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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 in vitro dissolution profilesComparative in vitro dissolution profiles (n=3 along with standard deviations) for all formulations along with the marketed formulation. F1 (–◆–); F2 (–■–); F3 (–Δ–); F4 (–×–); F5 (–●–); F6 (–□–); F7 (– ‌ –); F8 (–▲–) F9 (–––); Marketed Formulation (–◊–)
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Figure 0002: Comparative in vitro dissolution profilesComparative in vitro dissolution profiles (n=3 along with standard deviations) for all formulations along with the marketed formulation. F1 (–◆–); F2 (–■–); F3 (–Δ–); F4 (–×–); F5 (–●–); F6 (–□–); F7 (– ‌ –); F8 (–▲–) F9 (–––); Marketed Formulation (–◊–)

Mentions: In vitro studies were carried out for all the prepared formulations along with the marketed formulation (fig. 2) and the solubility enhancer for the drug (fig. 3). Order of influence for t50% of F1, F2 and F3 formulations with concentration of EC at lower levels (10% w/v) were F1 (13.16 h) > F2 (11.14 h) > F3 (9.26 h). Descending order of influence meant, incorporation of NaCl in F2 and F3 results in development of significant osmotic pressure inside the capsular system, creating an osmotic pressure gradient between inner portion of the capsular system and dissolution medium, which, increased the release rate of ketoprofen far more than F1 formulation, even though ketoprofen had poor solubility in SGF suggesting, release of ketoprofen from in situ formed AMC to be independent of pH. Order of influence for t50% of F4, F5 and F6 formulations with concentration of EC at medium level (15% w/v) were F4 (15.02 h) > F5 (12.50 h) > F6 (11.32 h). Here once again, influence of NaCl in increasing release rate from in-situ formed phase transited AMC was demonstrated even though, osmotic effect due to osmogen was constrained. Decreased ketoprofen release from these formulations as compared to F1, F2 and F3 formulations might probably be due to increased diffusional path for drug to traverse before being released into the dissolution medium. Order of influence for t50% of F7, F8 and F9 formulations with concentration of EC at higher level (20% w/v) were F7 (16.42 h) > F8 (15.190 h) > F9 (14.23 h) suggesting, influence of NaCl again, in drug release though here the influence of EC concentration at higher level was substantial in constraining drug release probably due to increased drug holding capacity for the polymer.


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 in vitro dissolution profilesComparative in vitro dissolution profiles (n=3 along with standard deviations) for all formulations along with the marketed formulation. F1 (–◆–); F2 (–■–); F3 (–Δ–); F4 (–×–); F5 (–●–); F6 (–□–); F7 (– ‌ –); F8 (–▲–) F9 (–––); Marketed Formulation (–◊–)
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 0002: Comparative in vitro dissolution profilesComparative in vitro dissolution profiles (n=3 along with standard deviations) for all formulations along with the marketed formulation. F1 (–◆–); F2 (–■–); F3 (–Δ–); F4 (–×–); F5 (–●–); F6 (–□–); F7 (– ‌ –); F8 (–▲–) F9 (–––); Marketed Formulation (–◊–)
Mentions: In vitro studies were carried out for all the prepared formulations along with the marketed formulation (fig. 2) and the solubility enhancer for the drug (fig. 3). Order of influence for t50% of F1, F2 and F3 formulations with concentration of EC at lower levels (10% w/v) were F1 (13.16 h) > F2 (11.14 h) > F3 (9.26 h). Descending order of influence meant, incorporation of NaCl in F2 and F3 results in development of significant osmotic pressure inside the capsular system, creating an osmotic pressure gradient between inner portion of the capsular system and dissolution medium, which, increased the release rate of ketoprofen far more than F1 formulation, even though ketoprofen had poor solubility in SGF suggesting, release of ketoprofen from in situ formed AMC to be independent of pH. Order of influence for t50% of F4, F5 and F6 formulations with concentration of EC at medium level (15% w/v) were F4 (15.02 h) > F5 (12.50 h) > F6 (11.32 h). Here once again, influence of NaCl in increasing release rate from in-situ formed phase transited AMC was demonstrated even though, osmotic effect due to osmogen was constrained. Decreased ketoprofen release from these formulations as compared to F1, F2 and F3 formulations might probably be due to increased diffusional path for drug to traverse before being released into the dissolution medium. Order of influence for t50% of F7, F8 and F9 formulations with concentration of EC at higher level (20% w/v) were F7 (16.42 h) > F8 (15.190 h) > F9 (14.23 h) suggesting, influence of NaCl again, in drug release though here the influence of EC concentration at higher level was substantial in constraining drug release probably due to increased drug holding capacity for the polymer.

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