Design, Characterisation and Evaluation Study for Immediate Release Formulation of Canagliflozin

The term "immediate release" (IR) describes how quickly a product, medication, or piece of information becomes available following administration or announcement. In medicine, it indicates that the medication dissolves rapidly for prompt effect. This term in the media refers to press releases intended for immediate publication. When timing is crucial, it guarantees quick effect or communication.

Canagliflozin is an oral antidiabetic medication that belongs to the sodium-glucose co-transporter 2 (SGLT2) inhibitor class. It is primarily used for managing type 2 diabetes mellitus by lowering blood glucose levels through a unique insulin-independent mechanism. By inhibiting SGLT2 in the kidneys, it reduces glucose reabsorption and promotes its excretion through urine, leading to improved glycemic control⁽¹⁾. In addition to its glucose-lowering effects, Canagliflozin also contributes to weight loss, lowers blood pressure, and provides cardiovascular and renal benefits, making it a valuable option for patients with diabetes and associated complications. However, its use is associated with potential side effects such as an increased risk of urinary tract and genital infections, dehydration, hypotension, and, in rare cases, diabetic ketoacidosis. Some studies have also linked it to an increased risk of bone fractures due to possible reductions in bone mineral density. Despite these concerns, canagliflozin remains an important therapeutic option, particularly for patients who require additional benefits beyond glucose control. Proper patient selection and monitoring are essential to minimize risks and optimize its effectiveness in diabetes management^(1,2).

MARKET OVERVIEW OF THE DRUG-

In approximately 80 countries in the world, such as Australia, Japan, the USA, and Europe, patients with type 2 diabetes are managed with canagliflozin. On the other hand, canagliflozin is not approved to be used for type 1 diabetic patients. Earlier, it was highlighted that a great number of patients suffering from type 2 diabetes experience renal illness and HF. Canagliflozin and other SGLT2is are essential drugs for the management of glycemia and the mitigation of type 2 diabetes in patients in over 80 countries, such as Australia, Japan, the USA, and European countries, take canagliflozin. While canagliflozin is prohibited for use in this demographic ⁽³⁾. It is essential to note that canagliflozin is not suitable for use in type 1 diabetic patients. It is noteworthy that patients with type 2 diabetes often have nephropathies and HF; therefore, this statement is true. SGLT2 is, like canagliflozin, an effective drug for maintaining glycemic control and also for kidney diseases and HF ⁽⁴⁾.

MATERIAL & METHODS-

MATERIAL –

The vendor provided me with Canagliflozin (CIPLA.LTD) which I used to create tablets while sourcing the additional components such as MCC, PVP-K30, SSG, Talc and magnesium stearate at the college laboratory.

METHODS-

Initially, this study commenced with a comprehensive Preformulation analysis to evaluate both the active pharmaceutical ingredient (API) and the selected excipients. This analytical phase involved the use of several techniques, such as infrared (IR) spectroscopy to identify functional groups and potential interactions, UV spectrophotometry for drug quantification and absorbance profiling, and solubility assessments to determine the drug’s behaviour in different solvents. Additional characterization included determining the melting point to assess purity and thermal stability and thin-layer chromatography (TLC) to identify the presence of impurities and evaluate the drug’s stability profile. Following this, the formulation study was carried out for three consecutive batches to ensure consistency and reproducibility of the dosage form⁽⁵⁾. A key aspect of the formulation development was the incorporation of a super-disintigrant, sodium starch glycolate, which was tested in varying polymer ratios to assess its impact on tablet performance. The in-vitro evaluation of the dosage form was conducted with a focus on both physical and chemical quality control parameters. These included disintegration time, to measure the speed at which the tablet breaks down in the body; dissolution testing, to evaluate the drug release profile; friability, to assess the tablet's resistance to crumbling during handling; and hardness testing, to determine the mechanical strength of the tablets⁽⁶⁾. Through these investigations, the study aimed to optimize the formulation by balancing polymer concentrations to achieve the most effective and stable dosage form.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

TIME	% OF DRUG RELEASE
5 min	25.5
10 min	28.5
15 min	48
20 min	88.2

 

 

DISSCUSSION

The study underscores the potential of polymer-based formulation strategies in transforming the pharmacokinetic properties of existing drugs, ultimately improving patient compliance, therapeutic outcomes, and overall disease management. Therefore, it can be concluded that Canagliflozin, when formulated as an immediate release tablet, offers a significant improvement in the treatment of type 2 diabetes mellitus, providing faster relief and more efficient control over blood glucose levels.

CONCLUSIONS

The present investigation highlights the successful development of an immediate release formulation of Canagliflozin, tailored specifically to meet the urgent therapeutic requirements in the management of type 2 diabetes mellitus. Traditionally, Canagliflozin exhibits a relatively long half-life and delayed onset of action, which, although effective for long-term glycemic control, may not be ideal in situations demanding rapid therapeutic response. This study addressed this limitation by designing a formulation capable of delivering the drug in a significantly shorter timeframe. Through a comprehensive preformulation study involving key analytical techniques such as IR Spectroscopy, UV-Spectrophotometry, solubility profiling, and melting point analysis, the compatibility of Canagliflozin with various pharmaceutical excipients was thoroughly evaluated. Sodium starch glycolate was selected as the primary disintegrating polymer due to its high swelling capacity and efficiency in promoting rapid tablet disintegration. Formulation trials were conducted in three consecutive batches with varying polymer ratios to fine-tune the drug release profile. These formulations were then subjected to in-vitro evaluation parameters, including disintegration time, dissolution studies, friability, and hardness testing. The findings revealed that the optimized formulation achieved a remarkable reduction in drug release time from approximately 10 hours to just 15 minutes for a 100 mg tablet, without compromising the physical integrity and quality of the dosage form. This advancement not only enhances the onset of Canagliflozin’s therapeutic action but also broadens its clinical applicability, especially in emergency scenarios where immediate glucose regulation is critical.

ABBREVIATIONS-

SGLT2- sodium-glucose co-transporter 2

UV- Ultra Violet

IR- Infra Red

ACKNOWLEDGMENTS

We acknowledge all of authors and co-authors.

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