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Design and optimization of floating drug delivery system of acyclovir.

Kharia AA, Hiremath SN, Singhai AK, Omray LK, Jain SK - Indian J Pharm Sci (2010)

Bottom Line: Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2).The closeness of predicted and observed values for t(50%) and t(70%) indicates validity of derived equations for the dependent variables.The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix.

View Article: PubMed Central - PubMed

Affiliation: Oriental College of Pharmacy, Raisen Road, Bhopal-462 021, India.

ABSTRACT
The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 3(2) full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t(50%)) and 70% (t(70%)) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t(50%) and t(70%) indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix.

No MeSH data available.


Related in: MedlinePlus

Response surface plot showing effect of factorial variables on t50%.HPMC indicates hydroxypropylmethylcellulose; Y1 indicates dissolution data at t70%. Time taken to dissolve 50% of drug from factorial formulations (t50%) were () 0-2; () 2-4; () 4-6; () 6-8; () 8-10; () 10-12.
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Figure 4: Response surface plot showing effect of factorial variables on t50%.HPMC indicates hydroxypropylmethylcellulose; Y1 indicates dissolution data at t70%. Time taken to dissolve 50% of drug from factorial formulations (t50%) were () 0-2; () 2-4; () 4-6; () 6-8; () 8-10; () 10-12.

Mentions: Validity of the above equations was verified by designing two check point formulations (C1 and C2) taking values of the independent variables for prefixed value of t50% and t70% and studying the drug release profiles. The dissolution parameters predicted from the equations derived and those observed from experimental results are summarized in the Table 7. The closeness of predicted and observed values for t50%and t70% indicates validity of derived equations for the dependent variables. Response surface plots are presented to show the effects of X1and X2on t50%and t70%. Good agreement was observed between the predicted and observed data of dissolution profiles is also a reflection of good applicability of the selected formulation. The computer generated (using ‘PCP Disso 2000 V3 software) response surfaces graph for the effect of factorial variables on t50%and t70% are shown in figs 4] and 5, respectively. The data demonstrate that both X1(amount of psyllium husk) and X2(amount of HPMC K4M) affect the drug release (t50%and t70%). As the amount of the polymer in the formulations increase, the drug release rate decreases. It can be concluded that the drug release pattern may be changed by appropriate selection of the X1 and X2 levels.


Design and optimization of floating drug delivery system of acyclovir.

Kharia AA, Hiremath SN, Singhai AK, Omray LK, Jain SK - Indian J Pharm Sci (2010)

Response surface plot showing effect of factorial variables on t50%.HPMC indicates hydroxypropylmethylcellulose; Y1 indicates dissolution data at t70%. Time taken to dissolve 50% of drug from factorial formulations (t50%) were () 0-2; () 2-4; () 4-6; () 6-8; () 8-10; () 10-12.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3116305&req=5

Figure 4: Response surface plot showing effect of factorial variables on t50%.HPMC indicates hydroxypropylmethylcellulose; Y1 indicates dissolution data at t70%. Time taken to dissolve 50% of drug from factorial formulations (t50%) were () 0-2; () 2-4; () 4-6; () 6-8; () 8-10; () 10-12.
Mentions: Validity of the above equations was verified by designing two check point formulations (C1 and C2) taking values of the independent variables for prefixed value of t50% and t70% and studying the drug release profiles. The dissolution parameters predicted from the equations derived and those observed from experimental results are summarized in the Table 7. The closeness of predicted and observed values for t50%and t70% indicates validity of derived equations for the dependent variables. Response surface plots are presented to show the effects of X1and X2on t50%and t70%. Good agreement was observed between the predicted and observed data of dissolution profiles is also a reflection of good applicability of the selected formulation. The computer generated (using ‘PCP Disso 2000 V3 software) response surfaces graph for the effect of factorial variables on t50%and t70% are shown in figs 4] and 5, respectively. The data demonstrate that both X1(amount of psyllium husk) and X2(amount of HPMC K4M) affect the drug release (t50%and t70%). As the amount of the polymer in the formulations increase, the drug release rate decreases. It can be concluded that the drug release pattern may be changed by appropriate selection of the X1 and X2 levels.

Bottom Line: Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2).The closeness of predicted and observed values for t(50%) and t(70%) indicates validity of derived equations for the dependent variables.The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix.

View Article: PubMed Central - PubMed

Affiliation: Oriental College of Pharmacy, Raisen Road, Bhopal-462 021, India.

ABSTRACT
The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 3(2) full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t(50%)) and 70% (t(70%)) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t(50%) and t(70%) indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix.

No MeSH data available.


Related in: MedlinePlus