CN100455285C - Albendazole new form for treating adenoid hypertrophy - Google Patents
Albendazole new form for treating adenoid hypertrophy Download PDFInfo
- Publication number
- CN100455285C CN100455285C CNB2004100784706A CN200410078470A CN100455285C CN 100455285 C CN100455285 C CN 100455285C CN B2004100784706 A CNB2004100784706 A CN B2004100784706A CN 200410078470 A CN200410078470 A CN 200410078470A CN 100455285 C CN100455285 C CN 100455285C
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- Prior art keywords
- albendazole
- nasal
- spray
- aerosol
- adenoid vegetation
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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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 43
- 229960002669 albendazole Drugs 0.000 title claims abstract description 43
- 201000003462 adenoid hypertrophy Diseases 0.000 title abstract description 3
- 206010001229 Adenoidal hypertrophy Diseases 0.000 claims abstract description 22
- 238000002360 preparation method Methods 0.000 claims abstract description 7
- 239000003814 drug Substances 0.000 claims description 15
- 229940098458 powder spray Drugs 0.000 abstract description 14
- 239000007921 spray Substances 0.000 abstract description 10
- 239000000443 aerosol Substances 0.000 abstract description 9
- 229940008126 aerosol Drugs 0.000 abstract 2
- 229940100662 nasal drops Drugs 0.000 abstract 2
- 239000007922 nasal spray Substances 0.000 description 17
- 239000007923 nasal drop Substances 0.000 description 13
- 210000003928 nasal cavity Anatomy 0.000 description 8
- 210000004907 gland Anatomy 0.000 description 7
- 206010041235 Snoring Diseases 0.000 description 6
- 230000028327 secretion Effects 0.000 description 6
- 206010020880 Hypertrophy Diseases 0.000 description 5
- 210000001989 nasopharynx Anatomy 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 208000000592 Nasal Polyps Diseases 0.000 description 4
- 230000003203 everyday effect Effects 0.000 description 4
- 208000016366 nasal cavity polyp Diseases 0.000 description 4
- 206010039083 rhinitis Diseases 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 206010044302 Tracheitis Diseases 0.000 description 3
- 210000002534 adenoid Anatomy 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 241000321096 Adenoides Species 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- 208000001705 Mouth breathing Diseases 0.000 description 2
- 201000007100 Pharyngitis Diseases 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
- 239000008280 blood Substances 0.000 description 2
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- 230000001684 chronic effect Effects 0.000 description 2
- 238000003745 diagnosis Methods 0.000 description 2
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 210000002388 eustachian tube Anatomy 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- 238000001727 in vivo Methods 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
- 230000033001 locomotion Effects 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 210000003563 lymphoid tissue Anatomy 0.000 description 2
- 210000003097 mucus Anatomy 0.000 description 2
- 210000001331 nose Anatomy 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 238000002560 therapeutic procedure Methods 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
- 206010007556 Cardiac failure acute Diseases 0.000 description 1
- 206010009152 Chronic tonsillitis Diseases 0.000 description 1
- 201000006306 Cor pulmonale Diseases 0.000 description 1
- 208000013558 Developmental Bone disease Diseases 0.000 description 1
- 206010013952 Dysphonia Diseases 0.000 description 1
- 206010058314 Dysplasia Diseases 0.000 description 1
- 206010016761 Flat chest Diseases 0.000 description 1
- 206010060891 General symptom 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
- 206010020046 High arched palate Diseases 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 206010028748 Nasal obstruction Diseases 0.000 description 1
- 206010034203 Pectus Carinatum Diseases 0.000 description 1
- 208000004186 Pulmonary Heart Disease Diseases 0.000 description 1
- 206010039085 Rhinitis allergic Diseases 0.000 description 1
- 206010072610 Skeletal dysplasia Diseases 0.000 description 1
- 102000004243 Tubulin Human genes 0.000 description 1
- 108090000704 Tubulin Proteins 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
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- 206010001093 acute tonsillitis Diseases 0.000 description 1
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- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 230000000507 anthelmentic effect Effects 0.000 description 1
- 150000003851 azoles Chemical class 0.000 description 1
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- 238000009395 breeding Methods 0.000 description 1
- 230000001488 breeding effect Effects 0.000 description 1
- 206010006451 bronchitis Diseases 0.000 description 1
- 239000006013 carbendazim Substances 0.000 description 1
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- 210000001983 hard palate Anatomy 0.000 description 1
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- 210000004283 incisor Anatomy 0.000 description 1
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- 239000003380 propellant Substances 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 210000001533 respiratory mucosa Anatomy 0.000 description 1
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Abstract
The present invention relates to an application of albendazole to the preparation of spray, aerosol, powder spray and nose drops. The present invention also relates to an application of the spray, the aerosol, the powder spray and the nose drops all containing albendazole to the treatment of adenoidal hypertrophy.
Description
The present invention relates to use albendazole to prepare spray, aerosol, powder spray and nasal drop, and these contain spray, aerosol, powder spray and the nasal drop application in the treatment adenoid vegetation of albendazole.
Adenoid vegetation (adenoidal hypertrophy) is the pharyngeal tonsil hypertrophy.Child's adenoid vegetation often belongs to physiological, and nasopharynx part has lymphoid tissue during baby due, and with the age hypertrophy, reach in the time of 6 years old at utmost, degenerate gradually later on, if it influences whole body health or adjacent organs person, just claim adenoid vegetation.
One, the cause of disease Childhood is easily suffered from acute rhinitis, acute tonsillitis and influenza etc., if outbreak repeatedly, gland sample body is the hypertrophy hypertrophy rapidly, cause and increase the weight of nasal obstruction, hinder the nasal cavity drain, rhinitis and nasosinusitis secretions stimulates gland sample body to make it to continue hypertrophy again, forms the vicious cycle of reciprocal causation.Be more common in the child, normal and chronic tonsillitis merges and exists.
Two, clinical manifestation
(1) local symptom: the child stops up choana and pharyngeal opening of auditory tube because of adenoid vegetation, and symptoms such as ear nasopharynx can take place.Mouth breathing when showing as sleep, weighing down behind the root of the tongue often has the sound of snoring, and it is not peaceful to sleep night, and the nose secretion is many, when speaking closed rhinolalia is arranged, and voice are ambiguous.Because of long-term mouth breathing, cause the facial bone dysplasia, upper jaw bone is elongated, high-arched palate, denture is not whole, and last incisor exposes, and lip is thick, and the facial expression that lacks has dull-witted performance, forms " adenoid face ".The coordinate movement imbalance is often choked and is coughed between swallowing and breathing.The dirty stimulation respiratory mucosa of secretions is easily suffered from tracheitis.Because of being obstructed, pharyngotympanic tube causes that easily non-suppurative otitis media causes suction and goes down otopiesis.
(2) General Symptoms: nutrition of whole body and dysplasia are often arranged, mainly show as chronic poisoning reflexive nervous symptoms, as the expansion of the uneasiness blunt, uncomfortable in chest of expressing one's feelings, lung is bad, with the passing of time causes pigeon chest or flat chest.Minority is because the resistance of chronic nose, long term hypoxia and pulmonary heart disease occurs, even acute heart failure.Adenoid face is seen in inspection, and hard palate is high, and there is pink on the visible nasopharynx of posterior rhinoscopy top and narrow, and lobulated lymphoid tissue piece, nasopharynx part palpation can touch soft lump, can make X line nasopharynx lateral projection in case of necessity, help diagnosis.
Three, treatment present situation
Excision gland sample body can excise simultaneously when operation on tonsils, or carry out separately, should not can consider X-ray therapy by operator.
Four, 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.。
Five, so far, all do not see any report or document record that albendazole is used for the treatment of chronic adenoid vegetation 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 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 albendazole or the nasal drop made from the compound recipe that contains albendazole, spray, aerosol and powder spray of the present invention, include, but are not limited to following disease: adenoid vegetation, allergic rhinitis, nasal polyp or nasal polyp, rhinitis, pharyngitis, tracheitis and bronchitis.
Use of the present inventionly with albendazole or the nasal drop made from the compound recipe that contains albendazole, spray, aerosol and powder spray, for the adenoid vegetation 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.
Adenoid vegetation 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.
By the preparation of following examples, and be described with the application of albendazole nasal drop, spray, aerosol and powder spray treatment adenoid vegetation to albendazole nasal drop of the present invention, spray, aerosol and powder spray.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.
The preparation of embodiment 1 albendazole nasal mist
In ten thousand grades of environment, albendazole 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 albendazole nasal mist with this liquid medicine filling.
The preparation of embodiment 2 albendazole nasal aerosol
In ten thousand grades of environment, albendazole 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 albendazole nasal aerosol.
The preparation of embodiment 3 albendazole nasal cavity powder sprays
In ten thousand grades of environment, with albendazole 20mg, hydroxypropyl cellulose (HPC) 980mg, Benasept 0.1mg co-blended, the albendazole 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 albendazole powder spray.Per nasal sprays into administration with the dust cloud device during use.
The preparation of embodiment 4 albendazole nasal drop
In ten thousand grades of environment, albendazole 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 albendazole nasal drop.
Embodiment 5 uses albendazole nasal mist treatment adenoid vegetation
Since childhood, the woman, 4 years old, sleep had the sound of snoring, is diagnosed as adenoid vegetation, intended excision gland sample body.Its father and mother adversary's art has doubt, albendazole nasal mist on probation, and every day, nasal-cavity administration was 2 times, and after 15 days, the sound of snoring disappears, and to hospital's further consultation, gland sample body obviously dwindles.
Embodiment 6 uses albendazole nasal aerosol treatment adenoid vegetation
Since childhood, the man, 6 years old, be diagnosed as adenoid vegetation, use the albendazole nasal aerosol, administration every day 1 time, after 20 days, the sound of snoring disappears, and to hospital's further consultation, gland sample body obviously dwindles.
Embodiment 7 uses albendazole powder spray treatment adenoid vegetation
Since childhood, the man, 4 years old, sleep had the sound of snoring, and the nasal mucus secretion is many, is diagnosed as adenoid vegetation, and with albendazole nasal cavity powder spray, administration every day 1 time, after 15 days, the sound of snoring disappears, the nasal mucus secretion reduces, and to hospital's further consultation, gland sample body obviously dwindles.
Embodiment 8 uses albendazole nasal drop treatment adenoid vegetation
6 years old girl makes a definite diagnosis adenoid vegetation, and with hydrochloric acid albendazole nasal cavity therapy, be administered once every day, continues 15 days, and symptom is obviously improved.
Claims (1)
1, the application of albendazole in the medicine of preparation treatment adenoid vegetation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100784706A CN100455285C (en) | 2004-09-14 | 2004-09-14 | Albendazole new form for treating adenoid hypertrophy |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100784706A CN100455285C (en) | 2004-09-14 | 2004-09-14 | Albendazole new form for treating adenoid hypertrophy |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1748696A CN1748696A (en) | 2006-03-22 |
| CN100455285C true CN100455285C (en) | 2009-01-28 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100784706A Expired - Fee Related CN100455285C (en) | 2004-09-14 | 2004-09-14 | Albendazole new form for treating adenoid hypertrophy |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100455285C (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1518978A (en) * | 2003-01-20 | 2004-08-11 | 王玉万 | Mouth cavity spraying agent containing benzimidazole family for expelling worms |
-
2004
- 2004-09-14 CN CNB2004100784706A patent/CN100455285C/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1518978A (en) * | 2003-01-20 | 2004-08-11 | 王玉万 | Mouth cavity spraying agent containing benzimidazole family for expelling worms |
Non-Patent Citations (2)
| Title |
|---|
| 药剂学. 毕殿洲主编，第229、388、393-394页，人民卫生出版社. 1999 |
| 药剂学. 毕殿洲主编，第229、388、393-394页，人民卫生出版社. 1999 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1748696A (en) | 2006-03-22 |
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|---|---|---|---|
| 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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| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20090128 Termination date: 20091014 |