annual sales amount rises to 2003 9100000000 dollars by 1,600,000,000 dollars in 1993.At present, world's transdermal delivery system is just with the development of 15% annual rate of growth, and annual rate of growth surpasses oral and sucks medicine-releasing system market.The transdermal delivery system market scale was 12,700,000,000 dollars in 2005, it is predicted to this market sales revenue in 2010 to reach 21,500,000,000 dollars, and 2015 is 31,500,000,000 dollars.Wherein only nicotine patch annual sales amount in the U.S. in 1994 reaches 1,000,000,000 dollars, is chosen as one of ten most popular then big best-selling products by U.S.'s " epoch " periodical.And that the innovation transdermal delivery system product that has independent intellectual property right at home has only is several, and great majority reach the rubber-emplastrum bigger to skin irritation for black, big, thick black plaster, and their inherent technically defectives are complicated components, easily produce anaphylaxis; Airtight, moisture content is low, and is poor with skin affinity, and easy-to-draw pain skin when tearing; The drug transdermal absorbance is low in addition, and withered and trickling can appear in the substrate instability when meeting cold and hot variation, all be difficult to enter international mainstream market.Main cause is exactly the domestic no manufacturer of pharmaceutic adjuvant of percutaneous dosing, the product that has is in plant produced but there is not medicinal authentication code, can not be as pharmaceutic adjuvant, caused the bottleneck of transdermal delivery system new-product development, be exactly can the approval of import, cost an arm and a leg, also be not suitable for domestic demand, the percutaneous dosing research and development are stayed cool.
Gel is the common name that a class contains the macromolecular network system of the above semi-solid jelly that comprises liquid of two components or two components and its dry system (dried glue).With medicine dissolution or be dispersed in the gel and both be gel, its can long period and the site of action tight adhesion, and bioadhesive is preferably arranged, and method for making is simple, it is comfortable to use." first record, 2005 edition " Chinese pharmacopoeia especially at one, two one respectively to gel carry out more detailed regulation explanation by 2000 editions by Chinese pharmacopoeia for gel.Gel is one of focus dosage form of research at present, the medicine that is applicable to the gel delivery system has hydrophilic medicament, hydrophobic drug, acidic drug, cationic drug, macromolecular drug, cell tissue etc., can be from the oral cavity, number of ways administrations such as nasal cavity, eye mucosa, gastrointestinal mucosal, vagina, rectum, skin, medicine for external use is the more gel medicine of preparation at present.
By the substrate difference, gel can be divided into aqueous gel and oil-base gel, selects suitable substrate for use according to the character of principal agent.Because hydrogel has excellent biological compatibility, but the release of medicine is had advantages such as slow release, controlled-release function and imbibition, caused the great interest of numerous researcheres, also studied application gradually at the field of Chinese medicines.Behind the hydrogel adhesive topical, easily be coated with exhibition, no greasy, to skin and mucosa nonirritant, surface skin absorb good, medicine film tack is good, not only reach controlled release, the gastrointestinal tract first pass effect of having avoided oral administration to exist, and untoward reaction is reduced greatly, alleviated the toxic and side effects of medicine; Simultaneously, fast, the easy eluting of the pharmaceutical drying of skin surface, sticking medicated clothing also make the patient take like a shot after the water-soluable gel administration, are the pharmaceutical dosage forms that a utmost point has application prospect.In China, gel still is in developmental stage at present, previously mainly as hospital preparation, uses to some extent at department of dermatologry, surgery etc., but does not all reach specification requirement, can't promote preferably.Shang Shi gel is few at home, main cause be the gel matrix material used of gel research also seldom, had a strong impact on applying of this dosage form.
Summary of the invention
For addressing the above problem, the purpose of this invention is to provide a kind of hydrogel medicine carrying substrate for preparing external use plaster and preparation method thereof, this substrate has been rich in bound water and unbound water, human body skin there is good affinity, be a kind of have attach comfortablely, hold the macromolecule hydrogel of advantages such as dose is big.
Technical scheme provided by the invention is: a kind of hydrogel medicine carrying substrate for preparing external use plaster, it is characterized in that prescription comprises following component: calculate by weight, 60～80 parts of deionized waters, 1～3 part of carbomer-940 resin, 10～20 parts of carbomer-941 resins, 0.01～0.03 part of Tween-80, EDTA-2-Na0.001～0.004 part, 1～3 part of ethanol.
A kind of preparation method for preparing the hydrogel medicine carrying substrate of external use plaster, it is characterized in that comprising following sequential steps: 1. calculate by weight, prepare 60～80 parts of deionized waters, 1～3 part of carbomer-940 resin, 10～20 parts of carbomer-941 resins, 0.001～0.004 part of 0.01～0.03 part of Tween-80, EDTA-2-Na, 1～3 part of ethanol; 2. above-mentioned deionized water, disodiumedetate, Tween 80, ethanol, carbomer-940 resin and resin carbomer-941 are mixed, dispersed with stirring is even; 3. the composite material of dispersed with stirring after evenly mediated and obtained base material.
Described step 2. in, with deionized water, disodiumedetate, ethanol and Tween 80 mixing, stirring at low speed adds recipe quantity carbomer-940 resin, middling speed stirs, and adds recipe quantity resin carbomer-941 in batches, stirring at low speed is to evenly.
Described step 3. in, the temperature of mediating technology is 40-60 ℃, stirs 1.5-2.5 hour.
Described step 3. in, stir to mediate the back evacuation 1-2 minute.
Described step 1. in, prescription also comprises nertralizer, glycerol and the medicine that is dissolved in ethanol; The base material that will 3. obtain through step is adjusted its pH value to 5-7 with nertralizer, adds glycerol, adding is dissolved in the medicine of ethanol again, and dispersed with stirring is even, leaves standstill.
Raw material of the present invention is a macromolecular material cheap and easy to get, has good biocompatibility, and is nontoxic, non-stimulated, mechanical strength meets preparation capable of permeating skin requirement and scalable, the medicine carrying mild condition, and drug loading is big, with penetrating agent, Chinese medicine extract, Chinese crude drug micropowders etc. the good compatibility is arranged, plurality of advantages such as preparation technology is easy, and formed product is good, and is pollution-free, the finished product hydrogel smooth in appearance that makes, color and luster evenly, do not have obvious mechanical admixture, the edge is neat.Water content 〉=60%, the noresidue stickum is affixed on human body skin and did not come off in 4 hours, and 45 ℃ of insulations 2 hours, finger pressure did not stay glue, and-2 ℃ are incubated 2 hours, and colloid does not freeze.After being attached to human body skin 8h, do not produce allergic phenomena.
The specific embodiment
The present invention is a kind of hydrogel medicine carrying substrate for preparing external use plaster, prescription comprises following component: calculate by weight, 60～80 parts of deionized waters, 1～3 part of carbomer-940 resin, 10～20 parts of carbomer-941 resins, 0.001～0.004 part of 0.01～0.03 part of Tween-80, EDTA-2-Na, 1～3 part of ethanol are by soaking material swelling, base material preparation, mixing to knead and make.
Material of the present invention is pharmaceutic adjuvant, wherein:
Carbomer-940 resin is white, loose shape; Tool acidity, hygroscopicity and little off-odor arranged can be water-soluble, ethanol, glycerol, and typical concentrations is 0.1%～3.0%.Owing to contain a large amount of carboxyls in its molecule, so should be specifically noted that with in the alkali and back, uses aqueous solution, to reduce stimulation to skin, mucosa.Nertralizer available hydrogen sodium oxide, potassium hydroxide, potassium bicarbonate, Borax, amino acids, polarity organic amine such as the triethanolamine of carbomer-940 resin.Lauryl amine and stearylamine can be made nertralizer in nonpolar system.Carbomer after the neutralization-940 resin hydrogel is thickness between pH6～11, and as pH＜3 or pH＞12, viscosity promptly reduces, and strong electrolyte exists also can reduce viscosity.The gel instability is exposed under the sunlight easy grow mold and loses viscosity rapidly, adds antioxidant and can slow down reaction.
Carbomer-941 resin has thickening effect efficiently, can form as clear as crystal gelinite with water, ethanol, and rheological characteristic is very strong.Carbomer-941 resin (conventional amount used 0.25～0.5%) under very low consumption just can produce thickening power efficiently, thereby prepares very emulsion, cream frost, gel and the preparation capable of permeating skin of wide range of viscosities and various flows degeneration.Be framework material in the hydrogel.Carbomer-941 resin, character same carbomer-940 resin is white powder, water solublity, tough high molecular weight acrylic polymer; There is certain difference with carbomer-940 molecular resin amount; It in hydrogel the hydrogel framework material.The two mixes gel, and it is safe and effective to be used for external preparation, and the active substance of medicine itself is not impacted, and has biological preferably adhibit quality, can be used for the stickup at positions such as oral cavity, eye, intestinal, nose and rectum.Prescription is simple, stable, has reduced many additional raw materials to the influence of medicine and to the zest of skin.
Preparation process: with deionized water, disodiumedetate, ethanol and the Tween 80 mixing of recipe quantity, stirring at low speed adds recipe quantity carbomer-940 resin, middling speed stirs, add recipe quantity resin carbomer-941, stirring at low speed 1.5-2.5h pours kneader into to evenly in batches, attemperation is 40-60 ℃, stir 1.5-2.5h until stirring, opened vacuum pump switch about 1-2 minute, close stirring, it is a burst of to wait, and then closes the switch of vacuum pump.Pour out base material from kneader in stainless steel cask, leave standstill, the substrate preparation is finished.
Mediating technology except kneading, also can comprise and add interpolation coloring agent, medicine, hydro-oxidation sodaization, the first time steps such as firming agent, its method is: the base material for preparing is added in the still of blender, stirring at low speed, slowly add NaOH (10%), till when its pH value is 5-7, slowly add the glycerol that accounts for interpolation back total amount volume 18-26% simultaneously.The various medicines that are dissolved in a certain amount of ethanol are added in the above-mentioned base material under the stirring at low speed condition slowly, and dispersed with stirring is even.In whipping process, the pigment that can slowly add abundant dilution (40 times) is in base material.Stop at last stirring, sealing and standing, promptly.Medicine also can directly add mixing in deionized water, disodiumedetate, ethanol and the Tween 80 when base material prepares.
By the following examples the present invention is further specified, but the present invention is not limited to this specific examples.
Embodiment 1 gets 60 parts of deionized waters, 0.001 part of disodiumedetate, 0.01 part of mixing of Tween 80, stirring at low speed adds 1 part of carbomer-940 resin, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 2h pours kneader into to evenly in batches, attemperation is 50 ℃, stir 2h, about 1.5 minutes of evacuation stirs, leave standstill, get substrate.
Embodiment 2 gets 60 parts of deionized waters, 0.002 part of disodiumedetate, 0.02 part of mixing of Tween 80, stirring at low speed adds 2 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 15 part, stirring at low speed 2.5h pours kneader into to evenly in batches, attemperation is 50 ℃, stir 2h, evacuation stirs, leave standstill, get substrate.
Embodiment 3 gets 60 parts of deionized waters, 0.004 part of disodiumedetate, 0.03 part of mixing of Tween 80, stirring at low speed adds 3 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 2h pours kneader into to evenly in batches, attemperation is 50 ℃, stir 2.5h, evacuation stirs, leave standstill, get substrate.
Embodiment 4 gets 70 parts of deionized waters, 0.001 part of disodiumedetate, 0.01 part of mixing of Tween 80, stirring at low speed adds 1 part of carbomer-940 resin, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 2h pours kneader into to evenly in batches, attemperation is 40 ℃, stir 2.5h, evacuation stirs, leave standstill, get substrate.
Embodiment 5 gets 70 parts of deionized waters, 0.002 part of disodiumedetate, 0.02 part of mixing of Tween 80, stirring at low speed adds 2 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 15 part, stirring at low speed 1.5h pours kneader into to evenly in batches, attemperation is 60 ℃, stir 2h, evacuation stirs, leave standstill, get substrate.
Embodiment 6 gets 70 parts of deionized waters, 0.004 part of disodiumedetate, 0.03 part of mixing of Tween 80, stirring at low speed adds 3 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 2h pours kneader into to evenly in batches, attemperation is 55 ℃, stir 2h, evacuation stirs, leave standstill, get substrate.
Embodiment 7 gets 80 parts of deionized waters, 0.001 part of disodiumedetate, 0.01 part of mixing of Tween 80, stirring at low speed adds 1 part of carbomer-940 resin, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 2h pours kneader into to evenly in batches, attemperation is 50 ℃, stir 2h, evacuation stirs, leave standstill, get substrate.
Embodiment 8 gets 80 parts of deionized waters, 0.002 part of disodiumedetate, 0.02 part of mixing of Tween 80, stirring at low speed adds 2 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 15 part, stirring at low speed 2.5h pours kneader into to evenly in batches, attemperation is 45 ℃, stir 2h, evacuation stirs, leave standstill, get substrate.
Embodiment 9 gets 80 parts of deionized waters, 0.004 part of disodiumedetate, 0.03 part of mixing of Tween 80, stirring at low speed adds 3 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 1.8h pours kneader into to evenly in batches, attemperation is 55 ℃, stir 1.5h, evacuation stirs, leave standstill, get substrate.
Embodiment 10 gets 80 parts of deionized waters, 0.004 part of disodiumedetate, 0.03 part of mixing of Tween 80, stirring at low speed adds 3 parts of carbomer-940 resins, and middling speed stirs, add recipe quantity resin carbomer-941 20 part, stirring at low speed 2h pours kneader into to evenly in batches, attemperation is 50 ℃, stir 2h, evacuation stirs, leave standstill, get substrate.
Add medicine and additives to this substrate again: the base material that will above-mentionedly make adds in the still of blender, and stirring at low speed slowly adds NaOH (10%), when its ph value is 5-7 till, the while slowly adding account for the glycerol of total amount volume 22.67%.Various medicines are dissolved in respectively in a certain amount of ethanol under the stirring condition of low speed, add in the above-mentioned base material slowly respectively again; Dispersed with stirring is even.Stir on the limit, and the limit slowly adds abundant dilution (40 times), and pigment is in base material, and dispersed with stirring is even.Stop to stir, sealing and standing, promptly.
Claims (4)
1. preparation method for preparing the hydrogel medicine carrying substrate of external use plaster is characterized in that comprising following sequential steps:
1. calculate by weight, prepare 60～80 parts of deionized waters, 1～3 part of carbomer-940 resin, 10～20 parts of carbomer-941 resins, 0.01～0.03 part of Tween 80,0.001～0.004 part of disodiumedetate, 1～3 part of ethanol;
2. with above-mentioned deionized water, disodiumedetate, Tween 80 and ethanol mixing, stirring at low speed; Add carbomer-940 resin, middling speed stirs; Add carbomer-941 resin again, stirring at low speed is to being uniformly dispersed in batches;
3. with the composite material of dispersed with stirring after evenly, stir down at 40～60 ℃ and to mediate in 1.5～2.5 hours, obtain base material;
4. add nertralizer the pH value of base material is adjusted to 5～7, add and account for the glycerol that adds base material cumulative volume 18%～26% behind the nertralizer, dispersed with stirring is even.
2. the preparation method of hydrogel medicine carrying substrate according to claim 1 is characterized in that: described step 3. in, stir to mediate the back evacuation 1～2 minute.
3. the preparation method of hydrogel medicine carrying substrate according to claim 1 is characterized in that: described nertralizer is sodium hydroxide, potassium hydroxide, potassium bicarbonate, Borax, amino acids, triethanolamine, lauryl amine or stearylamine.
4. the hydrogel medicine carrying substrate that makes by one of them described preparation method of claim 1 to 3.
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| CN2007100270689A CN101066455B (en) | 2007-03-06 | 2007-03-06 | Medicine carrying aquogel matrix for preparing plaster and its preparation process |
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| CN2007100270689A CN101066455B (en) | 2007-03-06 | 2007-03-06 | Medicine carrying aquogel matrix for preparing plaster and its preparation process |
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| CN104027836A (en) * | 2014-06-24 | 2014-09-10 | 南京仁天生物科技有限公司 | Dressing with synergistic effect with skin as well as preparation method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660121A (en) * | 2004-12-27 | 2005-08-31 | 广州中医药大学 | Paste agent of penetrating through skin for treating arthritid and preparation method |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660121A (en) * | 2004-12-27 | 2005-08-31 | 广州中医药大学 | Paste agent of penetrating through skin for treating arthritid and preparation method |
Non-Patent Citations (4)
| Title |
|---|
| B. W. Barry, M. C. Meyer."The rheological properties of carbopol gels 1. Contiousshear and creep properties of carbopol gels".Int. J. Pharm.2 1.1978,2(1),1-25. |
| B.W.Barry,M.C.Meyer."The rheological properties of carbopol gels 1.Contiousshear and creep properties of carbopol gels".Int.J.Pharm.2 1.1978,2(1),1-25. * |
| 熊佳佳等.卡波姆凝胶流变学特性及其影响因素研究.海峡药学18 4.2006,18(4),34-36. * |
| 郑俊民等.现代药物制剂技术丛书―经皮给药新剂型 第一版.人民卫生出版社,2006,381-385. * |
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