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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

Comparative release profiles of F5 in mediums of different osmotic pressureComparison of in vitro ketoprofen release profiles (n=3 along with standard deviations) from F5 in dissolution medium of different osmotic pressures. F-5a (–□–) (3.673 mm Hg), F-5b (–Δ–) (7.348 mm Hg), F-5c (–◊–) (11.012 mm Hg) and F-5d (–×–) (14.695 mm Hg).
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Figure 0004: Comparative release profiles of F5 in mediums of different osmotic pressureComparison of in vitro ketoprofen release profiles (n=3 along with standard deviations) from F5 in dissolution medium of different osmotic pressures. F-5a (–□–) (3.673 mm Hg), F-5b (–Δ–) (7.348 mm Hg), F-5c (–◊–) (11.012 mm Hg) and F-5d (–×–) (14.695 mm Hg).

Mentions: Since the study was based on osmotic delivery therefore, to study effect of varying osmotic pressure, release studies of optimized formulation F5 were conducted in media of different osmotic pressures (fig. 4). Cumulative % drug release after 12 h from F-5a was found to be 57.92±2.83, from F-5b i t was 50.36±0.65, from F-5c it was 30.59±0.93 and from F-5d it was 16.38±0.71. Results of release studies suggested, drug release to be highly dependant on osmotic pressure of release media. Ketoprofen release from F5 decreased as osmotic pressures of release medium increased. R2 of 0.9873 from linear line obtained when release rate was plotted against osmotic pressure difference (osmotic pressure inside the formulation was found to be 18.369 mm Hg) shown in fig. 5 suggested, osmotic pumping as primary mechanism governing drug release from the developed formulations.


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)

Comparative release profiles of F5 in mediums of different osmotic pressureComparison of in vitro ketoprofen release profiles (n=3 along with standard deviations) from F5 in dissolution medium of different osmotic pressures. F-5a (–□–) (3.673 mm Hg), F-5b (–Δ–) (7.348 mm Hg), F-5c (–◊–) (11.012 mm Hg) and F-5d (–×–) (14.695 mm Hg).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 0004: Comparative release profiles of F5 in mediums of different osmotic pressureComparison of in vitro ketoprofen release profiles (n=3 along with standard deviations) from F5 in dissolution medium of different osmotic pressures. F-5a (–□–) (3.673 mm Hg), F-5b (–Δ–) (7.348 mm Hg), F-5c (–◊–) (11.012 mm Hg) and F-5d (–×–) (14.695 mm Hg).
Mentions: Since the study was based on osmotic delivery therefore, to study effect of varying osmotic pressure, release studies of optimized formulation F5 were conducted in media of different osmotic pressures (fig. 4). Cumulative % drug release after 12 h from F-5a was found to be 57.92±2.83, from F-5b i t was 50.36±0.65, from F-5c it was 30.59±0.93 and from F-5d it was 16.38±0.71. Results of release studies suggested, drug release to be highly dependant on osmotic pressure of release media. Ketoprofen release from F5 decreased as osmotic pressures of release medium increased. R2 of 0.9873 from linear line obtained when release rate was plotted against osmotic pressure difference (osmotic pressure inside the formulation was found to be 18.369 mm Hg) shown in fig. 5 suggested, osmotic pumping as primary mechanism governing drug release from the developed formulations.

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