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Simvastatin is an Antilipidemic agent. The aim is to formulate and evaluate immediate release Simvastatin tablets prepared by wet granulation method. Sodium starch glycolate and crosscarmellose sodium were used as superdisintegrants. Formulations were prepared by Simvastatin with different concentration (1%, 2% and 3%) of crosscarmellose sodium and sodium starch glycolate. Formulations were evaluated for different pre and post compression parameter and in vitro drug release studies. The FTIR studies showed that there is no interaction between the drug and polymer. The results of pre compression parameters of batch I1 to I6 were compared with prescribed limits. It showed that batch I1 to I6 powder blend exhibit good flow property and compressibility property. In formulation I1-I6, disintegration time was observed 3–8 min and 100% drug released within 10–60 min time interval. Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablets of Simvastatin was successfully done and I2 showed almost 100% drug release at 10 min.

The objective of this investigation was to prepare mucoadhesive microspheres of ketorolac for nasal delivery to avoid gastrointestinal side effects of conventional dosage form. Mucoadhesive microspheres were prepared using carbopol, polycarbophil and chitosan as polymer by spray drying method. The process and formulation parameters were varied to study the effect on the yield and particle size. Microspheres were characterized for surface morphology, encapsulation efficiency, swelling behavior, mucoahesion properties, interaction studies using FTIR and DSC, in vitro drug release, ex vivo nasal cilio toxicity studies and in vivo anti-inflammatory and analgesic activity. Prepared microspheres were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 79-92%. The results showed that the process parameters significantly affect the particle size (10.29-16.75 μm) and yield of microspheres (36.53-56.69%). Interaction studies revealed that there were no drug to polymer interactions. Prepared microspheres exhibited good swelling and mucoadhesion strength which confined the strong mucoadhesive property of microspheres. Ketorolac release from the microspheres was extended up to 8 h and exhibited fickian drug release kinetics with best fit to higuchi model. The drug loaded microspheres were found to be nontoxic to nasal mucosa. The anti-inflammatory and analgesic effects of formulation showed a significant increase (p < 0.05) in percent inhibition value of up to 8 h when compared with ketorolac. In conclusion, spray dried microspheres based on chitosan could be suitable nasal delivery system for the administration of ketorolac.

The objective of this investigation was to achieve controlled drug release of Aceclofenac (ACE) microspheres and to minimize local side-effects in the gastrointestinal tract (GIT). Sustained release chitosan microspheres containing ACE were prepared using double-emulsion solvent evaporation method (O/W/O). Chitosan microspheres were prepared by varying drug to polymer ratio (1:3, 1:4, 1:5 and 1:6). Microspheres were characterized for morphology, swelling behavior, mucoadhesive properties, FTIR and DSC study, drug loading efficiency, in vitro release, release kinetics, and in vivo study was performed on rat model. ACE-loaded microspheres were successfully prepared having production yield, 57-70% w/w. Drug encapsulation efficiency was ranging from 53-72% w/w, Scanning electron microscopy (SEM) revealed particle size of microspheres was between 39 and 55 mum. FTIR spectra and DSC thermograms demonstrated no interaction between drug and polymer. The in vitro release profiles of drug from chitosan microspheres showed sustained-release pattern of the drug in phosphate buffer, pH 6.8. In vitro release data showed correlation (r20.98), good fit with Higuchi/Korsmeyer-Peppas models, and exhibited Fickian diffusion. ACE microspheres demonstrated controlled delivery of aceclofenac and apparently, no G.I.T. erosion was noticed.

Microencapsulation of the anti-inflammatory drug aceclofenac (ACE) was investigated as a means of controlling drug release and minimizing or eliminating local side effects.Microspheres were prepared by a spray-drying technique using solutions of ACE and three polymers, namely, carbopol, chitosan, and polycarbophil, in different weight ratios.The spray-dried mucoadhesive microspheres were characterized in terms of shape (scanning electron microscope), size (6.60-8.40 mum), production yield (34.10-55.62%), and encapsulation efficiency (58.14-90.57%). In vitro release studies were performed in phosphate buffer (pH 6.8) up to 10 hours. The spray-drying process of solutions of ACE with polymeric blends can give prolonged drug release. The in vitro release data were well fit into Higuchi and Korsmeyer-Peppas model and followed Fickian diffusion mechanism. In vivo data showed that the administration of ACE in polymeric microspheres prevented the gastric side effects.The formulations here described can be proposed for the oral administration of nonsteroidal anti-inflammatory drugs with minimal side effects on gastric mucosa.