CN101797413A - Drug carrier for nasal administration - Google Patents
Drug carrier for nasal administration Download PDFInfo
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- CN101797413A CN101797413A CN200910101175A CN200910101175A CN101797413A CN 101797413 A CN101797413 A CN 101797413A CN 200910101175 A CN200910101175 A CN 200910101175A CN 200910101175 A CN200910101175 A CN 200910101175A CN 101797413 A CN101797413 A CN 101797413A
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- spherical surface
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- intersecting
- pharmaceutical carrier
- chitin
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Abstract
The invention relates to a drug carrier for nasal administration, which has convenient use and good effect and is provided with a body capable of being filled into the nasal cavity. The body is formed by combining a spherical surface body (1) and a cylindrical intersecting body (3), wherein the spherical surface body is provided with a connecting port, two ends of the intersecting body are provided with openings, the opening at the inner end of the intersecting body is tightly connected with the connecting port of the spherical surface body to ensure that the intersecting body is connected with the spherical surface body into a whole and communicated with the spherical surface body, the body formed by combining the spherical surface body and the intersecting body is formed by compounding an inner surface layer (5) and an outer surface layer (6), the spherical surface body is provided with a through hole (4) it the top of the axial line direction of the spherical surface body and the intersecting body, and the inner wall of the body is provided with a filter screen layer (2) in a supporting way. The invention is suitable for being used as a carrier for the nasal administration.
Description
Technical field
The present invention relates to pharmaceutical carrier, particularly can fill in the pharmaceutical carrier of the nasal-cavity administration of nasal cavity.
Background technology
Medical practice proves, all there are slow, the problem such as waste is big, side effect is many that takes effect in traditional oral administration, drug administration by injection.
Theory of Chinese medical science and tcm clinical practice prove, the nasal-cavity administration instant effect, and its speed that takes effect exceeds several times than oral administration, quite intravenous effect.Enter blood because nasal-cavity administration is a medicinal liquid by direct absorption of nasal mucosa, the first road reaction of digestive tract and liver does not take place in medicine in vivo, and side effect is little, and ingredient is not damaged, absorbance height, instant effect.But, must guarantee eupnea, so directly just produce big difficulty to nasal-cavity administration because nasal cavity is the respiratory tract door.
The inventor's ZL 95205440.X China utility model patent description has disclosed a kind of dustproof Nasal filtering rhinobyon that is used for, and its structure and the selection of material still are confined to reduce dust pollution, and no medicine carries function.
Summary of the invention
The present invention will solve the big problem of nasal-cavity administration difficulty, and the pharmaceutical carrier of a kind of nasal-cavity administration of the present invention is provided for this reason, and this carrier can be filled in nasal cavity, with the drug effect of carrier carrying in nasal membrane, directly enter blood circulation, it is fast that drug effect produces speed, and do not influence eupnea.
For addressing the above problem, the technical solution used in the present invention is to have the body that can fill in nasal cavity, its special character is the intersecting body be combined into of described body by spherical surface body and tubular, described spherical surface body has one and connects the aperture, described intersecting body both ends open, the aperture that is connected of the interior end opening of intersecting body and described spherical surface body is connected airtight and is made intersecting body and spherical surface body be linked to be whole and connect mutually, described body by spherical surface body and intersecting body be combined into is by the endosexine and extexine is compound constitutes, described spherical surface body has through hole at the top of body axis direction, and described inner body wall support is provided with the filtration stratum reticulare.
Described filtration stratum reticulare mesh is advisable with 60～80 orders.
Described intersecting body can be that its osculum end of frustum tubular connects airtight the described connection aperture in spherical surface body.
The endosexine of described body contains chitin, hydroxypropyl cellulose, gelatin and glycerol, and the extexine of described body contains chitin, sodium alginate, gelatin, polyvinyl alcohol, sorbitol and glycerol.
Described endosexine and extexine can also contain magnetic powder, preferred NdFeB magnetic powder.
Described chitin is a soluble chitin.
The sieve cloth that described drainage screen is made into for the polyvinyl chloride superfine fibre.
Body described in the present invention is that mould dips in the glue back demoulding of condensing and forms.
Mould divides secondary to dip in endosexine and extexine that glue forms body.
The glue that forms endosexine and extexine is different.
The body endosexine is a primary raw material with chitin, hydroxypropyl cellulose, gelatin.Chitin belongs to the polysaccharose substance of alkalescence, is a kind of linear macromolecular material, also is a kind of natural chelate, and it highly cross-linked and branching can take place during with hydroxypropyl cellulose, gelatin complexation, makes endosexine formation pore structure.
The body extexine is a primary raw material with chitin, sodium alginate, gelatin, polyvinyl alcohol.Affinitys such as chitin and sodium alginate, polyvinyl alcohol are strong, the complex crystallization that forms is thick, hole big, pore rate height, make the network structure of extexine that the surface energy of enough storage medicinal liquids be arranged, extremely strong affinity is arranged, and body of the present invention is filled in do not have the difference thoughts and feelings in the nasal cavity with nasal membrane.
The standard of the selection of material of the present invention is:
Primary raw material: chitin becomes chitosan after taking off acetyl, claims soluble chitin again; Hydroxypropyl cellulose is the low rank (LS-HPC) that replaces; Gelatin is the pharmaceutical grade gelatin; The sodium alginate mean molecule quantity is 32000, and the polyvinyl alcohol mean molecule quantity is 30000.
Auxiliary material: polyvidone (PVP), mean molecule quantity are 40000; Dehydrated alcohol, glycerol, sorbitol, the acetate solution of 3% concentration, the glutaraldehyde solution of 5% concentration, distilled water (water purification).
Below the manufacturing of the pharmaceutical carrier of nasal-cavity administration of the present invention being done one specifies.
One, the mother solution of various raw materials preparation
1, chitin mother solution
Used chitin is meant soluble chitin.
Get 3 parts of chitins by weight, add 97 parts of the acetate solutions of 3% weight concentration, be stirred to complete molten stand-by under the room temperature.
2, hydroxypropyl cellulose mother solution
Get 2 parts of hydroxypropyl celluloses by weight, add 98 parts of water purification (steaming the outer water that heats up in a steamer, down together), stir complete molten stand-by under the room temperature.
3, gelatin mother solution
Get 40 parts in gelatin by weight, 3 parts of glycerol, 57 parts of water purification stir complete molten stand-by under 70～80 ℃ of heating in water bath.
4, sodium alginate mother solution
Get 5 parts of sodium alginates by weight, add 95 parts of water purification, at room temperature stir complete molten stand-by.
5, polyvinyl alcohol mother solution
Get 5 parts of polyvinyl alcohol by weight, add 95 parts of water purification, under 80～90 ℃ of water-soluble heating, stir complete molten stand-by.
6, glutaraldehyde alcoholic solution
Get 3 parts of the glutaraldehyde stock solutions of 95% weight concentration by weight, add 97 parts of dehydrated alcohol, stir complete molten stand-by under the room temperature.
7, polyvidone alcoholic solution
Get 6 parts of polyvidones by weight, add 94 parts of dehydrated alcohol, stir complete molten stand-by under the room temperature.
Two, body endosexine, extexine feed liquid (glue) preparation
1, endosexine feed liquid
Get 30 parts in described chitin mother solution by weight, 20 parts in hydroxypropyl cellulose mother solution, 40 parts in gelatin mother solution, 10 parts of glycerol add the neodymium iron boron super-fine magnetic powder (200 order) of gross weight 0.3% again, and dispersed with stirring is evenly stand-by under 65～70 ℃ of water-soluble heating.
2, extexine feed liquid
Get 40 parts in described chitin mother solution by weight, 20 parts in sodium alginate mother solution, 20 parts in gelatin mother solution, 15 parts in polyvinyl alcohol mother solution, 3 parts of glycerol, 2 parts of sorbitol, add the neodymium iron boron super-fine magnetic powder (200 order) of gross weight 0.2% again, evenly stand-by 65～70 ℃ of following dispersed with stirring.
Three, mould dips in the glue shaping
Its shape of mould among the present invention is identical with body shape among the present invention, definitely says identical with chamber body shape among the present invention.
The mould that cleans up is at first immersed the endosexine feed liquid to be proposed after 2 seconds, under 10～15 ℃ room temperature, placed 1 minute, the feed liquid for the treatment of die surface is solidified the back and is immersed the extexine feed liquid together with mould and take out after 2 seconds, under 10～15 ℃ room temperature, placed 5～8 minutes, after treating inside and outside top layer feed liquid gluing and solidifying, instant with specific purpose tool (spring exfoliation tool) demoulding, get the body crude product.The body crude product is arranged on the glass planar,, can enters next process through two days natural dryings.
Four, spherical surface body top punching
Dried body crude product is placed on the special-purpose puncher, is punched in its spherical surface body top, 4 of the disposable through holes of getting φ 2.5mm are perhaps only got 1 of the through hole of φ 5.5mm.The recyclable utilization of waste material that punching produces.
Five, inlay drainage screen
60～80 purpose sieve cloths are shaped as numb mushroom shape, and just as chamber body, filter screen inlays can firm attachment in chamber body.
It is to help on the interface of medicinal liquid attached to mesh that body of the present invention, its inner chamber inlay filter screen, can improve the storage supporting effect of this carrier to medicine, makes this pharmaceutical carrier that certain dustproof effect is arranged simultaneously.
Six, setting is disinfected
The body that will inlay net immerses described glutaraldehyde alcoholic solution, soaks and pulls airing out after 1 minute.The glutaraldehyde alcoholic solution can be sterilized and gelatin can be carried out the amine al and close reaction, gelatin is solidified and formalizes.
Seven, spraying wetting agent
The described polyvidone alcoholic solution of the last spraying of carrier through above-mentioned operation is produced makes the body of pharmaceutical carrier of the present invention keep certain humidity.
Eight, terminal disinfection
Terminal disinfection is to adopt ultraviolet rays collection to carrier Continuous irradiation of the present invention 3～5 minutes.
The inside and outside top layer of body of the present invention is mushy network structure, has big surface energy, can fully adsorb medicinal liquid.Being 2～3 times of body deadweight to the water solublity medicinal liquid when average single the net weight 0.13g of body finished product, maximum medicine carrying, is 1～2 times of body deadweight to pure dissolubility medicinal liquid.
Typical dimensions of the present invention can be divided into large and small two kinds of models, its spherical surface body diameter of large size 12mm, length overall 13mm, small size its spherical surface body diameter 8mm, length overall 10mm.
The present invention is the pharmaceutical carrier of disposable nasal-cavity administration.
The present invention fills in nasal cavity after soaking medicine, and the drug effect of the present invention's carrying enters blood circulation in nasal membrane rapidly by the nasal membrane absorption.The present invention soaks the medicine time and is, immerses the water solublity medicinal liquid time must not surpass 2 minutes, and immersing the pure dissolubility medicinal liquid time must not be above 5 minute.
The present invention fills in nasal cavity inwardly with the spherical surface body top, and the vertical through hole of spherical surface body is the respiratory ventilation hole.Use of the present invention does not influence eupnea.
The present invention soaks that be 6～8 hours service time behind the medicine, and the environment for use temperature is-40 ℃-40 ℃.Garbage after the use is about five days in no moisture environment phase of separating that descends, and has that degradative phase is about one day under the moisture environment.
The invention provides a kind of new method of nasal-cavity administration.The present invention is easy to use, has no side effect.The present invention can realize the medicament slow release effect.The present invention can also reduce the suction to harmful dust.
Body of the present invention is the complex of pbz polymer material, has elasticity.Inside and outside layer is added with magnetic powder, makes body have certain permanent magnetism performance, can fully activate the sensory nerve of nasal membrane during use, improves the drug absorption transmission capacity, improves the absorbability to dust.
Description of drawings
Fig. 1 is a structural representation of the present invention;
Fig. 2 is Fig. 1 vertical view.
The specific embodiment
Embodiment one
The embodiment of the invention provides with production method.
1, preparation mother solution
Get chitin 300 gram be dissolved in 3% weight concentration acetum 9700 grams, make 10 kilograms of the chitin solution of 3% weight concentration, stand-by.
Get hydroxypropyl cellulose 200 gram and be dissolved in 9800 gram water purification (distilled water, down with), make 10 kilograms of the hydroxypropyl cellulose solutions of 2% weight concentration, stand-by.
Get gelatin 4000 gram, glycerol 300 grams, water purification 5700 grams mix and through 10 kilograms of the complete gelatin solutions of making 40% weight concentration after molten of water-bath, and are stand-by.
Get sodium alginate 500 gram and be dissolved in water purification 9500 grams, through stir complete make after molten 5% weight concentration 10 kilograms of sodium alginate glues, stand-by.
Get polyvinyl alcohol 500 gram and be dissolved in water purification 9500 grams, 10 kilograms of the complete poly-vinyl alcohol solutions of making 5% weight concentration after molten, stand-by.
2, preparation feed liquid
Get glutaraldehyde stock solution 150 gram of 50% concentration, add dehydrated alcohol 4850 grams, stir 5 kilograms of the alcoholic solutions of the complete molten glutaraldehyde stock solution of making 3% weight concentration, stand-by.
Get polyvidone 300 gram, add dehydrated alcohol 4700 grams, 5 kilograms of the complete polyvidone alcoholic solutions of making 6% weight concentration after molten, stand-by.
3, preparation endosexine feed liquid
Get described chitin solution 300 grams, hydroxypropyl cellulose solution 200 grams, gelatin solution 400 grams, glycerol 100 grams, super-fine magnetic powder 3 grams are put into molten device and made 1 kilogram of endosexine feed liquid in 65～70 ℃ of insulation heating of water-bath, and are stand-by.
4, preparation extexine feed liquid
Get described chitin solution 400 grams, sodium alginate soln 200 grams, gelatin solution 200 grams, poly-vinyl alcohol solution 150 grams, glycerol 30 grams, sorbitol 20 grams, super-fine magnetic powder 2 grams, put into molten device in 65～70 ℃ of water-baths insulation heating, make 1 kilogram of extexine feed liquid after molten entirely, stand-by.
5, preparation body
Adopt and the isomorphous mould of body of the present invention.The mould of cleaning, dip in glue in the liquid bath of immersion endosexine feed liquid earlier, propose after 2 seconds, under 10～15 ℃ room temperature, placed 1 minute, immerse extexine feed liquid hopper again and take out after 2 seconds, under 10～15 ℃ room temperature, placed 5～8 minutes, inside and outside top layer is condensed compound, peels off the demoulding, behind the natural drying, make 14250 of the body crude products of described large size specification, every net weight 0.14 gram.
6, post processings such as Hu net are inlayed in punching
Described body crude product is placed on the puncher, to the punching of its spherical surface body top, 4 of the disposable through holes of getting φ 2.5mm.
60～80 purpose sieve cloths are shaped as numb mushroom shape, inlay in chamber body, with the setting of glutaraldehyde alcoholic solution, sterilization sprays described polyvidone alcoholic solution wetting agent, and disinfection by ultraviolet light is treated the processing of dipping medicinal liquid again.
Embodiment two
Press the method for embodiment one, obtain 1 kilogram of endosexine feed liquid, 1 kilogram of extexine feed liquid.Respectively in the liquid bath of the liquid bath of endosexine feed liquid and extexine feed liquid, dip in glue with small size mould, make 20000 of described small size body crude products by last example order, every net weight 0.1 gram, and make 20000 small size finished products by example one post-processing approach.
Soaking medicine one of implements
Making described body by embodiment one method, immerse aqueous solubility pharmaceutical formulations, soaked for 50 seconds, absorb medicament weight 0.28 gram, is 2 times of described body deadweight.
Soak two of medicine enforcement
Making described body by embodiment one method, immerse pure soluble drug preparation, soaked 2 minutes, absorb medicament weight 0.21 gram, is 1.5 times of body deadweight.
Claims (7)
1. the pharmaceutical carrier of nasal-cavity administration, has the body that to fill in nasal cavity, it is characterized in that intersecting body (3) be combined into of described body by spherical surface body (1) and tubular, described spherical surface body has one and connects the aperture, described intersecting body both ends open, the aperture that is connected of the interior end opening of intersecting body and described spherical surface body is connected airtight and is made intersecting body and spherical surface body be linked to be whole and connect mutually, described body by spherical surface body and intersecting body be combined into is by endosexine (5) and the compound formation of extexine (6), described spherical surface body has through hole (4) at the top of body axis direction, described inner body wall support is provided with filters stratum reticulare (2).
2. the pharmaceutical carrier of nasal-cavity administration as claimed in claim 1 is characterized in that described filtration stratum reticulare (2) mesh is 60～80 orders.
3. the pharmaceutical carrier of nasal-cavity administration as claimed in claim 1 is characterized in that described intersecting body (3) is that its osculum end of frustum tubular connects airtight the described connection aperture in spherical surface body.
4. the pharmaceutical carrier of nasal-cavity administration as claimed in claim 1, the endosexine that it is characterized in that described body contains chitin, hydroxypropyl cellulose, gelatin and glycerol, and the extexine of described body contains chitin, sodium alginate, gelatin, polyvinyl alcohol, sorbitol and glycerol.
5. the pharmaceutical carrier of nasal-cavity administration as claimed in claim 4 is characterized in that described endosexine and extexine contain magnetic powder.
6. as the pharmaceutical carrier of claim 4 or 5 described nasal-cavity administrations, it is characterized in that described chitin is a soluble chitin.
7. as the pharmaceutical carrier of the described nasal-cavity administration of any claim of claim 1～5, it is characterized in that the sieve cloth that described drainage screen is made into for the polyvinyl chloride superfine fibre.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910101175A CN101797413A (en) | 2009-07-27 | 2009-07-27 | Drug carrier for nasal administration |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910101175A CN101797413A (en) | 2009-07-27 | 2009-07-27 | Drug carrier for nasal administration |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101797413A true CN101797413A (en) | 2010-08-11 |
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ID=42593352
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200910101175A Pending CN101797413A (en) | 2009-07-27 | 2009-07-27 | Drug carrier for nasal administration |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101797413A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110799230A (en) * | 2017-06-27 | 2020-02-14 | 韩国联合制药株式会社 | Dry powder inhaler |
-
2009
- 2009-07-27 CN CN200910101175A patent/CN101797413A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110799230A (en) * | 2017-06-27 | 2020-02-14 | 韩国联合制药株式会社 | Dry powder inhaler |
| CN110799230B (en) * | 2017-06-27 | 2022-04-05 | 韩国联合制药株式会社 | Dry powder inhaler |
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Application publication date: 20100811 |