Indian Patents. 269019:A PHARMACEUTICAL COMPOSITION FOR TREATMENT OF RESPIRATORY TRACT INFECTIONS

Title of Invention	A PHARMACEUTICAL COMPOSITION FOR TREATMENT OF RESPIRATORY TRACT INFECTIONS
Abstract	The present invention relates to a pharmaceutical composition comprising ciprofloxacin or salts of thereof and amoxycillin or salts of thereof and other pharmaceutical excipients. The present invention provides more reliable effect against all bacteria responsible for especially respiratory tract infections. The invention makes up for the weakness of ciprofloxacin against streptococci

Full Text	FORM 2 THE PATENT ACT 1970 (39 of 1970) & The Patents Rules, 2003 PROVISIONAL SPECIFICATION (See section 10 and rule 13) 1. TITLE OF THE INVENTION A PHARMACEUTICAL COMPOSITION FOR TREATMENT OF RESPIRATORY TRACT INFECTIONS 2. APPLICANT (S) (a) NAME : Biochem Pharmaceutical Private Limited (b) NATIONALITY: an Indian Company (c) ADDRESS : Aidun Building, John Crasto Lane, Near Metro Theatre, Mumbai – 400 002 India. 3. PREMABLE TO THE DESCRIPTION ? PROVISIONAL The following specification describes the invention. COMPLETE The following specification particularly describes the invention and the manner in which it is to be performed. The present invention relates to a pharmaceutical composition for the treatment of respiratory tract infections. This composition comprises ciprofloxacin or salts of thereof and amoxicillin or salts of thereof. Ciprofloxacin has reliable effectiveness against all bacteria responsible especially for upper respiratory tract infections (URTI) and lower respiratory tract infections (LRTI) - except against streptococci species, which is one of the commonest pathogen for respiratory tract infections (RTIs). In view of amoxycillin’s continual reliability for streptococci, the combination of these two antimicrobials offers an effective option as preferred first line for empiric therapy of RTIs. Background of the Invention: Ciprofloxacin is a synthetic antibiotic, belonging to a group called fluoroquinolones. As far as streptococci are concerned, in recent years, these are inherently less susceptible to especially older fluoroquinolones. {Kaneko A et al. J Antimicrob Chemother 2000; 45: 771-775, Kaneko A et al. Chemotherapy (Tokyo) 1994; 42: 94-100. Coyle EA et al. Antimicrob Ag Chemother 2001; 45: 6: 1654-1659.} A major mechanism of resistance to fluoroquinolones in Gram-positive bacteria such as Streptococcus pneumoniae is target modification; mutations in the quinolone resistance determining region (QRDR) of the gyrA, parC and parE genes, resulting in decreased affinity for the quinolones. {Kaneko A et al. J Antimicrob Chemother 2000; 45: 771-775 Margerrison EE et al. J of Bacteriology 1992; 174: 1596-1603. Ferrero L et al. Antimicrob Ag Chemother 1995; 39: 1554-1558. Jorgensen JH et al. Antimicrob Ag Chemother 1999; 43: 329-334.} Besides being less susceptible, resistance of Streptococcus pneumoniae to ciprofloxacin is the most amongst quinolones, {Alou L et al. Antimicrob Ag Chemother 2001; 45: 10: 2955-2957.} and as many as 15% of these bacteria are possibly resistant to it. {Deshpande LM et al. Diagn Microbiol Infect Dis 2006; 54: 3: 157-164} In India, the resistance of streptococci to fluoroquinolones is more likely to be prevalent since ciprofloxacin and other similar agents are more used for children. This is because the reservoir for streptococci is children. (http://www.annals.org/cgi/content/full/129/11_Part_1/908. As read on 15th Nov 2008. ) Amoxycillin or amoxicillin is a moderate-spectrum, bactericidal, ß-lactam antibiotic used to treat bacterial infections caused by susceptible microorganisms. Amoxycillin is advocated as preferred agent for URTI. {Korner JR et al. BMJ 1994; 308: 191-192.} With the ever-changing pattern of bacterial resistance, use of conventional doses amoxycillin in LRTI to eradicate H influenzae is disastrous. {Spiteri M. BMJ 1994; 308: 657-658. Powell M et al. J Antimicrob Chemother 1991; 28: 249-259.} In fact, amoxycillin is even lesser effective than ampicillin against H influenzae. {The Use of Antibiotics. Kucers A et al (Eds) 5th Ed 1997; Butterworth / Heinemann pp 134-144.Kosmidis J et al. Brit J Clin Pract 1972; 26: 341.} Objects of the Present Invention: The main object of the present invention is to provide a pharmaceutical composition of ciprofloxacin and amoxycillin or salts of thereof that provides a more reliable effect against all bacteria responsible for especially RTIs. Further object of the invention is to give tolerated dosage of these two antibiotics. Another object of the invention is to makes up for the weakness of ciprofloxacin against streptococci. Yet an object of the invention is to provide a composition that shows synergistic effect with no evidence of antagonism. It is yet another object of the present invention to provide a simple process for preparing oral solid dosage forms comprising pharmaceutically effective amounts of ciprofloxacin and amoxycillin or salts of thereof. Summary of the Invention: The present invention relates to a pharmaceutical composition comprising ciprofloxacin and amoxycillin. In the invention ciprofloxacin or salts of thereof and amoxycillin or salts of thereof are used. Ciprofloxacin or salts of thereof is used in 100 to 750 mg/tablet and amoxycillin or salts of thereof are used in 200 to 1000 mg/tablet. Detail Description: Ciprofloxacin is indicated for treatment of acute uncomplicated cystitis in females, urinary tract infections (UTI), chronic bacterial prostatitis, LRTI, acute sinusitis, skin and skin structure infections (SSTI), bone and joint infections, complicated intra-abdominal infections, infectious diarrhea, enteric fever, uncomplicated cervical and urethral gonorrhea due to susceptible pathogens. Ciprofloxacin is bactericidal. Its mode of action depends upon blocking bacterial DNA replication by binding itself to an enzyme called DNA gyrase, thereby inhibiting the unwinding of bacterial chromosomal DNA during and after the replication. Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. Amoxycillin, a penicillinase-susceptible semi-synthetic penicillin, is a close chemical and pharmacological relative of ampicillin. The drug is stable in acid and is designed for oral use. It is more rapidly and completely absorbed from the gastrointestinal tract than is ampicillin, which is the major difference between the two. The antimicrobial spectrum of amoxicillin is essentially identical to that of ampicillin, with the important exception that of ampicillin, with the important exception that amoxycillin appears to be less effective than ampicillin for shigellosis. (P. A. Willium, Chapter 45 Antimicrobial Agents; Goodman & Gilman’s The Pharmacological Basis of Therapeutics; 10th Edition; McGraw-Hill Medical Publishing Division; Page: 1202). It is usually the drug of choice within the class because it is better absorbed, following oral administration, than other beta-lactam antibiotics. It is susceptible to degradation by ß-lactamases-producing bacteria, and so may be given with clavulanic acid to decrease its susceptibility. Amoxycillin acts by inhibiting the synthesis of bacterial cell wall. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the cell wall of Gram-positive bacteria. In the invention ciprofloxacin or salts of thereof and amoxycillin or salts of thereof are used. Ciprofloxacin or salts of thereof is used in 100 to 750 mg/tablet and amoxicillin or salts of thereof is used in 200 mg to 1000 mg/tablet. Further in present invention other pharmaceutical excipients are used. The pharmaceutical composition of the present invention can be prepared according to techniques that are well known in pharmaceutical chemistry, comprising mixing, dissolution, sterilization and like. The invention is illustrated more in detail in the following examples. The examples describe and demonstrate embodiments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not to be construed as limitations of the present invention, as many variations thereof are possible without departing from the spirit and scope. Example 1: Ingredient Amount Ciprofloxacin 125 mg Amoxicillin (as trihydrate) 200 mg Example 2: Ingredient Amount Ciprofloxacin 250 mg Amoxicillin (as trihydrate) 400 mg Example 3: Ingredient Amount Ciprofloxacin 500 mg Amoxicillin (as trihydrate) 800 mg ABSTRACT The present invention relates to a pharmaceutical composition comprising ciprofloxacin or salts of thereof and amoxycillin or salts of thereof and other pharmaceutical excipients. The present invention provides more reliable effect against all bacteria responsible for especially respiratory tract infections. The invention makes up for the weakness of ciprofloxacin against streptococci.

Full Text

FORM 2
THE PATENT ACT 1970
(39 of 1970)
&
The Patents Rules, 2003
PROVISIONAL SPECIFICATION
(See section 10 and rule 13)

1. TITLE OF THE INVENTION

A PHARMACEUTICAL COMPOSITION FOR TREATMENT OF RESPIRATORY TRACT INFECTIONS

2. APPLICANT (S)

(a) NAME : Biochem Pharmaceutical Private Limited
(b) NATIONALITY: an Indian Company
(c) ADDRESS : Aidun Building,
John Crasto Lane,
Near Metro Theatre,
Mumbai – 400 002
India.
3. PREMABLE TO THE DESCRIPTION

? PROVISIONAL

The following specification describes the invention.
COMPLETE

The following specification particularly describes the invention and the manner in which it is to be performed.

The present invention relates to a pharmaceutical composition for the treatment of respiratory tract infections. This composition comprises ciprofloxacin or salts of thereof and amoxicillin or salts of thereof.
Ciprofloxacin has reliable effectiveness against all bacteria responsible especially for upper respiratory tract infections (URTI) and lower respiratory tract infections (LRTI) - except against streptococci species, which is one of the commonest pathogen for respiratory tract infections (RTIs). In view of amoxycillin’s continual reliability for streptococci, the combination of these two antimicrobials offers an effective option as preferred first line for empiric therapy of RTIs.
Background of the Invention:
Ciprofloxacin is a synthetic antibiotic, belonging to a group called fluoroquinolones. As far as streptococci are concerned, in recent years, these are inherently less susceptible to especially older fluoroquinolones. {Kaneko A et al. J Antimicrob Chemother 2000; 45: 771-775, Kaneko A et al. Chemotherapy (Tokyo) 1994; 42: 94-100. Coyle EA et al. Antimicrob Ag Chemother 2001; 45: 6: 1654-1659.} A major mechanism of resistance to fluoroquinolones in Gram-positive bacteria such as Streptococcus pneumoniae is target modification; mutations in the quinolone resistance determining region (QRDR) of the gyrA, parC and parE genes, resulting in decreased affinity for the quinolones. {Kaneko A et al. J Antimicrob Chemother 2000; 45: 771-775 Margerrison EE et al. J of Bacteriology 1992; 174: 1596-1603. Ferrero L et al. Antimicrob Ag Chemother 1995; 39: 1554-1558. Jorgensen JH et al. Antimicrob Ag Chemother 1999; 43: 329-334.}

Besides being less susceptible, resistance of Streptococcus pneumoniae to ciprofloxacin is the most amongst quinolones, {Alou L et al. Antimicrob Ag Chemother 2001; 45: 10: 2955-2957.} and as many as 15% of these bacteria are possibly resistant to it. {Deshpande LM et al. Diagn Microbiol Infect Dis 2006; 54: 3: 157-164} In India, the resistance of streptococci to fluoroquinolones is more likely to be prevalent since ciprofloxacin and other similar agents are more used for children. This is because the reservoir for streptococci is children. (http://www.annals.org/cgi/content/full/129/11_Part_1/908. As read on 15th Nov 2008. )
Amoxycillin or amoxicillin is a moderate-spectrum, bactericidal, ß-lactam antibiotic used to treat bacterial infections caused by susceptible microorganisms. Amoxycillin is advocated as preferred agent for URTI. {Korner JR et al. BMJ 1994; 308: 191-192.} With the ever-changing pattern of bacterial resistance, use of conventional doses amoxycillin in LRTI to eradicate H influenzae is disastrous. {Spiteri M. BMJ 1994; 308: 657-658. Powell M et al. J Antimicrob Chemother 1991; 28: 249-259.} In fact, amoxycillin is even lesser effective than ampicillin against H influenzae. {The Use of Antibiotics. Kucers A et al (Eds) 5th Ed 1997; Butterworth / Heinemann pp 134-144.Kosmidis J et al. Brit J Clin Pract 1972; 26: 341.}
Objects of the Present Invention:
The main object of the present invention is to provide a pharmaceutical composition of ciprofloxacin and amoxycillin or salts of thereof that provides a more reliable effect against all bacteria responsible for especially RTIs. Further object of the invention is to give tolerated dosage of these two antibiotics.
Another object of the invention is to makes up for the weakness of ciprofloxacin against streptococci.
Yet an object of the invention is to provide a composition that shows synergistic effect with no evidence of antagonism.
It is yet another object of the present invention to provide a simple process for preparing oral solid dosage forms comprising pharmaceutically effective amounts of ciprofloxacin and amoxycillin or salts of thereof.
Summary of the Invention:
The present invention relates to a pharmaceutical composition comprising ciprofloxacin and amoxycillin. In the invention ciprofloxacin or salts of thereof and amoxycillin or salts of thereof are used. Ciprofloxacin or salts of thereof is used in 100 to 750 mg/tablet and amoxycillin or salts of thereof are used in 200 to 1000 mg/tablet.
Detail Description:
Ciprofloxacin is indicated for treatment of acute uncomplicated cystitis in females, urinary tract infections (UTI), chronic bacterial prostatitis, LRTI, acute sinusitis, skin and skin structure infections (SSTI), bone and joint infections, complicated intra-abdominal infections, infectious diarrhea, enteric fever, uncomplicated cervical and urethral gonorrhea due to susceptible pathogens. Ciprofloxacin is bactericidal. Its mode of action depends upon blocking bacterial DNA replication by binding itself to an enzyme called DNA gyrase, thereby inhibiting the unwinding of bacterial chromosomal DNA during and after the replication. Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Amoxycillin, a penicillinase-susceptible semi-synthetic penicillin, is a close chemical and pharmacological relative of ampicillin. The drug is stable in acid and is designed for oral use. It is more rapidly and completely absorbed from the gastrointestinal tract than is ampicillin, which is the major difference between the two. The antimicrobial spectrum of amoxicillin is essentially identical to that of ampicillin, with the important exception that of ampicillin, with the important exception that amoxycillin appears to be less effective than ampicillin for shigellosis. (P. A. Willium, Chapter 45 Antimicrobial Agents; Goodman & Gilman’s The Pharmacological Basis of Therapeutics; 10th Edition; McGraw-Hill Medical Publishing Division; Page: 1202). It is usually the drug of choice within the class because it is better absorbed, following oral administration, than other beta-lactam antibiotics. It is susceptible to degradation by ß-lactamases-producing bacteria, and so may be given with clavulanic acid to decrease its susceptibility. Amoxycillin acts by inhibiting the synthesis of bacterial cell wall. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the cell wall of Gram-positive bacteria.
In the invention ciprofloxacin or salts of thereof and amoxycillin or salts of thereof are used. Ciprofloxacin or salts of thereof is used in 100 to 750 mg/tablet and amoxicillin or salts of thereof is used in 200 mg to 1000 mg/tablet.
Further in present invention other pharmaceutical excipients are used. The pharmaceutical composition of the present invention can be prepared according to techniques that are well known in pharmaceutical chemistry, comprising mixing, dissolution, sterilization and like.
The invention is illustrated more in detail in the following examples. The examples describe and demonstrate embodiments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not to be construed as limitations of the present invention, as many variations thereof are possible without departing from the spirit and scope.
Example 1:
Ingredient Amount
Ciprofloxacin 125 mg
Amoxicillin (as trihydrate) 200 mg

Example 2:
Ingredient Amount
Ciprofloxacin 250 mg
Amoxicillin (as trihydrate) 400 mg

Example 3:
Ingredient Amount
Ciprofloxacin 500 mg
Amoxicillin (as trihydrate) 800 mg

ABSTRACT

The present invention relates to a pharmaceutical composition comprising ciprofloxacin or salts of thereof and amoxycillin or salts of thereof and other pharmaceutical excipients. The present invention provides more reliable effect against all bacteria responsible for especially respiratory tract infections. The invention makes up for the weakness of ciprofloxacin against streptococci.

Documents:

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Patent Number

269019

Indian Patent Application Number

108/MUM/2010

PG Journal Number

40/2015

Publication Date

02-Oct-2015

Grant Date

29-Sep-2015

Date of Filing

13-Jan-2010

Name of Patentee

TOYOCHEM LABORATORIES

Applicant Address

A-AIDUN BUILDING 1ST DHOBI TALAO LANE MUMBAI 400002

Inventors:

#	Inventor's Name	Inventor's Address
1	Shah Mayank Jasvantbhai	Aidun Building John Crasto Lane Near Metro Theatre Mumbai – 400002 India.

PCT International Classification Number

A61K31/496

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA