CN110420212A - One kind is for treating schizophrenia composition and preparation method thereof - Google Patents
One kind is for treating schizophrenia composition and preparation method thereof Download PDFInfo
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- CN110420212A CN110420212A CN201910761768.3A CN201910761768A CN110420212A CN 110420212 A CN110420212 A CN 110420212A CN 201910761768 A CN201910761768 A CN 201910761768A CN 110420212 A CN110420212 A CN 110420212A
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- fexofenadine hydrochloride
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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Abstract
The invention discloses one kind for treating schizophrenia composition and preparation method thereof, which includes following components according to mass parts: 20 parts -360 parts of fexofenadine hydrochloride, 1 part -6 parts of Risperidone, 5 parts -15 parts of Aldoforwe ester.The drug can substantially change schizoid negative symptoms, being capable of obvious curative effects compared with Risperidone is used alone;The existing cognitive ability that Risperidone improvement schizophreniac is used alone reaches 30%-40%, and triplicity together, is had synergistic effect, the cognitive ability that can improve schizophreniac, which reaches, is increased to 95%-96% by the present invention.
Description
Technical field
The invention belongs to technical field of medicine, and in particular to one kind is for treating schizoid composition, originally
Invention further relates to a kind of for treating the preparation method of schizoid composition.
Background technique
The dosage form of fexofenadine hydrochloride is mainly tablet, it is a kind of second generation H1 receptor antagonist, can be selectively
It blocks by H1 receptor, there is good antihistamine effect, but without anti-five hydroxytryptamine, cholinolytic and adrenolytic.Therefore
There is no sedation and the effect of other central nervous systems.Blood-brain barrier can not be passed through.This product is suitable for seasonal allergic
The treatment of the illnesss such as rhinitis, chronic idiopathic urticaria.
Risperidone, for treating acute and chronic schizophrenia.Especially to positive and negative symptoms and its occur together
Affective symptom (such as anxiety, depression) has a better effect.Also it can reduce affective symptom related with schizophrenia.For urgency
Property the phase treat effective patient, in the treatment of the phase of maintenance, this product can continue to play its clinical efficacy.Be used alone Risperidone for
The cognitive ability for improving schizophreniac is limited.
Aldoforwe ester is the precursor of adefovirdipivoxil, is hydrolyzed to adefovirdipivoxil in vivo and plays antivirus action.A Defu
Wei ester is the acyclic analog of 5 '-monophosphate deoxidation arabinosy ladenosines.For treating chronic hepatitis B, idicatio is liver function
Compensatory adult chronic hepatitis B patient.This medicine is particularly suitable for needing long-term administration or the person that occurred lamivudine resistance.Extremely
The present there are no Aldoforwe ester for treating schizoid report.
Schizophrenia is the unknown mental disease of one group of cause of disease, shows the blood of schizophreniac in the prior art
All there is raised proinflammatory cytokine in liquid and brain, histamine is apparently higher than normally in the big hydrocrania of schizophrenia patients
People.Nature records alzheimer's disease, parkinsonism and schizophrenia and is proved to related to immune system." in
State's health nutrient " the 4th phase in 2010 points out that schizophrenia is not only merely a kind of disease conceptually, but a kind of disease
Poison.Virus is contained according to the human gene that current research display is up to 8%, our gene of these virus insertions are answered
Processed wherein just includes that can cause the schizoid factor.Therefore, a large amount of evidences show that schizophrenia is a kind of siberian crabapple
The illness that system participates in, schizophrenia is a kind of virus infection, is a kind of a kind of infection of DNA virus combination body.
The curative compliance of schizophreniac is low in close relations with the side effect of therapeutic agent all the time.At present
Schizophrenia drug press pharmacological action, clinically used anti-smart drug dispensing is divided into typical and two class of atypia.Typical anti-essence point
Medicine is also known as the anti-smart drug dispensing of tradition, and representing drug has Risperidone, haloperidol etc., and this kind of drug is good to positive symptom therapeutic effect,
But invalid to negative symptoms, simultaneously often with more serious the extrapyramidal symptoms (EPS), patient compliance is poor for treatment.
Summary of the invention
The object of the present invention is to provide one kind for treating schizoid composition and preparation method thereof, solves existing
There is the bad problem of current treatment of schizophrenia effect present in technology.
The technical scheme adopted by the invention is that it is a kind of for treating schizoid composition, according to mass parts packet
Include following components: 20 parts -360 parts of fexofenadine hydrochloride, 1 part -6 parts of Risperidone, 5 parts -15 parts of Aldoforwe ester.
Optionally, according to mass parts, including 100 parts -240 parts of fexofenadine hydrochloride, 1 part -4 parts of Risperidone, A Defu
8 parts -12 parts of Wei ester.
Optionally, according to mass parts, including 120 parts of fexofenadine hydrochloride, 2 parts of Risperidone, 10 parts of Aldoforwe ester.
The invention also discloses a kind of for treating the preparation method of schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 10 parts -180 parts of fexofenadine hydrochloride, 0.5 part -3 of Risperidone
Part, 5 parts -15 parts of Aldoforwe ester, by load weighted fexofenadine hydrochloride, Risperidone and Aldoforwe ester mixing are prepared into
To component 1;
Step 2, according to mass parts weigh following components: 10 parts -180 parts of fexofenadine hydrochloride, 0.5 part -3 of Risperidone
Part, load weighted fexofenadine hydrochloride and Risperidone are mixed, component 2 is prepared;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
The beneficial effects of the present invention are: can be substantially change using the present invention for treating schizoid composition
Schizoid negative symptoms being capable of obvious curative effects compared with Risperidone is used alone;Existing exclusive use Risperidone changes
The cognitive ability of kind schizophreniac reaches 30%-40%, fexofenadine hydrochloride and Risperidone is combined together, energy
The cognitive ability for enough improving schizophreniac, which reaches, is increased to 90%, the present invention by fexofenadine hydrochloride, Risperidone and
Aldoforwe ester triplicity together, has synergistic effect, the cognitive ability that can improve schizophreniac, which reaches, to be mentioned
Height arrives 95%-96%.
In the drug, the value range of fexofenadine hydrochloride, Risperidone and Aldoforwe ester will affect therapeutic effect,
Fexofenadine hydrochloride is less than 20 parts, and Risperidone is less than 1 part, and less than 5 parts, the two does not act synergistically Aldoforwe ester, cannot
Cure rate is improved, curative effect is bad.Fexofenadine hydrochloride is greater than 360 parts, and Risperidone is greater than 6 parts, and Aldoforwe ester is greater than
15 parts, side effect is larger, and people will appear dull, excess sedation after eating.
Specific embodiment
The present invention is described in detail With reference to embodiment.
The invention discloses one kind for treating schizoid composition, includes following components according to mass parts: salt
20 parts -360 parts of sour fexofenadine, 1 part -6 parts of Risperidone, 5 parts -15 parts of Aldoforwe ester.
Preferably, according to mass parts, the composition includes 100 parts -240 parts of fexofenadine hydrochloride, 1 part -4 of Risperidone
Part, 8 parts -12 parts of Aldoforwe ester.
Preferably, according to mass parts, the composition includes 120 parts of fexofenadine hydrochloride, and 2 parts of Risperidone, adefovirdipivoxil
10 parts of ester.
The invention also discloses a kind of for treating the preparation method of schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 10 parts -180 parts of fexofenadine hydrochloride, 0.5 part -3 of Risperidone
Part, 5 parts -15 parts of Aldoforwe ester, by load weighted fexofenadine hydrochloride, Risperidone and Aldoforwe ester mixing are prepared into
To component 1;
Step 2, according to mass parts weigh following components: 10 parts -180 parts of fexofenadine hydrochloride, 0.5 part -3 of Risperidone
Part, load weighted fexofenadine hydrochloride and Risperidone are mixed, component 2 is prepared;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
Embodiment 1
One kind includes following components according to mass parts: fexofenadine hydrochloride for treating schizoid composition
120 parts, 2 parts of Risperidone, 10 parts of Aldoforwe ester.
The above-mentioned preparation method for being used to treat schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 60 parts of fexofenadine hydrochloride, 1 part of Risperidone, Aldoforwe ester
10 parts, by load weighted fexofenadine hydrochloride, component 1 is prepared in Risperidone and Aldoforwe ester mixing;
Step 2 weighs following components according to mass parts: 60 parts of fexofenadine hydrochloride, 1 part of Risperidone, will be load weighted
Fexofenadine hydrochloride and Risperidone mixing, are prepared component 2;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
Embodiment 2
One kind includes following components according to mass parts: fexofenadine hydrochloride for treating schizoid composition
20 parts, 6 parts of Risperidone, 5 parts of Aldoforwe ester.
The above-mentioned preparation method for being used to treat schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 10 parts of fexofenadine hydrochloride, 3 parts of Risperidone, Aldoforwe ester
5 parts, by load weighted fexofenadine hydrochloride, component 1 is prepared in Risperidone and Aldoforwe ester mixing;
Step 2 weighs following components according to mass parts: 10 parts of fexofenadine hydrochloride, 3 parts of Risperidone, will be load weighted
Fexofenadine hydrochloride and Risperidone mixing, are prepared component 2;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
Embodiment 3
One kind includes following components according to mass parts: fexofenadine hydrochloride for treating schizoid composition
360 parts, 1 part of Risperidone, 15 parts of Aldoforwe ester.
The above-mentioned preparation method for being used to treat schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 180 parts of fexofenadine hydrochloride, 0.5 part of Risperidone, A Defu
15 parts of Wei ester, by load weighted fexofenadine hydrochloride, component 1 is prepared in Risperidone and Aldoforwe ester mixing;
Step 2 weighs following components according to mass parts: 180 parts of fexofenadine hydrochloride, 0.5 part of Risperidone, will weigh
Good fexofenadine hydrochloride and Risperidone mixing, are prepared component 2;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
Embodiment 4
One kind includes following components according to mass parts: fexofenadine hydrochloride for treating schizoid composition
100 parts, 4 parts of Risperidone, 8 parts of Aldoforwe ester.
The above-mentioned preparation method for being used to treat schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 50 parts of fexofenadine hydrochloride, 2 parts of Risperidone, Aldoforwe ester
8 parts, by load weighted fexofenadine hydrochloride, component 1 is prepared in Risperidone and Aldoforwe ester mixing;
Step 2 weighs following components according to mass parts: 50 parts of fexofenadine hydrochloride, 2 parts of Risperidone, will be load weighted
Fexofenadine hydrochloride and Risperidone mixing, are prepared component 2;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
Embodiment 5
One kind includes following components according to mass parts: fexofenadine hydrochloride for treating schizoid composition
240 parts, 1 part of Risperidone, 12 parts of Aldoforwe ester.
The above-mentioned preparation method for being used to treat schizoid composition, comprising the following steps:
Step 1, according to mass parts weigh following components: 120 parts of fexofenadine hydrochloride, 0.5 part of Risperidone, A Defu
12 parts of Wei ester, by load weighted fexofenadine hydrochloride, component 1 is prepared in Risperidone and Aldoforwe ester mixing;
Step 2 weighs following components according to mass parts: 120 parts of fexofenadine hydrochloride, 0.5 part of Risperidone, will weigh
Good fexofenadine hydrochloride and Risperidone mixing, are prepared component 2;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
It is illustrated below with reference to specific experimental data:
One, clinical observation:
1 object and method
1.1 object cases select patient 120, inclusion criteria meet II-R of Chinese Spirit Disease Diagnosis Standard CCMD- about
Schizoid diagnostic criteria, total score > 35 point BPRS;Serious physical disease is not merged simultaneously, blood routine, liver function, ECG are just
Often.Enter group case 120, patient age 25~47 years old, average age (33.4 ± 12.4) year;Course of disease average course of disease (10 ±
1.4) year, average (8.3 ± 9.5) year.Enter treatment group, control group at random, treatment group's totally 5 groups (respectively corresponding embodiment 1-5),
Every group 20, control group 20.BPRS total score compares before two groups of ages, the course of disease, treatments examines difference to anticipate without statistics through t
Adopted P > 0.05.
1.2 method control group Risperidones are averaged daily 1mg points 2 times and take;The medicine being prepared in treatment group embodiment 1-5
Object is averaged daily 60mg points 2 times and takes (component 1 and component 2 are separately taken), takes for a long time.
2 results
2.1 curative treatment group (embodiment 1-5) obvious effective rate 95%-96%, control group obvious effective rate 30%-40%.Two groups have
Not statistically significant P > 0.05 of efficiency comparing difference.
The evaluation result of BPRS average total score before and after 2.2 two groups of Case treatments: it is shown in Table 1.
1 BPRS evaluation result of table
Group | Before treatment | After treatment |
Embodiment 1 | 47.23±3.45 | 26.17±3.56* |
Embodiment 2 | 48.56±2.31 | 26.21±2.22* |
Embodiment 3 | 47.34±4.05 | 26.84±1.67* |
Embodiment 4 | 48.06±3.32 | 27.01±2.54* |
Embodiment 5 | 47.26±4.89 | 28.01±1.22* |
Control group | 47.98±2.67 | 32.41±2.01 |
Note: experimental data is analyzed using the method for one-way analysis of variance.Compared with the control group, p < 0.05 *.
Two, adverse reaction and toxic side effect monitoring:
By detecting, the blood pressure of patient, pulse, Nausea and vomiting, the clinical symptoms of dizziness whether occur bad anti-to judge
It answers.Human normal systolic pressure is set between 90-140mmHg, between 60-90mmHg, human normal pulse is diastolic pressure
60-100 beats/min, blood pressure, the pulse of patient are measured during treatment, it is found that recorded blood pressure and pulse is all within just
In normal range, occur without departing from the phenomenon that normal interval, and the clinical symptoms of Nausea and vomiting, dizziness do not occur.This says
Bright pharmaceutical composition of the invention does not have apparent adverse reaction, and then proves that the drug makees human body that apparent poison is not secondary
With.
Claims (4)
1. one kind is for treating schizoid composition, which is characterized in that according to mass parts include following components: hydrochloric acid is non-
20 parts -360 parts of Fexofenadine, 1 part -6 parts of Risperidone, 5 parts -15 parts of Aldoforwe ester.
2. according to claim 1 for treating schizoid composition, which is characterized in that according to mass parts, packet
Include 100 parts -240 parts of fexofenadine hydrochloride, 1 part -4 parts of Risperidone, 8 parts -12 parts of Aldoforwe ester.
3. according to claim 1 for treating schizoid composition, which is characterized in that preferably, according to matter
Measure part, including 120 parts of fexofenadine hydrochloride, 2 parts of Risperidone, 10 parts of Aldoforwe ester.
4. a kind of for treating the preparation method of schizoid composition, which comprises the following steps:
Step 1, according to mass parts weigh following components: 10 parts -180 parts of fexofenadine hydrochloride, 0.5 part -3 parts of Risperidone, Ah
5 parts -15 parts of De Fuwei ester, by load weighted fexofenadine hydrochloride, component is prepared in Risperidone and Aldoforwe ester mixing
1;
Step 2 weighs following components according to mass parts: 10 parts -180 parts of fexofenadine hydrochloride, 0.5 part -3 parts of Risperidone, will
Load weighted fexofenadine hydrochloride and Risperidone mixing, are prepared component 2;
Step 3, component 1 and component 2 are packed respectively, is prepared for treating schizoid composition.
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Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2394664A1 (en) * | 2010-05-31 | 2011-12-14 | Laboratorios Farmaceuticos Rovi, S.A. | Antipsychotic injectable depot composition |
CN105456265A (en) * | 2015-12-08 | 2016-04-06 | 韩自勤 | Application of fexofenadine hydrochloride in preparation of medicine for treating schizophrenia |
-
2019
- 2019-08-19 CN CN201910761768.3A patent/CN110420212A/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2394664A1 (en) * | 2010-05-31 | 2011-12-14 | Laboratorios Farmaceuticos Rovi, S.A. | Antipsychotic injectable depot composition |
CN105456265A (en) * | 2015-12-08 | 2016-04-06 | 韩自勤 | Application of fexofenadine hydrochloride in preparation of medicine for treating schizophrenia |
Non-Patent Citations (4)
Title |
---|
VISHAL MADAAN等: "Clinical utility of the risperidone formulations in the management of schizophrenia", 《NEUROPSYCHIATR DIS TREAT》 * |
余元勋等: "《中国分子神经病学》", 31 August 2015, 安徽科学技术出版社 * |
余建民等: "《血液和肿瘤专业实用药物学》", 31 March 2019, 江西科学技术出版社 * |
关鹏: "精神病类药物的研究进展", 《中国实用医药》 * |
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