CN114886859A - Cefprozil granules - Google Patents

Cefprozil granules Download PDF

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Publication number
CN114886859A
CN114886859A CN202210643138.8A CN202210643138A CN114886859A CN 114886859 A CN114886859 A CN 114886859A CN 202210643138 A CN202210643138 A CN 202210643138A CN 114886859 A CN114886859 A CN 114886859A
Authority
CN
China
Prior art keywords
cefprozil
pharmaceutically acceptable
agent
granules
adhesive
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
CN202210643138.8A
Other languages
Chinese (zh)
Inventor
刘丹丹
臧红波
于哲
赵文利
孙玉环
唐珊珊
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.)
HARBIN CITY KAICHENG PHARMACEU
Original Assignee
HARBIN CITY KAICHENG PHARMACEU
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 HARBIN CITY KAICHENG PHARMACEU filed Critical HARBIN CITY KAICHENG PHARMACEU
Priority to CN202210643138.8A priority Critical patent/CN114886859A/en
Publication of CN114886859A publication Critical patent/CN114886859A/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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Medicinal Preparation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention relates to the technical field of pharmaceutical preparations and discloses cefprozil granules which comprise cefprozil, pharmaceutically acceptable pharmaceutic adjuvants and pharmaceutically acceptable carriers, wherein the pharmaceutically acceptable pharmaceutic adjuvants comprise phospholipid, mannitol and polysorbate, the pharmaceutically acceptable carriers comprise auxiliary materials comprising a disintegrating agent, an adhesive, a flavoring agent, an aromatic and a coloring agent, the disintegrating agent is one or more of carboxymethyl starch sodium, croscarmellose sodium or low-substituted hydroxypropyl cellulose, and the coloring agent is any one of phytochrome and mineral pigment. The cefprozil granules increase the solubility of the cefprozil active ingredients, improve the stability, effectively reduce the toxic and side effects of the medicament, effectively cover the bad taste of the medicament by adding the flavoring agent and the adhesive, and reduce the aversion of patients to the medicament, thereby improving the compliance of the patients, particularly children patients, in medication.

Description

Cefprozil granules
Technical Field
The invention relates to the technical field of pharmaceutical preparations, in particular to cefprozil granules.
Background
Cefprozil belongs to the second generation cephalosporin antibiotics, can be used for treating bronchitis or other bacterial infections, in vitro tests prove that cefprozil has obvious effects on staphylococcus aureus, streptococcus pneumoniae and streptococcus pyogenes in gram-positive aerobic bacteria, and also has certain antibacterial activity on enterococcus durans, listeria monocytogenes, staphylococcus epidermidis, staphylococcus saprophyticus and staphylococcus warnerei.
Chinese patent CN108743548A discloses a cefprozil granule and a preparation method thereof, the cefprozil granule prepared by adopting the prescription and the process has good dissolution rate, high stability and uniform particle size, and the dissolution rate of active ingredients in the cefprozil granule is effectively improved by adding diethyl palmitoyl aspartate, but the cefprozil granule has the following defects of insolubility in water, bitter taste and large use limitation, so the cefprozil granule is provided to solve the problems.
Disclosure of Invention
Technical problem to be solved
Aiming at the defects of the prior art, the invention provides cefprozil granules which have the advantages of good comprehensive performance and the like, and solves the problems of insolubility in water, bitter taste and large use limitation.
(II) technical scheme
In order to achieve the purpose of good comprehensive performance, the invention provides the following technical scheme: the cefprozil granules are composed of cefprozil, pharmaceutically acceptable pharmaceutic adjuvants and pharmaceutically acceptable carriers, the pharmaceutically acceptable pharmaceutic adjuvants are composed of phospholipid, mannitol and polysorbate, and the pharmaceutically acceptable carriers are composed of auxiliary materials including a disintegrating agent, an adhesive, a flavoring agent, an aromatic and a coloring agent.
Preferably, the mass ratio of the cefprozil, the phospholipid, the mannitol and the polysorbate is as follows: 100: 125-150:100-120: 110-130.
Preferably, the mass ratio of the cefprozil, the disintegrating agent, the adhesive, the flavoring agent and the coloring agent is 100: 7-18:3-8: 25-40: 8-15.
Preferably, the disintegrant is one or more of carboxymethyl starch sodium, croscarmellose sodium or low substituted hydroxypropyl cellulose.
Preferably, the binder is one or more of xanthan gum, arabic gum, hydroxypropyl methylcellulose or povidone.
Preferably, the flavoring agent is one or more of glucose, sodium cyclamate and citric acid.
Preferably, the colorant is any one of a plant pigment and a mineral pigment.
(III) advantageous effects
Compared with the prior art, the invention provides cefprozil granules which have the following beneficial effects:
the cefprozil granules have the advantages that the solubility of the cefprozil active ingredients is improved, the stability is improved, the toxic and side effects of the medicine can be effectively reduced, the flavoring agent and the adhesive are added to effectively cover the bad taste of the medicine, and the coloring agent can reduce the aversion of patients to medicine taking, so that the compliance of the patients, particularly children patients, in medicine taking is improved.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
The first embodiment is as follows:
a cefprozil granule comprises cefprozil, pharmaceutically acceptable pharmaceutic adjuvants and pharmaceutically acceptable carriers;
the pharmaceutically acceptable pharmaceutic adjuvants comprise phospholipids, mannitol and polysorbate, wherein the mass ratio of the cefprozil to the phospholipids to the mannitol to the polysorbate is 100: 125:100: 110;
the pharmaceutically acceptable carrier consists of auxiliary materials including a disintegrating agent, an adhesive, a flavoring agent, an aromatic and a coloring agent, wherein the mass ratio of the cefprozil to the disintegrating agent to the adhesive to the flavoring agent to the coloring agent is 100: 7:3: 25: 8, the disintegrating agent is carboxymethyl starch sodium, the adhesive is xanthan gum, the flavoring agent is glucose, and the coloring agent is phytochrome.
Example two:
a cefprozil granule comprises cefprozil, pharmaceutically acceptable pharmaceutic adjuvants and pharmaceutically acceptable carriers;
the pharmaceutically acceptable pharmaceutic adjuvants comprise phospholipids, mannitol and polysorbate, wherein the mass ratio of the cefprozil to the phospholipids to the mannitol to the polysorbate is 100: 135:110: 120 of a solvent;
the pharmaceutically acceptable carrier consists of auxiliary materials including a disintegrating agent, an adhesive, a flavoring agent, an aromatic and a coloring agent, wherein the mass ratio of the cefprozil to the disintegrating agent to the adhesive to the flavoring agent to the coloring agent is 100: 13:6: 35: 12, the disintegrating agent is croscarmellose sodium, the adhesive is acacia, the flavoring agent is sodium cyclamate, and the coloring agent is phytochrome.
Example three:
a cefprozil granule comprises cefprozil, pharmaceutically acceptable pharmaceutic adjuvants and pharmaceutically acceptable carriers;
the pharmaceutically acceptable pharmaceutic adjuvants comprise phospholipid, mannitol and polysorbate, wherein the mass ratio of the cefprozil to the phospholipid to the mannitol to the polysorbate is as follows: 100: 150:120: 130;
the pharmaceutically acceptable carrier consists of auxiliary materials including a disintegrating agent, an adhesive, a flavoring agent, an aromatic and a coloring agent, wherein the mass ratio of the cefprozil to the disintegrating agent to the adhesive to the flavoring agent to the coloring agent is 100: 18:8: 40: 15, disintegrating agent is low substituted hydroxypropyl cellulose, adhesive is polyvidone, taste correcting agent is citric acid, and coloring agent is mineral pigment.
The invention has the beneficial effects that: the dissolution performance of the cephalosporin active ingredients is increased, the stability is improved, the toxic and side effects of the medicament can be effectively reduced, the bad taste of the medicament can be effectively covered by adding the flavoring agent and the adhesive, and the aversion to the medicament taking of a patient can be reduced by adding the coloring agent, so that the medicament compliance of the patient, particularly a child patient, is improved.
Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that changes, modifications, substitutions and alterations can be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.

Claims (7)

1. The cefprozil granules are characterized in that: the granules comprise cefprozil, pharmaceutically acceptable pharmaceutic adjuvants and pharmaceutically acceptable carriers, wherein the pharmaceutically acceptable pharmaceutic adjuvants comprise phospholipid, mannitol and polysorbate, and the pharmaceutically acceptable carriers comprise adjuvants comprising a disintegrating agent, an adhesive, a flavoring agent, an aromatic and a coloring agent.
2. The cefprozil granule as claimed in claim 1, wherein the mass ratio of cefprozil, phospholipid, mannitol and polysorbate is 100: 125-150:100-120: 110-130.
3. The cefprozil granule formulation according to claim 1, wherein the mass ratio of cefprozil, disintegrant, binder, flavoring agent and coloring agent is 100: 7-18:3-8: 25-40: 8-15.
4. The cefprozil granule formulation according to claim 1, wherein the disintegrant is one or more of carboxymethyl starch sodium, croscarmellose sodium or low substituted hydroxypropylcellulose.
5. The cefprozil granule formulation according to claim 1, wherein the binder is one or more of xanthan gum, arabic gum, hydroxypropyl methylcellulose or povidone.
6. The cefprozil granule formulation according to claim 1, wherein the flavoring agent is one or more of glucose, sodium cyclamate and citric acid.
7. The cefprozil granule formulation according to claim 1, wherein the colorant is any one of phytochrome and mineral pigment.
CN202210643138.8A 2022-06-09 2022-06-09 Cefprozil granules Pending CN114886859A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202210643138.8A CN114886859A (en) 2022-06-09 2022-06-09 Cefprozil granules

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN202210643138.8A CN114886859A (en) 2022-06-09 2022-06-09 Cefprozil granules

Publications (1)

Publication Number Publication Date
CN114886859A true CN114886859A (en) 2022-08-12

Family

ID=82728642

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202210643138.8A Pending CN114886859A (en) 2022-06-09 2022-06-09 Cefprozil granules

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101953790A (en) * 2010-06-17 2011-01-26 王丽燕 Granules comprising cefprozil lipidosome and preparation method thereof
CN101966154A (en) * 2010-07-05 2011-02-09 王丽燕 Granular formulation containing cefixime liposomes and preparation method thereof
WO2011093828A2 (en) * 2010-01-29 2011-08-04 Mahmut Bilgic Solid dosage forms comprising cefprozil
CN108743548A (en) * 2018-06-28 2018-11-06 苏州中联化学制药有限公司 A kind of Cefprozil granule and preparation method thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011093828A2 (en) * 2010-01-29 2011-08-04 Mahmut Bilgic Solid dosage forms comprising cefprozil
CN101953790A (en) * 2010-06-17 2011-01-26 王丽燕 Granules comprising cefprozil lipidosome and preparation method thereof
CN101966154A (en) * 2010-07-05 2011-02-09 王丽燕 Granular formulation containing cefixime liposomes and preparation method thereof
CN108743548A (en) * 2018-06-28 2018-11-06 苏州中联化学制药有限公司 A kind of Cefprozil granule and preparation method thereof

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Application publication date: 20220812