CN105193805A - Compound pharmaceutical composition for motion sickness - Google Patents
Compound pharmaceutical composition for motion sickness Download PDFInfo
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- CN105193805A CN105193805A CN201510625710.8A CN201510625710A CN105193805A CN 105193805 A CN105193805 A CN 105193805A CN 201510625710 A CN201510625710 A CN 201510625710A CN 105193805 A CN105193805 A CN 105193805A
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- scopolamine
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Abstract
The invention discloses a compound pharmaceutical composition for motion sickness. The compound pharmaceutical composition comprises scopolamine and antihistamine type drugs, wherein chlorpheniramine, dimenhydrinate and levocetirizine are selected as the antihistamine type drugs preferably. Dosage forms suitable for the adult, the old and children can be prepared from the compound pharmaceutical composition and auxiliary materials acceptable in pharmaceutical preparation.
Description
Technical field
The invention belongs to pharmaceutical field, relate to a kind of compound medicament composition for motion sickness.
Background technology
Motion sickness also known as motion sickness (motionsickness), namely carsick, seasick, air-sickness and due to a variety of causes cause wave, jolt, rotate, the general designation of the associated diseases such as accelerated motion.
The pathogenesis of motion sickness is not yet completely clear, mainly with to affect vestibular function relevant.The utriculus of the inner ear membranous labyrinth of vestibular organ and the capsule speckle of sacculus experience up and down and the rectilinear motion of left and right, and three semicircular duct hair cells experience rotary motion.When capsule speckle or hair cell are subject to the neural impulse caused by a certain amount of abnormal Motor stimulation, reach vestibular nucleus successively by vestibular nerve, then reach cerebellum and hypothalamus, thus causing a series of is the clinical manifestation of cardinal symptom with dizzy.Affect network structure after vestibule irriate, cause blood pressure drops and vomiting.
Vestibular nucleus causes nystagmus by medial longitudinal fasciculus fiber to eye muscle nucleus motorius.Cerebellum and hypothalamus cause whole-body muscle tension change by after neural impulse.Motion sickness and vision may have certain relation.Such as, primary disease can be caused too when people stare the object of rapid movement or rotation.Cerebellum irriate also may be the another mechanism of primary disease.In addition, high temperature, high humidity, improper ventilation, noise, special odor, nervous, do not have enough sleep, overtired, hungry or satiety, physical weakness, disease of inner ear etc. all easily bring out primary disease.
It is reported that China is one of the world's " motion sickness " country that incidence rate is the highest, 2 ~ 12 years old child of 58% can be carsick, have the people of about 5% to 10% throughout one's life all can perplex by carsickness, the people of 80% once lived through cinetosis reaction in various degree.The way that " cinetosis " does not also thoroughly cure at present, and take the method that carsick medicine is more common pre-carsickness-proof.The people gone out in the past mainly works, goes to school, is on home leave, and based on person between twenty and fifty, now life, economic condition get well, old people, the getting more and more of child's out on tours.Although motion sickness all can occur in the crowd at various age, but old man, child fall ill, the order of severity can be more severe, if for tourism is gone out, original object is happy, but motion sickness allows people suffer misery, to destroy mood, so market is in the urgent need to all spendable carsick medicine of child, adult, old man safely and effectively.
Scopolamine is the anticholinergic agent that a kind of peripheral action is stronger, blocks M cholinoceptor.Its peripheral action is strong and hold time short compared with atropine, and have excitation to respiratory center, central action, to suppress, can suppress glandular secretion, removes blood capillary spasm, improves microcirculation, expansion bronchus, removes smooth muscle convulsion twin; There are calmness, syngignoscism to brain, have excitation to respiratory center.This product, mainly through suppressing the spasm of gastrointestinal smooth muscle, reduces the amplitude and frequency of wriggling and alleviates Nausea and vomiting symptom, thus prevention and therapy motion sickness.
H on the histamine competitive effect cell that Loratadine can discharge with neuron
1receptor, the allergy caused by antagonizing histamine, participates in the anticholinergic effect of nervus centralis simultaneously, and likely relevant with the synapse acting on oblongata EC chemoreceptor, thus suppresses the vomiting that motion sickness produces.The Loratadine of this kind of classics has chlorphenamine, dimenhydrinate, promethazine, diphenhydramine etc.These medicines, because of strong to central activities, completely to the contraction etc. of the gastrointestinal smooth muscle that antihistamine causes, can play significantly anti-corona and town and tell effect.Single optical isomer-the levocetirizine of cetirizine avoids the calmness of cetirizine, central nervous system's side effect such as drowsiness, but anti-histamine activity is still similar to cetirizine.It is because its pharmacological mechanism is comparatively extensive that levocetirizine anti-allergic effects is better than other Claritin, except there is stronger antagonism H1 receptor acting, also there is other antiallergic action mechanism, the pharmacological mechanism relevant to asthma comprise the gathering of the inflammatory cell suppressed based on acidophil in air flue and infiltration, suppression hypertrophy/basophilic leukocyte retting conditions reaction, suppress the bronchiectatic activity etc. of delayed asthma reaction and enhancing beta 2-adrenergic receptor agonist.
Through patent and pertinent literature retrieval, find no the patent application about this pharmaceutical composition or report.
Summary of the invention
The object of the invention is for extensive patients provides the compound medicament composition being used for the treatment of motion sickness safely and effectively.
Technical scheme of the present invention is summarized as follows:
For the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition includes acceptable adjuvant in the scopolamine of effective amount, the Loratadine of effective dose and pharmaceutical preparation.
For the compound medicament composition of motion sickness, it is characterized in that described Loratadine comprises chlorphenamine, dimenhydrinate, promethazine, diphenhydramine, cetirizine, levocetirizine etc., preferred chlorphenamine, dimenhydrinate and levocetirizine.
For the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition comprises scopolamine and chlorphenamine.Wherein the content of scopolamine is 0.02 ~ 0.1mg, the content of chlorphenamine is 0.6 ~ 2.0mg, and the content of preferred scopolamine is 0.06 ~ 0.1mg, and the content of chlorphenamine is 0.8 ~ 1.6mg, most preferably the content of scopolamine is 0.06mg, and the content of chlorphenamine is 0.91mg.
For the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition comprises scopolamine and dimenhydrinate.Wherein the content of scopolamine is 0.02 ~ 0.1mg, the content of dimenhydrinate is 2.0 ~ 15.0mg, and the content of preferred scopolamine is 0.06 ~ 0.1mg, and the content of dimenhydrinate is 4.0 ~ 12.5mg, most preferably the content of scopolamine is 0.06mg, and the content of dimenhydrinate is 6mg.
For the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition comprises scopolamine and levocetirizine.Wherein the content of scopolamine is 0.02 ~ 0.1mg, the content of levocetirizine is 0.5 ~ 5.0mg, and the content of preferred scopolamine is 0.06 ~ 0.1mg, and the content of levocetirizine is 1.0 ~ 3mg, most preferably the content of scopolamine is 0.06mg, and the content of levocetirizine is 2mg.
For the compound medicament composition of motion sickness, it is characterized in that the prescription of the molten film of compound recipe mouth of scopolamine and chlorphenamine form comprise 0.06 mass parts scopolamine, 0.91 mass parts chlorphenamine, the filmogen of 5 ~ 20 mass parts, the filler of 6 ~ 18 mass parts, the plasticizer of 3 ~ 8 mass parts and the sweeting agent of 0.7 ~ 1.5 mass parts, and appropriate aromatic and coloring agent.
For the compound medicament composition of motion sickness, it is characterized in that the prescription of the compound recipe chewable tablet of scopolamine and chlorphenamine forms scopolamine, the chlorphenamine of 0.91 mass parts, the correctives of 0 ~ 5 mass parts, the diluent of 80 ~ 160 mass parts, the sweeting agent of 1.0 ~ 2.0 mass parts, the stabilizing agent of 0 ~ 20 mass parts, the lubricant of 0 ~ 5 mass parts comprising 0.06 mass parts, and appropriate aromatic and coloring agent.
For the compound medicament composition of motion sickness, it is characterized in that the prescription of the molten film of compound recipe mouth of scopolamine and dimenhydrinate form comprise 0.06 mass parts scopolamine, 6 mass parts dimenhydrinate, the sweeting agent of the correctives of 5 ~ 10 mass parts, the filmogen of 5 ~ 18 mass parts, the filler of 6 ~ 20 mass parts, the plasticizer of 3 ~ 8 mass parts and 0.7 ~ 1.5 mass parts, and appropriate aromatic and coloring agent.
For the compound medicament composition of motion sickness, it is characterized in that the prescription of the compound recipe chewable tablet of scopolamine and levocetirizine forms scopolamine, the levocetirizine of 2 mass parts, the correctives of 0 ~ 20 mass parts, the diluent of 100 ~ 180 mass parts, the sweeting agent of 2.0 ~ 5.0 mass parts, the stabilizing agent of 10 ~ 30 mass parts, the lubricant of 2 ~ 5 mass parts comprising 0.06 mass parts, and appropriate aromatic and coloring agent.
Preparation method for the scopolamine of motion sickness and the molten film of compound recipe mouth of chlorphenamine comprises the steps:
(1) supplementary material is taken by recipe quantity;
(2) chlorphenamine is used plasticizer moistening, after adding the mixing of scopolamine, filmogen, filler and sweeting agent, the purified water adding 140 ~ 180 mass parts stirs; Place 20 ~ 40min;
(3) until swelling completely after, add appropriate amount of essence and coloring agent, stir evenly rear placement 20 ~ 40min;
(4) film, at 50 ~ 80 DEG C, dries 30 ~ 50min, to obtain final product.
Preparation method for the scopolamine of motion sickness and the compound recipe chewable tablet of chlorphenamine comprises the steps:
(1) supplementary material is taken by recipe quantity;
(2), after scopolamine, chlorphenamine and diluent equimultiple being increased progressively mixing, mix homogeneously with all the other adjuvants, direct compression, to obtain final product.
Comprise the steps: for the scopolamine of motion sickness and the preparation method of the molten film of dimenhydrinate compound recipe mouth
(1) supplementary material is taken by recipe quantity;
(2) dimenhydrinate is dissolved in the purified water of 30 ~ 100 mass parts, adds correctives and stir; In 60 DEG C of oven dry, after obtained taste masking, medicated powder end, crosses 80 mesh sieves for subsequent use;
(3) scopolamine is used plasticizer moistening, after after adding taste masking, medicated powder end, filmogen, filler and sweeting agent mix, the purified water adding 130 ~ 200 mass parts stirs; Place 20 ~ 40min;
(3) until swelling completely after, add appropriate amount of essence and coloring agent, stir evenly rear placement 20 ~ 40min;
(4) film, at 50 ~ 80 DEG C, dries 30 ~ 50min, to obtain final product.
Comprise the steps: for the scopolamine of motion sickness and the compound recipe chewable tablet preparation method of levocetirizine
(1) supplementary material is taken by recipe quantity;
(2), after levocetirizine and stabilizing agent being dissolved in the purified water of 20 ~ 40 mass parts, adding correctives and stir 20 ~ 40min; In 60 DEG C of oven dry, after obtained taste masking, medicated powder end, crosses 80 mesh sieves for subsequent use;
(3), after scopolamine and diluent equimultiple being increased progressively mixing, after adding taste masking, mix homogeneously with all the other adjuvants in medicated powder end, and direct compression, to obtain final product.
Compound medicament composition for motion sickness of the present invention is safe and effective, taste good, and Compliance is good, for patient's prevention, treatment motion sickness provide new selection.
Detailed description of the invention
The present invention is further elaborated by following examples, but scope of the present invention is not limited to these embodiments.For general technical staff of the technical field of the invention, without departing from the inventive concept of the premise, some simple dosage forms can also be made and change or adjuvant replacement, all should be considered as belonging to protection scope of the present invention.
embodiment 1
Recipe quantity for the scopolamine of motion sickness and the molten film of chlorphenamine compound mouth 1000 in the present invention is as follows:
| Composition | Every 1000 consumptions (g) |
| Scopolamine | 0.06 |
| Chlorphenamine | 0.91 |
| Hypromellose E-15 | 10 |
| Maltodextrin | 6 |
| Mannitol | 6 |
| Sucralose | 0.8 |
| Glycerol | 3 |
| Mint Essence | 0.6 |
| Titanium dioxide | 0.05 |
| Purified water | 140 |
Preparation technology:
(1) supplementary material is taken by recipe quantity;
(2) with glycerol moistening chlorphenamine, after adding the mixing of scopolamine, hydroxypropyl methylcellulose E-15, mannitol, maltodextrin and sucralose, the purified water adding 140g stirs; Place 30min;
(3) until swelling completely after, add Mint Essence and titanium dioxide, stir evenly rear placement 20min;
(4) film, at 60 DEG C, dries 40min, to obtain final product.
embodiment 2
Recipe quantity for the scopolamine of motion sickness and chlorphenamine compound chewable tablet 1000 in the present invention is as follows:
| Composition | Every 1000 consumptions (g) |
| Scopolamine | 0.06 |
| Chlorphenamine | 0.91 |
| Mannitol | 80 |
| Pregelatinized Starch | 50 |
| Maltodextrin | 25 |
| Citric acid | 15 |
| Magnesium stearate | 5 |
| Sucralose | 1.2 |
| Strawberry essence | 0.6 |
Preparation technology:
(1) supplementary material is taken by recipe quantity;
(2), after scopolamine, chlorphenamine and pregelatinized Starch equimultiple being increased progressively mixing, mix homogeneously with all the other adjuvants, direct compression, to obtain final product.
embodiment 3
Recipe quantity for the scopolamine of motion sickness and the molten film of dimenhydrinate compound recipe mouth 1000 in the present invention is as follows:
| Composition | Every 1000 consumptions (g) |
| Scopolamine | 0.06 |
| Dimenhydrinate | 6 |
| Polacrilin potassium resin (IRP88) | 6 |
| Methylcellulose | 12 |
| Hydroxypropyl cellulose | 4 |
| Pregelatinized Starch | 4 |
| Sucrose | 3 |
| Strawberry essence | 1 |
| Aspartame | 1.5 |
| Carmine pigment | 0.02 |
| Purified water | 180 |
| Polyethylene Glycol | 5 |
Preparation technology:
(1) supplementary material is taken by recipe quantity;
(2) dimenhydrinate is dissolved in the purified water of 80g, adds polacrilin potassium resin (IRP88) and stir; In 60 DEG C of oven dry, after obtained taste masking, medicated powder end, crosses 80 mesh sieves for subsequent use;
(3) scopolamine is used Polyethylene Glycol moistening, after after adding taste masking, dimenhydrinate medicated powder end, methylcellulose and hydroxypropyl cellulose, pregelatinized Starch, sucrose and aspartame mix, the purified water adding 180g stirs; Place 30min;
(4) until swelling completely after, add strawberry essence and carmine pigment, stir evenly rear placement 30min;
(5) film, at 60 DEG C, dries 30min, to obtain final product.
embodiment 4
Recipe quantity for the scopolamine of motion sickness and levocetirizine compound recipe chewable tablet 1000 in the present invention is as follows:
| Composition | Every 1000 consumptions (g) |
| Scopolamine | 0.06 |
| Levocetirizine | 2 |
| Beta cyclodextrin | 16 |
| Mannitol | 100 |
| Microcrystalline Cellulose | 80 |
| Citric acid | 20 |
| Magnesium stearate | 2.5 |
| Sucralose | 3 |
| Strawberry essence | 0.6 |
Preparation technology:
(1) supplementary material is taken by recipe quantity;
(2), after levocetirizine and citric acid being dissolved in the purified water of 30g, adding beta cyclodextrin and stir 20 ~ 40min; In 60 DEG C of oven dry, after obtained taste masking, medicated powder end, crosses 80 mesh sieves for subsequent use;
(3), after scopolamine and diluent equimultiple being increased progressively mixing, after adding taste masking, mix homogeneously with all the other adjuvants in levocetirizine medicated powder end, and direct compression, to obtain final product.
The curative effect of compound medicament composition of the present invention prevention, treatment motion sickness is verified by rotational chair test.Rotational chair test is the test checking vestibular function.The orientation of the vestibular function participant of people and balance, lowly easily there is illusion in vestibular function, vestibular function sensitivity then easily occurs motion sickness, is exactly the carsickness, seasick, airsick often said.
1, in the present invention for the clinical trial of the scopolamine of motion sickness and the molten film of chlorphenamine compound mouth
Choose the easy carsick adult human of 40 example, wherein man 21 example, female 19 example, at random patient is divided into test group 20 example and matched group 20 example, volunteer's all unification standard meals before test, and in starting test with two hours after the meal.Test group experiment starts to take 2 scopolamine and the molten film of chlorphenamine compound mouth (embodiment 1) front half an hour, and matched group takes 2 blank films.During inspection, person under inspection is sitting on swivel chair, fasten seat belts, put on an eyeshade, start electric revolving chair, rotate with two seconds kinds one rotating speed of enclosing the land, stop the rotation after turning 45 circles, open eyes after several seconds kind, bi-pedal ground after unfastening one's seat-belt, get back on original seat, observe experimenter and whether occur motion sickness symptom.Result shows, and test group volunteer occurs that the ratio of motion sickness symptom is far below matched group, illustrates that scopolamine prepared by embodiment 1 and the molten film of chlorphenamine compound mouth have certain curative effect.
2, in the present invention for the clinical trial of the scopolamine of motion sickness and levocetirizine compound recipe chewable tablet
Choose the easy carsick adult human of 40 example, wherein man 20 example, female 20 example, at random patient is divided into test group 20 example and matched group 20 example, volunteer's all unification standard meals before test, and in starting test with two hours after the meal.Test group experiment starts to take 2 scopolamine and levocetirizine compound recipe chewable tablet (embodiment 4) front half an hour, and matched group takes 2 blanks.During inspection, person under inspection is sitting on swivel chair, fasten seat belts, put on an eyeshade, start electric revolving chair, rotate with two seconds kinds one rotating speed of enclosing the land, stop the rotation after turning 45 circles, open eyes after several seconds kind, bi-pedal ground after unfastening one's seat-belt, get back on original seat, observe experimenter and whether occur motion sickness symptom.Result shows, and test group volunteer occurs that the ratio of motion sickness symptom is far below matched group, illustrates that scopolamine prepared by embodiment 4 and levocetirizine compound recipe chewable tablet have certain curative effect.
Claims (9)
1., for the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition includes acceptable adjuvant in the scopolamine of effective amount, the Loratadine of effective dose and pharmaceutical preparation.
2., for the compound medicament composition of motion sickness, it is characterized in that described Loratadine comprises chlorphenamine, dimenhydrinate, promethazine, diphenhydramine, cetirizine, levocetirizine etc., preferred chlorphenamine, dimenhydrinate and levocetirizine.
3. for the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition comprises scopolamine and chlorphenamine, wherein the content of scopolamine is 0.02 ~ 0.1mg, the content of chlorphenamine is 0.6 ~ 2.0mg, the content of preferred scopolamine is 0.06 ~ 0.1mg, the content of chlorphenamine is 0.8 ~ 1.6mg, and most preferably the content of scopolamine is 0.06mg, and the content of chlorphenamine is 0.91mg.
4. for the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition comprises scopolamine and dimenhydrinate, wherein the content of scopolamine is 0.02 ~ 0.1mg, the content of dimenhydrinate is 2.0 ~ 15.0mg, the content of preferred scopolamine is 0.06 ~ 0.1mg, the content of dimenhydrinate is 4.0 ~ 12.5mg, and most preferably the content of scopolamine is 0.06mg, and the content of dimenhydrinate is 6mg.
5. for the compound medicament composition of motion sickness, it is characterized in that described compound medicament composition comprises scopolamine and levocetirizine, wherein the content of scopolamine is 0.02 ~ 0.1mg, the content of levocetirizine is 0.5 ~ 5.0mg, the content of preferred scopolamine is 0.06 ~ 0.1mg, the content of levocetirizine is 1.0 ~ 3mg, and most preferably the content of scopolamine is 0.06mg, and the content of levocetirizine is 2mg.
6. for the compound medicament composition of motion sickness, it is characterized in that the prescription of the molten film of compound recipe mouth of scopolamine and chlorphenamine form comprise 0.06 mass parts scopolamine, 0.91 mass parts chlorphenamine, the filmogen of 5 ~ 20 mass parts, the filler of 6 ~ 18 mass parts, the plasticizer of 3 ~ 8 mass parts and the sweeting agent of 0.7 ~ 1.5 mass parts, and appropriate aromatic and coloring agent.
7. for the compound medicament composition of motion sickness, it is characterized in that the prescription of the compound recipe chewable tablet of scopolamine and chlorphenamine forms scopolamine, the chlorphenamine of 0.91 mass parts, the correctives of 0 ~ 5 mass parts, the diluent of 80 ~ 160 mass parts, the sweeting agent of 1.0 ~ 2.0 mass parts, the stabilizing agent of 0 ~ 20 mass parts, the lubricant of 0 ~ 5 mass parts comprising 0.06 mass parts, and appropriate aromatic and coloring agent.
8. for the compound medicament composition of motion sickness, it is characterized in that the prescription of the molten film of compound recipe mouth of scopolamine and dimenhydrinate form comprise 0.06 mass parts scopolamine, 6 mass parts dimenhydrinate, the sweeting agent of the correctives of 5 ~ 10 mass parts, the filmogen of 5 ~ 18 mass parts, the filler of 6 ~ 20 mass parts, the plasticizer of 3 ~ 8 mass parts and 0.7 ~ 1.5 mass parts, and appropriate aromatic and coloring agent.
9. for the compound medicament composition of motion sickness, it is characterized in that the prescription of the compound recipe chewable tablet of scopolamine and levocetirizine forms scopolamine, the levocetirizine of 2 mass parts, the correctives of 0 ~ 20 mass parts, the diluent of 100 ~ 180 mass parts, the sweeting agent of 2.0 ~ 5.0 mass parts, the stabilizing agent of 10 ~ 30 mass parts, the lubricant of 2 ~ 5 mass parts comprising 0.06 mass parts, and appropriate aromatic and coloring agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510625710.8A CN105193805A (en) | 2015-09-28 | 2015-09-28 | Compound pharmaceutical composition for motion sickness |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510625710.8A CN105193805A (en) | 2015-09-28 | 2015-09-28 | Compound pharmaceutical composition for motion sickness |
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| CN105193805A true CN105193805A (en) | 2015-12-30 |
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| CN201510625710.8A Pending CN105193805A (en) | 2015-09-28 | 2015-09-28 | Compound pharmaceutical composition for motion sickness |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106540122A (en) * | 2016-11-07 | 2017-03-29 | 成都泠汐尚品科技有限公司 | A kind of preventing and treating motion sickness patch containing hyoscine |
| CN110772524A (en) * | 2019-12-11 | 2020-02-11 | 方科伟 | Pharmaceutical composition for treating motion sickness |
-
2015
- 2015-09-28 CN CN201510625710.8A patent/CN105193805A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106540122A (en) * | 2016-11-07 | 2017-03-29 | 成都泠汐尚品科技有限公司 | A kind of preventing and treating motion sickness patch containing hyoscine |
| CN110772524A (en) * | 2019-12-11 | 2020-02-11 | 方科伟 | Pharmaceutical composition for treating motion sickness |
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