Details for Patent: 5,286,754

Summary for Patent: 5,286,754

Title:	Pharmaceutical formulations of ciprofloxacin
Abstract:	A pharmaceutical formulation comprising by weight 30 to 95% of 1cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carb oxylic acid; 4.5 to 25% of a dry binder based on cellulose; 0 to 30% of a disintegration auxiliary based on starch; 0.5 to 10% of a disintegration auxiliary based on a cellulose derivative and/or a cross-linked polyvinyl-pyrrolidone; 0 to 2% of a flow-improving agent, and 0 to 3% of a lubricant. Tablets and capsules made from granules of the formulation, about 0.8 to 2 mm in size, exhibit high bioavailability and excellent storage stability.
Inventor(s):	Streuff; Bernd (Wermelskirchen, DE), Luchtenberg; Helmut (Niederkassel, DE)
Assignee:	Bayer Aktiengesellschaft (Leverkusen, DE)
Application Number:	07/246,576
Patent Claim Types: see list of patent claims	Formulation; Compound;

Detailed Analysis of the Scope and Claims of United States Patent 5,286,754

Introduction

United States Patent 5,286,754, titled "Pharmaceutical formulations of ciprofloxacin," is a significant patent in the field of pharmaceuticals, particularly focusing on the formulation and preparation of ciprofloxacin, a widely used antibiotic. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background of Ciprofloxacin

Ciprofloxacin is a fluoroquinolone antibiotic known for its broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria. It is used to treat various bacterial infections, including those resistant to other antibiotics[1].

Scope of the Patent

The patent describes pharmaceutical formulations of ciprofloxacin that are designed for oral administration. These formulations are composed of several key components:

Active Ingredient

• The formulations contain 30.0 to 95.0% by weight of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid, which is the chemical name for ciprofloxacin[1].

Excipients

• Dry Binder: 4.5 to 25.0% by weight of a dry binder based on cellulose.
• Disintegration Auxiliary: 0.0 to 30.0% by weight of a disintegration auxiliary based on starch, and 0.5 to 10.0% by weight based on cellulose derivatives and/or cross-linked polyvinylpyrrolidones.
• Flow-Improving Agent: 0.0 to 2.0% by weight.
• Lubricant: 0.0 to 3.0% by weight, with magnesium stearate being the preferred lubricant[1][2].

Claims of the Patent

The patent includes several claims that define the scope of the invention:

Composition Claims

• Claims related to the specific composition of the pharmaceutical formulations, including the percentages of ciprofloxacin and various excipients.
• For example, Claim 1 describes a pharmaceutical formulation containing ciprofloxacin, a dry binder, a disintegration auxiliary, a flow-improving agent, and a lubricant within the specified weight ranges[1].

Process Claims

• Claims related to the processes for preparing these formulations, including the steps involved in mixing, granulating, and compressing the ingredients into tablets or filling into capsules[1][2].

Use Claims

• Claims related to the use of these formulations in human and veterinary medicine for the prophylaxis and chemotherapy of local and systemic infections caused by Gram-positive and Gram-negative bacteria[1].

Patent Landscape

Related Patents and Applications

• The patent is part of a family of applications and patents, including priority applications filed in Germany (DE3601566) and subsequent continuation applications in the United States (US07/246,576 and US14380893A)[1].
• Other related patents, such as U.S. Pat. No. 5,286,754, also describe similar formulations and processes for ciprofloxacin hydrochloride[5].

Cited Patents and Citations

• The patent has been cited by several other patents, indicating its influence on subsequent research and development in pharmaceutical formulations[1].

Expiration and Legal Status

• The patent has expired, which means that the formulations and processes described are now in the public domain and can be freely used without infringing on the original patent[1].

Impact on Pharmaceutical Industry

Broad-Spectrum Antibacterial Activity

• The formulations described in the patent are active against a broad spectrum of micro-organisms, making them highly effective in treating various bacterial infections[1].

Stability and Bioavailability

• The granule-based formulations exhibit high bioavailability and excellent storage stability, which are critical factors in the development of reliable pharmaceutical products[1].

Patent Analytics and Claim Coverage

In managing intellectual property related to this patent, companies can use patent analytics tools to track and analyze the claims and scope concepts. Here’s how:

Claim Coverage Matrix

• A Claim Coverage Matrix can help identify which patents and claims are actively protecting the intellectual property related to ciprofloxacin formulations. This tool categorizes patents by claims and overarching scope concepts, facilitating a comprehensive analysis of the patent landscape[3].

Interactive Claim Charts

• Interactive claim charts generated by tools like ClaimScape® software can be used to review patent coverage with technical experts. These charts help in determining whether specific scope concepts are applicable to target products or methods, highlighting gaps in current coverage and future design opportunities[3].

Key Takeaways

• Composition and Process: The patent details specific compositions and processes for preparing ciprofloxacin formulations.
• Broad-Spectrum Activity: The formulations are effective against a wide range of Gram-positive and Gram-negative bacteria.
• Stability and Bioavailability: The granule-based formulations offer high bioavailability and excellent storage stability.
• Patent Landscape: The patent is part of a larger family of applications and has been cited by several other patents.
• Expiration: The patent has expired, making the described formulations and processes publicly available.

FAQs

What is the main active ingredient in the pharmaceutical formulations described in U.S. Patent 5,286,754?

The main active ingredient is ciprofloxacin, specifically 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid.

What are the key excipients used in these formulations?

The key excipients include a dry binder based on cellulose, a disintegration auxiliary based on starch and cellulose derivatives, a flow-improving agent, and a lubricant such as magnesium stearate.

What is the significance of the granule size in these formulations?

The granules, which are about 0.8 to 2 mm in size, exhibit high bioavailability and excellent storage stability.

How does the patent impact the pharmaceutical industry?

The patent provides formulations and processes that are highly effective against a broad spectrum of micro-organisms, contributing to the development of reliable and effective pharmaceutical products.

What tools can be used to analyze the patent claims and scope concepts?

Tools like Claim Coverage Matrix and interactive claim charts generated by ClaimScape® software can be used to analyze and manage the patent claims and scope concepts.

Sources

1. US5286754A - Pharmaceutical formulations of ciprofloxacin - Google Patents
2. United States Patent (19) - googleapis.com
3. Patent Analytics - SLWIP
4. Pharmaceutical formulations of ciprofloxacin - PubChem
5. Tablets comprising ciprofloxacin hydrochloride - Justia Patents

Drugs Protected by US Patent 5,286,754

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 5,286,754

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Germany	3601566	Jan 21, 1986

International Family Members for US Patent 5,286,754

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	63460
Canada	1296634
China	1084188
China	87100810
Germany	3601566
Germany	3770001
European Patent Office	0230881