Objectives: This research was aimed to evaluate a novel approach for preparation of mucoadhesive microspheres which can reside in the gastrointestinal tract for an extended time period. The microspheres contained amoxicillin, an anti-bacterial agent useful for the eradication of Helicobacter pylori. Methods: Ten different formulations were prepared by chemical cross-linking technique using gluteraldehyde as a cross linking agent and chitosan as mucoadhesive polymer. Natural release retardant polymers like guar gum, gum ghatti and xanthan gum were employed. All the microspheres were characterized for morphology, particle size, drug entrapment efficiency, swelling index, bioadhesion to mucosal tissue and in vitro drug dissolution and anti-bacterial activity against E. coli. Results: The FTIR and DSC data indicated that there were no interactions between the drug and polymers used. All the microspheres exhibited good flow properties. The microspheres had a spherical shape with rough surface. The microspheres showed a good mucoadhesivity and also anti-bacterial activity. The release of the drug was prolonged to 12h when incorporated into mucoadhesive microspheres. Conclusion: Data obtained in this study concluded that mucoadhesive microspheres of amoxicillin can be used to effectively clear H. pylori from the gastrointestinal tract due to prolonged residence time resulting from mucoadhesion. In this study drug release was diffusion controlled and followed zero order kinetics.
The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.
Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are the major constraints during the development of new product. Various approaches have been used for enhancement of solubility of poorly aqueous soluble drugs, but success of these approaches depends on physical and chemical nature of the molecules being developed. Co-crystallization of drug substances offers a great opportunity for the development of new drug products with superior physicochemical such as melting point, tabletability, solubility, stability, bioavailability and permeability, while preserving the pharmacological properties of the active pharmaceutical ingredient. Co-crystals are multi component systems in which two components, an active pharmaceutical ingredient and a coformer are present in stoichiometric ratio and bonded together with non-covalent interactions in the crystal lattice. This review article presents a systematic overview of pharmaceutical co-crystals, differences between co-crystals with salts, solvates and hydrates are summarized along with the advantages of co-crystals with examples. The theoretical parameters underlying the selection of coformers and screening of co-crystals have been summarized and different methods of co-crystal formation and evaluation have been explained.
Vomiting or emesis is the abnormal emptying of stomach and upper part of intestine through esophagus and mouth. It occurs due to stimulation of the emetic (vomiting) centre situated in the medulla oblongata. Domperidone, a D2 receptor antagonist has antiemetic and prokinetic action is used as a model drug in the present work to prepare Sustained release matrix tablets using various synthetic polymers like Eudragit and HPMC K15 M. The tablets are designed to have a pH dependent release profile in order to prevent initial drug release in the stomach to reduce the possible gastro-irritant and ulcerogenic effects of the drug. Different polymer and diluent concentrations and various compression techniques like wet granulation technique and direct compression techniques were used in order to release the contents of the tablets in a sustained manner over a certain period of time. Domperidone is BCS Class II drug and its solubility was enhanced by preparing solid dispersions using solvent evaporation technique. In the present work solid dispersions containing drug and polymer mixture in the ratio 1:1 was further formulated into tablets by incorporating various synthetic polymers in three different concentrations. The tablets were prepared using different granulating techniques. Formulation (F3) containing drug and polymers in the ratio 1:1 prepared by wet granulation technique could sustain the drug release over a period of 12h and hence considering all the post compression parameters it was optimized as the better formulation. FTIR, DSC, X-Ray Diffraction, SEM studies were performed for optimized solid dispersion mixture and also the optimized formulation. Keywords: Solubility enhancement, Solid dispersions, Solvent Evaporation, Wet granulation, Direct Compression.
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