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Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits.

Razavi M, Karimian H, Yeong CH, Chung LY, Nyamathulla S, Noordin MI - Drug Des Devel Ther (2015)

Bottom Line: Post-compression studies showed that there were no interactions between the active drug and the polymers.The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models.The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia.

ABSTRACT
The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1-F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm2O3) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics.

No MeSH data available.


Related in: MedlinePlus

The X-ray diffraction analysis of optimum formulation, pure drug, and polymers.Abbreviation: TKP, tamarind kernel powder.
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f5-dddt-9-4373: The X-ray diffraction analysis of optimum formulation, pure drug, and polymers.Abbreviation: TKP, tamarind kernel powder.

Mentions: The X-ray diffractograms of metformin HCl, salep, xanthan, TKP, and the F10 formulation are presented in Figure 5. The X-ray diffractogram of the pure drug displayed characteristic peaks at 12.7, 17.8, 22.35, 23.3, 24.55, 27.4, 28.5, 29.5, 31.4, 35.85, and 37.35 angles (°2θ). These sharp peaks represent the drug crystallinity. Salep and xanthan showed characteristic peaks at 20.4 and 20.2 angles (°2θ), respectively; the broad peaks of these polymers indicate their amorphous nature. In the X-ray diffractogram of the F10 formulation, drop in crystallinity of the metformin HCl was reflected by a decrease in the peak’s intensity. No missing peaks were detected in the F10 formulation. The insignificant differences detected in the XRD can be due to physical interactions that occurred while the tablet was prepared and compressed.


Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits.

Razavi M, Karimian H, Yeong CH, Chung LY, Nyamathulla S, Noordin MI - Drug Des Devel Ther (2015)

The X-ray diffraction analysis of optimum formulation, pure drug, and polymers.Abbreviation: TKP, tamarind kernel powder.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4532171&req=5

f5-dddt-9-4373: The X-ray diffraction analysis of optimum formulation, pure drug, and polymers.Abbreviation: TKP, tamarind kernel powder.
Mentions: The X-ray diffractograms of metformin HCl, salep, xanthan, TKP, and the F10 formulation are presented in Figure 5. The X-ray diffractogram of the pure drug displayed characteristic peaks at 12.7, 17.8, 22.35, 23.3, 24.55, 27.4, 28.5, 29.5, 31.4, 35.85, and 37.35 angles (°2θ). These sharp peaks represent the drug crystallinity. Salep and xanthan showed characteristic peaks at 20.4 and 20.2 angles (°2θ), respectively; the broad peaks of these polymers indicate their amorphous nature. In the X-ray diffractogram of the F10 formulation, drop in crystallinity of the metformin HCl was reflected by a decrease in the peak’s intensity. No missing peaks were detected in the F10 formulation. The insignificant differences detected in the XRD can be due to physical interactions that occurred while the tablet was prepared and compressed.

Bottom Line: Post-compression studies showed that there were no interactions between the active drug and the polymers.The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models.The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia.

ABSTRACT
The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1-F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm2O3) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics.

No MeSH data available.


Related in: MedlinePlus