CN1748678A - Medendazole new form for treating chronic nasosinusitis - Google Patents
Medendazole new form for treating chronic nasosinusitis Download PDFInfo
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- CN1748678A CN1748678A CN 200410078452 CN200410078452A CN1748678A CN 1748678 A CN1748678 A CN 1748678A CN 200410078452 CN200410078452 CN 200410078452 CN 200410078452 A CN200410078452 A CN 200410078452A CN 1748678 A CN1748678 A CN 1748678A
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- nasal
- mebendazole
- spray
- aerosol
- sinusitis
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- 230000001684 chronic effect Effects 0.000 title abstract description 4
- BAXLBXFAUKGCDY-UHFFFAOYSA-N mebendazole Chemical compound [CH]1C2=NC(NC(=O)OC)=NC2=CC=C1C(=O)C1=CC=CC=C1 BAXLBXFAUKGCDY-UHFFFAOYSA-N 0.000 claims abstract description 40
- 229960003439 mebendazole Drugs 0.000 claims abstract description 40
- 239000000443 aerosol Substances 0.000 claims abstract description 10
- 206010009137 Chronic sinusitis Diseases 0.000 claims description 18
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims description 16
- 239000007923 nasal drop Substances 0.000 claims description 16
- 229940098458 powder spray Drugs 0.000 claims description 14
- 239000007921 spray Substances 0.000 claims description 11
- 210000003928 nasal cavity Anatomy 0.000 claims description 10
- 239000002552 dosage form Substances 0.000 claims description 4
- 239000004615 ingredient Substances 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 abstract description 6
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- 239000003814 drug Substances 0.000 description 13
- 210000003695 paranasal sinus Anatomy 0.000 description 6
- 208000024891 symptom Diseases 0.000 description 6
- 208000000592 Nasal Polyps Diseases 0.000 description 5
- 201000010099 disease Diseases 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 208000016366 nasal cavity polyp Diseases 0.000 description 5
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- 206010019233 Headaches Diseases 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 206010028748 Nasal obstruction Diseases 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 230000003203 everyday effect Effects 0.000 description 4
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- 206010044302 Tracheitis Diseases 0.000 description 3
- 230000001154 acute effect Effects 0.000 description 3
- -1 amine methyl ester Chemical class 0.000 description 3
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- 206010039083 rhinitis Diseases 0.000 description 3
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- 206010061218 Inflammation Diseases 0.000 description 2
- 241000209094 Oryza Species 0.000 description 2
- 235000007164 Oryza sativa Nutrition 0.000 description 2
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- LXBGSDVWAMZHDD-UHFFFAOYSA-N 2-methyl-1h-imidazole Chemical compound CC1=NC=CN1 LXBGSDVWAMZHDD-UHFFFAOYSA-N 0.000 description 1
- 241001465677 Ancylostomatoidea Species 0.000 description 1
- 241000244203 Caenorhabditis elegans Species 0.000 description 1
- TWFZGCMQGLPBSX-UHFFFAOYSA-N Carbendazim Natural products C1=CC=C2NC(NC(=O)OC)=NC2=C1 TWFZGCMQGLPBSX-UHFFFAOYSA-N 0.000 description 1
- 206010008635 Cholestasis Diseases 0.000 description 1
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- 206010014096 Echinococciasis Diseases 0.000 description 1
- 208000009366 Echinococcosis Diseases 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
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- YSMRWXYRXBRSND-UHFFFAOYSA-N TOTP Chemical compound CC1=CC=CC=C1OP(=O)(OC=1C(=CC=CC=1)C)OC1=CC=CC=C1C YSMRWXYRXBRSND-UHFFFAOYSA-N 0.000 description 1
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- RWCCWEUUXYIKHB-UHFFFAOYSA-N benzophenone Chemical compound C=1C=CC=CC=1C(=O)C1=CC=CC=C1 RWCCWEUUXYIKHB-UHFFFAOYSA-N 0.000 description 1
- 239000012965 benzophenone Substances 0.000 description 1
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- 208000013804 chronic ethmoidal sinusitis Diseases 0.000 description 1
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- 201000008836 maxillary sinusitis Diseases 0.000 description 1
- XLSZMDLNRCVEIJ-UHFFFAOYSA-N methylimidazole Natural products CC1=CNC=N1 XLSZMDLNRCVEIJ-UHFFFAOYSA-N 0.000 description 1
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Abstract
The present invention relates to the preparation process of nebula, aerosol, powder spraying agent and nose drop of mebendazole and their application in treating chronic nasosinusitis.
Description
The present invention relates to use mebendazole to prepare spray, aerosol, powder spray and nasal drop, and these contain spray, aerosol, powder spray and the nasal drop application in the treatment chronic sinusitis of mebendazole.
One, chronic sinusitis brief introduction
Chronic sinusitis generally promptly refers to chronic purulent sinusitis, is nasal sinuses mucosa chronic suppurative inflammation, and is wherein maximum with chronic maxillary sinusitis, and normal and chronic ethmoidal sinusitis merges and exists, and how to be treated delay timely and reasonably because of acute purulent nasosinusitis and causes.Infection, allergic rhinitis also are its main causes.In recent years, the pathological changes of nasal meatus complex causes that nasal sinuses drain obstacle is caused extensive attention, and has therefore carried out the sinusitis operation under the functional nasal endoscope.
1, cardinal symptom is: pus tears, nasal obstruction, headache (often show as dull pain or head sense of heaviness, daytime is heavy, and night is light), abundant expectoration, foreign body sensation or dry pharynx pain etc., sometimes tinnitus, deafness can be arranged, the course of disease surpasses 6-8 week, if the course of disease is shorter, may be acute or subacute sinusitis.
2, general treatment comprises furacilin-ephedrine solution collunarium, antibiotics and puncture and irrigation of maxillary sinus etc.
If 3 general treatment effects are not good enough.Should carry out nasal cavity inspection or nasal sinuses CT examination under the detailed conchoscope, main understanding has or not the pathological changes that influences the nasal sinuses drain.The CT in left side takes the photograph the inflammation that sheet shows the bilateral maxillary sinus, and has liquid flat.
4, operative treatment comprises and removes the operation that removes the cause of disease, (as the capable nasal septal construction of high-order deviation of nasal septum; To the middle nasal concha that hypertrophy or polypoid become, feasible partial middle turbinectomy is if there is nasal polyp then to go nasal polypectomy), radical maxillary sinusotomy.
5, more popular at present operation method is a functional endoscopic sinus surgery.The method surgical injury is little, meets The normal anatomic and physiological, and effect is better.As might go this operation as far as possible
Two, mebendazole brief introduction
Mebendazole, english common name are Mebendazole; Generic name is: 5-benzoyl Carbendazim, benzoyl miaow amine methyl ester, benzophenone guanidine methyl ester, benzophenone rice amine ester, mebendazole, Methylimidazole. etc.Be broad-spectrum de-worming medicine.Can influence the multiple biochemical metabolism approach of polypide.This medicine can suppress the picked-up of Enterozoa to glucose, causes the intravital glycogen depletion of worm; Also can combine and suppress micropipe aggregation with the polypide tubulin, thus transhipment of secretion inhibitor granule and the motion of other subcellular organelle; Also can suppress polypide mitochondrion fumaric reductase system, reduce ATP and generate, thereby disturb polypide existence and breeding and cause its death.This medicine has and kills the effect that hookworm ovum and whipworm ovum and part are killed roundworm egg fully.In vitro tests proof 5mg/L can suppress the growth of ancylostome larva.In addition, use this medicine heavy dose of, the long course of treatment, treats the effect of trichonematosis and echinococcosis in addition.The human oral mebendazole absorbs few (5%-10%).The 2-5 hour blood drug level peaking in oral back, but less than 0.3% of dosage.Take 200mg every day, blood drug level is no more than 0.3mg/L after 3 days.Medicine is distributed in positions such as blood plasma, liver, lung in vivo, mainly at intrahepatic metabolism.Half-life is 2.5-5.5 hour, and hepatic disfunction (cholestasis) Shi Zeke reaches 35 hours.This medicine is drained through digestive tract with original shape or the amino metabolite of 2-in oral back 24 hours, and 5%-10% is with homaluria.
Three, so far, all do not see any report or document record that mebendazole is used for the treatment of chronic sinusitis both at home and abroad as yet.
The present invention is made into compound recipe with mebendazole as independent effective ingredient or with other medicines, makes the dosage form of nasal-cavity administration, and these dosage forms include, but are not limited to: nasal drop, spray, aerosol and powder spray.
Indication with mebendazole or the nasal drop made from the compound recipe that contains mebendazole, spray, aerosol and powder spray of the present invention, include, but are not limited to following disease: chronic sinusitis, nasal polyp or nasal polyp, rhinitis, pharyngitis, tracheitis and bronchitis.
Use of the present inventionly with mebendazole or the nasal drop made from the compound recipe that contains mebendazole, spray, aerosol and powder spray, for the chronic sinusitis patient, directly nasal-cavity administration can be alleviated relevant symptom effectively.
Nasal drop of the present invention, spray, aerosol and powder spray all meet the definition of the Pharmacopoeia of the People's Republic of China (version was two ones in 2000) about nasal drop, spray, aerosol and powder spray.
Chronic sinusitis of the present invention is that those skilled in the art is known, has it to define accurately in the modern medical book.Its pathological change as previously mentioned.Rhinitis of the present invention, pharyngitis, tracheitis and bronchitis also are that the ordinary artisan of this area is known, have it to define accurately in the modern medical book.
By the preparation of following examples, and be described with the application of mebendazole nasal drop, spray, aerosol and powder spray treatment chronic sinusitis to mebendazole nasal drop of the present invention, spray, aerosol and powder spray.It should be noted that, following embodiment is unrestricted the present invention with the rice explanation just, well-known to those skilled in the artly by other administration route mebendazole is used for the treatment of nasal polyp or nasal polyp, rhinitis, pharyngitis, tracheitis and bronchitic technology all within the scope of the invention.
The preparation of embodiment 1 mebendazole nasal mist
In ten thousand grades of environment, mebendazole is dissolved in normal saline, be prepared into the solution of 1mg/ml, add geramine, the concentration that makes geramine is 0.02%.In the nasal mist bottle, the spray valve of screwing on promptly gets the mebendazole nasal mist with this liquid medicine filling.
The preparation of embodiment 2 mebendazole nasal aerosol
In ten thousand grades of environment, mebendazole is dissolved in normal saline, be prepared into the solution of 1mg/ml, add geramine, the concentration that makes geramine is 0.02%.This liquid medicine filling in the nasal aerosol bottle, is added propellant, load onto aerosol valve, promptly get the mebendazole nasal aerosol.
The preparation of embodiment 3 mebendazole nasal cavity powder sprays
In ten thousand grades of environment, with mebendazole 20mg, hydroxypropyl cellulose (HPC) 980mg, Benasept 0.1mg co-blended, the mebendazole that obtains homogeneous is the powder body of 1 μ g/mg, and diameter of particle should be 30～150 μ m, be filled in the hard capsule, get nasal-cavity administration mebendazole powder spray.Per nasal sprays into administration with the dust cloud device during use.
The preparation of embodiment 4 mebendazole nasal drop
In ten thousand grades of environment, mebendazole is dissolved in normal saline, be prepared into the solution of 1mg/ml, add geramine, the concentration that makes geramine is 0.02%.This liquid medicine filling in the nasal drop bottle, is promptly got the mebendazole nasal drop.
Embodiment 5 uses mebendazole nasal mist treatment chronic sinusitis
Among the 10 routine patients, male 5 examples, women 5 examples; 15～43 years old age; Course of disease April～1 year.Maxillary sinusitis 3 examples wherein, frontal sinusitis 4 examples, ethmoiditis 3 examples.Symptom all has nasal obstruction, stream turbid nasal discharge, headache, or fear of cold, heating are arranged, symptom such as feel sick.Department of eye is checked: the nasal mucosa congestion and edema, nasal cavity has purulent secretion.The X line is taken the photograph sheet: the increase in density of hole chamber, acute stage total white blood cells and neutrophilic granulocyte raise.
Therapeutic Method: use mebendazole nasal mist spray nose secondary every day, continue January.
Result: cure (transference cure, it is no abnormal that X line nasal sinuses is taken the photograph sheet) 2 examples, (symptom is obviously improved, and nasal cavity checks that mucous hyperemia swelling alleviates, and X line nasal sinuses is taken the photograph sheet and obviously improved) 6 examples that take a turn for the better, invalid (interruption of taking medicine) 2 examples.All case was followed up a case by regular visits to 6 months, and half a year is recidivist's 9 examples not.
Embodiment 6 uses mebendazole nasal aerosol treatment chronic sinusitis
Repeat " embodiment 1 " described experiment, what adopt except that curative is that patient's state of an illness of hydrochloric acid mebendazole nasal aerosol and observation is with quantity is different, patient goes into group standard, therapeutic scheme, curative effect judging standard all with " embodiment 1 ", and experimental result is similar with " embodiment 1 ".
Embodiment 7 uses mebendazole nasal cavity powder spray treatment chronic sinusitis
44 years old women is diagnosed as chronic sinusitis, and with the treatment of hydrochloric acid mebendazole nasal cavity powder spray, be administered once every day, continues 15 days, and symptom is obviously improved.
Embodiment 8 uses mebendazole nasal drop treatment chronic sinusitis
An adult female, pus tears, nasal obstruction, headache are diagnosed as chronic sinusitis, and with " embodiment 7 " described tricresyl phosphate imidazoles nasal drop treatment, every day, secondary continued 25 days, and nasal obstruction, headache are obviously alleviated, and the pus tears reduce.
Claims (2)
1. the dosage form of the nasal-cavity administration that mebendazole is made as effective ingredient, these dosage forms comprise:
1. nasal drop;
2. spray;
3. aerosol;
4. powder spray.
2. the application of mebendazole in the production of the nasal drop that is used as the treatment chronic sinusitis, spray, aerosol, powder spray.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100784528A CN100496492C (en) | 2004-09-14 | 2004-09-14 | Medendazole new formulation for treating chronic nasosinusitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100784528A CN100496492C (en) | 2004-09-14 | 2004-09-14 | Medendazole new formulation for treating chronic nasosinusitis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1748678A true CN1748678A (en) | 2006-03-22 |
| CN100496492C CN100496492C (en) | 2009-06-10 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100784528A Expired - Fee Related CN100496492C (en) | 2004-09-14 | 2004-09-14 | Medendazole new formulation for treating chronic nasosinusitis |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100496492C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019121996A3 (en) * | 2017-12-19 | 2019-08-08 | Repos Pharma Ab | Treatment for inflammatory disease |
-
2004
- 2004-09-14 CN CNB2004100784528A patent/CN100496492C/en not_active Expired - Fee Related
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019121996A3 (en) * | 2017-12-19 | 2019-08-08 | Repos Pharma Ab | Treatment for inflammatory disease |
| CN111601598A (en) * | 2017-12-19 | 2020-08-28 | 瑞柏斯制药有限公司 | Treatment of inflammatory diseases |
| JP2021509119A (en) * | 2017-12-19 | 2021-03-18 | レポス ファーマ アーベー | Treatment of inflammatory diseases |
| US11504356B2 (en) | 2017-12-19 | 2022-11-22 | Repos Pharma Ab | Treatment for inflammatory disease |
| JP7343190B2 (en) | 2017-12-19 | 2023-09-12 | レポス ファーマ アーベー | Treatment of inflammatory diseases |
Also Published As
| Publication number | Publication date |
|---|---|
| CN100496492C (en) | 2009-06-10 |
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Effective date of registration: 20070302 Address after: No. 12, Huayuan Road, Jiangsu, Nanjing Applicant after: Jiangsu Simcere Pharmaceutical Research Company Limited Address before: 5C, building six, 6 District, far road, century garden, Beijing, Haidian District Applicant before: Zheng Wenjie Co-applicant before: Wang Heyao |
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