Gastroretentive formulations and manufacturing process thereof
Inventors
Chaudhari, Mahendra • Chandwani, Omprakash D. • Yelegaonkar, Rajashree S.
Assignees
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Publication Number
US-9629800-B2
Publication Date
2017-04-25
Expiration Date
Abstract
The present invention concerns gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent, a strong gelling agent, and a gas generating agent and process for manufacturing said formulation.
Core Innovation
The invention relates to a gastroretentive formulation in the form of a monolithic sustained-release tablet in which an active substance is granulated with a mixture comprising a weak gelling agent (A), a strong gelling agent (B), and a gas generating agent. The weak gelling agent (A) is a co-processed material of microcrystalline cellulose and sodium carboxy methylcellulose, and the strong gelling agent (B) is defined by a viscosity of at least 600 centipoise in a 1% W/V aqueous solution at 25°C. The weak gelling agent and strong gelling agent are used in a ratio from 1:1 to 1:10.
The problem being solved is to provide a gastroretentive monolithic sustained-release system that retains the tablet in the stomach for an extended period while modulating erosion and dissolution via swelling, rigidity, and gas entrapment. In the gastric environment, the formulation releases gas in gastric acid and forms a bubbled gel layer that affects subsequent erosion and dissolution behavior. This mechanism is intended to increase gastric retention and sustain drug release over time.
The formulation addresses drug suitability by providing example active substances including metformin hydrochloride and ciprofloxacin and related fluoroquinolones. The active substance is granulated together with the weak and strong gelling agent mixture and the gas generating agent, which includes water-soluble carbonates, sulfites, bicarbonates, or mixtures thereof. The weak and strong gelling balance is presented as enabling rapid swelling, rigidity, and gas entrapment in the gel matrix to form the bubbled layer on a gel surface.
Claims Coverage
The independent claim is clm-00001. It requires one inventive feature set for a monolithic gastroretentive formulation: an active substance granulated with a specific weak gelling agent, a viscosity-defined strong gelling agent, and a gas generating agent at a defined weak:strong gelling agent ratio.
Co-processed weak and viscosity-defined strong gelling agents with gas generation
A gastroretentive formulation comprising an active substance granulated with a mixture of a weak gelling agent (A), which is a co-processed material of microcrystalline cellulose and sodium carboxy methylcellulose; a strong gelling agent (B), which is a compound having a viscosity of at least 600 centipoise when it is in the form of a 1% W/V aqueous solution at 25°C; and a gas generating agent.
Monolithic gastroretentive formulation with defined weak:strong ratio
The gastroretentive formulation is monolithic, and a ratio of the weak gelling agent (A) to the strong gelling agent (B) ranges from 1:1 to 1:10.
The claims coverage is centered on a monolithic gastroretentive granulated composition using a co-processed weak gelling agent, a strong gelling agent defined by viscosity, and a gas generating agent, with a weak:strong gelling agent ratio of 1:1 to 1:10.
Stated Advantages
Provides stomach retention through a gastroretentive monolithic sustained-release design.
Modulates erosion and dissolution behavior via swelling, rigidity, and gas entrapment forming a bubbled gel layer.
Supports sustained drug release over time in acidic media.
Documented Applications
Gastroretentive sustained-release formulations including metformin hydrochloride and ciprofloxacin and related fluoroquinolones.
Drug release in acidic media, exemplified by dissolution in 0.1N HCl for metformin HCl and ciprofloxacin base.
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