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CN106265541A - A kind of injection olanzapine and preparation method thereof - Google Patents

A kind of injection olanzapine and preparation method thereof Download PDF

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Publication number
CN106265541A
CN106265541A CN201610792779.4A CN201610792779A CN106265541A CN 106265541 A CN106265541 A CN 106265541A CN 201610792779 A CN201610792779 A CN 201610792779A CN 106265541 A CN106265541 A CN 106265541A
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CN
China
Prior art keywords
olanzapine
injection
add
water
stirring
Prior art date
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.)
Pending
Application number
CN201610792779.4A
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Chinese (zh)
Inventor
孙明哲
方存杰
赵冬生
方从彬
孙延标
徐奎
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Anhui Runsheng Pharmaceutical Ltd By Share Ltd
Original Assignee
Anhui Runsheng Pharmaceutical Ltd By Share Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Anhui Runsheng Pharmaceutical Ltd By Share Ltd filed Critical Anhui Runsheng Pharmaceutical Ltd By Share Ltd
Priority to CN201610792779.4A priority Critical patent/CN106265541A/en
Publication of CN106265541A publication Critical patent/CN106265541A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses a kind of injection olanzapine and preparation method thereof, described injection olanzapine is made up of the raw material of following weight/mass percentage composition: olanzapine 0.8 2.0%, mannitol 0.3 0.8%, astaxanthin 0.1 0.3%, sodium alginate 0.01 0.05%, solvent 17 22%, water for injection surplus.The olanzapine lyophilized injectable powder good stability that the present invention prepares, active ingredient character does not changes, and short texture porous after lyophilizing is dissolved after adding water quickly and completely, and Clinical practice safety is high, and facilitates the patient of old man and dysphagia to use.

Description

A kind of injection olanzapine and preparation method thereof
Technical field
The present invention relates to pharmaceutical preparations technology field, be specifically related to a kind of injection olanzapine and preparation method thereof.
Background technology
Schizophrenia is psychiatric department the most modal principal characteristic mental sickness, and crowd's sickness rate is close to 1%, and it is clinical Feature is easy recurrent exerbation, due to this kind of reason, for effective prevention of recurrence, it is necessary to long term maintenance Drug therapy, otherwise can Become lifelong participation disease, serious harm patient and family, society, cause many HDs.At present, olanzapine is mental sickness treatment What field was generally acknowledged has remarkable curative effect and the most wide variety of medicine, and it is applicable to schizophrenia and other has sternly The psychotic acute stage of the heavy positive symptom and/or negative symptoms and the treatment of the phase of maintenance, it is possible to alleviate schizophrenia and phase The Secondary cases affective symptom of related disorders.
Existing Olanzapine medicine is typically oral cavity disintegration tablet, and its tablet absorbs in vivo and has to pass through disintegrate and dissolution etc. Process could arrive blood circulation through gastrointestinal tract, and sheet is the most usually because the reason such as dressing and technique causes sheet Being difficult to disintegrate, drug release is incomplete, makes medicine be unable to reach anticipated therapeutical effect.Additionally, use traditional handicraft to make Old or dysphagia patient medication is brought constant by tablet.Olanzapine medicine is relatively big for schizophrenia demand, And dosage form is single, it is impossible to meet the market demand.
Summary of the invention
For the deficiencies in the prior art, the invention provides a kind of injection olanzapine and preparation method thereof.
For realizing object above, the present invention is achieved by the following technical programs:
A kind of injection olanzapine, is made up of the raw material of following weight/mass percentage composition: olanzapine 0.8-2.0%, mannitol 0.3-0.8%, astaxanthin 0.1-0.3%, sodium alginate 0.01-0.05%, solvent 17-22%, water for injection surplus.
Preferably, it is made up of the raw material of following weight/mass percentage composition: olanzapine 1.5%, mannitol 0.6%, astaxanthin 0.2%, sodium alginate 0.03%, solvent 20%, water for injection surplus.
Preferably, the dosage form of described injection olanzapine is olanzapine lyophilized injectable powder.
Preferably, described solvent one or more compositionss in ethanol, glycerol, PEG400.
The preparation method of injection olanzapine, comprises the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to entirely Portion dissolves;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add Surplus water for injection;
5) by step 4) solution that obtains carries out fill, and use Vacuum Freezing & Drying Technology lyophilizing, obtain lyophilized powder.
Preferably, described freeze-drying time is 22-24h.
The method have the benefit that astaxanthin that the present invention adds and sodium alginate can improve the steady of olanzapine aqueous solution very well Lyophilized injectable powder good stability that is qualitative, that prepare, active ingredient character does not changes, and short texture porous after lyophilizing adds water Quickly and completely, Clinical practice safety is high, and facilitates the patient of old man and dysphagia to use in rear dissolving.
Detailed description of the invention
For making the purpose of the embodiment of the present invention, technical scheme and advantage clearer, below in conjunction with the embodiment of the present invention, Technical scheme in the embodiment of the present invention is clearly and completely described, it is clear that described embodiment is the present invention one Divide embodiment rather than whole embodiments.Based on the embodiment in the present invention, those of ordinary skill in the art are not making The every other embodiment obtained under creative work premise, broadly falls into the scope of protection of the invention.
Embodiment 1:
A kind of injection olanzapine, is made up of the raw material of following weight/mass percentage composition: olanzapine 1.5%, mannitol 0.6%, astaxanthin 0.2%, sodium alginate 0.03%, PEG400 20%, water for injection surplus.
The preparation method of injection olanzapine, comprises the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to entirely Portion dissolves;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add Surplus water for injection;
5) by step 4) solution that obtains carries out fill, uses Vacuum Freezing & Drying Technology lyophilizing, and freeze-drying time is 23h, Obtain olanzapine lyophilized injectable powder.
Embodiment 2:
A kind of injection olanzapine, is made up of the raw material of following weight/mass percentage composition: olanzapine 1%, mannitol 0.5%, Astaxanthin 0.15%, sodium alginate 0.02%, ethanol 10%, glycerol 10%, water for injection surplus.
The preparation method of injection olanzapine, comprises the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to entirely Portion dissolves;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add Surplus water for injection;
5) by step 4) solution that obtains carries out fill, uses Vacuum Freezing & Drying Technology lyophilizing, and freeze-drying time is 22h, Obtain olanzapine lyophilized injectable powder.
Embodiment 3:
A kind of injection olanzapine, is made up of the raw material of following weight/mass percentage composition: olanzapine 1.7%, mannitol 0.6%, astaxanthin 0.25%, sodium alginate 0.04%, glycerol 8%, PEG400 14%, water for injection surplus.
The preparation method of injection olanzapine, comprises the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to entirely Portion dissolves;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add Surplus water for injection;
5) by step 4) solution that obtains carries out fill, uses Vacuum Freezing & Drying Technology lyophilizing, and freeze-drying time is 24h, Obtain olanzapine lyophilized injectable powder.
Embodiment 4:
A kind of injection olanzapine, is made up of the raw material of following weight/mass percentage composition: olanzapine 0.8%, mannitol 0.8%, astaxanthin 0.1%, sodium alginate 0.05%, ethanol 7%, Polyethylene Glycol solvent 10%, water for injection surplus.
The preparation method of injection olanzapine, comprises the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to entirely Portion dissolves;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add Surplus water for injection;
5) by step 4) solution that obtains carries out fill, uses Vacuum Freezing & Drying Technology lyophilizing, and freeze-drying time is 23h, Obtain olanzapine lyophilized injectable powder.
Embodiment 5:
A kind of injection olanzapine, is made up of the raw material of following weight/mass percentage composition: olanzapine 2.0%, mannitol 0.3%, astaxanthin 0.3%, sodium alginate 0.01%, glycerol 22%, water for injection surplus.
The preparation method of injection olanzapine, comprises the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to entirely Portion dissolves;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add Surplus water for injection;
5) by step 4) solution that obtains carries out fill, uses Vacuum Freezing & Drying Technology lyophilizing, and freeze-drying time is 22h, Obtain olanzapine lyophilized injectable powder.
Above example only in order to technical scheme to be described, is not intended to limit;Although with reference to previous embodiment The present invention is described in detail, it will be understood by those within the art that: it still can be to aforementioned each enforcement Technical scheme described in example is modified, or wherein portion of techniques feature is carried out equivalent;And these amendment or Replace, do not make the essence of appropriate technical solution depart from the spirit and scope of various embodiments of the present invention technical scheme.

Claims (6)

1. an injection olanzapine, it is characterised in that be made up of the raw material of following weight/mass percentage composition: olanzapine 0.8- 2.0%, mannitol 0.3-0.8%, astaxanthin 0.1-0.3%, sodium alginate 0.01-0.05%, solvent 17-22%, injection Water surplus.
2. injection olanzapine as claimed in claim 1, it is characterised in that be made up of the raw material of following weight/mass percentage composition: Olanzapine 1.5%, mannitol 0.6%, astaxanthin 0.2%, sodium alginate 0.03%, solvent 20%, water for injection surplus.
3. injection olanzapine as claimed in claim 2, it is characterised in that the dosage form of described injection olanzapine is olanzapine Lyophilized injectable powder.
4. injection olanzapine as claimed in claim 2, it is characterised in that described solvent is selected from ethanol, glycerol, Polyethylene Glycol One or more compositionss in 400.
5. the preparation method of the injection olanzapine as described in claim 1-4 is arbitrary, it is characterised in that comprise the following steps:
1) weigh mannitol, astaxanthin in proportion, add the stirring of appropriate water for injection and extremely dissolve, obtain mixed solution;
2) adding sodium alginate in mixed solution, stirring is to dissolving;
3) continuing to add solvent in solution, add olanzapine, mend and inject water to the 70% of total amount, stirring is to the most molten Solve;
4) add activated carbon stirring, filter, in filtrate, add most water for injection, regulate solution ph, add surplus Water for injection;
5) by step 4) solution that obtains carries out fill, and use Vacuum Freezing & Drying Technology lyophilizing, obtain lyophilized powder.
6. the preparation method of injection olanzapine as claimed in claim 5, it is characterised in that described freeze-drying time is 22- 24h。
CN201610792779.4A 2016-08-31 2016-08-31 A kind of injection olanzapine and preparation method thereof Pending CN106265541A (en)

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Application Number Priority Date Filing Date Title
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Application Number Priority Date Filing Date Title
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Publication Number Publication Date
CN106265541A true CN106265541A (en) 2017-01-04

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1056693A (en) * 1990-04-25 1991-12-04 利利工业公司 drug compound
CN101106972A (en) * 2004-11-16 2008-01-16 伊兰制药国际有限公司 Injectable nanoparticulate olanzapine formulations
CN103417492A (en) * 2012-05-25 2013-12-04 上海现代药物制剂工程研究中心有限公司 Olanzapine-containing biodegradable microsphere preparation and preparation method thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1056693A (en) * 1990-04-25 1991-12-04 利利工业公司 drug compound
CN101106972A (en) * 2004-11-16 2008-01-16 伊兰制药国际有限公司 Injectable nanoparticulate olanzapine formulations
CN103417492A (en) * 2012-05-25 2013-12-04 上海现代药物制剂工程研究中心有限公司 Olanzapine-containing biodegradable microsphere preparation and preparation method thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
唐春红: "《天然防腐剂与抗氧化剂》", 31 May 2010 *
毕殿洲: "《药剂学》", 28 February 2003, 人民卫生出版社 *
罗明生、高天惠: "《药剂辅料大全》", 31 January 2006 *

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