Formulation of Extended-Release Metformin Hydrochloride Matrix Tablets

Purpose: To develop and characterize an oral extended-release matrix tablet of metformin hydrochloride using a combination of a hydrophobic carrier and a hydrophilic polymer, and two types of formulation techniques. Methods: Various metformin hydrochloride formulations containing a hydrophobic carrier (stearic acid) and a hydrophilic polymer (polyethylene oxide) were prepared using a 32 factorial design. Two types of formulation techniques – melt granulation and direct compression – were evaluated. The influence of the carrier, polymer and preparation method on metformin release from the formulations in vitro as well as other physicochemical properties were studied. The release data were subjected to various release kinetic models and also compared with those of a commercial brand. Results: The physicochemical characteristics of all the granules and tablets were generally satisfactory. Optimization results indicate that the release rate of metformin HCl was directly proportional to the levels of stearic acid (SA) and polyethylene oxide (PEO) in the tablet formulations. Release rate was also dependent on the method of granulation used. Kinetic analysis showed that the formulation containing 30 %w/w of polymer exhibited release similar to that of the commercial brand with a similarity factor (f2) of 81.1. Melt granulation was more effective in extending drug release than direct compression. Release mechanism followed most closely the Korsemeyer-Peppas model with a correlation coefficient (r2) and 0.991. Conclusion: The use of a hydrophobic carrier along with a hydrophilic polymer effectively controls the initial rapid release of a highly water soluble drug such as metformin HCl. Hot melt granulation method was especially more effective in achieving this than the direct compression method

Nanosized Technological Approaches for the Delivery of Poorly Water Soluble Drugs: Delivery of poorly water soluble drugs

A major hurdle in pharmaceutical formulation is water insolubility of most of drugs affecting their stability and bioavailability. If the drug is also insoluble in organic medium, it is difficult to deliver it in a sufficiently bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although some approaches are available for enhancing the dissolution of poorly solubledrugs, there has been certain draw backs like use of organic solvents, low drug loading and large doses. However, a new solution to poorly water soluble drug candidates is now available, i.e. nanonisation that leads to much more soluble, more biologically available and safer dosage form of poorly soluble and poorly bioavailable drugs. Controlled release of these drugs is also possible by forming nanostructuredmatrices. In this article, a brief description of production methods of drug nanoparticles and commercialized methods are presented along with brief overview on second generation of drug nanocrystal (Smart crystal technology), controlled release of hydrophobic drugs and recent works thereof are also presented

Functions of Lipids for Enhancement of Oral Bioavailability of Poorly Water-Soluble Drugs

Lipid-based formulations encompass a diverse group of formulations with very different physical appearance, ranging from simple triglyceride vehicles to more sophisticated formulations such as self-emulsifying drug delivery systems (SEDDS). Lipid-based drug delivery systems may contain a broad range of oils, surfactants, and co-solvents. They represent one of the most popular approaches to overcome the absorption barriers and to improve the bioavailability of poorly water-soluble drugs. Diversity and versatility of pharmaceutical grade lipid excipients and drug formulations as well as their compatibility with liquid, semi-solid and solid dosage forms make lipid systems most complex. Digestion of triglyceride lipids, physicochemical characteristics and solubilisation of lipid digestion products as well as intestinal permeability are some of the variable parameters of such formulations. Furthermore, among the factors affecting the bioavailability of the drug from lipid-based formulations are the digestion of lipid, the mean emulsion droplet diameter, the lipophilicity of the drug and the type of lipids. The solubility of the Active Pharmaceutical Ingredient in the Lipid System, the desorption /sorption isotherm and the digestibility of lipid vehicle are important issues to be considered for formulations of isotropic lipid formulations. This review also describes the fate of lipid formulations in the gut and the factors influencing the bioavailability from lipid-based formulations. Novel formulation systems and currently marketed products conclude this review

Isolation and morphological characterization of antibiotic producing actinomycetes

Purpose: To isolate and characterize antibiotic producing actinomycetes from soil samples in Belgaum, Karnataka, India. Methods: Crowded plate technique was used for the isolation of actinomycetes in media such as soybean - casein digest medium and actinomycetes isolation agar. The morphological and cultural characterization of one of the selected strains, designated A-4, was performed as per International Streptomycete Project (ISP). Results: Morphological and cultural studies showed that A-4 belonged to the Actinomycete genus. The morphological and cultural characteristics of the A-4 mutant showed cellular and aerial growth as well as soluble pigment formation in various ISP media. Conclusion: Findings from this investigation revealed that the selected strain, A-4, is an actinomycete

Production of antibiotics from soil-isolated actinomycetes and evaluation of their antimicrobial activities

Purpose : To investigate the production of antibiotic from actinomycetes isolated from soil and evaluate its antimicrobial activities. Methods : In a medium formulation study, A-4 and A-4 actinomycete mutant strains (out of the six strains selected from the nine actinomycetes that were screened) were evaluated for maximum antibiotic production using various carbon and nitrogen sources. Zone of inhibition and packed cell volume were the parameters used for the evaluation. Various fermentation conditions such as pH, temperature and dissolved oxygen were also optimized for maximal production of antibiotic from both A-4 and A-4 mutant. Results : Some actinomycetes strains showed promising antimicrobial activity against different strains of bacteria and fungi. Out of the six strains selected, one strain, designated A-4, showed maximum antimicrobial property against Gram positive and Gram negative strains as well as against various fungi. Conclusion : Findings from this investigation reveal that strain A-4 and A-4 mutant strains, in that order, exhibited superior antimicrobial activities to other soil isolates of actinomycetes