CN105193839A - Preparation for resisting altitude sickness and application of preparation - Google Patents

Preparation for resisting altitude sickness and application of preparation Download PDF

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Publication number
CN105193839A
CN105193839A CN201510717944.5A CN201510717944A CN105193839A CN 105193839 A CN105193839 A CN 105193839A CN 201510717944 A CN201510717944 A CN 201510717944A CN 105193839 A CN105193839 A CN 105193839A
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China
Prior art keywords
preparation
altitude sickness
acetazolamide
selenium
application
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CN201510717944.5A
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Chinese (zh)
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叶亚东
叶季峨
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CHANGZHOU ADAM BIOTECH Inc
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CHANGZHOU ADAM BIOTECH Inc
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Abstract

The invention discloses a preparation for resisting altitude sickness and an application of the preparation and relates to the field of medicinal preparations. The preparation for resisting the altitude sickness comprises 0.05-0.2 g of acetazolamide, 10-20 mg of coenzyme Q10, 500-1,000 mg of tyrosine and 1-2 mg of selenium, wherein selenium can be selenium salt and selenium yeast. The preparation is used for preventing altitude sickness symptoms such as headache, insomnia, dyspnea and the like. According to the application, the altitude sickness symptoms can be prevented in multiple drug-delivery ways including subcutaneous injection or intramuscular injection, intravenous injection or intravenous drip, oral administration including pills, capsules, tablets and the like and a nasal drug delivery system such as nasal spray and the like. The preparation has the benefits that the preparation can prevent altitude sickness symptoms such as headache, insomnia, dyspnea and the like, can effectively prevent altitude sickness and can overcome side effects of acetazolamide when the use quantity of the preparations is smaller than a conventional dosage of acetazolamide.

Description

A kind of altitude sickness prevention preparation and application thereof
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to altitude sickness prevention formulation art.
Technical background
The various pathologic reactions that altitude sickness produces after to be that human body is radical be exposed to hypobaric hypoxia environment are the exclusive commonly encountered diseases in highlands.Common symptom has headache, insomnia, and loss of appetite is tired, dyspnea etc.There will be insensitive, irritable emotion time serious, spirit be excited, contemplative faculty, note meaning power goes down, listen, depending on, smell, parageusia, to hallucinate, also may there is the phenomenons such as edema, shock or spasm.
Acetazolamide is a kind of weak effect diuretic, is mainly used in treating glaucoma, of short duration reduction intraocular pressure.But in fact, acetazolamide is recommended as altitude sickness prevention medicine by international alpinist club.The DIAMOX that Germany produces is exactly the trade name of acetazolamide, is used for preventing altitude sickness by Xizang road bridge person.
Although acetazolamide has better effects in control acute high altitude reaction, and has certain antioxidation.On plateau, oral acetazolamide can increase pulmonary ventilation volume, improves blood oxygen saturation (SaO2) and sleep quality.Clinical recommendation prevention altitude sickness oral dose be 0.25 gram/times, 2 times/day.But, when oral dose is 0.25 ~ 0.3 gram/day, just there will be face and the side effect such as hands, foot numbness, pain, polyuria.
Therefore, wish to have one to prevent altitude sickness, the composite preparation of acetazolamide side effect can be overcome again.
Research finds, coenzyme Q10, mainly for the protection of heart, promotes Conversion of energy, promotes energy, improves immunity, slow down aging.Coenzyme q-10 contributes to for cardiac muscle provides sufficient oxygen, and prevention sudden heart disease, especially in myocardial ischemia process, coenzyme Q10 plays pivotal role.It is the required energy (as ATP) of cells survival that coenzyme q-10 helps food conversion, and make cell keep optimum state, people is felt, and energy is more abundant; Coenzyme q-10 is the Natural antioxidant that cell self produces, and can stop the formation of free radical, contribute to safeguarding immune normal operation and slow down aging.Selenium can be main in active cell antioxidase-glutathion antiperoxidase, it is the trace element of needed by human.Tyrosine is a kind of non essential amino acid, is the important substance participating in body physiological function adjustment.These coenzyme Q10s, selenium and tyrosine can share with acetazolamide, play potentiation, subtract secondary effect.But document is not reported at present.
Summary of the invention
Goal of the invention
The present invention is directed to existing acetazolamide for preventing the feature of altitude sickness, designing a kind of altitude sickness prevention preparation, can altitude sickness be prevented, acetazolamide side effect can be overcome again.
Technical scheme
Technical scheme of the present invention is a kind of altitude sickness prevention preparation, by acetazolamide 0.05-0.2g, ubiquinone 1010-20mg, tyrosinase 15 00-1000mg and selenium 1-2mg form.Described selenium can be selenium salt, selenium yeast.The present invention for preventing mountain sickness, as symptoms such as headache, insomnia, dyspnea.This purposes, by multiple administering mode prevention altitude sickness symptom, comprises subcutaneous or intramuscular injection, intravenous injection or intravenous drip; Oral administration is as pill, capsule, tablet etc.; Per nasal delivery system is as nasal spray etc.
Beneficial effect
Acetazolamide and coenzyme Q10, tyrosine and selenium are formed preparation by the present invention.First, under the synergism of tyrosine, can the oral dose taking acetazolamide be reduced, reach prevention altitude sickness effect preferably simultaneously.Again, coenzyme Q10 and selenium can alleviate the face and the side effect such as hands, foot numbness, pain, polyuria that acetazolamide causes.Therefore, the present invention can prevent altitude sickness, can overcome acetazolamide side effect again.Result of the test shows, and preparation of the present invention when lower than acetazolamide routine dose, can play the plateau reaction symptoms such as prevention insomnia, headache, anoxia.
Detailed description of the invention
Embodiment 1
Acetazolamide 50mg, ubiquinone 1010mg, tyrosinase 15 00mg and selenium 1mg.After each component being taken, mixing, then add calcium silicates, maltodextrin, silicon dioxide, magnesium stearate, after mixing, load in starchiness capsule, obtain capsule.
Embodiment 2
Acetazolamide 200mg, coenzyme Q10 20mg, tyrosine 1000mg and selenium 2mg.After each component being taken, mixing, then add calcium silicates, maltodextrin, silicon dioxide, magnesium stearate, after mixing, load in starchiness capsule, obtain capsule.
Embodiment 3
The sedation of embodiment 1 preparation: adopt spontaneous activity experiment, using mice as animal subject, get 50 mices, male and female half and half, body weight is 18-22g, is divided into 5 groups at random: high dose group, middle dosage group, low dose group, acetazolamide matched group, normal group, only often organizes l0.Normal group is according to the dosage gavage normal saline of 0.2ml/10g; Acetazolamide matched group gavage 40mg/kg acetazolamide tablet; High, normal, basic dosage component does not give invention formulation 220,110,55mg/kg gavage, successive administration 4 days.After last administration 50min, mice is put into successively the multiplex instrument of SD-5G type pharmacology Physiological Experiment, after conforming, the autonomic activities number of times of mice in record 5min.
Result: in table 1.Embodiment 1 preparation high, normal, basic dosage energy significance reduces the autonomic activities number of times of mice, compares have significant difference (P<0.05) with normal group.
Table 1 embodiment 1 preparation is on the impact (means ± s) of spontaneous activity in mice number of times
* p<0.05, * * p<0.01 is compared with normal group
Embodiment 4:
Embodiment 1 preparation is to the effect of sleep: the test adopting the pentobarbital sodium incubation period length of one's sleep and duration.Get 50 mices and be divided into 5 groups at random: high dose group, middle dosage group, low dose group, acetazolamide matched group, normal group, only often organize l0.Normal group is according to the dosage gavage normal saline of 0.2ml/10g; Acetazolamide matched group gavage 40mg/kg acetazolamide tablet; High, normal, basic dosage component does not give embodiment 1 preparation 220,110,55mg/kg gavage, successive administration 4 days.After last administration 50min, each group mice equal lumbar injection pentobarbital sodium 35mg/Kg after 30min, the incubation period of record mice sleep, duration.
Result: as table 2.Compared with normal group mice, embodiment 1 preparation basic, normal, high dosage energy significance shortens mice sleep incubation period (P<0.05), extends the duration (P<0.05).
Table 2 embodiment 1 preparation is on the impact (means ± s) of the pentobarbital sodium incubation period length of one's sleep and duration
* p<0.05, * * p<0.01 is compared with normal group
Embodiment 5:
Embodiment 1 preparation is to the effect of headache: adopt the test of rat Nerve in Migraine Model.Get 50 rats and be divided into 5 groups at random: high dose group, middle dosage group, low dose group, acetazolamide matched group, model group, only often organize l0.Model group is according to the dosage gavage normal saline of 0.2ml/10g; Acetazolamide matched group gavage 20mg/kg acetazolamide tablet; High, normal, basic dosage component does not give embodiment 1 preparation 110,55,28mg/kg gavage, successive administration 7 days, and after administration in the 4th day, animal lumbar injection nitroglycerin, makes Nerve in Migraine Model, dosage 10mg/kg.For three days on end, observed behavior index in 4 hours after last modeling: rat is scratched one's head or gets rid of the time of a number of times and appearance and elimination.
Table 3 embodiment 1 preparation is on migrainous impact (means ± s)
* p<0.05, * * p<0.01 is compared with model group
Result: as table 3.About 30min after animal model, all occurs that ears are rubescent, forelimb is frequently scratched one's head, climbs cage increased frequency, dysphoria phenomenon.Upon administration, above-mentioned phenomenon fades away treatment group animal, is tending towards normal.The above-mentioned phenomenon of model group animal continues about 3 hours, then occurs curling oneself up, movable minimizing state.Compared with model group mice, embodiment 1 preparation basic, normal, high dosage energy significance reduces rat and scratches one's head and get rid of the number of times (P<0.05) of head.
Embodiment 6:
Embodiment 1 preparation is on the impact of oxygen deficit tolerance performance: get 50 mices and be divided into 5 groups at random: high dose group, middle dosage group, low dose group, acetazolamide matched group, normal group, only often organizes l0.Normal group is according to the dosage gavage normal saline of 0.2ml/10g; Acetazolamide matched group gavage 40mg/kg acetazolamide tablet; High, normal, basic dosage component does not give embodiment 1 preparation 220,110,55mg/kg gavage, successive administration 7 days.1h after last gastric infusion, puts into the 250mL wide mouthed bottle that 10g sodica calx is housed one by one by mice, smear vaseline sealing, make it air tight, timing immediately after adding a cover around bottle cap; Take respiratory arrest as standard, the beginning and ending time is index, and the time of record mice death because of anoxia tests.Standard hypoxic tolerance Time Calculation: T=(T1-T0)/(V0-W0/0.94) × 100 are (in formula: T1 is mouse diing time; T0 is the time of airtight beginning; V0 is effective bottle volume; W0 is Mouse Weight; The 0.94 little rodent density measured for drainage).
Table 4 embodiment 1 preparation is on the impact (means ± s) of oxygen deficit tolerance performance
* p<0.05, * * p<0.01 is compared with normal group
Result: as table 4.Compared with normal group mice, embodiment 1 preparation basic, normal, high dosage energy significance extends the mouse survival time (P<0.05).

Claims (5)

1. an altitude sickness prevention preparation, is characterized in that: by acetazolamide 0.05-0.2g, ubiquinone 1010-20mg, tyrosinase 15 00-1000mg and selenium 1-2mg form.
2. the altitude sickness prevention preparation according to claims 1, is characterized in that: described selenium can be selenium salt, selenium yeast.
3. the application of the altitude sickness prevention preparation according to claims 1, is characterized in that: for preventing mountain sickness.
4. the application of the altitude sickness prevention preparation according to claims 3, is characterized in that: the symptom of described mountain sickness is headache, insomnia, dyspnea etc.
5. according to the application of the arbitrary described altitude sickness prevention preparation of claims 2, it is characterized in that: by the altitude sickness symptom described in multiple administering mode prevention, comprise subcutaneous or intramuscular injection, intravenous injection or intravenous drip; Oral administration is as pill, capsule, tablet etc.; Per nasal delivery system is as nasal spray etc.
CN201510717944.5A 2015-10-29 2015-10-29 Preparation for resisting altitude sickness and application of preparation Pending CN105193839A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020062912A1 (en) 2018-09-25 2020-04-02 中国人民解放军总医院 Medical application of pyrimidine sulfonamides derivatives
WO2020062913A1 (en) 2018-09-25 2020-04-02 中国人民解放军总医院 Medical use of prostacyclin receptor agonist
CN112972686A (en) * 2021-02-20 2021-06-18 施懿宸 Medicine for resisting altitude stress and production equipment

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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WO2020062913A1 (en) 2018-09-25 2020-04-02 中国人民解放军总医院 Medical use of prostacyclin receptor agonist
CN112972686A (en) * 2021-02-20 2021-06-18 施懿宸 Medicine for resisting altitude stress and production equipment

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