Characterization Of Gastrorenettive Properties Nata De Coco Matrix And Hydroxyphythiplyl Methylcellulose Polymer Containing Metformin Hydrochloride
Characterization of Gastrorenettive Properties Nata de Coco Matrix and Hydroxyphiplyl Methylcellulose Polymer Containing Metformin Hydrochloride
Introduction
Metformin Hydrochloride (HCL) is a widely used medication for treating type 2 diabetes. Despite its high water solubility, the absorption of HCl metformin is limited, leading to side effects such as nausea and vomiting, particularly in the upper digestive tract. Approximately 40% of the administered dose is absorbed in the upper small intestine (duodenum and proximal jejunum), while only 10% is absorbed in the ileum and colon. Therefore, the development of a gradual release system for Metformin HCL is crucial. However, the side effects of the gradual release system often outweigh those of the conventional direct release system. One potential solution lies in the use of gastrorenettive systems that can initiate release in the stomach and complete it in the jejunum, providing continuous release during the transit from the stomach to the jejunum.
Research Objectives
This study aims to characterize the physical properties of gastrorenettive Metformin HCl print granules made from nata de coco matrix and hydroxypropyl methylcellulose (HPMC) polymers that can withstand the stomach environment and provide sustained release.
Methodology
Gastrorenettive Metformin HCl print granules were prepared using nata de coco pulp, 10% HPMC mucilage in water distillation, and lactose in various ratios. The nata de coco pulp mixture, HPMC mucilage, and lactose containing HCl metformin were formed using a pipette with a 1.2 cm diameter, then dried at room temperature for 5 days. The nature of floating, swelling, integrity, and release of print granules was tested using a Paddle dissolution tool according to the USP method on a stomach-made medium with a pH of 1.2 for 12 hours. Mucoadhesive properties were evaluated using a 1 cm × 1 cm gastric mucosa on the Dunuoy tensiometer.
Research Results
The F6A print granules with a nata de coco ratio: HPMC (1: 2) containing 0.4 g lactose exhibited good characteristics as a gastrorenettive drug delivery system with a gradual release. These print grains floated before gastric emptying (2-3 hours), indicated by a delayed time of floating of 21 ± 0.3 minutes and a duration of floating for 12 hours. Additionally, print granules showed a good swelling nature, with the diameter of print granules reaching 1.33 cm in 60 minutes, exceeding the diameter of the pylorus before emptying (1.28 ± 0.07 cm). The integrity of print granules remained intact for 12 hours, and the mucoadhesive nature showed results of 525.06 ± 0.45 dyne/cm². F6A print granules (1: 2) also provided a good gradual release profile in 180, 360, and 720 minutes, each of 44.62%, 61.75%, and 77.91%. The release results of F6A granules were able to provide slow release in accordance with the criteria for gradual release, which is 20-50%, 45-75%, and ≥75%.
Conclusion
This study demonstrates that Nata de Coco-HPMC print granules with the F6A formula (Nata de Coco: HPMC 1: 2) possess physical characteristics, gastrorenettive properties, and a good gradual release. Therefore, this study provides promising alternatives in the development of Metformin HCl drug formulations that are more effective and safe for patients with type 2 diabetes.
Future Directions
The findings of this study suggest that the use of nata de coco matrix and HPMC polymers can be a viable approach for developing gastrorenettive systems for Metformin HCl. Future studies can focus on optimizing the formulation and processing conditions to further improve the physical and release properties of the print granules. Additionally, in vivo studies can be conducted to evaluate the efficacy and safety of the gastrorenettive system in a clinical setting.
Limitations
This study has several limitations. The use of a Paddle dissolution tool and a stomach-made medium with a pH of 1.2 may not accurately simulate the in vivo conditions. Furthermore, the mucoadhesive properties were evaluated using a 1 cm × 1 cm gastric mucosa, which may not be representative of the actual mucosal surface. Future studies should aim to address these limitations and provide more comprehensive evaluation of the gastrorenettive system.
Implications
The development of gastrorenettive systems for Metformin HCl has significant implications for the treatment of type 2 diabetes. By providing sustained release and reducing the side effects associated with the conventional direct release system, gastrorenettive systems can improve the quality of life for patients with type 2 diabetes. The findings of this study suggest that the use of nata de coco matrix and HPMC polymers can be a viable approach for developing gastrorenettive systems for Metformin HCL.
Q&A: Characterization of Gastrorenettive Properties Nata de Coco Matrix and Hydroxyphiplyl Methylcellulose Polymer Containing Metformin Hydrochloride
Q: What is the purpose of this study?
A: The purpose of this study is to characterize the physical properties of gastrorenettive Metformin HCl print granules made from nata de coco matrix and hydroxypropyl methylcellulose (HPMC) polymers that can withstand the stomach environment and provide sustained release.
Q: What are the limitations of the conventional direct release system for Metformin HCl?
A: The conventional direct release system for Metformin HCl has several limitations, including limited absorption in the upper small intestine, side effects such as nausea and vomiting, and a short duration of action.
Q: What are the advantages of using a gastrorenettive system for Metformin HCl?
A: The use of a gastrorenettive system for Metformin HCl can provide several advantages, including sustained release, reduced side effects, and improved efficacy.
Q: What is the role of nata de coco matrix in the gastrorenettive system?
A: The nata de coco matrix plays a crucial role in the gastrorenettive system by providing a sustained release of Metformin HCl and protecting the drug from degradation in the stomach.
Q: What is the role of HPMC polymers in the gastrorenettive system?
A: The HPMC polymers play a crucial role in the gastrorenettive system by providing mucoadhesive properties, which help to retain the print granules in the stomach and facilitate sustained release.
Q: What are the physical characteristics of the F6A print granules?
A: The F6A print granules have a good floating nature, with a delayed time of floating of 21 ± 0.3 minutes and a duration of floating for 12 hours. They also exhibit a good swelling nature, with the diameter of print granules reaching 1.33 cm in 60 minutes.
Q: What are the mucoadhesive properties of the F6A print granules?
A: The F6A print granules have a mucoadhesive nature, with results of 525.06 ± 0.45 dyne/cm².
Q: What are the release properties of the F6A print granules?
A: The F6A print granules provide a good gradual release profile in 180, 360, and 720 minutes, each of 44.62%, 61.75%, and 77.91%.
Q: What are the implications of this study for the treatment of type 2 diabetes?
A: The findings of this study suggest that the use of nata de coco matrix and HPMC polymers can be a viable approach for developing gastrorenettive systems for Metformin HCl, which can improve the quality of life for patients with type 2 diabetes.
Q: What are the future directions for this research?
A: Future studies can focus on optimizing the formulation and processing conditions to further improve the physical and release properties of the print granules. Additionally, in vivo studies can be conducted to evaluate the efficacy and safety of the gastrorenettive system in a clinical setting.
Q: What are the limitations of this study?
A: This study has several limitations, including the use of a Paddle dissolution tool and a stomach-made medium with a pH of 1.2, which may not accurately simulate the in vivo conditions. Additionally, the mucoadhesive properties were evaluated using a 1 cm × 1 cm gastric mucosa, which may not be representative of the actual mucosal surface.
Q: What are the potential applications of this research?
A: The findings of this study can be applied to the development of gastrorenettive systems for other drugs, including those used to treat gastrointestinal disorders, such as irritable bowel syndrome (IBS) and gastroesophageal reflux disease (GERD).