CN105596313B - A kind of capsule preparations for treatment insomnia with reversed pharmacological function - Google Patents
A kind of capsule preparations for treatment insomnia with reversed pharmacological function Download PDFInfo
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- CN105596313B CN105596313B CN201610088269.9A CN201610088269A CN105596313B CN 105596313 B CN105596313 B CN 105596313B CN 201610088269 A CN201610088269 A CN 201610088269A CN 105596313 B CN105596313 B CN 105596313B
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- capsule
- diazepam
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- flumazenil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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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
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The invention discloses a kind of capsule preparations for treatment insomnia with reversed pharmacological function, it is to be prepared by the raw material of following parts by weight, 46 parts of diazepam, 22 27 parts of Flumazenil, 25 35 parts of caffeine, 100 150 parts of ethyl cellulose, 25 35 parts of starch, 24 parts of 18 22 parts of polyvinylpyrrolidone and magnesium stearate, specific preparation process is that diazepam and starch are added in distilled water after mixing to be granulated, after drying and magnesium stearate mixes whole grain, then by Flumazenil and caffeine respectively using ethyl cellulose as capsule material, micro-capsule is prepared using emulsion solvent diffusion method, the capsule preparations for treatment insomnia for obtaining that there is reversed pharmacological function in capsule are dispensed into after the particle mixing being made into again with diazepam.The capsule preparations of the present invention can play the role of night promotion sleep and not influence the normal work of user on daytime.
Description
Technical field
The invention belongs to treat the technical field of pharmaceuticals of insomnia, and in particular to a kind of to be used to control with reversed pharmacological function
Treat the capsule preparations of insomnia.
Background technology
Insomnia is mainly shown as difficult or early awakening of falling asleep, and is often accompanied by sleep not depth and dreaminess.Insomnia is common sleep barrier
Hinder.Caused by insomnia is frequently due to mental element and physical factors.With the continuous quickening of modern society's life rhythm, insomnia
Incidence it is higher and higher, insomnia have become restrict modern life serious factor.The current medicine for treatment insomnia
Object, be typically due to the presence of side effect still can be in the state having dizzy spells after people get up morning, inevitably
Influence the normal work on people's daytime.
Invention content
The technical problem to be solved by the present invention is to provide a kind of preferable Small side effects of curative effect and with reversed pharmacological function
For treating the capsule preparations of insomnia.
The present invention adopts the following technical scheme that solve above-mentioned technical problem, a kind of to be used to control with reversed pharmacological function
Treat the capsule preparations of insomnia, it is characterised in that it is to be prepared by the raw material of following parts by weight, 4-6 parts of diazepam, fluorine Ma Xi
22-27 parts of Buddhist nun, 25-35 parts of caffeine, 100-150 parts of ethyl cellulose, 25-35 parts of starch, 18-22 parts of polyvinylpyrrolidone
With 2-4 parts of magnesium stearate, specific preparation process be by diazepam and starch add in after mixing distilled water be granulated, after drying and
Magnesium stearate mixes whole grain, then expands Flumazenil and caffeine using emulsified solvent respectively using ethyl cellulose as capsule material
Arching pushing prepares micro-capsule, then is dispensed into after the particle mixing being made into diazepam and obtains having being used for for reversed pharmacological function in capsule
Treat the capsule preparations of insomnia.
It further limits, the capsule preparations for treatment insomnia of the present invention with reversed pharmacological function are special
Sign is that the raw material by following parts by weight is prepared, and 5 parts of diazepam, 25 parts of Flumazenil, 30 parts of caffeine, ethyl are fine
100 parts of dimension element, 30 parts of starch, 20 parts of polyvinylpyrrolidone and 3 parts of magnesium stearate, specific preparation process are by diazepam and shallow lake
Powder adds in distilled water granulation after mixing, and after drying and magnesium stearate mixes whole grain, then by Flumazenil and caffeine point
Be not made micro-capsule, then be dispensed into after the particle mixing being made into diazepam obtain having in capsule reversed pharmacological function for controlling
Treat the capsule preparations of insomnia.
Reversed pharmacological preparation is that pharmacological action antipodal two kinds or two groups of drugs are fabricated to a kind of dosage form, purpose
It is exactly that one of which or one group of drug light the pharmacological action for blocking former drug completely in the regular hour.Such as diazepam
Class drug（Benzene phenodiazine oar）Drug treat have a sleepless night when, dosage hour effect is bad, when dosage is big, to morning from when drug not yet generation
Thank and finish, the drug effect of drug still remains, will continue to it is drowsiness, it is dizzy and slow in reacting.Have in drug to diazepam class
Special efficacy solution cure, such as Flumazenil, the syngignoscism of the rapid agonist drug of energy, are quickly wakened.Caffeine is hypnotic sedative agent
The non-specific class solution cure of object can effectively alleviate the dizziness caused by downern, drowsiness and slow in reacting.
The discrete particles of quick-release are made in diazepam class drug by the present invention, and sustained release system is made in Flumazenil and caffeine
Then the capsule and pill of agent is fitted into two kinds of dosage forms in same capsule, takes simultaneously, such diazepam class drug quick acting, patient
Sleep state is rapidly entered, Flumazenil and caffeine start to discharge when being selected 4 points of the next morning to five, and 6 whens reach medicine
The peak of object concentration, patient awoke get up, and start the preparation of one day.The capsule preparations of the present invention can play night promotion
The effect of sleep, and the normal work of user can not be influenced on daytime.
Specific embodiment
The above of the present invention is described in further details by the following examples, but this should not be interpreted as to this
The range for inventing above-mentioned theme is only limitted to following embodiment, and all technologies realized based on the above of the present invention belong to this hair
Bright range.
Embodiment
1st, raw material is weighed by following proportionings（Gram）：
（1）Diazepam 5, Flumazenil 25, caffeine 30, ethyl cellulose 100, starch 30, polyvinylpyrrolidone 20
With magnesium stearate 3；
（2）Diazepam 4, Flumazenil 27, caffeine 25, ethyl cellulose 125, starch 25, polyvinylpyrrolidone 22
Part and magnesium stearate 2；
（3）Diazepam 6, Flumazenil 22, caffeine 35, ethyl cellulose 150, starch 35, polyvinylpyrrolidone 18
With magnesium stearate 4.
2nd, preparation method
Raw material is weighed according to said ratio respectively, diazepam and starch are added in distilled water after mixing is granulated, drying
Whole grain is mixed with magnesium stearate afterwards, it is molten using emulsifying then by Flumazenil and caffeine respectively using ethyl cellulose as capsule material
Agent diffusion method prepares micro-capsule, then obtain that there is reversed pharmacological function in capsule with being dispensed into after the stable particle mixing being made into
For treating the capsule preparations of insomnia.
3rd, model case
3.1 Suns, female 48 years old, suffer from nervous functional disorder for many years.Hospital time takes tranquilizing the mind sedative and imitates less.Before 20 days,
It lies awake all night, dizziness and tinnitus, hectic fever, night sweat is dysphoria in chestpalms-soles, soreness and weakness of waist and knees, it is difficult to fall asleep.Take capsule preparations 15 of the present invention
My god, sleep has clear improvement, and continues to take 30 days, and sleep restores normal, and gets up not occurring dizziness early in the morning and feel sleepy phenomenon.
3.2 Mr. Wang, males 42 years old, lie awake all night for many years, are in a trance, upset, and take capsule preparations 15 of the present invention
My god, sleep has clear improvement, and continues to take 30 days, and sleep restores normal, and gets up not occurring dizziness early in the morning and feel sleepy phenomenon.
3.3 Zhangs, man, 55 years old, night can not fall asleep, and usually be waken up with a start even if falling asleep, and wake up in the morning, malaise, dizzy
It is dizzy.Take capsule preparations of the present invention 15 days, sleep has clear improvement, and continues to take 30 days, and sleep restores normal, and early in the morning
Get up not to occur dizziness to feel sleepy phenomenon.
Basic principle, main features and advantages embodiment above describes the present invention, the technical staff of the industry should
Understand, the present invention is not limited to the above embodiments, and the above embodiments and description only describe the originals of the present invention
Reason, under the range for not departing from the principle of the invention, various changes and improvements may be made to the invention, these changes and improvements are each fallen within
In the scope of protection of the invention.
Claims (2)
1. a kind of capsule preparations for treatment insomnia with reversed pharmacological function, it is characterised in that be by following parts by weight
What raw material was prepared, 4-6 parts of diazepam, 22-27 parts of Flumazenil, 25-35 parts of caffeine, 100-150 parts of ethyl cellulose,
2-4 parts of 25-35 parts of starch, 18-22 parts of polyvinylpyrrolidone and magnesium stearate, specific preparation process are by diazepam and starch
It adds in distilled water after mixing to be granulated, after drying and magnesium stearate mixes whole grain, then distinguishes Flumazenil and caffeine
Using ethyl cellulose as capsule material, micro-capsule is prepared using emulsion solvent diffusion method, then is dispensed after the particle mixing being made into diazepam
The capsule preparations for treatment insomnia with reversed pharmacological function are obtained in capsule.
2. the capsule preparations for treatment insomnia according to claim 1 with reversed pharmacological function, it is characterised in that
It is to be prepared by the raw material of following parts by weight, 5 parts of diazepam, 25 parts of Flumazenil, 30 parts of caffeine, ethyl cellulose
3 parts of 100 parts, 30 parts of starch, 20 parts of polyvinylpyrrolidone and magnesium stearate, specific preparation process is to mix diazepam and starch
Close uniformly after add in distilled water be granulated, after drying and magnesium stearate mix whole grain, then by Flumazenil and caffeine respectively with
Ethyl cellulose is capsule material, and micro-capsule is prepared using emulsion solvent diffusion method, then is dispensed into after the particle mixing being made into diazepam
The capsule preparations for treatment insomnia with reversed pharmacological function are obtained in capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610088269.9A CN105596313B (en) | 2016-02-17 | 2016-02-17 | A kind of capsule preparations for treatment insomnia with reversed pharmacological function |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610088269.9A CN105596313B (en) | 2016-02-17 | 2016-02-17 | A kind of capsule preparations for treatment insomnia with reversed pharmacological function |
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| Publication Number | Publication Date |
|---|---|
| CN105596313A CN105596313A (en) | 2016-05-25 |
| CN105596313B true CN105596313B (en) | 2018-06-29 |
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| Application Number | Title | Priority Date | Filing Date |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101267819A (en) * | 2005-08-19 | 2008-09-17 | 赛诺菲-安万特 | Combination of a long-acting hypnotic agent and a short-acting hypnotic agent and therapeutic use thereof |
| CN103502224A (en) * | 2011-02-23 | 2014-01-08 | 克鲁莱斯有限公司 | Flumazenil complexes, compositions comprising same and uses thereof |
| CN104586793A (en) * | 2014-12-25 | 2015-05-06 | 海南卫康制药(潜山)有限公司 | Diazepam composition freeze-dried tablet and preparation method thereof |
| CN104840465A (en) * | 2015-04-27 | 2015-08-19 | 海口通用康力制药有限公司 | Flumazenil injection and preparation method thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7387793B2 (en) * | 2003-11-14 | 2008-06-17 | Eurand, Inc. | Modified release dosage forms of skeletal muscle relaxants |
-
2016
- 2016-02-17 CN CN201610088269.9A patent/CN105596313B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101267819A (en) * | 2005-08-19 | 2008-09-17 | 赛诺菲-安万特 | Combination of a long-acting hypnotic agent and a short-acting hypnotic agent and therapeutic use thereof |
| CN103502224A (en) * | 2011-02-23 | 2014-01-08 | 克鲁莱斯有限公司 | Flumazenil complexes, compositions comprising same and uses thereof |
| CN104586793A (en) * | 2014-12-25 | 2015-05-06 | 海南卫康制药(潜山)有限公司 | Diazepam composition freeze-dried tablet and preparation method thereof |
| CN104840465A (en) * | 2015-04-27 | 2015-08-19 | 海口通用康力制药有限公司 | Flumazenil injection and preparation method thereof |
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| CN105596313A (en) | 2016-05-25 |
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| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: Dong Tingfang Inventor after: Pei Sujuan Inventor after: Chi Yuling Inventor after: Zhang Weiguo Inventor after: Qin Xiaofei Inventor after: Zhang Yongxiang Inventor after: Wang Yemin Inventor before: Dong Tingfang Inventor before: Chi Yuling Inventor before: Pei Sujuan Inventor before: Hui Hongyan Inventor before: Deng Zhijian Inventor before: Zhang Yongfan |
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