SU1218919A3 - Method of producing cephalexin of prolonged action for peroral application - Google Patents

Method of producing cephalexin of prolonged action for peroral application Download PDF

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Publication number
SU1218919A3
SU1218919A3 SU772485596A SU2485596A SU1218919A3 SU 1218919 A3 SU1218919 A3 SU 1218919A3 SU 772485596 A SU772485596 A SU 772485596A SU 2485596 A SU2485596 A SU 2485596A SU 1218919 A3 SU1218919 A3 SU 1218919A3
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SU
USSR - Soviet Union
Prior art keywords
cefalexin
coated
preparation
normal
cephalexin
Prior art date
Application number
SU772485596A
Other languages
Russian (ru)
Inventor
Маекава Хидеюки
Такагиси Ясуси
Като Хироси
Original Assignee
Сионоги Энд Ко,Лтд (Фирма)
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Publication of SU1218919A3 publication Critical patent/SU1218919A3/en

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Classifications

    • 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
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • 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
    • A61K31/54—Heterocyclic 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
    • A61K31/542—Heterocyclic 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
    • A61K31/545—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

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

Abstract

LONG ACTING PREPARATION OF CEFALEXIN FOR EFFECTIVE TREATMENTS OF BACTERIAL INFECTION SENSITIVE TO CEFALEXIN A cefalexin preparation coated with a coating layer the solubility of which layer is pH-dependent and dissolves at upper intestine is preferably administered concurrently with a normal (plain, quick-releasing) cefalexin preparation. The coated preparation is preferably coated, in the particle form and when administered orally, exists in the particle form at stomach. Preferably, the coating layer is made from coating base material having dissolution pH of from 5.5 to 6.5, and the ratio in potency of the coated cefalexin to the normal cefalexin is between 15 : 85 and 60 : 40. The coated cefalexin and the normal cefalexin can be composed to a pharmaceutical preparation preferably in a unit-dosage form, e.g. capsules, tablets or particles or in strip-packages.

Description

1one

Изобретение относитс  к медицине а именно к фармацевтической промьйп- ленности и касаетс  способа получени  препарата, примен емого в качестве лекарственного средства. The invention relates to medicine, namely to the pharmaceutical industry, and relates to a method for producing a preparation used as a medicine.

Цель изобретени  - увеличение продолжительности действи .The purpose of the invention is to increase the duration of action.

Пример. Смесь цефалексина 11117 г, лактозы (270 г) и куку- рузного крахмала (97 г) тщательно разминают с 8%-ной пастой крахмала (500 г) и смесь подвергают гранулированию в цилиндрическом гранул то- ре с последующей сушкой в течение 1 ч при 60°С.Example. A mixture of cephalexin 11117 g, lactose (270 g) and maize starch (97 g) is thoroughly kneaded with 8% starch paste (500 g) and the mixture is granulated in a cylindrical granulator followed by drying for 1 h at 60 ° C.

Высушенные гранулы дроб т в мельнице и просеивают дл  получени  однородных гранул размером 16-24 мешThe dried granules are crushed in a mill and sieved to obtain uniform granules of 16-24 mesh

Гранулы обычного цефалексина (1000 г) помещают в противень дл  нанесени  оболочки (диаметром 40 см и оболочку нанос т путем опрыскивани  спиртовым раствором, содержащим 52 г сополимера метилметакрилата иPellets of conventional cephalexin (1000 g) are placed in a pan for applying a casing (40 cm in diameter and the casing is applied by spraying with an alcohol solution containing 52 g of methyl methacrylate copolymer and

Редактор Н, КиштулинецEditor H, Kistoulinets

Заказ 1141/63Тираж 659 ПодписноеOrder 1141/63 Circulation 659 Subscription

ВНИШ1И Государственного комитета СССРVNISH1I USSR State Committee

по делам изобретений и открытий 113035, Москва, Ж-35, Раушска  наб. , д. 4/5for inventions and discoveries 113035, Moscow, Zh-35, Raushsk nab. D. 4/5

Филиал ППП Патент, г. Ужгород, ул. Проектна , 4Branch PPP Patent, Uzhgorod, st. Project, 4

метакриловой кислоты Эвдрагита при рН 5,5-6,5 (при соотношении мономеров 30:70), 52 г талька р 1000 г этанола, общий вес 3500 г дл  получени  однородного покрыти  гранул. Распыление может быть осуществлено при комнатной температуре, давление распыл емого воздуха 2 кг/см , диаметр используемого сопла 1,2 мм, скорость 5 г/с, распьшение в течение 20 b и высушивание гор чим воздухом при 70 С при скорости 8 м /мин в течение 25 с, осуществл етс  повторно .Eudragit methacrylic acid at pH 5.5-6.5 (with a monomer ratio of 30:70), 52 g of talcum p 1000 g of ethanol, the total weight of 3500 g to obtain a uniform coating of the granules. Spraying can be carried out at room temperature, the pressure of the sprayed air is 2 kg / cm, the diameter of the nozzle used is 1.2 mm, the speed is 5 g / s, dispersion for 20 b and drying with hot air at 70 C at a speed of 8 m / min. within 25 seconds, is repeated.

Проведенные эксперименты по инги- бированию роста бактерий подтвердили Наличие этого действи  у препарата , получаемого предлагаемым способом .Experiments on the inhibition of bacterial growth confirmed the presence of this effect in the preparation obtained by the proposed method.

Цефалексин продленного действи  может быть дан больному с заболеванием , вызванным бактериальной инфекцией , через интервалы времени в 12 ч.A prolonged cephalexin can be given to a patient with a disease caused by a bacterial infection at intervals of 12 h.

Составитель В, Брусшювска  Техред Т.Тулик, Корректор И. ЭрдейиCompiled by B, Brusyuwska Tehred T. Tulik, Proofreader I. Erdeyi

Claims (1)

СПОСОБ ПОЛУЧЕНИЯ ЦЕФАЛЕКСИ-; НА ПРОДЛЕННОГО ДЕЙСТВИЯ ДЛЯ ΠΕΡρРАЛЬНОГО ПРИМЕНЕНИЯ, включающий нанесение на активное вещество оболочки, отличающийся тем, что, с целью увеличения продолжительности действия, цефалексин в форме гранул покрывают оболочкой из сополимера метилметакрилата и метакриловой кислоты, растворимого при pH 5,5-6,5 и имеющего кислотное число 200-400, преимущественно 300330, при соотношении мономеров (3070):(70-30), затем смешивают с неимеющим покрытия цефалексином при их соотношении (85-15) : (40-60), преимущественно 70:30, после чего смесь таблетируют в присутствии связующего средства.METHOD FOR PRODUCING CEPHALEXI-; FOR LONG-TERM ACTION FOR INDUSTRIAL USE, including applying a coating to the active substance, characterized in that, in order to increase the duration of action, cephalexin in the form of granules is coated with a copolymer of methyl methacrylate and methacrylic acid, soluble at pH 5.5-6.5 and having the acid number is 200-400, mainly 300330, with a ratio of monomers (3070) :( 70-30), then mixed with uncoated cephalexin at a ratio of (85-15): (40-60), mainly 70:30, after which the mixture is tableted in the presence of a binder his means. ьоb QOQO СО соSO with
SU772485596A 1976-05-13 1977-05-12 Method of producing cephalexin of prolonged action for peroral application SU1218919A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP5492576A JPS52139713A (en) 1976-05-13 1976-05-13 Sustained release cefalexin preparations

Publications (1)

Publication Number Publication Date
SU1218919A3 true SU1218919A3 (en) 1986-03-15

Family

ID=12984185

Family Applications (1)

Application Number Title Priority Date Filing Date
SU772485596A SU1218919A3 (en) 1976-05-13 1977-05-12 Method of producing cephalexin of prolonged action for peroral application

Country Status (27)

Country Link
JP (1) JPS52139713A (en)
AR (1) AR224494A1 (en)
AT (1) AT351159B (en)
AU (1) AU508793B2 (en)
BE (1) BE854640A (en)
CA (1) CA1085296A (en)
CS (1) CS208196B2 (en)
DD (1) DD132232A5 (en)
DE (1) DE2721785A1 (en)
DK (1) DK208077A (en)
ES (1) ES458710A1 (en)
FI (1) FI771491A (en)
FR (1) FR2350836A1 (en)
GB (1) GB1543543A (en)
GR (1) GR68895B (en)
HU (1) HU184196B (en)
IE (1) IE45415B1 (en)
IL (1) IL52075A (en)
MX (1) MX5976E (en)
NL (1) NL7704879A (en)
NZ (1) NZ183927A (en)
PL (1) PL111183B1 (en)
PT (1) PT66514B (en)
RO (1) RO72935A (en)
SE (1) SE426780B (en)
SU (1) SU1218919A3 (en)
ZA (1) ZA772757B (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5545601A (en) * 1978-09-26 1980-03-31 Toyo Jozo Co Ltd Long-acting cephalexin and its preparation
FR2453639A1 (en) * 1979-04-09 1980-11-07 Sanofi Sa NAFTIDROFURYL-BASED IMMEDIATE-DELAYED RELEASE DRUG COMPOSITION
JPS5659707A (en) * 1979-10-19 1981-05-23 Toyo Jozo Co Ltd Lasting antibiotic pharmaceutical and its preparation
JPS5826816A (en) * 1981-08-11 1983-02-17 Teisan Seiyaku Kk Compounded granule having prolonged effect consisting of spherical granule
JPS5846019A (en) * 1981-09-14 1983-03-17 Kanebo Ltd Nifedipine preparation with prolonged action
JPS5883613A (en) * 1981-11-10 1983-05-19 Toa Eiyou Kagaku Kogyo Kk Isosorbitol nitrate pharmaceutical
JPS5883106U (en) * 1981-11-30 1983-06-06 松下電工株式会社 Oil dump pot in electromagnetic equipment
US4525339A (en) * 1982-10-15 1985-06-25 Hoffmann-La Roche Inc. Enteric coated oral dosage form
JPS601128A (en) * 1983-06-15 1985-01-07 Shionogi & Co Ltd Long-acting cefaclor preparation
JPS6144811A (en) * 1984-08-10 1986-03-04 Ss Pharmaceut Co Ltd Sustained release diclofenac sodium pharmaceutical
FR2577800B1 (en) * 1985-02-22 1990-09-07 Grimberg Georges GASTRO-RESISTANT GALENIC MEDICINE
JPS62226926A (en) * 1986-03-27 1987-10-05 Teisan Seiyaku Kk Long acting complex granule
US20080069870A1 (en) * 2005-04-12 2008-03-20 Elan Corporation Pic Controlled Release Compositions Comprising a Cephalosporin for the Treatment of a Bacterial Infection
CN114617855A (en) * 2020-12-14 2022-06-14 江苏贝佳制药有限公司 Preparation method of cefalexin capsule

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
За вка DE № 2325410, кл. 12 С 3/00, .1974. *

Also Published As

Publication number Publication date
DD132232A5 (en) 1978-09-13
MX5976E (en) 1984-09-12
ATA341877A (en) 1978-12-15
PL198058A1 (en) 1979-03-26
GR68895B (en) 1982-03-15
PT66514A (en) 1977-06-01
ZA772757B (en) 1978-04-26
PL111183B1 (en) 1980-08-30
CS208196B2 (en) 1981-08-31
SE426780B (en) 1983-02-14
IL52075A0 (en) 1977-07-31
SE7705502L (en) 1977-11-14
DK208077A (en) 1977-11-14
DE2721785C2 (en) 1989-03-16
GB1543543A (en) 1979-04-04
PT66514B (en) 1978-10-16
CA1085296A (en) 1980-09-09
IL52075A (en) 1980-06-30
NL7704879A (en) 1977-11-15
JPS52139713A (en) 1977-11-21
FR2350836B1 (en) 1981-02-06
HU184196B (en) 1984-07-30
FI771491A (en) 1977-11-14
NZ183927A (en) 1980-02-21
BE854640A (en) 1977-09-01
DE2721785A1 (en) 1977-11-24
IE45415B1 (en) 1982-08-25
AU2507877A (en) 1978-11-16
FR2350836A1 (en) 1977-12-09
IE45415L (en) 1977-11-13
RO72935A (en) 1982-07-06
JPS5547611B2 (en) 1980-12-01
AR224494A1 (en) 1981-12-15
AU508793B2 (en) 1980-04-03
ES458710A1 (en) 1978-03-01
AT351159B (en) 1979-07-10

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