CN104490851B - Iseganan quick-release film agent - Google Patents
Iseganan quick-release film agent Download PDFInfo
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- CN104490851B CN104490851B CN201410855629.4A CN201410855629A CN104490851B CN 104490851 B CN104490851 B CN 104490851B CN 201410855629 A CN201410855629 A CN 201410855629A CN 104490851 B CN104490851 B CN 104490851B
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- release film
- iseganan
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- 108010078256 antimicrobial peptide IB-367 Proteins 0.000 title claims abstract description 35
- GUCYBPFJNGVFEB-XELKFLSISA-N iseganan Chemical compound C([C@H]1C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CC=3C=CC=CC=3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)CNC(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(N1)=O)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)CCCNC(N)=N)CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)C(C)C)C1=CC=C(O)C=C1 GUCYBPFJNGVFEB-XELKFLSISA-N 0.000 title claims abstract description 35
- 229950000488 iseganan Drugs 0.000 title claims abstract description 34
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 17
- 239000007853 buffer solution Substances 0.000 claims abstract description 13
- 239000004014 plasticizer Substances 0.000 claims abstract description 7
- 239000004094 surface-active agent Substances 0.000 claims abstract description 7
- 239000000945 filler Substances 0.000 claims abstract description 6
- 239000002994 raw material Substances 0.000 claims abstract description 6
- 238000002360 preparation method Methods 0.000 claims description 30
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 20
- 239000003814 drug Substances 0.000 claims description 13
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 13
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 13
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 12
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 12
- 239000008363 phosphate buffer Substances 0.000 claims description 12
- 239000000811 xylitol Substances 0.000 claims description 12
- 235000010447 xylitol Nutrition 0.000 claims description 12
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 12
- 229960002675 xylitol Drugs 0.000 claims description 12
- 235000011187 glycerol Nutrition 0.000 claims description 10
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 9
- 229930195725 Mannitol Natural products 0.000 claims description 9
- 235000016257 Mentha pulegium Nutrition 0.000 claims description 9
- 235000004357 Mentha x piperita Nutrition 0.000 claims description 9
- 235000001050 hortel pimenta Nutrition 0.000 claims description 9
- 239000000594 mannitol Substances 0.000 claims description 9
- 235000010355 mannitol Nutrition 0.000 claims description 9
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 9
- 229920000053 polysorbate 80 Polymers 0.000 claims description 9
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 8
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 8
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 8
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 8
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 8
- 229940075582 sorbic acid Drugs 0.000 claims description 8
- 235000010199 sorbic acid Nutrition 0.000 claims description 8
- 239000004334 sorbic acid Substances 0.000 claims description 8
- 239000000463 material Substances 0.000 claims description 6
- 208000003265 stomatitis Diseases 0.000 claims description 6
- 229940037201 oris Drugs 0.000 claims description 4
- 230000008961 swelling Effects 0.000 claims description 4
- 230000000873 masking effect Effects 0.000 claims description 3
- 238000001914 filtration Methods 0.000 claims description 2
- 239000012467 final product Substances 0.000 claims description 2
- 208000014674 injury Diseases 0.000 claims description 2
- 238000011017 operating method Methods 0.000 claims description 2
- 230000008733 trauma Effects 0.000 claims description 2
- 210000001215 vagina Anatomy 0.000 claims description 2
- 241001479543 Mentha x piperita Species 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 241000894006 Bacteria Species 0.000 abstract description 8
- 239000003910 polypeptide antibiotic agent Substances 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 2
- 108700042778 Antimicrobial Peptides Proteins 0.000 abstract 1
- 102000044503 Antimicrobial Peptides Human genes 0.000 abstract 1
- 239000000796 flavoring agent Substances 0.000 abstract 1
- 235000013355 food flavoring agent Nutrition 0.000 abstract 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 8
- 244000246386 Mentha pulegium Species 0.000 description 8
- 230000000694 effects Effects 0.000 description 8
- 241000220223 Fragaria Species 0.000 description 6
- 235000016623 Fragaria vesca Nutrition 0.000 description 6
- 235000011363 Fragaria x ananassa Nutrition 0.000 description 6
- 239000002202 Polyethylene glycol Substances 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 210000000214 mouth Anatomy 0.000 description 6
- 229920001223 polyethylene glycol Polymers 0.000 description 6
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 5
- 235000010445 lecithin Nutrition 0.000 description 5
- 239000000787 lecithin Substances 0.000 description 5
- 229940067606 lecithin Drugs 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 229910000019 calcium carbonate Inorganic materials 0.000 description 4
- 235000010980 cellulose Nutrition 0.000 description 4
- 229920002678 cellulose Polymers 0.000 description 4
- 239000001913 cellulose Substances 0.000 description 4
- 239000004372 Polyvinyl alcohol Substances 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000000377 silicon dioxide Substances 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 230000000857 drug effect Effects 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 210000004400 mucous membrane Anatomy 0.000 description 2
- 244000052769 pathogen Species 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 210000003296 saliva Anatomy 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 208000034493 Mucous membrane disease Diseases 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 241000170793 Phalaris canariensis Species 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 241000235342 Saccharomycetes Species 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 239000005864 Sulphur Substances 0.000 description 1
- 101000730859 Sus scrofa Protegrin-1 Proteins 0.000 description 1
- 208000025865 Ulcer Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000001785 acacia senegal l. willd gum Substances 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 125000003275 alpha amino acid group Chemical group 0.000 description 1
- 244000052616 bacterial pathogen Species 0.000 description 1
- 208000020670 canker sore Diseases 0.000 description 1
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 description 1
- 230000005779 cell damage Effects 0.000 description 1
- 208000037887 cell injury Diseases 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 239000002158 endotoxin Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000002949 hemolytic effect Effects 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 238000007654 immersion Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 229920006008 lipopolysaccharide Polymers 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004379 membrane Anatomy 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 229940083466 soybean lecithin Drugs 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000397 ulcer Toxicity 0.000 description 1
- 229940126572 wide-spectrum antibiotic Drugs 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
The invention provides an iseganan quick-release film agent. The film agent is prepared from the following raw materials in percentage by weight: 0.001-0.3 percent of iseganan, 30-80 percent of a film forming agent, 0.01-9 percent of plasticizer, 0.2-3.0 percent of a flavoring agent, 0.02-0.5 percent of surfactant, 0-20 percent of filler and the balance of a buffer solution. The quick-release film agent can be quickly released in 1 minute, so that antimicrobial peptide can quickly reach high concentration in an administration position, and the bacterium resisting and inhibiting effect can be effectively achieved.
Description
Technical field
The present invention relates to the quick-release film of Iseganan.
Background technology
Iseganan (iseganan；IB-367；CAS257277-05-7 amino acid sequence H-Arg-Gly-Gly-)
Leu-Cys-Tyr-Cys-Arg-Gly-Arg-Phe-Cys-Val-Cys-Val-Gly-Arg-NH2(5-14,7-12；Two sulphur
Key), molecular formula is C78H126N30O18S4, molecular weight is the (protegrin- of pig Neutrophil peptide -1 for 1900.29Iseganan
1, PG-1) analog, can be combined with the extracellular composition such as lipopolysaccharides of bacterium or adipose membrane acid etc., cause bacterium to expand, rupture,
Bacterium is killed by destroying cell membrane.
Due to its particular mechanism of Iseganan, it has broad-spectrum sterilization to oral microorganism, does not produce drug resistance,
Have no toxic side effect, possess instead of the potential quality of conventional antibiotic.In vitro study shows its, negative bacteria positive to Gram and true
Bacterium, saccharomycete/eucaryon protozoon etc. is respectively provided with inhibitory action, can reduce the seriousness of oral mucositis, and shortens the course of disease, for connecing
By the patient of chemotherapy, iseganan can reduce the pain and symptom of its oral mucositis, and to human erythrocyte haemocylolysis
Very little.Iseganan is 0.13~64 μ g/ml to the MIC of gram-positive bacteria；It is cloudy to the Glanz related to oral mucositis
Property bacterium MIC be 0.06~8 μ g/ml.
Pelliculae pro cavo oris direct effect oral cavity mucous membrane tissue, can be played rapidly as a kind of new oral drug delivery system
Drug effect simultaneously keeps finite concentration, both with tablet content of dispersion is accurate, good stability the characteristics of, be provided simultaneously with liquid preparation absorption
Hurry up, the advantage that curative effect is high, and preparation process is simple strong operability.Because its volume is small and light, transport easy to carry.Due to oral cavity
In often there is saliva to stop, film can both extend the holdup time of medicine, can heighten the effect of a treatment again, play the collaboration of lasting drug effect
Effect.With nontoxic, nonirritant, determined curative effect, dosage is small, and goes wrong and can remove immediately.
Film is divided into sustained release film formulation, quick-release film again, wherein, quick-release film can quickly release the drug in a short time so that
Drug concentration reaches peak value in a short time, so as to reach optimum curative effect.Yet there are no and Iseganan is prepared into quick-release film
The research of agent.
The content of the invention
It is an object of the invention to provide a kind of Iseganan film of quick release, another object of the present invention is to carry
For the preparation method and purposes of film.
Specifically, the invention provides the quick-release film of Iseganan, its raw material contains the component of following weight proportion：
Iseganan 0.001~0.3%, film forming agent 30~80%, plasticizer 0.01~9%, flavouring 0.2~3.0%,
Surfactant 0.02~0.5%, filler 12~24%, balance of buffer solution；
Wherein, the film forming agent is selected from PVA05-88, Arabic gum, CMC-Na, PVA17-88, one or two in HPMC
Combination above；The plasticizer is selected from one or more the combination in glycerine, polyethylene glycol, sorbierite；It is described to fill out
Fill agent and be selected from one or more combination in mannitol, silica, microcrystalline cellulose, calcium carbonate；The buffer solution choosing
From the phosphate buffer of PH6.5~7.1；The surfactant is selected from Tween 80, fatty acid sorbitan, soybean lecithin
One or more combination；The flavouring is selected from one or more the group in xylitol, strawberry essence, peppermint
Close.
Although current film is varied, however, yet there are no for Iseganan to be prepared into oral cavity quick-release film, how to select
Qualified quick-release film can be prepared with auxiliary material, is a problem of the invention.Although the present invention has used various medicines
Thing film layer supplementary product kind and consumption proportion, but it is possible to meet in 1min quick release and filming performance and mouthfeel are good
Ratio of adjuvant species and few, such as Chinese patent application：A kind of cellulose derivative is disclosed in 201010297888.1 to answer
Film is closed, is mainly made up of cellulose hydrophilic derivative 1~10, polyvinyl alcohol 1~10, the cellulose hydrophilic derivative is
Carboxymethylcellulose calcium, hydroxypropyl cellulose or HPMC, the polyvinyl alcohol are PVA05-88 or/and PVA17-
88, such film has good translucency, swellability and permeability, but, found in research process of the present invention (be shown in Table 1,
2), using the auxiliary material and proportioning referred in above-mentioned patent application, pelliculae pro cavo oris of the present invention cannot be allowed at all while meeting good
Rate of release, film forming and mouthfeel, if desired prepare the good quick-release film of various aspects of performance, only use following suitable spy
Fixed proportioning：
The raw material contains the component of following weight proportion：
Iseganan 0.001~0.3%, film forming agent 50%, plasticizer 8.2%, flavouring 2.5%, surfactant
0.04%th, filler 16%, balance of buffer solution.
Further, film forming agent is selected from PVA05-88：HPMC=48：2, plasticizer is selected from glycerine：Sorbic acid=8:
0.2, flavouring is selected from xylitol：Peppermint=0.4：2.1, surfactant is selected from Tween 80；Filler is selected from mannitol：Crystallite
Cellulose=1：1, buffer solution is selected from the phosphate buffer of PH6.8.
In film of the present invention, the content of Iseganan can be converted according to the common dose of the antibacterial peptide, can also
The adjustment of adaptability is carried out according to actual conditions.In a specific embodiment of the invention, the content of Iseganan is 0.03%.
Wherein, the film is pelliculae pro cavo oris.
Wherein, the thickness of the film is 11~87um.
Present invention also offers the preparation method of above-mentioned quick-release film, it includes following operating procedure：
(1) raw material is taken by proportioning；
(2) it is PVA05-88 is swelling with buffer solution, dissolving is heated to, filtering adds other auxiliary materials while hot, after dissolving,
Iseganan is added when being cooled to 40-44 DEG C, adds buffer solution to make enough, be sufficiently stirred for making to be well mixed, de-bubbled, masking,
Obtain final product.
Present invention also offers above-mentioned quick-release film in the medicine for preparing treatment oral mucositis, skin trauma or burn
Purposes.
Further, the medicine is sublingual administration preparation, vagina administration preparation, external preparation skin, oral film agent.
In a specific embodiment of the invention, it is possible to use film of the present invention treats canker sore, when ulcer occurs, stick
Film integrality is destroyed, and medicine can enter in the surface of a wound, directly acts on oral cavity pathogen and produces therapeutic effect, it is to avoid mucous membrane
To the inhibition of medicine.Although the present invention is designed mainly for oral keritonocytes, by the present invention for treating phase
It is also feasible to answer the skin or mucous membrane disease at other positions of human body caused by pathogenic bacteria.
Quick-release film advantage of the present invention is as follows：
1. the quick-release film is using antibacterial peptide as active component, the antibacterial peptide：With unique bactericidal mechanism, with wide spectrum
Antibiotic property, can efficiently kill and suppress various oral cavity pathogens, and low hemolytic does not result in human normal cell's injury, without resistance to
The property of medicine and be easy to by human body decompose discharge；The antibacterial peptide has low dose of, low concentration antibacterial, strong to high level salt solution tolerance, easy
Preserve, be difficult by characteristics such as proteases for decomposing.
2. quick-release film of the present invention can in 1min quick release so that antibacterial peptide is rapidly achieved highly concentrated in agents area
Degree, can more effectively kill bacterium.Meanwhile, on the premise of preferable mouthfeel is ensured, medicine goes directly focus film of the present invention
Rapid antibacterial, improves compliance, easy to use；Often there is saliva to stop in oral cavity, general formulation is difficult to be retained in oral mucositis
Curative effect is played at disease, the qucik-acting agent viscosity is good, medicine energy quick release, worked quick.
3. said preparation is free of ethanol, and materials safety and precise, gentle nonirritant, good mouthfeel is adapted to all groups, including
Pregnant woman, child, old man.
Specific embodiment
The preparation (each embodiment prescription is defined by table 1) of the quick-release film of the present invention of embodiment 1
Quick-release film prescription
The sorbic acid 0.2% of 0.03% glycerine of Iseganan, 14% polyethylene glycol 8%
The microcrystalline cellulose 16% of 0.4% strawberry essence of xylitol, 0.4% mannitol 8%
The HPMC 24% of 0.01% PVA05-88 of Tween 80 24%
Balance of phosphate buffer (PH6.8)
Preparation method：
1. make it fully swelling with the immersion of enough buffer solutions PVA05-88, by fully swelling PVA05-88 with 65 DEG C-
80 DEG C of heating are allowed to dissolve for 2 hours, and filter；
2. mix：Other auxiliary materials in addition to flavouring are slowly added in PVA05-88 upon dissolution, it is stirring while adding,
Add flavouring and be slowly stirred to after solution is cooled to 40-44 DEG C and be gradually slowly added to Iseganan, it is stirring while adding；
3. add buffer solution to make enough, and be sufficiently stirred for being well mixed solution, stand 8-12 hours, de-bubbled, masking,
.
The preparation of the quick-release film of the present invention of embodiment 2
Quick-release film prescription
The xylitol 0.2% of 0.03% glycerine of Iseganan, 8% polyethylene glycol 8%
The Tween 80 0.02% of 8% silica of mannitol, 8% calcium carbonate 8%
The HPMC 30% of 2% PVA05-88 of Fabaceous Lecithin 12%
Balance of phosphate buffer (PH6.8)
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 3
Quick-release film prescription
The sorbic acid 0.2% of 0.03% polyethylene glycol of Iseganan 8%
The microcrystalline cellulose 8% of 0.6% peppermint of xylitol, 1.7% mannitol 4%
The PVA17-88 24% of 0.32% PVA05-88 of Tween 80 12%
The balance of phosphate buffers (PH6.8) of HPMC 36%
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 4
Quick-release film prescription
The xylitol 0.4% of 0.03% polyethylene glycol of Iseganan 8%
The Tween 80 0.16% of 0.2% peppermint of strawberry essence, 0.9% mannitol 12%
The balance of phosphate buffers (PH6.8) of 48% HPMC of PVA05-88 4%
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 5
Quick-release film prescription
The sorbic acid 0.2% of 0.03% glycerine of Iseganan, 8% polyethylene glycol 8%
The microcrystalline cellulose 16% of 0.4% strawberry essence of xylitol, 0.8% peppermint 3.3%
The PVA17-88 6% of 8% Fabaceous Lecithin of calcium carbonate, 2% PVA05-88 6%
The balance of phosphate buffers (PH6.8) of HPMC 26.4%
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 6
Quick-release film prescription
The xylitol 0.4% of 0.03% glycerine of Iseganan 8%
The Tween 80 0.08% of 8% silica of mannitol, 8% microcrystalline cellulose 8%
The HPMC 3.2% of 4% PVA05-88 of Fabaceous Lecithin, 24% PVA17-88 24%
Balance of phosphate buffer (PH6.8)
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 7
Quick-release film prescription
The xylitol 0.4% of 0.03% glycerine of Iseganan, 8% sorbic acid 0.2%
The Tween 80 0.04% of 2.1% microcrystalline cellulose of peppermint 8%
The balance of phosphate buffers (PH6.8) of 48% HPMC of PVA05-88 2%
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 8
Quick-release film prescription
The xylitol 0.4% of 0.03% glycerine of Iseganan, 8% sorbic acid 0.1%
The Fabaceous Lecithin 0.08% of 0.6% peppermint of strawberry essence, 2.1% calcium carbonate 16%
The balance of phosphate buffers (PH6.8) of 48% HPMC of PVA05-88 1%
Preparation method is with embodiment 1.
The preparation of the quick-release film of the present invention of embodiment 9
Quick-release film prescription
The xylitol 0.4% of 0.03% glycerine of Iseganan, 8% sorbic acid 0.4%
The microcrystalline cellulose 4% of 0.1% peppermint of strawberry essence, 2.1% mannitol 8%
The HPMC 6% of 0.04% PVA05-88 of Fabaceous Lecithin 48%
Balance of phosphate buffer (PH6.8)
Preparation method is with embodiment 1.
Prepared by embodiment 1~9 into film to be investigated, as a result referring to table 2
Each embodiment prescription of table 1
Table 2
It can be seen from upper table content, the film that only prepared by the prescription of embodiment 7 can meet the requirements, and can not only meet
The quick-release release in 1min, and filming performance, appearance character, mouthfeel are optimal；Wherein, embodiment 3,5,6,9 etc., use into
Film comes from Chinese patent application 201010297888.1, it is demonstrated experimentally that the film forming agent proportioning of the patent application is not appropriate for
Iseganan quick-release film is prepared, gained film performance is substantially not as good as embodiment 7.As can be seen here, although various embodiments of the present invention
Film former component is more similar, however, the change of a portion composition and consumption is just enough to cause the huge difference of film performance
It is different, thus the selected embodiment 7 of the present invention prescription be quick-release film of the present invention best prescription.
The quick-release film weight differential of embodiment 10 is checked
1. inspection technique：Test sample 20 prepared by Example 7, accurately weighed weight tries to achieve average weight, then essence respectively
The weight of close weighed each.Per sheet weight compared with average weight
2. test result is as follows
Table 3
Check result of determination：It is qualified.
Claims (7)
1. the quick-release film of Iseganan, it is characterised in that：Its raw material contains the component of following weight proportion：
Iseganan 0.001~0.3%, film forming agent 50%, plasticizer 8.2%, flavouring 2.5%, surfactant 0.04%,
Filler 16%, balance of buffer solution；
Wherein, film forming agent is selected from PVA05-88：HPMC=48：2, plasticizer is selected from glycerine：Sorbic acid=8:0.2, flavouring choosing
From xylitol：Peppermint=0.4：2.1, surfactant is selected from Tween 80；Filler is selected from mannitol：Microcrystalline cellulose=1：1,
Buffer solution is selected from the phosphate buffer of pH6.8.
2. quick-release film according to claim 1, it is characterised in that：The content of Iseganan is 0.03%.
3. quick-release film according to claim 1, it is characterised in that：The film is pelliculae pro cavo oris.
4. the quick-release film according to claims 1 to 3 any one, it is characterised in that：The thickness of the film be 11~
87μm。
5. the preparation method of quick-release film described in claim 1, it is characterised in that：It includes following operating procedure：
(1) raw material is taken by proportioning；
(2) it is PVA05-88 is swelling with buffer solution, dissolving is heated to, filtering adds other auxiliary materials while hot, after dissolving, cooling
Iseganan is added during to 40-44 DEG C, adds buffer solution to make enough, be sufficiently stirred for making to be well mixed, de-bubbled, masking is obtained final product.
6. claim 1,2 or quick-release film described in 4 any one are preparing treatment oral mucositis, skin trauma or burn
Purposes in medicine.
7. purposes according to claim 6, it is characterised in that：The medicine be sublingual administration preparation, vagina administration preparation,
External preparation, oral film agent.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410855629.4A CN104490851B (en) | 2014-12-31 | 2014-12-31 | Iseganan quick-release film agent |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410855629.4A CN104490851B (en) | 2014-12-31 | 2014-12-31 | Iseganan quick-release film agent |
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| CN104490851B true CN104490851B (en) | 2017-05-24 |
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| CN105288586A (en) * | 2015-08-28 | 2016-02-03 | 广东海纳川生物科技股份有限公司 | Antibacterial peptide plectasin film-forming agent and preparation method and application thereof |
| CN108324724A (en) * | 2018-04-10 | 2018-07-27 | 苏州芝宇生物科技有限公司 | The preparation method of a kind of gram of vertical boron sieve dissolvable film preparation and its application |
| CN108815141A (en) * | 2018-08-24 | 2018-11-16 | 中国农业科学院饲料研究所 | Antibacterial peptide film and the preparation method and application thereof |
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| CN1524577A (en) * | 2003-02-27 | 2004-09-01 | 珠海亿胜生物制药有限公司 | Alkaline fibroblast growth factor pellicle and its production method |
| CN1899600A (en) * | 2005-07-22 | 2007-01-24 | 上海高科联合生物技术研发有限公司 | Antibiotic peptide spray film forming agent and its preparing method |
| CN1931148A (en) * | 2006-09-28 | 2007-03-21 | 上海大学 | Prepn process of levofloxacin lactate oral film |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1524577A (en) * | 2003-02-27 | 2004-09-01 | 珠海亿胜生物制药有限公司 | Alkaline fibroblast growth factor pellicle and its production method |
| CN1899600A (en) * | 2005-07-22 | 2007-01-24 | 上海高科联合生物技术研发有限公司 | Antibiotic peptide spray film forming agent and its preparing method |
| CN1931148A (en) * | 2006-09-28 | 2007-03-21 | 上海大学 | Prepn process of levofloxacin lactate oral film |
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| Antimicrobial therapy to prevent or treat oral mucositis;J Peter Donnelly，et al;《The lancet infectious diseases》;20030731;第3卷;405-412 * |
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