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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

Scanning electron microscope photographs of the in situ formed AMCScanning electron microphotographs of coating membrane obtained A) before dissolution, showing outer dense nonporous region and containing 8% w/v glycerol at 1000 X, B) before dissolution showing large inner porous region and containing 12% w/v glycerol at 2000 X, C) after complete dissolution showing net like structure and containing 8% w/v glycerol at 2000 X.
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Figure 0001: Scanning electron microscope photographs of the in situ formed AMCScanning electron microphotographs of coating membrane obtained A) before dissolution, showing outer dense nonporous region and containing 8% w/v glycerol at 1000 X, B) before dissolution showing large inner porous region and containing 12% w/v glycerol at 2000 X, C) after complete dissolution showing net like structure and containing 8% w/v glycerol at 2000 X.

Mentions: For SEM studies, 15% w/v EC membranes with varying proportions, as mentioned above of pore forming agent (glycerol) were obtained before and after complete dissolution. SEM revealed, membrane obtained before dissolution (8% w/v glycerol) had an outer dense non porous region (fig. 1 A) and an inner lighter porous region. After complete dissolution, the exhausted membrane showed large number of pores similar to a net like structure (fig. 1 C) and formulation prepared with this membrane did not show swelling or rupturing. Membrane containing 12% w/v of glycerol showed similar nonporous but larger inner porous regions (fig. 1 B) with swelling or elongation and slight rupture at the end of 7 h of dissolution study. Membrane containing higher proportion of glycerol (20% w/v) showed larger pores and formulation prepared with this membrane caused bursting within an hour of dissolution study. SEM studies suggested concentration of plasticizer to be an important parameter in deciding membrane strength as, high concentrations of glycerol made asymmetric membrane correspondingly weak and then caused rupturing. Membranes with 12%,16% and 20% w/v glycerol showed flimsy nature (which could account for their rupturing during dissolution) during preparation process which, involved pouring of coating solution inside hard gelatin capsule but were hardened during drying process. These results could probably be due to presence of plasticizer in hard gelatin capsule itself which might infact add up to the concentration of plasticizer present in asymmetric membrane inside hard gelatin capsule. Based on SEM study, 8% w/v glycerol as a plasticizer was selected for further studies.


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)

Scanning electron microscope photographs of the in situ formed AMCScanning electron microphotographs of coating membrane obtained A) before dissolution, showing outer dense nonporous region and containing 8% w/v glycerol at 1000 X, B) before dissolution showing large inner porous region and containing 12% w/v glycerol at 2000 X, C) after complete dissolution showing net like structure and containing 8% w/v glycerol at 2000 X.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 0001: Scanning electron microscope photographs of the in situ formed AMCScanning electron microphotographs of coating membrane obtained A) before dissolution, showing outer dense nonporous region and containing 8% w/v glycerol at 1000 X, B) before dissolution showing large inner porous region and containing 12% w/v glycerol at 2000 X, C) after complete dissolution showing net like structure and containing 8% w/v glycerol at 2000 X.
Mentions: For SEM studies, 15% w/v EC membranes with varying proportions, as mentioned above of pore forming agent (glycerol) were obtained before and after complete dissolution. SEM revealed, membrane obtained before dissolution (8% w/v glycerol) had an outer dense non porous region (fig. 1 A) and an inner lighter porous region. After complete dissolution, the exhausted membrane showed large number of pores similar to a net like structure (fig. 1 C) and formulation prepared with this membrane did not show swelling or rupturing. Membrane containing 12% w/v of glycerol showed similar nonporous but larger inner porous regions (fig. 1 B) with swelling or elongation and slight rupture at the end of 7 h of dissolution study. Membrane containing higher proportion of glycerol (20% w/v) showed larger pores and formulation prepared with this membrane caused bursting within an hour of dissolution study. SEM studies suggested concentration of plasticizer to be an important parameter in deciding membrane strength as, high concentrations of glycerol made asymmetric membrane correspondingly weak and then caused rupturing. Membranes with 12%,16% and 20% w/v glycerol showed flimsy nature (which could account for their rupturing during dissolution) during preparation process which, involved pouring of coating solution inside hard gelatin capsule but were hardened during drying process. These results could probably be due to presence of plasticizer in hard gelatin capsule itself which might infact add up to the concentration of plasticizer present in asymmetric membrane inside hard gelatin capsule. Based on SEM study, 8% w/v glycerol as a plasticizer was selected for further studies.

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