FIELD OF THE INVENTION:
The invention relates to pharmaceutical formulations of erythromycin derivatives .that have
an extended release of an active compound in the gastrointestinal environment
Specifically, the invention is directed to compositions containing with drug structures of
clarithromycin which are ingested day to day as a solitary oral organization.
BACKGROUND OF THE INVENTION:
ERY is a macrolide compound that has an expansive scope of antimicrobial movement and is
utilized to treat different bacterial contaminations influencing various pieces of the body.
ERY's effectiveness against drug-resistant pathogens has been widely used since its
discovery in 1952, but it has several limitations that pose significant clinical challenges.
These limitations include drug resistance and undesirable effects at higher doses, as well as
low solubility in water, instability under acidic conditions, limited efficacy, and
bioavailability. Over the past few decades, various formulations of ERY, including
nanoparticles, have been developed by researchers to overcome these disadvantages.
However, despite the growing interest in these ERY formulations, no in-depth analysis of
their features exists. As a result, the purpose of this review is to examine the efforts made
to encapsulate ERY in formulations of various sizes, morphologies, and chemical
compositions, as well as their physicochemical properties and outcomes. Additionally, the
review addresses these studies' limitations, such as the quantification of ERY.
According to the literature, a wide variety of vesicular systems are utilized for drug delivery.
· These systems include, but are not limited to, lipid particles, liposomes, niosomes,
sphingo~omes, pharmacosomes, transferosomes, and polymeric micelles. These vesicular
carriers are primarily designed to solve issues with drug delivery and improve therapeutic
outcomes. A few benefits of utilizing lipid-based drug conveyance incorporate the capacity
to typify both hydrophilic and lipophilic medications, further developed bioavailability,
broadened drug course time, decrease of poisonousness, and diminished remedial dose
prerequisites.
2
Erythromycin and its derivatives are typically administered as immediate release (IR)
formulations two to three times per day for 10 to 14 days. They have potent antibacterial
activity against a variety of organisms. However, their sour taste, especially in the case of 6-
0-methoxyerythromycin A (clarithromycin), can make patients less likely to take their
medications and may prompt the use of less efficient therapeutic options. Controlled
release solid preparations containing erythromycin derivatives in an alginate matrix have
been developed as one method for increasing compliance. Alginates and other monolithic
hydrogel tablets, on the other hand, were found to be unsuitable for reproducibly
bioavailable controlled release formulations in in vivo animal studies. Improved controlled ·
release formulations with a citric acid matrix and a poorly soluble basic drug have been
developed to address this issue. The goal of these once-daily formulations is to achieve
bioequivalence with the current twice-daily IR formulations by increasing bioavailability.
However, they· do not address the negative effects of taste perversion or gastrointestinal
(GI} disorders. To handle the last option issue, acceptable fluid oral measurement types of
these medications have been grown, yet they actually require two times day to day
organization and don't limit the antagonistic impacts connected with Gl problems·; As a
result, a pharmaceutical composition that is equivalent to or better than the current IR
tablet or liquid formulations in terms of minimizing side effects and controlling drug plasma
concentration must be developed.
Summary of the invention:
The present invention relates to a pharmaceutical composition that a wide variety of
vesicular systems are utilized for drug delivery. These systems include, but are not limited
to, lipid particles, liposomes, niosomes, sphingosomes, pharmacosomes, transferosomes,
and polymeric micelles. These vesicular carriers are primarily designed to solve issues with
drug delivery and improve therapeutic outcomes. A few benefits of utilizing lipid-based drug
conveyance incorporate the capacity to typify both hydrophilic and lipophilic medications,
further developed bioavailability, broadened drug course time, decrease of poisonousness,
and diminished remedial dose prerequisites.
3
Erythromycin and its derivatives are typically administered as immediate release (IR)
formu.lations two to three times per day for 10 to 14 days. They have potent antibacterial
activity against a variety of organisms. However, their sour taste, especially in the case of 6-
0-methoxyerythromycin A (clarithromycin), can make patients less likely to take their
medications .and may prompt the use of less efficient therapeutic options. Controlled
release solid preparations containing erythromycin derivatives in an alginate matrix have
been developed as one method for increasing compliance. Alginates and other monolithic
hydrogel tablets, on the other hand, were found to be unsuitable for reproducibly
bioavailable controlled release formulations in in vivo animal studies. Improved controlled
release formulations with a citric acid matrix and a poorly soluble basic drug have been
developed to address this issue. The goal of these once-daily formulations is to achieve
bioequivalence with the current twice-daily IR formulations by increasing bioavailability.
However, they do not address the negative effects of taste perversion or gastrointestinal
(GI) disorders. To handle the last option issue, acceptable fluid oral measurement types of
these medications have been grown, yet they actually require two times day to day
organization and don't limit the antagonistic impacts connected with Gl problems. As a
result, a pharmaceutical composition that is equivalent to or better than the current IR
tablet or liquid formulations in terms of minimizing side effects and controlling drug plasma
concentration must be developed.
;
A controlled-release pharmaceutical composition for the treatment of bacterial infections in
mammals is provided by the present invention in another embodiment. A pharmaceutically
acceptable polymer and a derivative of erythromycin