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pH-Sensitive Mebeverine Microspheres for Colon Delivery.

Dandagi PM, Mastiholimath VS, Gadad AP, Kulkarni AR, Konnur BK - Indian J Pharm Sci (2009)

Bottom Line: Mebeverine hydrochloride is known to suffer from extensive first pass effect.Scanning electron microscopy confirmed that the microsphere structures were smooth, spherical, and discrete and the particles were of the size range 200 to 300 mum.On the basis of drug content, particle size, in vitro release and in vivo studies, formulation F-3 was found to be optimal.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, K. L. E. S's College of Pharmacy, J. N. M. C. Campus, Nehru Nagar, Belgaum-590 010, India.

ABSTRACT
Mebeverine hydrochloride is known to suffer from extensive first pass effect. In an attempt to improve its oral bioavailability and possibility to restrict its absorption only to the colon, mebeverine microspheres were prepared by emulsion solvent evaporation method. Four formulations were prepared with varying drug and polymer ratio. These formulations were subjected to various evaluation parameters like percent practical yield, entrapment efficiency, particle size, in vitro drug release, in vivo activity. Practical yield of the microspheres was up to 89.59% with encapsulation efficiency up to 79.4%. Scanning electron microscopy confirmed that the microsphere structures were smooth, spherical, and discrete and the particles were of the size range 200 to 300 mum. In vitro release of the drug showed biphasic release pattern with non-Fickian diffusion release in 12 h. On the basis of drug content, particle size, in vitro release and in vivo studies, formulation F-3 was found to be optimal. Antiirritable bowel syndrome activity was performed in colorectal distention in rat, which is a model for constipation-induced irritable bowel syndrome. The formulations F-2 and F-3 showed significant effect in fecal output when compared to the control as well as the marketed preparation in the constipation-induced irritable bowel syndrome in rats.

No MeSH data available.


Related in: MedlinePlus

SEM Images of different formulations of mebeverine hydrochloride microspheresSEM Images Showing (a) Formulation (F-1) with core and coat ratios of 1:0.5; (b) Formulation (F-2) with 1:1; (c) Formulation (F-3) with 1:1.5 and (d) formulation (F-4) with 1:2.
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Figure 0001: SEM Images of different formulations of mebeverine hydrochloride microspheresSEM Images Showing (a) Formulation (F-1) with core and coat ratios of 1:0.5; (b) Formulation (F-2) with 1:1; (c) Formulation (F-3) with 1:1.5 and (d) formulation (F-4) with 1:2.

Mentions: Particle size analysis by optical microscope indicated the presence of almost uniform sized microspheres. The average mean particle sizes of the microspheres were found to be uniform and consistent (Table 1). The average mean particle size of the microspheres increased significantly with increase in polymer concentration due to high viscosity of medium at a higher polymer concentration resulting in enhanced interfacial tension and diminished shearing efficiency. Scanning electron microscope studies shows particles of F-1 and F-2 were rough surfaced and crystals of the drug are visible on surface, indicating the concentration of polymeric solution is insufficient for complete encapsulation. The F-3 and F-4 were found to be spherical, smooth and discrete. Smoothness of microspheres increases with increasing the polymer concentration, which is observed from scanning electron photomicrographs of four formulations (fig. 1). The drug content was found to be high in all the cases probably due to polymer loss by adherence to the container as a result of viscous nature of slurry. It was observed that entrapment efficiency increased with increase in concentration of polymer added in formulations (Table 1).


pH-Sensitive Mebeverine Microspheres for Colon Delivery.

Dandagi PM, Mastiholimath VS, Gadad AP, Kulkarni AR, Konnur BK - Indian J Pharm Sci (2009)

SEM Images of different formulations of mebeverine hydrochloride microspheresSEM Images Showing (a) Formulation (F-1) with core and coat ratios of 1:0.5; (b) Formulation (F-2) with 1:1; (c) Formulation (F-3) with 1:1.5 and (d) formulation (F-4) with 1:2.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2865826&req=5

Figure 0001: SEM Images of different formulations of mebeverine hydrochloride microspheresSEM Images Showing (a) Formulation (F-1) with core and coat ratios of 1:0.5; (b) Formulation (F-2) with 1:1; (c) Formulation (F-3) with 1:1.5 and (d) formulation (F-4) with 1:2.
Mentions: Particle size analysis by optical microscope indicated the presence of almost uniform sized microspheres. The average mean particle sizes of the microspheres were found to be uniform and consistent (Table 1). The average mean particle size of the microspheres increased significantly with increase in polymer concentration due to high viscosity of medium at a higher polymer concentration resulting in enhanced interfacial tension and diminished shearing efficiency. Scanning electron microscope studies shows particles of F-1 and F-2 were rough surfaced and crystals of the drug are visible on surface, indicating the concentration of polymeric solution is insufficient for complete encapsulation. The F-3 and F-4 were found to be spherical, smooth and discrete. Smoothness of microspheres increases with increasing the polymer concentration, which is observed from scanning electron photomicrographs of four formulations (fig. 1). The drug content was found to be high in all the cases probably due to polymer loss by adherence to the container as a result of viscous nature of slurry. It was observed that entrapment efficiency increased with increase in concentration of polymer added in formulations (Table 1).

Bottom Line: Mebeverine hydrochloride is known to suffer from extensive first pass effect.Scanning electron microscopy confirmed that the microsphere structures were smooth, spherical, and discrete and the particles were of the size range 200 to 300 mum.On the basis of drug content, particle size, in vitro release and in vivo studies, formulation F-3 was found to be optimal.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, K. L. E. S's College of Pharmacy, J. N. M. C. Campus, Nehru Nagar, Belgaum-590 010, India.

ABSTRACT
Mebeverine hydrochloride is known to suffer from extensive first pass effect. In an attempt to improve its oral bioavailability and possibility to restrict its absorption only to the colon, mebeverine microspheres were prepared by emulsion solvent evaporation method. Four formulations were prepared with varying drug and polymer ratio. These formulations were subjected to various evaluation parameters like percent practical yield, entrapment efficiency, particle size, in vitro drug release, in vivo activity. Practical yield of the microspheres was up to 89.59% with encapsulation efficiency up to 79.4%. Scanning electron microscopy confirmed that the microsphere structures were smooth, spherical, and discrete and the particles were of the size range 200 to 300 mum. In vitro release of the drug showed biphasic release pattern with non-Fickian diffusion release in 12 h. On the basis of drug content, particle size, in vitro release and in vivo studies, formulation F-3 was found to be optimal. Antiirritable bowel syndrome activity was performed in colorectal distention in rat, which is a model for constipation-induced irritable bowel syndrome. The formulations F-2 and F-3 showed significant effect in fecal output when compared to the control as well as the marketed preparation in the constipation-induced irritable bowel syndrome in rats.

No MeSH data available.


Related in: MedlinePlus