CN1748693A - Albendazole jelly for treating chronic nasosinusitis - Google Patents
Albendazole jelly for treating chronic nasosinusitis Download PDFInfo
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- CN1748693A CN1748693A CN 200410078467 CN200410078467A CN1748693A CN 1748693 A CN1748693 A CN 1748693A CN 200410078467 CN200410078467 CN 200410078467 CN 200410078467 A CN200410078467 A CN 200410078467A CN 1748693 A CN1748693 A CN 1748693A
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- albendazole
- nasal
- jelly
- add
- sinusitis
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- HXHWSAZORRCQMX-UHFFFAOYSA-N albendazole Chemical compound CCCSC1=CC=C2NC(NC(=O)OC)=NC2=C1 HXHWSAZORRCQMX-UHFFFAOYSA-N 0.000 title claims abstract description 40
- 229960002669 albendazole Drugs 0.000 title claims abstract description 40
- 235000015110 jellies Nutrition 0.000 title abstract description 15
- 239000008274 jelly Substances 0.000 title abstract description 15
- 230000001684 chronic effect Effects 0.000 title abstract description 4
- 206010009137 Chronic sinusitis Diseases 0.000 claims description 13
- 208000027157 chronic rhinosinusitis Diseases 0.000 claims description 11
- 229940100652 nasal gel Drugs 0.000 claims description 8
- 239000004615 ingredient Substances 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 abstract description 3
- 239000003814 drug Substances 0.000 description 13
- 238000003756 stirring Methods 0.000 description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
- 239000007922 nasal spray Substances 0.000 description 6
- 210000003695 paranasal sinus Anatomy 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
- 239000007788 liquid Substances 0.000 description 5
- 208000016366 nasal cavity polyp Diseases 0.000 description 5
- 201000009890 sinusitis Diseases 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 230000002421 anti-septic effect Effects 0.000 description 4
- 239000012153 distilled water Substances 0.000 description 4
- 239000000499 gel Substances 0.000 description 4
- 210000003928 nasal cavity Anatomy 0.000 description 4
- 239000007923 nasal drop Substances 0.000 description 4
- 238000005303 weighing Methods 0.000 description 4
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 3
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 3
- 229920003091 Methocel™ Polymers 0.000 description 3
- 201000007100 Pharyngitis Diseases 0.000 description 3
- 206010044302 Tracheitis Diseases 0.000 description 3
- 230000001154 acute effect Effects 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 229940071826 hydroxyethyl cellulose Drugs 0.000 description 3
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 3
- 229960003943 hypromellose Drugs 0.000 description 3
- 230000036285 pathological change Effects 0.000 description 3
- 231100000915 pathological change Toxicity 0.000 description 3
- 206010039083 rhinitis Diseases 0.000 description 3
- 206010019233 Headaches Diseases 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 206010028748 Nasal obstruction Diseases 0.000 description 2
- 208000002193 Pain Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- VXTGHWHFYNYFFV-UHFFFAOYSA-N albendazole S-oxide Chemical compound CCCS(=O)C1=CC=C2NC(NC(=O)OC)=NC2=C1 VXTGHWHFYNYFFV-UHFFFAOYSA-N 0.000 description 2
- 229950010075 albendazole sulfoxide Drugs 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 206010006451 bronchitis Diseases 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 231100000869 headache Toxicity 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 230000000749 insecticidal effect Effects 0.000 description 2
- 210000003734 kidney Anatomy 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 210000004086 maxillary sinus Anatomy 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 210000002850 nasal mucosa Anatomy 0.000 description 2
- 229940097496 nasal spray Drugs 0.000 description 2
- 230000028327 secretion Effects 0.000 description 2
- OXFSTTJBVAAALW-UHFFFAOYSA-N 1,3-dihydroimidazole-2-thione Chemical class SC1=NC=CN1 OXFSTTJBVAAALW-UHFFFAOYSA-N 0.000 description 1
- KTPMVZCGIJJWCD-UHFFFAOYSA-N 1-hydroxypyridin-2-imine Chemical compound ON1C=CC=CC1=N KTPMVZCGIJJWCD-UHFFFAOYSA-N 0.000 description 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 206010011878 Deafness 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
- 229920002527 Glycogen Polymers 0.000 description 1
- 206010020565 Hyperaemia Diseases 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 208000032984 Intraoperative Complications Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 206010036790 Productive cough Diseases 0.000 description 1
- 206010039085 Rhinitis allergic Diseases 0.000 description 1
- 206010039101 Rhinorrhoea Diseases 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 208000009205 Tinnitus Diseases 0.000 description 1
- 102000004243 Tubulin Human genes 0.000 description 1
- 108090000704 Tubulin Proteins 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000004220 aggregation Methods 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 230000000507 anthelmentic effect Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 150000003851 azoles Chemical class 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 210000005098 blood-cerebrospinal fluid barrier Anatomy 0.000 description 1
- 238000009395 breeding Methods 0.000 description 1
- 230000001488 breeding effect Effects 0.000 description 1
- 239000006013 carbendazim Substances 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 208000013804 chronic ethmoidal sinusitis Diseases 0.000 description 1
- 201000010761 chronic ethmoiditis Diseases 0.000 description 1
- 201000006918 chronic maxillary sinusitis Diseases 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 231100000895 deafness Toxicity 0.000 description 1
- 238000013129 endoscopic sinus surgery Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229960002179 ephedrine Drugs 0.000 description 1
- 201000009320 ethmoid sinusitis Diseases 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 201000006916 frontal sinusitis Diseases 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 229940096919 glycogen Drugs 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 210000003714 granulocyte Anatomy 0.000 description 1
- 238000001631 haemodialysis Methods 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 208000016354 hearing loss disease Diseases 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000000322 hemodialysis Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000002262 irrigation Effects 0.000 description 1
- 238000003973 irrigation Methods 0.000 description 1
- 210000000265 leukocyte Anatomy 0.000 description 1
- 201000008836 maxillary sinusitis Diseases 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 210000003470 mitochondria Anatomy 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 208000010753 nasal discharge Diseases 0.000 description 1
- 210000000492 nasalseptum Anatomy 0.000 description 1
- 230000003448 neutrophilic effect Effects 0.000 description 1
- 210000001331 nose Anatomy 0.000 description 1
- 210000003463 organelle Anatomy 0.000 description 1
- 210000003800 pharynx Anatomy 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 150000003457 sulfones Chemical class 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 231100000886 tinnitus Toxicity 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 210000001944 turbinate Anatomy 0.000 description 1
Abstract
The present invention relates to the preparation process of nasal albendazole jelly and the application of the nasal albendazole jelly in treating chronic nasosinusitis.
Description
The present invention relates to use albendazole to prepare nasal gel, and treat chronic sinusitis with the nasal gel of albendazole.
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, albendazole brief introduction
Albendazole, english common name are Albendazole; Generic name is: Albendazole, Albendazole, 5-rosickyite-2-Carbendazim, rosickyite reach azoles, the third mercapto imidazoles, albendazole 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 is the high-efficiency broad spectrum anthelmintic, is the strongest a kind of of insecticidal action in the benzimidazole medicine.Oral absorption is slow.The 2.5-3 hour blood drug level peaking in oral back, 15mg/kg on the one are at twice or divide three oral area under curve that reach (AUC) identical.This medicine bioavailability is distributed in liver, kidney, muscle in vivo and can sees through blood-cerebrospinal fluid barrier, so finite concentration is also arranged in the cerebral tissue less than 5%.This medicine is converted into Albendazole-sulfoxide and Albendazole-sulfone in liver, the former is an insecticidal constituent.Former medicine and the sulfone derivative concentration in blood is extremely low, can not measure, and the concentration change of Albendazole-sulfoxide is very big, does not wait from 0.04 μ g/mL to 0.55 μ g/mL, average 0.16 μ g/mL.Former medicine and metabolite thereof had 87% with homaluria in 24 hours, the kidney clearance rate is 0.16-0.81L/h, and 13% drains through digestive tract.Half-life is 8.5-10.5 hour.Medicine does not have depot action in vivo.Do not removed by hemodialysis.
Three, so far, all do not see any report or document record that albendazole is used for the treatment of chronic sinusitis both at home and abroad as yet.
The present invention is made into compound recipe with albendazole as independent effective ingredient or with other medicines, makes nasal gel.
The indication of the nasal gel made from albendazole or with the compound recipe that contains albendazole of the present invention includes, 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 albendazole or the nasal gel made with the compound recipe that contains albendazole, for the chronic sinusitis patient, directly nasal-cavity administration can be alleviated relevant symptom effectively.
Nasal gel of the present invention, for nasal spray one in, mean in nasal spray to add the adjuvant that can increase medicinal liquid viscosity, medicinal liquid can be adhered on the nasal mucosa better, thereby made medicine can be from medicinal liquid slowly or continue to discharge.The described adjuvant that can increase medicinal liquid viscosity, include, but are not limited to: the hypromellose of hydroxyethyl-cellulose, all size or the type of hydroxy methocel, all size or the type of card pool general (Carbopol), all size or the type of all size or type etc.
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 following examples to the preparation of Albendazole jelly of the present invention, be described with application of its treatment chronic sinusitis.It should be noted that, following embodiment just is used for explanation and unrestricted the present invention, well-known to those skilled in the artly by other administration route albendazole is used for the treatment of nasal polyp or nasal polyp, rhinitis, pharyngitis, tracheitis and bronchitic technology all within the scope of the invention.
Embodiment 1 adopts the general preparation Albendazole jelly of card pool
Take by weighing card pool general 940 (Carbopol940) 2g; Get the sterile distilled water of about 80 ℃ of 100ml; It is general to add the card pool while stirring in hot water, after whole adding card pools are general, continues stirring 12h.After treating that temperature reduces, add the 100mg albendazole, add an amount of antiseptic again, behind the restir 30min, and the albendazole gel, divide to install in the nasal mist bottle or in the nasal drop bottle, promptly get Albendazole jelly.
Embodiment 2 adopts hydroxy methocel to prepare Albendazole jelly
Take by weighing hydroxy methocel 2g; Get the sterile distilled water of about 80 ℃ of 100ml; It is general to add the card pool while stirring in hot water, after whole adding card pools are general, continues stirring 12h.After treating that temperature reduces, add the 100mg albendazole, add an amount of antiseptic again, behind the restir 30min, and the albendazole gel, divide to install in the nasal mist bottle or in the nasal drop bottle, promptly get Albendazole jelly.
Embodiment 3 adopts hydroxyethyl-cellulose to prepare Albendazole jelly
Take by weighing hydroxyethyl-cellulose 2g; Get the sterile distilled water of about 80 ℃ of 100ml; It is general to add the card pool while stirring in hot water, after whole adding card pools are general, continues stirring 12h.After treating that temperature reduces, add the 100mg albendazole, add an amount of antiseptic again, behind the restir 30min, and the albendazole gel, divide to install in the nasal mist bottle or in the nasal drop bottle, promptly get Albendazole jelly.
Embodiment 4 adopts hypromellose to prepare Albendazole jelly
Take by weighing hypromellose 2g; Get the sterile distilled water of about 80 ℃ of 100ml; It is general to add the card pool while stirring in hot water, after whole adding card pools are general, continues stirring 12h.After treating that temperature reduces, add the 100mg albendazole, add an amount of antiseptic again, behind the restir 30min, and the albendazole gel, divide to install in the nasal mist bottle or in the nasal drop bottle, promptly get Albendazole jelly.
Embodiment 5 uses Albendazole jelly treatment chronic sinusitis
Among the 10 routine patients, male 4 examples, women 6 examples; 12～49 years old age; Course of disease April～3 years.Maxillary sinusitis 3 examples wherein, frontal sinusitis 2 examples, ethmoiditis 5 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 Albendazole jelly 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) 6 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) 3 examples that take a turn for the better, invalid (interruption of taking medicine) 1 example.All case was followed up a case by regular visits to 3 months～1 year, and half a year is recidivist's 8 examples not.
Claims (2)
1. the nasal gel that albendazole is made as one of effective ingredient or effective ingredient.
2. the application of power albendazole in the production of the nasal gel that is used for the treatment of chronic sinusitis.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410078467 CN1748693A (en) | 2004-09-14 | 2004-09-14 | Albendazole jelly for treating chronic nasosinusitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410078467 CN1748693A (en) | 2004-09-14 | 2004-09-14 | Albendazole jelly for treating chronic nasosinusitis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1748693A true CN1748693A (en) | 2006-03-22 |
Family
ID=36604472
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410078467 Pending CN1748693A (en) | 2004-09-14 | 2004-09-14 | Albendazole jelly for treating chronic nasosinusitis |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1748693A (en) |
-
2004
- 2004-09-14 CN CN 200410078467 patent/CN1748693A/en active Pending
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20070309 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: Wang Heyao Co-applicant before: Zheng Wenjie |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |