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In situ formed phase transited drug delivery system of ketoprofen for achieving osmotic, controlled and level a in vitro in vivo correlation.

Philip AK, Pathak K - Indian J Pharm Sci (2008)

Bottom Line: In vitro release studies and statistical test for all the prepared and marketed formulation were done at P >0.05.The drug release was found to be independent of the pH, but dependent on the osmotic pressure of the dissolution medium.In vivo pharmacokinetic studies showed a level A correlation (R(2)>0.99) with 39.24 % relative bioavailability compared to immediate release tablet of ketoprofen.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, Uttar Pradesh-281001, India.

ABSTRACT
A dry process induced phase transited, non disintegrating, controlled release, in situ formed asymmetric membrane capsular system for poorly water soluble drug, ketoprofen, was developed and evaluated both in vitro and in vivo for osmotic and controlled release of the drug. In situ formed asymmetric membrane capsules were prepared using fabricated glass capsule holders via dry, phase inversion process. Effect of varying osmotic pressure of the dissolution medium on drug release was studied. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores and an inner porous region for the prepared asymmetric membrane. In vitro release studies and statistical test for all the prepared and marketed formulation were done at P >0.05. The drug release was found to be independent of the pH, but dependent on the osmotic pressure of the dissolution medium. In vivo pharmacokinetic studies showed a level A correlation (R(2)>0.99) with 39.24 % relative bioavailability compared to immediate release tablet of ketoprofen. Excellent correlation achieved suggested that the in vivo performance of the phase transited in situ formed AMCs could be accurately predicted from their in vitro release profiles and could a means for controlled delivery of drugs with varying solubility.

No MeSH data available.


Related in: MedlinePlus

In vivo release profile of test and reference formulationsComparative plasma concentration time profile (n =3 along with standard deviation) of test formulation (–□–) and reference formulation (–◆–).
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Figure 0006: In vivo release profile of test and reference formulationsComparative plasma concentration time profile (n =3 along with standard deviation) of test formulation (–□–) and reference formulation (–◆–).

Mentions: The relevant pharmacokinetic parameters are listed in Table 2. From fig. 6, it is apparent that the specially designed dosage form effectively sustained and controlled the release of ketoprofen and also maintained elevated plasma concentrations up to the 10th h. Although the statistical analysis of the Cmax and Tmax values for the conventional tablets and the test AMCs were statistically insignificant (P>0.01) at 99% confidence level, there was statistically significant difference (P<0.01) between the elimination half life and AUC for the two formulations of the drug. This suggested the capacity of the test formulation to sustain the release of drug. The reduction in AUC for the conventional tablet could be interpreted as that the formulation with a rapid rate of drug release tends to attain lower systemic bioavailability. This observation could be attributed to the fact that as the drug releases at a rate that exceeds the rate of absorption; it leads not only to side effects but also to first pass metabolism. Test formulations with increased AUC could be attributed to sustained drug release at a lower rate thus not only enhancing the bioavailability which meant enhanced absorption (% relative bioavailability showed an improvement of 39.24%), but also minimizing the first pass metabolism.


In situ formed phase transited drug delivery system of ketoprofen for achieving osmotic, controlled and level a in vitro in vivo correlation.

Philip AK, Pathak K - Indian J Pharm Sci (2008)

In vivo release profile of test and reference formulationsComparative plasma concentration time profile (n =3 along with standard deviation) of test formulation (–□–) and reference formulation (–◆–).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3040868&req=5

Figure 0006: In vivo release profile of test and reference formulationsComparative plasma concentration time profile (n =3 along with standard deviation) of test formulation (–□–) and reference formulation (–◆–).
Mentions: The relevant pharmacokinetic parameters are listed in Table 2. From fig. 6, it is apparent that the specially designed dosage form effectively sustained and controlled the release of ketoprofen and also maintained elevated plasma concentrations up to the 10th h. Although the statistical analysis of the Cmax and Tmax values for the conventional tablets and the test AMCs were statistically insignificant (P>0.01) at 99% confidence level, there was statistically significant difference (P<0.01) between the elimination half life and AUC for the two formulations of the drug. This suggested the capacity of the test formulation to sustain the release of drug. The reduction in AUC for the conventional tablet could be interpreted as that the formulation with a rapid rate of drug release tends to attain lower systemic bioavailability. This observation could be attributed to the fact that as the drug releases at a rate that exceeds the rate of absorption; it leads not only to side effects but also to first pass metabolism. Test formulations with increased AUC could be attributed to sustained drug release at a lower rate thus not only enhancing the bioavailability which meant enhanced absorption (% relative bioavailability showed an improvement of 39.24%), but also minimizing the first pass metabolism.

Bottom Line: In vitro release studies and statistical test for all the prepared and marketed formulation were done at P >0.05.The drug release was found to be independent of the pH, but dependent on the osmotic pressure of the dissolution medium.In vivo pharmacokinetic studies showed a level A correlation (R(2)>0.99) with 39.24 % relative bioavailability compared to immediate release tablet of ketoprofen.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, Uttar Pradesh-281001, India.

ABSTRACT
A dry process induced phase transited, non disintegrating, controlled release, in situ formed asymmetric membrane capsular system for poorly water soluble drug, ketoprofen, was developed and evaluated both in vitro and in vivo for osmotic and controlled release of the drug. In situ formed asymmetric membrane capsules were prepared using fabricated glass capsule holders via dry, phase inversion process. Effect of varying osmotic pressure of the dissolution medium on drug release was studied. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores and an inner porous region for the prepared asymmetric membrane. In vitro release studies and statistical test for all the prepared and marketed formulation were done at P >0.05. The drug release was found to be independent of the pH, but dependent on the osmotic pressure of the dissolution medium. In vivo pharmacokinetic studies showed a level A correlation (R(2)>0.99) with 39.24 % relative bioavailability compared to immediate release tablet of ketoprofen. Excellent correlation achieved suggested that the in vivo performance of the phase transited in situ formed AMCs could be accurately predicted from their in vitro release profiles and could a means for controlled delivery of drugs with varying solubility.

No MeSH data available.


Related in: MedlinePlus