Enhancement of dissolution profile by solid dispersion (kneading) technique

Abstract

This article investigates enhancement of the dissolution profile of valdecoxib using solid dispersion with PVP. The article also describes the preparation of fast-dissolving tablets of valdecoxib by using a high amount of superdisintegrants. A phase solubility method was used to evaluate the effect of various water-soluble polymers on aqueous solubility of valdecoxib. Polyvinyl pyrrolidone (PVP K-30) was selected and solid dispersions were prepared by the method of kneading. Dissolution studies using the USP paddle method were performed for solid dispersions of valdecoxib. Infrared (IR) spectroscopy, differential scanning calorimetry (DSC), and x-ray diffractometry (XRD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Tablets were formulated containing solid dispersion products and compared with commercial products. IR spectroscopy, XRD, and DSC showed no change in the crystal structure of valdecoxib. Dissolution of valdecoxib improved significantly in solid dispersion products (< 85% in 5 minutes). Tablets containing solid dispersion exhibited better dissolution profile than commercial tablets. Thus, the solid dispersion technique can be successfully used for improvement of dissolution of valdecoxib.

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“…Which results in a lack of crystallinity, solubilization effect of carrier and improved wettability. [26] …”

Improved dissolution of a poorly water soluble drug in solid dispersions with polymeric and non-polymeric hydrophilic additives

“…These »amorphous alloys« permit creation of custom pharmaceuticals with unique properties by selection of appropriate interacting excipients (12). Numerous reports have cited dissolution rate improvement of poorly soluble drugs through production of SDs using various hydrophilic carriers, such as polyvinylpyrrolidone, hydroxypropyl methylcellulose, sugars, and mannitol (13)(14)(15)(16). Dispersions of IBS were formed using two non-polymeric excipients, tartaric acid and mannitol, and two polymeric excipients, PVP and HPMC.…”

“…Sample mass maintaining the sink conditions (i.e., three times the solubility) was filled into hard gelatin capsule shells. At predetermined intervals (5,15,30,60,90,120,240, 360 and 480 min), samples were withdrawn (with replacement of equal volume of an pre-warmed medium into the vessel), filtered, appropriately diluted and analyzed for drug concentration using HPLC. It was first confirmed that the method was specific for the analysis of IBS and additives did not interfere with the drug.…”

Formulation of Nanoparticles of Telmisartan Incorporated in Carboxymethylchitosan for the Better Drug Delivery and Enhanced Bioavailability

“…Poor bioavailability after oral administration of the TLM is due to its bioavailability that is 42-58%, and biological half-life is only 24 hrs. Thus, increasing dissolution and aqueous solubility of TLM is of therapeutic importance [42][43][44][45][46][47][48][49]. Various approaches for enhancing solubility and oral efficacy of TLM used were solid dispersion and inclusion complexation [50][51][52].…”