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Objective To establish an in vitro accelerated release method of triptorelin acetate microspheres with good in vi-tro/in vivo correlation(IVIVC). Methods The in vivo release of triptorelin acetate from microspheres was obtained by residual method in rats. Influences of pH value,concentration of ethanol,temperature,rotation speed and concentration of antiseptic on the in vitro accel-erated release were studied,then the correlation between in vitro accelerated release and in vivo release of the microspheres was estab-lished by adjusting the release conditions. Results The in vitro accelerated release medium of triptorelin acetate microspheres composed of 15%ethanol solution(containing 0.06%Tween 80 and 0.1%benzalkonium chloride)at 55℃with rotating rate of 200 r/min. The cumulative release of triptorelin acetate from microspheres was 87.35%at 30 h under accelerated release condition,equivalent to in vivo release for 30 days. The established in vitro accelerated release had a good correlation with that of in vivo(y=0.8845x+12.4510, R2=0.9938). Conclusion The in vitro accelerated release of triptorelin acetate microspheres could correlate well with in vivo release and has a potential application in rapid and effective evaluation of triptorelin acetate microspheres.
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A single dose, randomized, complete and four treatment cross over study was conducted in healthy human subjects for IVIVC of venlafaxine.HCl, Plasma concentrations were estimated by a simple, rapid, sensitive and validated LCMS method, Cetirizine was used as the internal standard (IS), The analytes and the IS were extracted from the human plasma by liquid?liquid extraction technique, The reconstituted samples were chromatographed on Kromasil C18 column using an isocratic solvent mixture [acetonitrile?water, 90:10 (v/v)] at a flow rate of 0.5 mL/min, Method validation was performed as per FDA guidelines and the results met the acceptance criteria, USP dissolution apparatus I (Basket) and pH 6.8 at 100 rpm was found to yield acceptable IVIVC for the drug, The developed dissolution method would discriminate bioinequivalent batches, A ?Level A? correlation was observed for the selected formulations at the in vitro dissolution conditions developed, The dissolution method predicted the best absorption rate for the selected modified release formulations, The validity of the correlation was assessed by determining how well the IVIVC model could predict the rate and the extent of absorption as characterized by Cmax and AUC, A percent prediction error of = 10 % for C max and AUC obtained establishes the predictability of the developed IVIVC model, It may, therefore, be concluded that the developed dissolution method can surrogate for human bioequivalence study.
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Aims: Oxcarbazepine was formulated as suspension in order to perk up the palatability, augment bioavailability of the product, furthermore extended to estimate good degree of in vitro in vivo correlation (IVIVC). Study Design: Formulation and Evaluation of Oxcarbazepine Suspension: In Vitro/In Vivo Correlation Place and Duration of Study: Birla Institute of Technological Sciences- Hyderabad, India between July 2011 to January 2012 Methodology: Oxcarbazepine had poor aqueous solubility, thus the solubility was increased by hydrotropes then formulated into suspension using taragum as viscosity enhancer. Further validity of dissolution study was extended by In vitro/In vivo correlation using level A method. Results: These suspensions were observed for in vitro dissolution profile and studied for in vivo pharmacokinetic profile, from the obtained values, a level A IVIVC modeling was observed, interestingly from the results attained suspension showed almost 98% drug release (FDR) and 85% drug absorbed (FDA) in 90min. Fascinatingly, from the correlation between FDR and FDA, slope and regression co-efficient obtained was near to 1.0 indicated good linearity. Conclusion: In conclusion, a point-to-point link from the level A which was a keystone of acceptable and reliable correlation was achieved.
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The recent study on gastric retenting drug delivery system (GRDDS) used in Chinese medicinal formule has been summaried and overviewed in this paper. The key problems about the development of GRDDS have been explored, the influence about absence of the system for in vivo-in vitro correlation (IVIVC) analyzed, especially the evaluation on IVIVC model discussed, and the possible approach that artificial neural networks (ANN) are applied in GRDDS for Chinese medicinal formule has been put forward. The processing technology, evaluation of IVIVC, and the advantage, characteristic, and problems of the application of ANN have been studied in order to provide the reference for innovating research of Chinese medicinal formule.