CN101919828A - Transdermal absorption adhesive patch for curing onychomycosis and preparation method thereof - Google Patents
Transdermal absorption adhesive patch for curing onychomycosis and preparation method thereof Download PDFInfo
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- CN101919828A CN101919828A CN2010102570849A CN201010257084A CN101919828A CN 101919828 A CN101919828 A CN 101919828A CN 2010102570849 A CN2010102570849 A CN 2010102570849A CN 201010257084 A CN201010257084 A CN 201010257084A CN 101919828 A CN101919828 A CN 101919828A
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Abstract
The invention provides a transdermal absorption adhesive patch for curing onychomycosis. The adhesive patch comprises a back lining layer, a viscous polymer layer and a protective film layer, wherein the viscous polymer layer contains a medicine for curing onychomycosis, viscous polymer and a penetration enhancer, wherein the medicine is ciclopirox olamine, and the penetration enhancer is laurocapram or a traditional Chinese medicinal mixture with laurocapram. The invention also provides a preparation method of the adhesive patch. The adhesive patch of the invention can effectively promote ciclopirox olamine to penetrate the skin and realize the effect of curing onychomycosis. By adopting precutaneous administration, the gastrointestinal enzymolysis and the first-pass effect of the liver can be avoided, the toxic or side effects can be reduced and the individual differences of administration can be reduced. In addition, ciclopirox olamine in the adhesive patch can be released in a stable rate and the drug effect can be maintained stably for about 3 days, thus the frequency of use can be reduced. The raw materials of the adhesive patch of the invention are simple and accessible, the cost is cheap; and the adhesive patch is convenient to remove or paste and is also convenient to use, thus avoiding the pollution of clothes and the loss of medicines. Therefore, the adhesive patch of the invention has high practicability.
Description
Technical field
The present invention relates to a kind of patch, specifically be meant a kind of percutaneous absorption patch for the treatment of tinea unguium, the invention still further relates to the preparation method of the percutaneous absorption patch of this treatment tinea unguium by transdermal administration.
Background technology
Tinea unguium is the infectious disease on a kind of people's of occurring in first, medically is called tinea unguium, and it is caused by fungal infection.The tinea unguium pathological changes starts from first far-end, lateral margin or first pleat portion, shows as first color and paramophia.Ill deck is canescence more, and tarnishes, and the deck becomes fragile and breakage comes off.
The method of existing treatment tinea unguium has: 1. use the crisp sick first of pocket knife scraping, or with sick first skiving, be coated with iodine tincture or glacial acetic acid solution then.This method will adhere to just taking effect in 1 year at least, and is consuming time longer.
2. first is pulled out in operation.Though method is simple, be difficult to thoroughly remove sick first, and recurrence easily, severe pain that operation causes and the secondary infection that may cause all bring inconvenience to live and work, few at present the employing.
3. oral antifungal drug has griseofulvin, ketoconazole etc.These curative effect of medication instabilities, antibacterial range are little, and relapse rate is higher and side effect arranged.Need simultaneously to take medicine for up to half a year to a year and a half, therefore also less use.
4. be coated with broad-spectrum antiseptic class ointment outside, as miconazole, ketoconazole frost, bifonazole frost, Ciclopirox Olamine Ointment in Treatment and compound preparation.But this method is not easy to grasp dosage, and administration number of times is frequent, and easy pollution clothes, causes drug wastage.
Summary of the invention
It is good to the purpose of this invention is to provide a kind of curative effect, and administration continually and steadily reduces administration number of times, also can avoid the dirty first pass effect of gastrointestinal tract enzymolysis regulating liver-QI simultaneously, reduces poisonous side effect of medicine, and the percutaneous absorption patch of the convenient treatment tinea unguium of using.
The present invention adopts following technical scheme: a kind of percutaneous absorption patch for the treatment of tinea unguium, it is made up of backing layer, sticky polymers layer and protective film, wherein the sticky polymers layer includes medicine, sticky polymers and the penetration enhancer of treatment tinea unguium, and it is characterized in that: the medicine of described treatment tinea unguium is a ciclopirox olamine; Described penetration enhancer is the Chinese medicine intermixture that contains laurocapram and eucalyptus oil.
Described Chinese medicine intermixture includes and accounts for sticky polymers layer weight fraction is the laurocapram of 1-10%, and accounting for sticky polymers layer weight fraction is the eucalyptus oil of 1-10%.
Described Chinese medicine intermixture includes and accounts for sticky polymers layer weight fraction is the laurocapram of 1-10%, accounting for sticky polymers layer weight fraction is the eucalyptus oil of 1-10%, also includes to account in terpenes that sticky polymers layer weight fraction is 1-50%, saturated or unsaturated fatty acid and ester, alcohols, silicone, sulfoxide, amide, lactams, phenol or the ketopyrrolidine one or more.Wherein, terpenes for example: menthol; Saturated or unsaturated fatty acid and ester thereof, for example: capric acid, myristic acid, oleic acid, lauric acid, Hamposyl S, diethylene glycol distearate, diethylene glycol dilaurate, diethylene glycol list cinnamate, diethylene glycol monolaurate, diethylene glycol monostearate, triglycerin monostearate, six glyceryl monostearates, ten glycerol, eight oleates, SY-Glyster DAO 750, isopropyl myristic acid ester, isopropyl cetylate, ethyl oleate, ethyl lactate.Alcohols is for example: ethanol, propylene glycol, oleyl alcohol, lauryl alcohol, hexadecanol, poly-diethanol, terpinol; Silicone is for example: dimethicone; Sulfoxide is for example: dimethyl sulfoxide, dodecyl methyl sulfoxide; Amide is for example: N, dinethylformamide, N,N-dimethylacetamide; Lactams is for example: dodecyl nitrogen oxadiazon, farnesyl nitrogen oxadiazon; Phenol is for example: thymol; Ketopyrrolidine is 1-Methyl-2-Pyrrolidone for example.
The weight fraction that described ciclopirox olamine accounts for the sticky polymers layer is 1-15%; The weight fraction that described sticky polymers accounts for the sticky polymers layer is 20-80%.
Described sticky polymers is a polyacrylate pressure-sensitive.
Described backing layer is a kind of impermeable membrane of making that is selected from high density polyethylene (HDPE), low density polyethylene (LDPE), polypropylene, polrvinyl chloride, ethylene-vinyl acetate copolymer, polyester, polyvinylpyrrolidone, polyvinyl alcohol, poly-amino methyl, the metal aluminum foil, or the composite membrane made of metal aluminum foil and aforementioned polymer.
Described backing layer is a kind of in low density polyethylene films and metal aluminum foil PAP polyethylene-aluminum-polyethylene composite membrane, low density polyethylene films or the poly-amino methyl film made.
Described sticky polymers laminar surface also is provided with adhesive phase; The material of described adhesive phase is a polyacrylate pressure-sensitive.
Another object of the present invention provides the preparation method of above-mentioned paster.
A kind of method for preparing the percutaneous absorption patch of above-mentioned treatment tinea unguium; it is characterized in that: with sticky polymers, ciclopirox olamine, penetration enhancer and solvent evenly after; said mixture is coated on obtains the sticky polymers layer on the protective film; carry out dried then; and after the cooling, cutting into behind the backing layer on sticky polymers layer another side covers needs size promptly to obtain the percutaneous absorption patch of described treatment tinea unguium again.
Contain ciclopirox olamine 1-14 milligram in the percutaneous absorption patch of every square centimeter treatment tinea unguium.
The sticky polymers layer comprises sticky polymers, medicine ciclopirox olamine and penetration enhancer, and it has drug-reservoir and adheres to two functions.Sticky polymers layer of the present invention is to be the controlled release matrix material with the polyacrylate pressure-sensitive, the ciclopirox olamine of doses be dissolved in laurocapram and eucalyptus oil penetration enhancer or contain laurocapram and the mixing penetration enhancer of eucalyptus oil after, by solvent evaporation method the form with the liquid microcoulomb is uniformly distributed in the skeleton.By changing polymer Chinese medicine content, liquid microcoulomb density, the ratio of penetration enhancer are regulated the ciclopirox olamine rate of release in the paster.
The present invention adopts laurocapram (being 1-dodecyl-aza-cycloheptane alkane-2-ketone) penetration enhancer or contains the drug transdermal paster of the treatment tinea unguium that the Chinese medicine intermixture of laurocapram makes, can effectively promote the ciclopirox olamine skin permeation, play the effect of treatment tinea unguium.Also can avoid the dirty first pass effect of gastrointestinal tract enzymolysis regulating liver-QI by percutaneous drug delivery, reduce toxic and side effects, reduce the individual variation of medication.Simultaneously, the ciclopirox olamine among the present invention can discharge with steady rate, so drug effect can stable maintenance about 3 days, and the consumption that paster was made many days just reduces administration number of times.In addition, raw material of the present invention is simple and easy to, and with low cost, paster conveniently tears subsides, and is easy to use, also can avoid pollution clothes, cause the loss of medicine, therefore has very strong practicality.
The specific embodiment
Below further specify the present invention by specific embodiment:
Embodiment 1
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 185g, ciclopirox olamine 5g, penetration enhancer laurocapram 9g, eucalyptus oil 6g, propylene glycol 65g, put into wide mouthed bottle together with solvent ethyl acetate 100g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, PAP polyethylene-aluminum-polyethylene composite membrane backing layer on sticky polymers layer another side covers is cut into 5cm more again
2The paster of size makes every square centimeter paster contain ciclopirox olamine 5mg, promptly obtains the percutaneous absorption patch 1 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 46%, ciclopirox olamine 3%, laurocapram 6%, eucalyptus oil 4%, propylene glycol 41%.
Embodiment 2
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 225g, ciclopirox olamine 14g, penetration enhancer laurocapram 9g, eucalyptus oil 3g, ethanol 52g, put into wide mouthed bottle together with solvent ethyl acetate 125g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, after the cooling, low density polyethylene films backing layer on sticky polymers layer another side covers is cut into 5cm more again
2The paster of size makes every square centimeter paster contain ciclopirox olamine 14mg, promptly obtains the percutaneous absorption patch 2 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 54%, ciclopirox olamine 8%, laurocapram 5%, eucalyptus oil 3%, ethanol 30%.
Embodiment 3
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 300g, ciclopirox olamine 9g, penetration enhancer laurocapram 6g, eucalyptus oil 9g, dimethicone and oleyl alcohol mixture 40g, put into wide mouthed bottle together with solvent ethyl acetate 134g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, density polyethylene film with high backing layer on sticky polymers layer another side covers is cut into 5cm more again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 9mg, promptly obtain the percutaneous absorption patch 3 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 65%, ciclopirox olamine 5%, laurocapram 3%, eucalyptus oil 5%, dimethicone and oleyl alcohol mixture 22%.
Embodiment 4
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 215g, ciclopirox olamine 10g, penetration enhancer laurocapram 5g, eucalyptus oil 9g, lauric acid, Hamposyl S, lauryl alcohol and dimethyl sulfoxide mixture 10g, put into wide mouthed bottle together with solvent ethyl acetate 120g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, polypropylene screen backing layer on sticky polymers layer another side covers is cut into 5cm more again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 10mg, promptly obtain the percutaneous absorption patch 4 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 73%, ciclopirox olamine 8%, laurocapram 4%, eucalyptus oil 7%, lauric acid, Hamposyl S, lauryl alcohol and dimethyl sulfoxide mixture 8%.
Embodiment 5
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 176g, ciclopirox olamine 7g, penetration enhancer laurocapram 9g, eucalyptus oil 10g, hexadecanol and N, dinethylformamide mixture 6g, put into wide mouthed bottle together with solvent ethyl acetate 135g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, poly-amino methyl film backing layer on sticky polymers layer another side covers is cut into 10cm more again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 10mg, promptly obtain the percutaneous absorption patch 5 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 69%, ciclopirox olamine 7%, laurocapram 9%, eucalyptus oil 9%, hexadecanol and N, dinethylformamide mixture 6%.
Embodiment 6
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 200g, ciclopirox olamine 9g, penetration enhancer laurocapram 10g, eucalyptus oil 1g and solvent ethyl acetate 147g put into wide mouthed bottle together, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, polychloroethylene film backing layer on sticky polymers layer another side covers is cut into 10cm more again
2The paster of size makes every square centimeter paster contain ciclopirox olamine 10mg, promptly obtains the percutaneous absorption patch 6 of described treatment tinea unguium, and wherein the sticky polymers layer contains polyacrylate pressure-sensitive 80%, ciclopirox olamine 9%, laurocapram 10%, eucalyptus oil 1%.
Embodiment 7
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 100g, ciclopirox olamine 10g, penetration enhancer laurocapram 2g, eucalyptus oil 8g, terpinol 100g and solvent ethyl acetate 160g put into wide mouthed bottle together, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, ethylene-vinyl acetate copolymer film backing layer on sticky polymers layer another side covers is cut into 10cm more again
2The paster of size makes every square centimeter paster contain ciclopirox olamine 8mg, promptly obtains the percutaneous absorption patch 7 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 40%, ciclopirox olamine 5%, laurocapram 1%, eucalyptus oil 4%, terpinol 50%.
Embodiment 8
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 50g, ciclopirox olamine 10g, penetration enhancer laurocapram 10g, eucalyptus oil 10g, diethylene glycol list cinnamate, thymol and dodecyl nitrogen oxadiazon mixture 50g, put into wide mouthed bottle together with solvent ethyl acetate 100g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, following dry 4 minutes at 40 ℃ then, drying is 2 minutes under 60 ℃, drying is 2 minutes under 90 ℃, after the cooling, be coated with last layer polyacrylate pressure-sensitive adhesive phase at sticky polymers layer another side again, cover again and go up polyvinylpyrrolidone film backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 8mg, promptly obtain the percutaneous absorption patch 8 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 20%, ciclopirox olamine 10%, laurocapram 10%, eucalyptus oil 10%, diethylene glycol list cinnamate, thymol and dodecyl nitrogen oxadiazon mixture 50%.
Embodiment 9
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 198g, ciclopirox olamine 1g, penetration enhancer laurocapram 5g, eucalyptus oil 5g, oleic acid and ethyl oleate mixture 10g, put into wide mouthed bottle together with solvent ethyl acetate 150g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, drying is 2 minutes under 90 ℃, after the cooling, is coated with last layer polyacrylate pressure-sensitive adhesive phase at sticky polymers layer another side again, cover again and go up the polyvinyl alcohol film backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 1mg, promptly obtain the percutaneous absorption patch 9 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 79%, ciclopirox olamine 1%, laurocapram 5%, eucalyptus oil 5%, oleic acid and ethyl oleate mixture 10%.
Embodiment 10
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 60g, ciclopirox olamine 15g, penetration enhancer laurocapram 1g, eucalyptus oil 10g, diethylene glycol monolaurate and diethylene glycol dilaurate mixture 50g, put into wide mouthed bottle together with solvent ethyl acetate 120g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, drying is 2 minutes under 90 ℃, after the cooling, is coated with last layer polyacrylate pressure-sensitive adhesive phase at sticky polymers layer another side again, cover again and go up metal aluminum foil film backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 14mg, promptly obtain the percutaneous absorption patch 10 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 24%, ciclopirox olamine 15%, laurocapram 1%, eucalyptus oil 10%, diethylene glycol monolaurate and diethylene glycol dilaurate mixture 50%.
Embodiment 11
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 125g, ciclopirox olamine 5g, penetration enhancer laurocapram 5g, eucalyptus oil 10g, diethylene glycol monostearate, diethylene glycol distearate and dodecyl methyl sulfoxide mixture 30g, put into wide mouthed bottle together with solvent ethyl acetate 150g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, drying is 2 minutes under 90 ℃, after the cooling, is coated with last layer polyacrylate pressure-sensitive adhesive phase at sticky polymers layer another side again, cover again and go up the polyester film backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 5mg, promptly obtain the percutaneous absorption patch 11 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 50%, ciclopirox olamine 5%, laurocapram 5%, eucalyptus oil 10%, diethylene glycol monostearate, diethylene glycol distearate and dodecyl methyl sulfoxide mixture 30%.
Embodiment 12
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 175g, ciclopirox olamine 5g, penetration enhancer laurocapram 5g, eucalyptus oil 10g, triglycerin monostearate and six glyceryl monostearate mixture 10g, put into wide mouthed bottle together with solvent ethyl acetate 175g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, cover again and go up PAP polyethylene-aluminum-polyethylene composite membrane backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 5mg, promptly obtain the percutaneous absorption patch 12 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 70%, ciclopirox olamine 5%, laurocapram 5%, eucalyptus oil 10%, triglycerin monostearate and six glyceryl monostearate mixture 10%.
Embodiment 13
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 150g, ciclopirox olamine 20g, penetration enhancer laurocapram 20g, eucalyptus oil 10g, ten glycerol, eight oleates, SY-Glyster DAO 750 and N, N-dimethyl acetylamide mixture 90g, put into wide mouthed bottle together with solvent ethyl acetate 200g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, cover again and go up PAP polyethylene-aluminum-polyethylene composite membrane backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 10mg, promptly obtain the percutaneous absorption patch 13 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 30%, ciclopirox olamine 10%, laurocapram 10%, eucalyptus oil 5%, ten glycerol, eight oleates, SY-Glyster DAO 750 and N,N-dimethylacetamide mixture 45%.
Embodiment 14
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 125g, ciclopirox olamine 10g, penetration enhancer laurocapram 5g, eucalyptus oil 5g, myristic acid, isopropyl myristic acid ester and farnesyl nitrogen oxadiazon mixture 30g, put into wide mouthed bottle together with solvent ethyl acetate 150g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, cover again and go up PAP polyethylene-aluminum-polyethylene composite membrane backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 10mg, promptly obtain the percutaneous absorption patch 14 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 50%, ciclopirox olamine 10%, laurocapram 5%, eucalyptus oil 5%, myristic acid, isopropyl myristic acid ester and N,N-dimethylacetamide mixture 30%.
Embodiment 15
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 125g, ciclopirox olamine 15g, penetration enhancer laurocapram 10g, eucalyptus oil 10g, capric acid, isopropyl cetylate and poly-diethanol mixture 15g, put into wide mouthed bottle together with solvent ethyl acetate 150g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, cover again and go up PAP polyethylene-aluminum-polyethylene composite membrane backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 14mg, promptly obtain the percutaneous absorption patch 15 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 50%, ciclopirox olamine 15%, laurocapram 10%, eucalyptus oil 10%, capric acid, isopropyl cetylate and poly-diethanol mixture 15%.
Embodiment 16
With the sticky polymers polyacrylate pressure-sensitive (is PSA, wherein solids accounts for 40%) 125g, ciclopirox olamine 10g, penetration enhancer laurocapram 10g, eucalyptus oil 10g, ethyl lactate and 1-Methyl-2-Pyrrolidone mixture 20g, put into wide mouthed bottle together with solvent ethyl acetate 150g, the bottleneck sealing, vibration is 15 hours on agitator, leaves standstill until bubble collapse again.Said mixture is coated on the separate paper, then 40 ℃ dry 4 minutes down, 60 ℃ dry 2 minutes down, 90 ℃ dry 2 minutes down, after the cooling, cover again and go up PAP polyethylene-aluminum-polyethylene composite membrane backing layer, be cut into 5cm again
2The paster of size, make every square centimeter paster contain ciclopirox olamine 10mg, promptly obtain the percutaneous absorption patch 16 of described treatment tinea unguium, wherein the sticky polymers layer contains polyacrylate pressure-sensitive 50%, ciclopirox olamine 10%, laurocapram 10%, eucalyptus oil 10%, ethyl lactate and 1-Methyl-2-Pyrrolidone mixture 20%.
It is 69.4,74.6,71.3,72.6,68.5,62.8,73.3,71.5,69.3,67.6,72.2,69.6,70.2,66.7,64.9,67.3 μ g/cm that above-mentioned paster 1-16 adopts improved Franz diffusion cell device can record infiltration rate
2/ h.
Paster of the present invention is studied through pharmacological toxicology, has carried out sensitivity test, hemolytic and local irritation test.
Sensitivity test: the result shows that Cavia porcellus is movable normal, 1-20 order reaction symptom do not occur, is judged to be the anaphylaxis feminine gender.
The hemolytic test: after the laboratory animal administration, blood drawing all finds no hemolytic reaction, shows that this medicine does not have haemolysis and do not have agglutination.
The local irritation test: through the skin irritation test, observe dermoreaction under available light or full gloss spectrum light, perusal drug of topical application position does not have situations such as erythema and edema after removing medicine.
More than experiment detects and positive findings all do not occur, paster of the present invention is described to the skin nonirritant, no haemolysis, and anaphylaxis is negative, shows that drug safety is good.
Simultaneously, Clinical results shows that paster of the present invention has significant curative effect to tinea unguium, and drug effect can stable maintenance 3 days.Therefore paster of the present invention is a kind of percutaneous absorption patch safe, effective, long-acting, easy to use, can be used for the treatment of tinea unguium.
Claims (10)
1. percutaneous absorption patch for the treatment of tinea unguium, it is made up of backing layer, sticky polymers layer and protective film, wherein the sticky polymers layer includes medicine, sticky polymers and the penetration enhancer of treatment tinea unguium, and it is characterized in that: the medicine of described treatment tinea unguium is a ciclopirox olamine; Described penetration enhancer is the Chinese medicine intermixture that contains laurocapram and eucalyptus oil.
2. the percutaneous absorption patch of treatment tinea unguium according to claim 1, it is characterized in that: described Chinese medicine intermixture includes and accounts for sticky polymers layer weight fraction is the laurocapram of 1-10%, and accounting for sticky polymers layer weight fraction is the eucalyptus oil of 1-10%.
3. the percutaneous absorption patch of treatment tinea unguium according to claim 1, it is characterized in that: described Chinese medicine intermixture includes and accounts for sticky polymers layer weight fraction is the laurocapram of 1-10%, accounting for sticky polymers layer weight fraction is the eucalyptus oil of 1-10%, also includes to account in terpenes that sticky polymers layer weight fraction is 1-50%, saturated or unsaturated fatty acid and ester, alcohols, silicone, sulfoxide, amide, lactams, phenol or the ketopyrrolidine one or more.
4. the percutaneous absorption patch of treatment tinea unguium according to claim 1 is characterized in that: the weight fraction that described ciclopirox olamine accounts for the sticky polymers layer is 1-15%; The weight fraction that described sticky polymers accounts for the sticky polymers layer is 20-80%.
5. the percutaneous absorption patch of treatment tinea unguium according to claim 1 is characterized in that: described sticky polymers is a polyacrylate pressure-sensitive.
6. the percutaneous absorption patch of treatment tinea unguium according to claim 1, it is characterized in that: described backing layer is a kind of impermeable membrane of making that is selected from high density polyethylene (HDPE), low density polyethylene (LDPE), polypropylene, polrvinyl chloride, ethylene-vinyl acetate copolymer, polyester, polyvinylpyrrolidone, polyvinyl alcohol, poly-amino methyl, the metal aluminum foil, or the composite membrane made of metal aluminum foil and aforementioned polymer.
7. the percutaneous absorption patch of treatment tinea unguium according to claim 1 is characterized in that: described backing layer is a kind of in low density polyethylene films and metal aluminum foil PAP polyethylene-aluminum-polyethylene composite membrane, low density polyethylene films or the poly-amino methyl film made.
8. the percutaneous absorption patch of treatment tinea unguium according to claim 1 is characterized in that: described sticky polymers laminar surface also is provided with adhesive phase; The material of described adhesive phase is a polyacrylate pressure-sensitive.
9. method for preparing the percutaneous absorption patch of the described treatment tinea unguium of claim 1; it is characterized in that: with sticky polymers, ciclopirox olamine, penetration enhancer and solvent evenly after; said mixture is coated on obtains the sticky polymers layer on the protective film; carry out dried then; and after the cooling, cutting into behind the backing layer on sticky polymers layer another side covers needs size promptly to obtain the percutaneous absorption patch of described treatment tinea unguium again.
10. the preparation method of the percutaneous absorption patch of treatment tinea unguium according to claim 9 is characterized in that: contain ciclopirox olamine 1-14 milligram in the percutaneous absorption patch of every square centimeter treatment tinea unguium.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102570849A CN101919828A (en) | 2010-08-19 | 2010-08-19 | Transdermal absorption adhesive patch for curing onychomycosis and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010102570849A CN101919828A (en) | 2010-08-19 | 2010-08-19 | Transdermal absorption adhesive patch for curing onychomycosis and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101919828A true CN101919828A (en) | 2010-12-22 |
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| CN2010102570849A Pending CN101919828A (en) | 2010-08-19 | 2010-08-19 | Transdermal absorption adhesive patch for curing onychomycosis and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1579373A (en) * | 2003-08-06 | 2005-02-16 | 北京扬新科技有限公司 | Transparent disappearing external administration carrier |
| CN1654073A (en) * | 2004-02-11 | 2005-08-17 | 张恒建 | Paster for treating tinea unguium |
| CN1927190A (en) * | 2006-09-28 | 2007-03-14 | 哈尔滨健迪医药技术有限公司 | Letrozole transdermal drug administration plaster and its preparation method |
| CN101116656A (en) * | 2006-08-03 | 2008-02-06 | 上海汇伦生命科技有限公司 | Ciclopirox olamine gelling agent, method for preparing the same and pharmaceutical use thereof |
-
2010
- 2010-08-19 CN CN2010102570849A patent/CN101919828A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1579373A (en) * | 2003-08-06 | 2005-02-16 | 北京扬新科技有限公司 | Transparent disappearing external administration carrier |
| CN1654073A (en) * | 2004-02-11 | 2005-08-17 | 张恒建 | Paster for treating tinea unguium |
| CN101116656A (en) * | 2006-08-03 | 2008-02-06 | 上海汇伦生命科技有限公司 | Ciclopirox olamine gelling agent, method for preparing the same and pharmaceutical use thereof |
| CN1927190A (en) * | 2006-09-28 | 2007-03-14 | 哈尔滨健迪医药技术有限公司 | Letrozole transdermal drug administration plaster and its preparation method |
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Application publication date: 20101222 |