CN104208042A - Percutaneous absorption preparation - Google Patents
Percutaneous absorption preparation Download PDFInfo
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- CN104208042A CN104208042A CN201410484374.5A CN201410484374A CN104208042A CN 104208042 A CN104208042 A CN 104208042A CN 201410484374 A CN201410484374 A CN 201410484374A CN 104208042 A CN104208042 A CN 104208042A
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- tobramycin
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- 238000010521 absorption reaction Methods 0.000 title claims abstract description 16
- 238000002360 preparation method Methods 0.000 title abstract description 19
- NLVFBUXFDBBNBW-PBSUHMDJSA-N tobramycin Chemical compound N[C@@H]1C[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N NLVFBUXFDBBNBW-PBSUHMDJSA-N 0.000 claims abstract description 40
- 229960000707 tobramycin Drugs 0.000 claims abstract description 40
- 239000000203 mixture Substances 0.000 claims abstract description 23
- 239000003961 penetration enhancing agent Substances 0.000 claims abstract description 14
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims abstract description 11
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims abstract description 11
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims abstract description 11
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims abstract description 3
- 239000010410 layer Substances 0.000 claims description 61
- 239000012790 adhesive layer Substances 0.000 claims description 24
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 22
- 238000009472 formulation Methods 0.000 claims description 11
- 239000011241 protective layer Substances 0.000 claims description 11
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 8
- 239000000463 material Substances 0.000 claims description 7
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 6
- ZFPGARUNNKGOBB-UHFFFAOYSA-N 1-Ethyl-2-pyrrolidinone Chemical compound CCN1CCCC1=O ZFPGARUNNKGOBB-UHFFFAOYSA-N 0.000 abstract 2
- 239000003814 drug Substances 0.000 description 19
- 230000000052 comparative effect Effects 0.000 description 15
- 229940079593 drug Drugs 0.000 description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 6
- 239000006185 dispersion Substances 0.000 description 6
- 230000001464 adherent effect Effects 0.000 description 5
- 208000015181 infectious disease Diseases 0.000 description 5
- 230000035515 penetration Effects 0.000 description 5
- 230000001580 bacterial effect Effects 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 239000002562 thickening agent Substances 0.000 description 4
- 241000894006 Bacteria Species 0.000 description 3
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical group C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 239000002671 adjuvant Substances 0.000 description 3
- 235000013877 carbamide Nutrition 0.000 description 3
- 239000004202 carbamide Substances 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000002362 mulch Substances 0.000 description 3
- 239000002985 plastic film Substances 0.000 description 3
- 229920006255 plastic film Polymers 0.000 description 3
- 229960000502 poloxamer Drugs 0.000 description 3
- 229920001983 poloxamer Polymers 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- 238000005070 sampling Methods 0.000 description 3
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 description 2
- 241000193830 Bacillus <bacterium> Species 0.000 description 2
- 241000588724 Escherichia coli Species 0.000 description 2
- 229920002367 Polyisobutene Polymers 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 241000589517 Pseudomonas aeruginosa Species 0.000 description 2
- 229940126575 aminoglycoside Drugs 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 238000010579 first pass effect Methods 0.000 description 2
- 239000011521 glass Substances 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 230000003014 reinforcing effect Effects 0.000 description 2
- 231100000331 toxic Toxicity 0.000 description 2
- 230000002588 toxic effect Effects 0.000 description 2
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 description 1
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical group OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 206010061695 Biliary tract infection Diseases 0.000 description 1
- 206010051548 Burn infection Diseases 0.000 description 1
- 241000282470 Canis latrans Species 0.000 description 1
- 241000588923 Citrobacter Species 0.000 description 1
- 241000588914 Enterobacter Species 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
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- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 1
- 239000005642 Oleic acid Substances 0.000 description 1
- 102000011195 Profilin Human genes 0.000 description 1
- 108050001408 Profilin Proteins 0.000 description 1
- 241000588769 Proteus <enterobacteria> Species 0.000 description 1
- 206010040047 Sepsis Diseases 0.000 description 1
- 241000607720 Serratia Species 0.000 description 1
- 241000607764 Shigella dysenteriae Species 0.000 description 1
- 206010040880 Skin irritation Diseases 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 241000194017 Streptococcus Species 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
- 230000009056 active transport Effects 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 230000000845 anti-microbial effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 208000003167 cholangitis Diseases 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 210000003746 feather Anatomy 0.000 description 1
- 239000010408 film Substances 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 210000000232 gallbladder Anatomy 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 239000012982 microporous membrane Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 230000000149 penetrating effect Effects 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 210000002729 polyribosome Anatomy 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 229920002477 rna polymer Polymers 0.000 description 1
- 208000013223 septicemia Diseases 0.000 description 1
- 229940007046 shigella dysenteriae Drugs 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000004003 subcutaneous fat Anatomy 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 238000013271 transdermal drug delivery Methods 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to an externally-applied TDS preparation and in particular relates to a frame type percutaneous absorption preparation with tobramycin as an active component and a preparation process of the frame type percutaneous absorption preparation. According to the frame type percutaneous absorption preparation, a composition of serine, N-ethyl pyrrolidone and sodium laurylsulfate is used as a penetration enhancer, and the weight proportion of the serine to the N-ethyl pyrrolidone to the sodium laurylsulfate is 1:4:6.
Description
Technical field
The application relates to a kind of external TDS preparation, particularly, is take tobramycin as matrix-type transdermal absorbable preparation and the preparation technology thereof of active component.
Background technology
Tobramycin is a kind of aminoglycoside medicine, and through active transport by bacterial cell membrane, with the specific receptor protein binding of bacterial ribosome 30S subunit, the formation of initiation complex between interfere information ribonucleic acid and 30S subunit, Profilin is synthesized; DNA is mispronounced, causes the synthesis of non-functioning protein; Polysome is divided and loses the function of synthetic proteins.The clinical local infection for the external eyes caused by sensitive bacterial and appendages.It is compared with other aminoglycoside antibioticss, and antimicrobial spectrum is wider, and curative effect is higher, and toxic reaction is little.Some serratia marcecens and shigella dysenteriae etc. in staphylococcus aureus in gram positive bacteria, streptococcus etc. and gram-negative bacteria are all responsive to tobramycin.
Tobramycin can be bound up on the coupled position of 30S and 50S, hinders the formation of 70S complex, makes mRNA not translate into protein, cause cell death.Main to gram-negative bacteria, as effective in bacillus pyocyaneus, escherichia coli, klebsiella bacillus, Enterobacter, Bacillus proteus, citrobacter.The clinical severe infections being mainly used in sensitive bacterial and causing, as gram-negative bacteria particularly burn infection, septicemia, respiratory system infection, urinary system infection, gallbladder biliary tract infection and the soft tissue severe infections etc. that cause such as bacillus pyocyaneus, escherichia coli and pneumobacillus.
Tobramycin mainly contains the dosage forms such as eye drop, oral formulations, injection at present for Clinical practice, because oral formulations easily produces first pass effect toxic to hepatocyte in the gastrointestinal tract, injection easily produces pain and lump in injection site, and access times are many, patient is easily made to produce psychological burden.
Traditional black plaster uses inconvenience, and skin irritation is large, and anaphylaxis is many.And transdermal drug delivery system have administration time long, avoid first pass effect, reduce the untoward reaction of medicine and the advantage such as easy to use, be a kind of more satisfactory form of administration.Matrix-type transdermal absorbable preparation at present about tobramycin does not also have research.
Summary of the invention
The present invention uses inconvenient, that targeting is poor shortcoming to solve existing tobramycin, has invented tobramycin matrix-type transdermal absorbable preparation.
The invention provides a kind of pharmaceutical preparation, comprising tobramycin.
The invention provides a kind of transdermal absorption formulation, comprising tobramycin.
The invention provides a kind of tobramycin transdermal absorption formulation, comprise storage layer, adhesive-layer, backing layer and protective layer four part, storage layer comprises tobramycin 11-15 part, framework material 50-54 part, penetration enhancer 9-12 part and other 1-25 parts.Preferred tobramycin 12 parts, framework material 52 parts, penetration enhancer 11 parts and pressure sensitive adhesive 1 part.
The preparation method of tobramycin transdermal absorption formulation is: be dispersed in framework material by medicine and penetration enhancer, is then placed on glass plate in fixing mould or clean, plastic film mulch, dry, demoulding, puts into reinforce and pastes, add up-protective layer and get final product.
Preferably, transdermal absorption formulation formation of the present invention is followed successively by backing layer, adhesive-layer, storage layer, adhesive-layer, storage layer, adherent layer; Or backing layer, adhesive-layer, storage layer, adhesive-layer, adherent layer; Or backing layer, adhesive-layer, storage layer, adherent layer;
Described framework material is polrvinyl chloride or polyvinyl alcohol or polyacrylic resin;
Also containing penetration enhancer in described storage layer, penetration enhancer is poloxamer, carbamide, Borneolum Syntheticum, N-N-ethyl pyrrole N-ketone, sodium laurylsulfate or oleic acid or their mixture;
Applicant is surprised to find that and adopts specific penetration enhancer, and adds a small amount of serine wherein, can significantly strengthen Transdermal absorption effect.Preferably, use the compositions of serine, N-N-ethyl pyrrole N-ketone and sodium laurylsulfate as penetration enhancer, and the part by weight of three is 1:4:6.
Described backing layer and adhesive-layer are to reinforce and paste;
Described adhesive-layer surface is also provided with adherent layer, and adherent layer is separate paper.Protective layer is separate paper.
Embodiment 1
Comprise storage layer, adhesive-layer, backing layer and protective layer four part, wherein the drug storehouse layer of storage layer comprises drug storehouse layer 1 and drug storehouse layer 2 is two-layer, drug storehouse layer 1 consist of tobramycin 6g, polrvinyl chloride 52g, serine 0.5g, N-N-ethyl pyrrole N-ketone 2g, sodium laurylsulfate 4g; Drug storehouse layer 2 consist of tobramycin 6g, pressure sensitive adhesive 1g, serine 0.5g, N-N-ethyl pyrrole N-ketone 2g, sodium laurylsulfate 2g; Adhesive-layer comprises pressure sensitive adhesive 3g.Other compositions of the present embodiment are water.Preferably, above-mentioned 1 " g " represents 1 gram.
Preparation method is: after the medicine tobramycin water dissolution in drug storehouse layer 1, mixs homogeneously, is placed on the glass plate of clean flat smooth, makes into a thin film, 60-80 DEG C of drying, demoulding with polrvinyl chloride, serine, N-N-ethyl pyrrole N-ketone, sodium laurylsulfate.By pressure sensitive adhesive and thickening agent mixing, plastic film mulch on separate paper, dry, paste as reinforcing.By the tobramycin in medicine layer 2, pressure sensitive adhesive and serine, N-N-ethyl pyrrole N-ketone, sodium laurylsulfate mix homogeneously, heating deaeration, be placed in the mould being lined with separate paper, plastic film mulch, removing mould, drying 2 hours under 80 DEG C of conditions, film in medicine layer 1 is pasted on the reinforcing removing separate paper to paste on (backing layer), medicine layer 1 and 2 is pasted together by adhesive-layer.Backing layer is pasted on the protection layer, cuts into 5*6cm
2paster.Every square centimeter of content of dispersion is 0.20-0.30mg.
Pressure sensitive adhesive selected by the present invention and thickening agent are pressure sensitive adhesive and the thickening agent of the use of field of pharmaceutical preparations routine, preferred pressure sensitive adhesive is polyisobutylene class pressure sensitive adhesive, particularly, be high molecular weight polyisobutylene (number-average molecular weight is 120,000 ~ 250,000, viscosity-average molecular weight 300,000 ~ 1,200,000).Thickening agent is carbomer.
Comparative example 1
The present embodiment comprises storage layer, adhesive-layer, backing layer and protective layer four part, and wherein the drug storehouse layer of storage layer comprises tobramycin 12g, polrvinyl chloride 52g, N-N-ethyl pyrrole N-ketone 5g, sodium laurylsulfate 6g, pressure sensitive adhesive 1g; Adhesive-layer comprises pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 2
The present embodiment comprises storage layer, adhesive-layer, backing layer and protective layer four part, and wherein the drug storehouse layer of storage layer comprises tobramycin 12g, polyvinyl alcohol 52g, poloxamer 11g, pressure sensitive adhesive 1g; Adhesive-layer comprises pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 3
The present embodiment comprises storage layer, adhesive-layer, backing layer and protective layer four part, and wherein the drug storehouse layer of storage layer comprises tobramycin 12g, polrvinyl chloride 52g, N-N-ethyl pyrrole N-ketone 11g, pressure sensitive adhesive 1g; Adhesive-layer comprises pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 4
The present embodiment comprises storage layer, adhesive-layer, backing layer and protective layer four part, and wherein the drug storehouse layer of storage layer comprises tobramycin 12g, polyvinylpyrrolidone 55g, azone 4g, carbamide 2g, pressure sensitive adhesive 1g; Adhesive-layer comprises pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Comparative example 5
The present embodiment comprises storage layer, adhesive-layer, backing layer and protective layer four part, and wherein the drug storehouse layer of storage layer comprises tobramycin 10g, polrvinyl chloride 55g, serine 5g, N-N-ethyl pyrrole N-ketone 2g, sodium laurylsulfate 4g, pressure sensitive adhesive 1g; Adhesive-layer comprises pressure sensitive adhesive 3g.Other compositions are water.Every square centimeter of content of dispersion is 0.20-0.30mg.
Preparation method is with embodiment 1.
Illustrate: the adjuvant used relative to embodiment 1 and consumption, following comparative example has made following amendment:
The penetration enhancer of comparative example 1 does not use serine;
Comparative example 2 uses poloxamer as penetration enhancer;
Comparative example 3 only uses N-N-ethyl pyrrole N-ketone as penetration enhancer;
Comparative example 4 uses polyvinylpyrrolidone as framework material, uses azone and carbamide as penetration enhancer;
Comparative example 5 changes each Ingredient Amount.
Above-described embodiment 1 is identical with the unit of weight that comparative example 1-5 adopts, and namely 1 " part " represents identical weight.Preferably, 1 " part " represents 1 gram.
The permeation test in vitro of tobramycin transdermal absorption formulation
1. skin treatment peels off the skin of abdomen of the 24h mice that lost hair or feathers, and removes subcutaneous fat, cleans and soaks, put 4 DEG C of Refrigerator stores for subsequent use with normal saline.
2. the skin handled well lies in Franz diffusion cell by penetrating absorption, fixing, embodiment 1 and comparative example 1-5 paster is given to coyote hole, receiving liquid is normal saline 6mL, magnetic stirrer, makes Corium Mus and accepts liquid level and contact, under 39 DEG C ± 0.1 DEG C condition, continuous stirring, respectively samples 2mL, for the mensuration of tobramycin transdermal amount respectively at 7h continuous after application of sample.Normal saline 2mL is added after every sub-sampling.Sample is with after 0.45 μm of filtering with microporous membrane, and get 20 μ L and carry out HPLC mensuration, replication 3 times, records peak area and calculate content.
The accumulative transdermal penetration amount M of different sample point is calculated as follows:
M＝C
nV+Σ
n-1i＝1C
iV
i
In formula, M is accumulative transdermal penetration amount; C
nfor sampling the concentration of liquid during each sample point; V is reception tank volume; C
ifor the concentration of each sample point sampling liquid; V
ifor sample volume.
Tobramycin total amount in tobramycin transdermal penetration rate=tobramycin transdermal penetration amount × 100%/paster
The results are shown in Table 1.
Matched group: comprise storage layer, adhesive-layer, backing layer and protective layer four part, wherein the drug storehouse layer of storage layer comprises tobramycin 12 parts, polrvinyl chloride 52 parts, pressure sensitive adhesive 1 part; Adhesive-layer comprises pressure sensitive adhesive 3 parts.Other compositions are water.Preparation method is with embodiment 1.
In table 1 by tobramycin transdermal penetration rate referred to as tobramycin transmitance.
Table 1
From table 1 data, in comparative example 1-5, tobramycin transmitance is far below embodiment 1, and when 7h, in embodiment 1, tobramycin transmitance is 84%, and in comparative example 1-5, tobramycin transmitance is all no more than 50%, has significant difference.As can be seen here, the adjuvant that the tobramycin transdermal absorption formulation that request of the present invention is protected is selected and consumption are all specific, and its effect is also beat all good.That adjuvant type change or supplementary product consumption change all can obviously reduce Transdermal absorption effect.
Claims (4)
1. a pharmaceutical preparation, comprising tobramycin.
2. pharmaceutical preparation as claimed in claim 1, it is a kind of transdermal absorption formulation, comprising tobramycin.
3. pharmaceutical preparation as claimed in claim 2; wherein tobramycin transdermal absorption formulation comprises storage layer, adhesive-layer, backing layer and protective layer four part; storage layer comprises tobramycin 12 parts, framework material 52 parts, penetration enhancer 11 parts and pressure sensitive adhesive 1 part, by weight.
4. pharmaceutical preparation as claimed in claim 3, wherein in storage layer, framework material is polrvinyl chloride, and penetration enhancer is the compositions of serine, N-N-ethyl pyrrole N-ketone and sodium laurylsulfate, and the part by weight of three is 1:4:6.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410484374.5A CN104208042B (en) | 2014-09-19 | 2014-09-19 | A kind of transdermal absorption formulation |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410484374.5A CN104208042B (en) | 2014-09-19 | 2014-09-19 | A kind of transdermal absorption formulation |
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| Publication Number | Publication Date |
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| CN104208042A true CN104208042A (en) | 2014-12-17 |
| CN104208042B CN104208042B (en) | 2016-08-31 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106509652A (en) * | 2016-11-08 | 2017-03-22 | 雅安职业技术学院 | Method for preparing diced pork in pot by use of microwave heating sterilization |
| CN107233333A (en) * | 2017-06-12 | 2017-10-10 | 重庆安格龙翔医药科技有限公司 | A kind of epinastine hydrochloride transdermal patch and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002032459A2 (en) * | 2000-10-17 | 2002-04-25 | Massachusetts Institute Of Technology | Method of increasing the efficacy of antibiotics by complexing with cyclodextrins |
| CN1969971A (en) * | 2006-12-01 | 2007-05-30 | 哈尔滨商业大学 | Transdermal absorption formulation of total alkaloid of common monkshood root and preparation process thereof |
| CN102014886A (en) * | 2008-03-07 | 2011-04-13 | Lectec公司 | Hand sanitizing patch |
-
2014
- 2014-09-19 CN CN201410484374.5A patent/CN104208042B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002032459A2 (en) * | 2000-10-17 | 2002-04-25 | Massachusetts Institute Of Technology | Method of increasing the efficacy of antibiotics by complexing with cyclodextrins |
| CN1969971A (en) * | 2006-12-01 | 2007-05-30 | 哈尔滨商业大学 | Transdermal absorption formulation of total alkaloid of common monkshood root and preparation process thereof |
| CN102014886A (en) * | 2008-03-07 | 2011-04-13 | Lectec公司 | Hand sanitizing patch |
Non-Patent Citations (1)
| Title |
|---|
| 崔福德: "《药剂学》", 29 February 2004, 人民卫生出版社出版 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106509652A (en) * | 2016-11-08 | 2017-03-22 | 雅安职业技术学院 | Method for preparing diced pork in pot by use of microwave heating sterilization |
| CN107233333A (en) * | 2017-06-12 | 2017-10-10 | 重庆安格龙翔医药科技有限公司 | A kind of epinastine hydrochloride transdermal patch and preparation method thereof |
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| Publication number | Publication date |
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| CN104208042B (en) | 2016-08-31 |
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