Formulation Development of Porous Mannitol carrier: Improving the dissolution of poorly soluble drugs

Abstract

Major challenges in the design of oral dosage forms are their low solubility and low bioavailability. Improving the dissolution of these oral dosage forms are one of the most challenging tasks for the formulation scientists as most of the drug candidates are highly lipophilic in nature. Telmisartan and Ezetimibe belongs to the BCS class II, having high lipophilicity, poor water solubility and poor dissolution. The objective of this work was to improve the dissolution rate of poorly water soluble drugs by using porous carrier drug delivery system. Templating based spray drying methodology was used to prepare porous mannitol. Drug (Telmisartan, Ezetimibe) loaded porous mannitol carriers then characterized by P-XRD, DSC, SEM, BET surface area analysis and ATR-FTIR. ATR-FTIR studies showed complete removal of templating agent from carrier. P-XRD and DSC studies confirmed nano- confinement of drug in crystalline form. In vitro dissolution study results indicated that porous mannitol prepared using tartaric acid as templating agent showed significant improvement in dissolution rate than pure drugs and respective physical mixtures .These results suggest that, these porous carriers can be useful as drug carriers for improving the dissolution of lipophilic drugs.
 Keywords: Templating agent, Spray drying, Mannitol, Surface area, Tartaric acid.

Design and Evaluation of Liquisolid Compacts of Nebivolol Hydrochloride

“…X-ray powder diffraction patterns were recorded on XRD Maxima 7000 Shimadzu, Japan. The scanning rate employed was 6 ° min -1 over the 10 to 50 ° diffraction angle (2θ) range [41].…”

“…The optimized liquisolid formulation was subjected to accelerated stability study and carried out at 40±2 °C/75±5 % RH., as per ICH guidelines Q1A (R2) 2003. The formulation was kept in air-tight glass vials and assayed periodically, at the time points of 0,1, 2, 3 mo means on 1 st , 30 th , 60 th, and 90 th day, for drug content dissolution performance [27,41].…”

Formulation Development and Evaluation of Injectable Depot Suspension

“…At the end of three weeks physical mixture of excipient with drug were analysed by using FTIR spectrophotometer (FTIR-8400S; Shimadzu, Asia Specific Pvt. Ltd. Singapore) Sample (2 mg) was mixed with KBr (50 mg) and formed pellet in manual press(KBr press-1.5 kg pressure) was placed in the sample holder and spectral scanning was taken in the wavelength region between 4000-700 cm/s with scan speed of 1 cm/ [18].…”

“…A small drop of suspension was tiled at glass slide to observe the morphology of micro-suspension under the high times optics microscope. Samples place on the glass surface were air dried and then follow by oven drying quickly [18]. After oven-drying, the samples were fixed on an SEM stab using double-sided adhesive tape and coated with gold at 20 mA for 2 minute using an auto fine coater (Ion sputter JFC 1600).…”