CN1579393A - Transparaent and disappearing external medicine preparation containing benzotolazo - Google Patents
Transparaent and disappearing external medicine preparation containing benzotolazo Download PDFInfo
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- CN1579393A CN1579393A CN 200410039087 CN200410039087A CN1579393A CN 1579393 A CN1579393 A CN 1579393A CN 200410039087 CN200410039087 CN 200410039087 CN 200410039087 A CN200410039087 A CN 200410039087A CN 1579393 A CN1579393 A CN 1579393A
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- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- 239000003814 drug Substances 0.000 title claims abstract description 12
- 239000003364 biologic glue Substances 0.000 claims abstract description 17
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 16
- 239000000203 mixture Substances 0.000 claims description 75
- 229940040145 liniment Drugs 0.000 claims description 51
- 239000000865 liniment Substances 0.000 claims description 51
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 30
- OCAPBUJLXMYKEJ-UHFFFAOYSA-N 1-[biphenyl-4-yl(phenyl)methyl]imidazole Chemical compound C1=NC=CN1C(C=1C=CC(=CC=1)C=1C=CC=CC=1)C1=CC=CC=C1 OCAPBUJLXMYKEJ-UHFFFAOYSA-N 0.000 claims description 29
- 229960002206 bifonazole Drugs 0.000 claims description 29
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol group Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 29
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 24
- 230000002421 anti-septic effect Effects 0.000 claims description 15
- 239000004014 plasticizer Substances 0.000 claims description 15
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 claims description 10
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 claims description 10
- GYCKQBWUSACYIF-UHFFFAOYSA-N o-hydroxybenzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 claims description 10
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 8
- 238000003756 stirring Methods 0.000 claims description 8
- 229920002125 Sokalan® Polymers 0.000 claims description 7
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical group CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 claims description 6
- 239000000227 bioadhesive Substances 0.000 claims description 6
- 229920000642 polymer Polymers 0.000 claims description 6
- 229960001631 carbomer Drugs 0.000 claims description 5
- -1 poly-alkyl sucrose Chemical compound 0.000 claims description 5
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 claims description 4
- 230000008569 process Effects 0.000 claims description 4
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 4
- 239000000725 suspension Substances 0.000 claims description 4
- 230000008961 swelling Effects 0.000 claims description 4
- 238000005303 weighing Methods 0.000 claims description 4
- 239000011248 coating agent Substances 0.000 claims description 3
- 238000000576 coating method Methods 0.000 claims description 3
- 239000000084 colloidal system Substances 0.000 claims description 3
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- 239000004202 carbamide Substances 0.000 claims description 2
- 235000013877 carbamide Nutrition 0.000 claims description 2
- 229920001577 copolymer Polymers 0.000 claims description 2
- 238000004132 cross linking Methods 0.000 claims description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 2
- 229940059574 pentaerithrityl Drugs 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims description 2
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims description 2
- 229960003415 propylparaben Drugs 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 238000010521 absorption reaction Methods 0.000 claims 1
- 239000003623 enhancer Substances 0.000 claims 1
- 239000000463 material Substances 0.000 abstract description 5
- 208000015181 infectious disease Diseases 0.000 abstract description 4
- 229940079593 drug Drugs 0.000 abstract description 3
- 239000007888 film coating Substances 0.000 abstract 3
- 238000009501 film coating Methods 0.000 abstract 3
- LDZSKLOBVMBMRH-UHFFFAOYSA-N 2-benzyl-1H-pyrrole 1,1'-biphenyl Chemical class C(C1=CC=CC=C1)C=1NC=CC1.C1(=CC=CC=C1)C1=CC=CC=C1 LDZSKLOBVMBMRH-UHFFFAOYSA-N 0.000 abstract 2
- 108010025899 gelatin film Proteins 0.000 abstract 1
- 239000000499 gel Substances 0.000 description 24
- 239000010408 film Substances 0.000 description 18
- 238000012856 packing Methods 0.000 description 9
- 206010017533 Fungal infection Diseases 0.000 description 8
- 208000031888 Mycoses Diseases 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 8
- 230000000694 effects Effects 0.000 description 6
- WLAMNBDJUVNPJU-UHFFFAOYSA-N 2-methylbutyric acid Chemical compound CCC(C)C(O)=O WLAMNBDJUVNPJU-UHFFFAOYSA-N 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 229940082484 carbomer-934 Drugs 0.000 description 3
- 239000012467 final product Substances 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000010409 thin film Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 206010005913 Body tinea Diseases 0.000 description 2
- 206010048768 Dermatosis Diseases 0.000 description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
- 208000002474 Tinea Diseases 0.000 description 2
- 208000007712 Tinea Versicolor Diseases 0.000 description 2
- 201000010618 Tinea cruris Diseases 0.000 description 2
- 206010067197 Tinea manuum Diseases 0.000 description 2
- 206010056131 Tinea versicolour Diseases 0.000 description 2
- 208000025865 Ulcer Diseases 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 230000000843 anti-fungal effect Effects 0.000 description 2
- 229940121375 antifungal agent Drugs 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 230000002950 deficient Effects 0.000 description 2
- 210000000416 exudates and transudate Anatomy 0.000 description 2
- 230000002538 fungal effect Effects 0.000 description 2
- 230000003902 lesion Effects 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- WGYKZJWCGVVSQN-UHFFFAOYSA-N propylamine Chemical compound CCCN WGYKZJWCGVVSQN-UHFFFAOYSA-N 0.000 description 2
- 208000017520 skin disease Diseases 0.000 description 2
- 201000003875 tinea corporis Diseases 0.000 description 2
- 201000004647 tinea pedis Diseases 0.000 description 2
- 231100000397 ulcer Toxicity 0.000 description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 1
- 208000035473 Communicable disease Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 241000233866 Fungi Species 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 206010027336 Menstruation delayed Diseases 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
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- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
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- 230000000845 anti-microbial effect Effects 0.000 description 1
- 244000052616 bacterial pathogen Species 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229940049638 carbomer homopolymer type c Drugs 0.000 description 1
- 229940043234 carbomer-940 Drugs 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
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- 239000002552 dosage form Substances 0.000 description 1
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- 210000004905 finger nail Anatomy 0.000 description 1
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- 230000036541 health Effects 0.000 description 1
- 150000002460 imidazoles Chemical class 0.000 description 1
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- 230000008595 infiltration Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
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- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
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- 239000000843 powder Substances 0.000 description 1
- BGKFMRKZNTYDQB-UHFFFAOYSA-N propane-1,1-diol;propane-1,2,3-triol Chemical compound CCC(O)O.OCC(O)CO BGKFMRKZNTYDQB-UHFFFAOYSA-N 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 206010040872 skin infection Diseases 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 229920002994 synthetic fiber Polymers 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- FQXXSQDCDRQNQE-VMDGZTHMSA-N thebaine Chemical class C([C@@H](N(CC1)C)C2=CC=C3OC)C4=CC=C(OC)C5=C4[C@@]21[C@H]3O5 FQXXSQDCDRQNQE-VMDGZTHMSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a film coating agent, as an external application medicinal preparation used for guarding against shallow part mycotic infections, especially a gel film coating agent which comprises biphenyl benzyl-azoles therein and is characterized by the biphenyl benzyl-azoles, film forming materials, a biological adhesive agent as well as an elasticizer contained therein. Said film coating agent, as a gel, will dry itself, after being coated to skins for 2-3 minutes, to form homogeneous, colorlessful and transparent adelomorphic films and begin to release medicines.
Description
Technical field of the present invention
The present invention relates to a kind of external medicine preparation that is used to prevent mycotic infection of superficial part, particularly a kind of gel liniment that comprises bifonazole is applied to and forms layer of transparent, cryptomorphic film on skin or the fingernail.
Background technology of the present invention
The top layer fungal infection is the caused infectious disease of the pathogenic bacterium by parasitizing the keratoprotein tissue common in people's daily life, be a kind of common and have certain communicable multiple dermatosis, as the tinea manuum, tinea pedis, tinea corporis, tinea cruris, tinea versicolor and some gynaecopathia or the like.Show that according to the WHO statistics whole world has 20% people that the top layer fungal infection is arranged.Because the deterioration of a large amount of uses of antibiotic etc, human body immunity's decline and human body existence external environment condition, the sickness rate of top layer fungal infection is still improving constantly.The top layer fungal infection has had a strong impact on people's Health and Living quality, more and more is subject to people's attention so can effectively treat and/or prevent the development of the medicine of top layer fungal infection.
The means of treatment top layer fungal infection mainly are to use various antibacterial at present, and up to now, there have many antibacterial to be used for to be clinical.At present used antibacterial can be divided into antibacterial agent, antifungal, antimicrobial according to the object of its onset, its structure is varied, and for example azole (imidazoles and triazole), propylamine, sulfo-amino methyl ester class, thebaine class, pyrrones, miazines or the like are arranged.
In numerous antifungal drugs, bifonazole has the characteristics of broad-spectrum antiseptic when the treatment mycotic infection of superficial part, pathomycete to 90% is inhibited, clinical cure rate reaches more than 91%, minimal inhibitory concentration is below 5mg/ml, block also has antibacterium and antiinflammatory action simultaneously rapidly.On the mechanism of action, it works by two action sites: suppress the synthetic double inhibition effect of cell respectively simultaneously in film formed early stage of fungal cell and late period, thereby can more effectively kill fungus, so effect is more outstanding by destroying fungal cell membrane.It can be used with the form of parenterai administrations such as oral formulations forms such as tablet, capsule or injection, also can use with the form of external preparation such as ointment, ointment, gel, liniment, solution.But oral and parenterai administration mode generally can produce general action, also can produce certain effect to intravital other tissue and organ, so the untoward reaction meeting increases, also can increase the drug resistance of other tissue and organ, and because it is very limited to arrive the medicine in affected part, so curative effect is not high, so the topical mode of preferred external when the fungal infection of treatment top layer.
All there are certain shortcoming in skin preparation such as powder agent, spray, solution, lotion and preparations such as unguentum, gel commonly used at present; for example medicine is to the inefficiency of lesions position transmission; when patient's normal activity, cause drug loss owing to rubbing; be easy to pollute patient's medicated clothing, when untoward reaction takes place, be difficult for removing etc.; and the patch with backing layer may produce allergy even ulcer phenomenon owing to the breathability difference; and these problems of being brought by dosage form also may cause patient's compliance to reduce, and come therapeutic effect thereby further reduce.Therefore, need a kind of topical formulations easy to clean to obtain more effective treatment.
Membrane or the liniment made with macromolecular material appearred in recent years, for example US 5,888,494 A disclose a kind of liniment that contains opioid with filmogen preparation commonly used, but be inconvenient to carry, and this liniment only comprises filmogen commonly used, does not solve film caducous problem when being subjected to rubbing that liniment forms.There is not the relevant report that can overcome the bifonazole external preparation of above-mentioned defective in the prior art, so need a kind of novel bifonazole preparation that does not have above-mentioned defective so that can the relevant dermatosis of more effective treatment.
Description of the invention
The objective of the invention is to provide a kind of external preparation composition for the treatment of the evident in efficacy, easy to use of skin infection and not having above-mentioned defective---comprise the gel liniment of bifonazole.Though in the prior art relevant for the report of making liniment with macromolecular material, but the present invention finds surprisingly, film former, a kind of biological adhesive and plasticizer mixed in certain proportion can obtain a kind of liniment with unexpected effect, this liniment is a gel, just can dryly voluntarily form uniform water white stealthy film and begin to discharge medicine being coated on the skin after 2-3 minute.Its formed this thin film has good cohesive, contractility and wearability, be not in the situation that will deliberately be removed, and it can continue closely to stick on and reaches on the skin about 24 hours.In addition, this thin film also has good permeability, has the good compatibility with skin, and the patient is in use without any sense of discomfort, and also imperceptible have foreign body to exist; This liniment can be used for the skin affected part of Any shape and size; And because this film is water white, so can clearly observe the progression of disease situation in affected part; In case need stop treatment, the formed film of this liniment can be removed from skin easily.Thereby film former and bioadhesive polymer are not used in combination the instruction of the bifonazole gel liniment of the water white stealthy film that obtains after application, can to obtain to have good adhesiveness and breathability in the prior art.
The formed film of this liniment can also effectively absorb the exudate in affected part; reducing sense of discomfort and reducing transudate makes the affected part that the danger of ulcer take place; simultaneously; the formed film of liniment of the present invention can also effectively protect the skin of lesions position to make it to avoid external pollution and friction stimulates; and can keep being capped the moisture of position skin in right amount; thereby soften cuticle increases medicine to the infiltration of skin than the depths focus.
The invention provides a kind of bifonazole gel liniment that comprises film former, biological adhesive and the plasticizer of some, this liniment also can randomly comprise external preparation such as cutaneous permeable agent, antiseptic additive commonly used.
The definition of used among the present invention " bioadhesive " refer to biological or synthetic material adhesion on the skin and/or mucosa of biology, thereby make this material can retain the long time thereon.The definition of " biological adhesive " refers to the material with bioadhesive among the present invention.
The definition of " stealthy film " refers to a kind of water white visually non-existent seemingly film among the present invention.
The present composition contains bifonazole, and the content of bifonazole is common dose clinically.In one embodiment of the invention, it contains and accounts for composition total weight 0.1-5% weight, preferred 0.5-1.5% weight, the particularly bifonazole of 1% weight.
The present composition contains and accounts for composition total weight 2% to 30% weight, the film former of preferred 1%-15% weight.Employed film former is the filmogen with pliability, hygroscopicity and water solublity characteristics commonly used in the prior art in the present composition, the polyvinyl alcohol of preferred various models (PVA) more preferably is PVA04-86 and PVA17-88 as PVA124,04-86,05-88,17-88 or its mixture.PVA can obtain by commercial sources.
The present composition contains and accounts for composition total weight 0.5%-10% weight, preferred 0.5%-5% weight, the particularly bioadhesive polymer of 1-3% weight.Employed bioadhesive polymer is a kind of acrylic acid crosslinked resin in the present composition, the copolymer of particularly poly-alkyl sucrose or poly-alkyl tetramethylolmethane and acrylic crosslinking polymer, carbomer (Carbopol) for example, the present invention can use the carbomer of various models, as carbomer 934,940,910 or its mixture, preferred carbomer 934 and 940, preferred especially Acritamer 940.Carbomer can obtain by commercial sources, for example can be from BF Goodrich company with Carbopol
Title bought.
The present composition contains and accounts for composition total weight 5%-20% weight, the plasticizer of preferred 5%-10% weight.Employed plasticizer has for example glycerol, propylene glycol, dibutyl phthalate or its mixture in the present composition, preferably glycerine, propylene glycol or its mixture, be the mixture of glycerol and propylene glycol more preferably, for example it is with 1: 0.5-1: the mixture that 3 ratio forms.
Compositions of the present invention can also randomly comprise antiseptic and/or cutaneous permeable agent, and suitable antiseptic has for example methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben or its mixture, preferred ethyl hydroxybenzoate; Suitable cutaneous permeable agent has for example azone, dimethyl sulfoxide, carbamide, propylene glycol or its mixture, preferred dimethyl sulfoxide, azone, propylene glycol, with and composition thereof.The content of antiseptic is about 0.001%-0.5% weight of said composition gross weight, is preferably 0.05%-0.2% weight.The content of cutaneous permeable agent is about 0.1%-40% weight of said composition gross weight, is preferably 5%-10% weight.
In one embodiment of the invention, the content of bifonazole is the 0.1-3% weight of composition total weight in this liniment, the content of filmogen is the 2%-30% weight of composition total weight, the content of biological adhesive is the 0.5%-10% of composition total weight, and the content of plasticizer is the 5%-20% weight of composition total weight.In preferred embodiments, the content of bifonazole is the 0.5%-1.5% weight of composition total weight in this liniment, the content of filmogen is the 5%-15% weight of composition total weight, the content of biological adhesive is the 0.5%-3% weight of composition total weight, and the content of plasticizer is the 5%-10% weight of composition total weight.In another preferred embodiment, the content of bifonazole is 1% weight of composition total weight in this liniment, and the content of filmogen is the 5%-15% weight of composition total weight, and the content of biological adhesive is the 1-3% weight of composition total weight.
In one embodiment of the invention, this liniment contains the antiseptic that accounts for composition total weight 0.001%-0.5% weight and/or accounts for the cutaneous permeable agent of coating combination gross weight 0.1%-40% weight.In preferred embodiments, this liniment contains the antiseptic that accounts for composition total weight 0.05%-0.2% weight and/or accounts for the cutaneous permeable agent of coating combination gross weight 5%-10% weight.
The invention provides a kind of method for preparing described liniment, it comprises the steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) biological adhesive is added water-soluble expanding, placement is spent the night, and makes gel;
(3) take by weighing in the bifonazole adding ethanol of requirement, make suspension, join immediately in the gel of (1), stir so that its homodisperse through supersound process;
(4) in the gel of (3), add plasticizer, mix homogeneously;
(5) gel with (2) adds in the gel of (4), stirs rapidly, and mix homogeneously obtains white gels; This gel is carried out packing with the flexible pipe of required specification to get final product.
The present invention also provides another method for preparing described liniment, and it comprises following step:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) biological adhesive is added water-soluble expanding, placement is spent the night, and makes gel;
(3) antiseptic is dissolved in the ethanol, gained solution is joined in the gel of (1) mix homogeneously;
(4) take by weighing in the bifonazole and antiseptic adding ethanol of requirement, make suspension, join immediately in the gel of (3), stir so that its homodisperse through supersound process;
(5) in the gel of (4), add plasticizer and/or cutaneous permeable agent, mix homogeneously;
(6) gel with (2) adds in the gel of (5), stirs rapidly, and mix homogeneously obtains white colloid; This gel is carried out packing with the flexible pipe of required specification to get final product.
When using the liniment of the milky gel form of gained evenly is applied in the affected part and gets final product, it is a drying and forming-film after 2-3 minute.
The gained liniment can be preserved with the medicinal flexible pipe packing of different size.
Liniment of the present invention can be used for cutaneous fungal infection, for example the tinea manuum, tinea pedis, tinea corporis, tinea cruris, tinea versicolor etc.
Now the present invention is further detailed with the following examples.
Embodiment
Embodiment 1
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| Bifonazole | 1 |
| PVA04-86 | 6.7 |
| PVA17-88 | 6.7 |
| Acritamer 940 | 1 |
| Glycerol | 3.3 |
| Propylene glycol | 5 |
| Azone | 2 |
| Ethyl hydroxybenzoate | 0.1 |
| Ethanol | 13 |
| Water | 61.2 |
| Amount to | 100 |
By different size it is carried out packing with flexible pipe.
This liniment can form water white thin film after 2-3 minute, the film forming good toughness of institute's shape has been difficult for the limit, and rub resistance can peel off when specially removing.
Embodiment 2
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| Bifonazole | 1 |
| PVA04-86 | 5 |
| Carbomer 934 | 3 |
| Glycerol | 3 |
| Propylene glycol | 5 |
| Azone | 2 |
| Ethyl hydroxybenzoate | 0.1 |
| 95% ethanol | Surplus |
By different needs it is carried out packing with flexible pipe.
Obtain having the liniment of above-mentioned character.
Embodiment 3
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| Bifonazole | 1 |
| PVA04-86 | 2 |
| PVA17-88 | 6 |
| Acritamer 940 | 2 |
| Glycerol | 6 |
| Dimethyl sulfoxide | 0.4 |
| Ethyl hydroxybenzoate | 0.1 |
| Ethanol | 26 |
| Water | In right amount |
By different size it is carried out packing with flexible pipe.
Obtain having the liniment of above-mentioned character.
Embodiment 4
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| Bifonazole | 1 |
| PVA17-88 | 15 |
| Acritamer 940 | 1 |
| Glycerol | 7.5 |
| Dimethyl sulfoxide | 0.4 |
| Ethyl hydroxybenzoate | 0.1 |
| Ethanol | 30 |
| Water | In right amount |
By different size it is carried out packing with flexible pipe.
Obtain having the liniment of above-mentioned character.
Embodiment 5
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| Bifonazole | 1 |
| PVA17-88 | 15 |
| Acritamer 940 | 1 |
| Glycerol | 3 |
| Dimethyl sulfoxide | 0.4 |
| Ethyl hydroxybenzoate | 0.1 |
| Ethanol | 30 |
| Water | In right amount |
By different size it is carried out packing with flexible pipe.
Obtain having the liniment of above-mentioned character.
Embodiment 6
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| Bifonazole | 1 |
| PVA124 | 10 |
| Carbomer 934 | 1 |
| Glycerol | 5 |
| Dimethyl sulfoxide | 0.4 |
| Ethyl hydroxybenzoate | 0.1 |
| Ethanol | 20 |
| Water | In right amount |
By different size it is carried out packing with flexible pipe.
Obtain having the liniment of above-mentioned character.
Claims (14)
1. a bifonazole external preparation composition is characterized in that it comprises bifonazole, filmogen, bioadhesive polymer and plasticizer.
2. preparation as claimed in claim 1 is characterized in that it is the gel liniment, just can dryly voluntarily form uniform water white stealthy film and begin to discharge medicine being coated on the skin after 2-3 minute.
3. liniment as claimed in claim 1 or 2, it is characterized in that wherein the content of bifonazole is the 0.1-5% weight of composition total weight, the content of filmogen is the 2%-30% weight of composition total weight, the content of biological adhesive is the 0.5%-5% of composition total weight, and the content of plasticizer is the 5%-20% weight of composition total weight.
4. liniment as claimed in claim 3, the content that it is characterized in that bifonazole is the 0.5%-1.5% weight of composition total weight, the content of filmogen is the 5%-20% weight of composition total weight, the content of biological adhesive is the 0.5%-3% weight of composition total weight, and the content of plasticizer is the 5%-10% weight of composition total weight.
5. liniment as claimed in claim 4, the content that it is characterized in that bifonazole is 1% weight of composition total weight, the content of filmogen is the 5%-15% weight of composition total weight, and the content of biological adhesive is the 1-3% weight of composition total weight.
6. as any described preparation of claim in front, it is characterized in that wherein said filmogen is selected from the polyvinyl alcohol of various models; And/or said biological adhesive is selected from the copolymer of poly-alkyl sucrose or poly-alkyl tetramethylolmethane and acrylic crosslinking polymer; And/or said plasticizer is selected from glycerol, propylene glycol, dibutyl phthalate or their mixture.
7. liniment as claimed in claim 6 is characterized in that wherein said filmogen is selected from PVA124,04-86,05-88,17-88 or its mixture; And/or said biological adhesive is selected from carbomer 934,940,910 or its mixture; And/or said plasticizer is the mixture of glycerol and propylene glycol.
8. liniment as claimed in claim 7 is characterized in that wherein said filmogen is selected from PVA04-86, PVA17-88 or its mixture; And/or said biological adhesive is selected from Acritamer 940.
9. liniment as claimed in claim 1 or 2 is characterized in that it also comprises antiseptic and/or Percutaneous absorption enhancer.
10. liniment as claimed in claim 9 is characterized in that wherein containing the antiseptic that accounts for composition total weight 0.001%-0.5% weight and/or accounts for the cutaneous permeable agent of coating combination gross weight 0.1%-40% weight.
11. liniment as claimed in claim 10 is characterized in that wherein said cutaneous permeable agent is selected from azone, dimethyl sulfoxide, carbamide, propylene glycol or their mixture; And/or wherein said antiseptic is selected from methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben or their mixture.
12. liniment as claimed in claim 11 is characterized in that wherein said cutaneous permeable agent is the mixture of azone and propylene glycol; And/or wherein said antiseptic is selected from ethyl hydroxybenzoate.
13. one kind prepares the method for liniment as claimed in claim 1 or 2, it is characterized in that it comprises following steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) biological adhesive is added water-soluble expanding, placement is spent the night, and makes gel;
(3) take by weighing in the bifonazole adding ethanol of requirement, make suspension, join immediately in the gel of (1), stir so that its homodisperse through supersound process;
(4) in the gel of (3), add plasticizer, mix homogeneously;
(5) gel with (2) adds in the gel of (4), stirs rapidly, and mix homogeneously obtains white colloid.
14. one kind prepares the method for liniment as claimed in claim 1 or 2, it is characterized in that it comprises following steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) biological adhesive is added water-soluble expanding, placement is spent the night, and makes gel;
(3) antiseptic is dissolved in the ethanol, gained solution is joined in the gel of (1) mix homogeneously;
(4) take by weighing in the bifonazole and antiseptic adding ethanol of requirement, make suspension, join immediately in the gel of (3), stir so that its homodisperse through supersound process;
(5) in the gel of (4), add plasticizer and/or cutaneous permeable agent, mix homogeneously;
(6) gel with (2) adds in the gel of (5), stirs rapidly, and mix homogeneously obtains white colloid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410039087 CN1286459C (en) | 2003-08-06 | 2004-02-02 | Transparaent and disappearing external medicine preparation containing benzotolazo |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN03149772.1 | 2003-08-06 | ||
| CNA031497721A CN1480128A (en) | 2003-08-06 | 2003-08-06 | Preparation of transparent, cryptomorphic external remedy |
| CN 200410039087 CN1286459C (en) | 2003-08-06 | 2004-02-02 | Transparaent and disappearing external medicine preparation containing benzotolazo |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1579393A true CN1579393A (en) | 2005-02-16 |
| CN1286459C CN1286459C (en) | 2006-11-29 |
Family
ID=34593085
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410039087 Expired - Lifetime CN1286459C (en) | 2003-08-06 | 2004-02-02 | Transparaent and disappearing external medicine preparation containing benzotolazo |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1286459C (en) |
-
2004
- 2004-02-02 CN CN 200410039087 patent/CN1286459C/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CN1286459C (en) | 2006-11-29 |
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Assignee: HAINAN YANGSHENGTANG PHARMACEUTICAL Co.,Ltd. Assignor: YANG SHENG TANG Co.,Ltd. Contract fulfillment period: 2008.9.25 to 2013.9.24 Contract record no.: 2008460000019 Denomination of invention: Transparaent and disappearing external medicine preparation containing benzotolazo Granted publication date: 20061129 License type: Exclusive license Record date: 20081113 |
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Free format text: EXCLUSIVE LICENSE; TIME LIMIT OF IMPLEMENTING CONTACT: 2008.9.25 TO 2013.9.24; CHANGE OF CONTRACT Name of requester: HAINAN YANGSHENGTANG PHARMACEUTICAL CO., LTD. Effective date: 20081113 |
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