It was also reported that due to this poor dissolution rate ATC has bioavailability of only 12% from a tablets dosage form (40 mg). This undesired characteristic makes ATC to stay long time in gastro intestinal mucosa, which leads to gastro intestinal damage. ATC belongs to BCS II drugs, like all BCS class II drugs, solubility and dissolution is the rate limiting step for oral bioavailability. It is most widely used anti-hyperlipidemic drug among the all statin derivatives and it was also known by bestselling statin. It acts by inhibiting HMG Co A reductase enzymes like other statins. ATC belongs to class of anti-hyperlipidemic drugs. Hence, the current project work deals with the improving of the dissolution rate and solid state stability by restricting the movement of Atorvastatin calcium (ATC) using gel liquisolid compact systems. Some of the other applications of gel liquisolid technique are solubility and dissolution improvement, flowability and compressibility, designing of sustained release tablets, solid state stability enhancement and bioavailability enhancement. A good bioavailability was also related to the fact that the drug did not precipitate out, but staying in a solubilized form when the gel interacted with the aqueous gastric fluids. Gel based liquisolid compact approach is an extreme case of viscosity enhancement that restricts the molecular motion of drug molecules, in which the movement of the dispersion phase is restricted by interlacing three dimensional network of particles or solvated macromolecules of dispersed medium. Among all these methods the use of liquisolid system is considered to be the most promising method to enhance dissolution.
The dissolution characteristics of poorly water soluble dugs can be enhanced by different methods via pH adjustment, solubilization, co-solvents, self-emulsification, micro emulsion, drug complexation, polymeric modification, particle size reduction, the pro-drug approach, use of a solid solutions and surfactant as a solubilizing agent. The oral absorption of drugs is most often controlled by dissolution in the gastrointestinal tract. The major hindrance in developing a pharmaceutical dosage form of water insoluble drug is its poor dissolution rate. From the obtained pharmacokinetic data such as AUC, t max and C max through in vivo bioavailability studies it was established that GLS have shown better bioavailability compared to that of prepared DCT tablets.Ĭonclusion: This study confirms that Atorvastatin calcium prepared by GLS have better dissolution and bioavailability compare to conventional DCT dosage form and therefore GLS could be a promising drug delivery for Atorvastatin calcium.Ītorvastatin calcium Gel liquisolid compact Neusilin ® US2 Dissolution rate BioavailabilityīCS class II and IV drugs, which have low solubility, provide a number of challenges for formulation scientists working on oral delivery of drugs. DSC and XRD studies revealed that the drug in the GLS had been solubilized. in vitro dissolution studies of the prepared GLS had shown maximum dissolution within one hour when compared to that of prepared DCT tablets. Results: The solubility was found to be highest in propylene glycol (150.05 ± 0.4278 mg/mL). Finally, the ideal batches (GLS1 and DCT 1) were subjected for in vivo bioavailability studies.
Structural analysis of GLS was done using differential scanning calorimetry (DSC) and X- ray powder diffraction (XRD) techniques. Gel liquisolid compacts (GLS1-GLS10) and directly compressible tablets (DCT 1 and DCT 2) of Atorvastatin calcium were prepared and evaluated for flow properties, post compression parameters and in vitro dissolution studies. Materials and Methods: The preformulation studies like solubility studies of API in different non-volatile solvents, optimization of gelling agent and adsorbent quantity were performed. Background: BCS class II and IV drugs, which have low solubility, provide a number of challenges for formulation scientists working on oral delivery of drugs.Īims: The aim and purpose of the present work was to design a gel liquisolid tablets for Atorvastatin calcium a water insoluble drug to increase its dissolution rate there by its bioavailability.
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