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Solid Dispersion Matrix Tablet Comprising Indomethacin-PEG-HPMC Fabricated with Fusion and Mold Technique.

Mesnukul A, Yodkhum K, Phaechamud T - Indian J Pharm Sci (2009)

Bottom Line: This inert carrier system comprising 7:3 polyethylene glycol 4000: polyethylene glycol 400 could effectively enhance the solubility of indomethacin and an addition of hydroxypropylmethylcellulose could sustain the drug release.Least square fitting the experimental dissolution data to the mathematical expressions (power law, first-order, Higuchi's and zero-order) indicated the drug release kinetics primarily as Fickian diffusion.Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, indomethacin, by using polyethylene glycol-hydroxypropylmethylcellulose matrix system prepared with melting and mold technique.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.

ABSTRACT
The purpose of this study is to fabricate the polyethylene glycol matrix tablet by mold technique. Indomethacin and hydroxypropylmethylcellulose were used as model drug and polymer, respectively, in PEG matrix system. The physical and drug release characteristics of developed matrix tablet were studied. This inert carrier system comprising 7:3 polyethylene glycol 4000: polyethylene glycol 400 could effectively enhance the solubility of indomethacin and an addition of hydroxypropylmethylcellulose could sustain the drug release. Scanning electron microscope photomicrograph indicated the drug diffusion outward through the porous network of this developed matrix tablet into the dissolution fluid. Least square fitting the experimental dissolution data to the mathematical expressions (power law, first-order, Higuchi's and zero-order) indicated the drug release kinetics primarily as Fickian diffusion. Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, indomethacin, by using polyethylene glycol-hydroxypropylmethylcellulose matrix system prepared with melting and mold technique.

No MeSH data available.


Force displacement profiles of tablets.Force displacement profiles for formulation of tablets containing 25% HPMC in 70:30 PEG 4000:PEG 400 system at different time points (n=3)
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Figure 0002: Force displacement profiles of tablets.Force displacement profiles for formulation of tablets containing 25% HPMC in 70:30 PEG 4000:PEG 400 system at different time points (n=3)

Mentions: Dry tablet (before dissolution test) containing 25% HPMC exhibited higher total work penetration than tablet after dissolution test at different time intervals (figs. 2 and 3). Total work penetration of tablet containing 25% HPMC was decreased with time during dissolution test. The dynamic structural changes of the gel layer formed during swelling of tablets containing HPMC were followed by force-displacement measurements (fig. 2). The force required for probe to penetrate the swollen tablet decreased with time as the swelling proceeded and gel strength was reduced. Similar resulted has been reported for the relation between the physical properties of a xanthan matrix in the absence or presence of calcium ions and its influence on the release of pentoxifylline[11]. Force transition regions in a force displacement textural profile of a swollen tablet has been defined earlier[2021]. The total work of penetration calculated as the area under the force displacement curve indicating matrix stiffness or rigidity[22]. Change in work of penetration versus time of tablets after exposure to medium was extended as the hydration increased. A sharp decrease in work of penetration from 0 h (dry tablet) to 1 h could be observed which reflected the initial high rate of hydration of tablets which incidentally coincided with high rate of water uptake and gel formation. Hydrated tablets demonstrated lower values for work of penetration during 2 to 8 h. Total work penetration of tablet after dissolution test was decreased with time. The total tablet thickness and swelling front movement using force-displacement profiles provided more evidence that the rate and extent of gel formation was significantly influenced by the nature of excipient used[11]. In fact, the obtained results confirmed that the system containing a gel with a lower strength was greater susceptible to erosion and chains disentanglement as mentioned previously[9]. Linear correlations were observed among drug dissolution, polymer content and parameters of texture analysis including hydrogel thickness for formulations containing hydrophilic polyethylene oxide (PEO)[23]. In addition, the results of textural analysis indicated that the total work of penetration was higher for matrix with polymer blend compared to HPMC-only matrix in water and phosphate buffer pH 6.8[24].


Solid Dispersion Matrix Tablet Comprising Indomethacin-PEG-HPMC Fabricated with Fusion and Mold Technique.

Mesnukul A, Yodkhum K, Phaechamud T - Indian J Pharm Sci (2009)

Force displacement profiles of tablets.Force displacement profiles for formulation of tablets containing 25% HPMC in 70:30 PEG 4000:PEG 400 system at different time points (n=3)
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2865813&req=5

Figure 0002: Force displacement profiles of tablets.Force displacement profiles for formulation of tablets containing 25% HPMC in 70:30 PEG 4000:PEG 400 system at different time points (n=3)
Mentions: Dry tablet (before dissolution test) containing 25% HPMC exhibited higher total work penetration than tablet after dissolution test at different time intervals (figs. 2 and 3). Total work penetration of tablet containing 25% HPMC was decreased with time during dissolution test. The dynamic structural changes of the gel layer formed during swelling of tablets containing HPMC were followed by force-displacement measurements (fig. 2). The force required for probe to penetrate the swollen tablet decreased with time as the swelling proceeded and gel strength was reduced. Similar resulted has been reported for the relation between the physical properties of a xanthan matrix in the absence or presence of calcium ions and its influence on the release of pentoxifylline[11]. Force transition regions in a force displacement textural profile of a swollen tablet has been defined earlier[2021]. The total work of penetration calculated as the area under the force displacement curve indicating matrix stiffness or rigidity[22]. Change in work of penetration versus time of tablets after exposure to medium was extended as the hydration increased. A sharp decrease in work of penetration from 0 h (dry tablet) to 1 h could be observed which reflected the initial high rate of hydration of tablets which incidentally coincided with high rate of water uptake and gel formation. Hydrated tablets demonstrated lower values for work of penetration during 2 to 8 h. Total work penetration of tablet after dissolution test was decreased with time. The total tablet thickness and swelling front movement using force-displacement profiles provided more evidence that the rate and extent of gel formation was significantly influenced by the nature of excipient used[11]. In fact, the obtained results confirmed that the system containing a gel with a lower strength was greater susceptible to erosion and chains disentanglement as mentioned previously[9]. Linear correlations were observed among drug dissolution, polymer content and parameters of texture analysis including hydrogel thickness for formulations containing hydrophilic polyethylene oxide (PEO)[23]. In addition, the results of textural analysis indicated that the total work of penetration was higher for matrix with polymer blend compared to HPMC-only matrix in water and phosphate buffer pH 6.8[24].

Bottom Line: This inert carrier system comprising 7:3 polyethylene glycol 4000: polyethylene glycol 400 could effectively enhance the solubility of indomethacin and an addition of hydroxypropylmethylcellulose could sustain the drug release.Least square fitting the experimental dissolution data to the mathematical expressions (power law, first-order, Higuchi's and zero-order) indicated the drug release kinetics primarily as Fickian diffusion.Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, indomethacin, by using polyethylene glycol-hydroxypropylmethylcellulose matrix system prepared with melting and mold technique.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.

ABSTRACT
The purpose of this study is to fabricate the polyethylene glycol matrix tablet by mold technique. Indomethacin and hydroxypropylmethylcellulose were used as model drug and polymer, respectively, in PEG matrix system. The physical and drug release characteristics of developed matrix tablet were studied. This inert carrier system comprising 7:3 polyethylene glycol 4000: polyethylene glycol 400 could effectively enhance the solubility of indomethacin and an addition of hydroxypropylmethylcellulose could sustain the drug release. Scanning electron microscope photomicrograph indicated the drug diffusion outward through the porous network of this developed matrix tablet into the dissolution fluid. Least square fitting the experimental dissolution data to the mathematical expressions (power law, first-order, Higuchi's and zero-order) indicated the drug release kinetics primarily as Fickian diffusion. Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, indomethacin, by using polyethylene glycol-hydroxypropylmethylcellulose matrix system prepared with melting and mold technique.

No MeSH data available.