FLOATING PULSATILE DRUG DELIVERY SYSTEM OF FAMOTIDINE: DESIGN, STATISTICAL OPTIMIZATION, AND IN VITRO EVALUATION

Objective: Pulsatile systems are gaining a lot of significance as they deliver the drug at the right site of action at the right time and in the right amount, thus providing spatial and temporal delivery and increasing patient compliance. These systems are designed according to the circadian rhythm of the body. The aim of the present research work was to design and optimize compression coated floating pulsatile drug delivery system of Famotidine. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release.Methods: Floating pulsatile tablets were prepared by using press coated technology. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The burst release core tablet was prepared by using super disintegrants with the active ingredient. Press coating of optimized burst release core tablets was done by the polymer. A 32 full factorial design was used for optimization. The amount of HPMCE4M and Polyox WSRN60K was selected as independent variables. Lag period, drug release, buoyancy and swelling index were selected as dependent variables.Results: Floating pulsatile release formulation (FPRF) F4 at level 0 (65 mg) for HPMC E4M and level-1 (75 mg) for Polyox WSR N60K showed lag time of 4 h with>90% drug release. The data were statistically analyzed using ANOVA, and ð‘ƒ<0.05 was statistically significant.Conclusion: The present research work demonstrates that famotidine could be successfully delivered to provide night-time relief of gastric acidity by formulating floating pulsatile drug delivery system. The press-coated formulation containing HPMCE4M and Polyox WSR N60K at 0,-1 level was in the optimum zone and has the potential for time-controlled pulsatile delivery of Famotidine.Keywords: Floating pulsatile, Famotidin

Dizajniranje i evaluacija oralnih raspadajućih tableta dekstrometorfan hidrobromida s maskiranim okusom

The present study is aimed to develop dextromethorphan hydrobromide (DXM) oral disintegrating tablets (ODT) with acceptable palatability to help patients of all age group. The bitter taste of the drug was masked by binding the drug to ion exchange resin. The effect of particle size of resin on drug loading was studied. In vitro and in vivo disintegration time and in vitro drug release studies were performed. Drug loading increased significantly with a decrease in the particle size of the resin. DSC and XRPD studies reveal that the molecular state of the drug changed from crystalline to amorphous form. The dissolution efficiency calulated for optimized ODT and conventional directly compressed tablet were almost comparable, indicating free dissociation of the drug from the resinate. The bitter taste of DXM can be masked by binding with ion exchange resin and the resinate can be successfully formulated into oral disintegrating tablets.Cilj rada bio je pripraviti raspadajuće tablete dekstrometorfan hidrobromida (DXM) za oralnu primjenu (ODT) prihvatljivog okusa s namjerom da se pomogne pacijentima svih dobnih skupina. Gorki okus ljekovite tvari maskiran je vezanjem lijeka na ionsko-izmjenjivačku smolu. Proučavan je utjecaj veličine čestica smole na količinu ljekovite tvari koja se može na nju vezati, vrijeme raspadanja in vitro i in vivo, te oslobađanje lijeka in vitro. Količina vezanog lijeka značajno se povećava sa smanjenjem veličine čestica smole. DSC i XRPD studije pokazuju da prilikom vezanja kristalinični oblik lijeka prelazi u amorfni. Oslobađanje ljekovite tvari izračunato za optimizirane ODT i izravno komprimirane tablete vrlo je slično, što ukazuje na slobodno oslobađanje lijeka iz smole. Gorki okus DXM može se maskirati vezanjem ljekovite tvari na ionsko-izmjenjivačku smolu iz koje se mogu pripraviti raspadajuće tablete za oralnu primjenu

In vitro transcutaneous permeation of acyclovir sodium from HPMC gels: role of chemical permeation enhancers

The main objective of the present study is to improve the permeation of acyclovir sodium (ACV) across stratum corneum (SC) from HPMC gel formulations. We have also investigated the role of chemical permeation enhancers like dimethyl sulfoxide, ethanol, limonene and sodium taurodeoxycholate on the transcutaneous permeation of ACV from HPMC gels. The optimized formulations were characterized and subjected to in vitro permeation study using excised rat abdominal skin. The histological examination of the skin was studied to understand the mechanisms involved in the permeation of ACV across skin. The cumulative amount of ACV permeated and the increase in permeation parameters (Jss, Kp and ER) were significantly higher for gel formulations compared to marketed formulation. A 2 to 4 fold increase in enhancement ratio clearly indicates the potential of formulating ACV into a gel.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Venlafaxine hydrochloride transdermal patches: effect of hydrophilic and hydrophobic matrix on in vitro characteristics

Transdermal drug delivery systems of venlafaxine hydrochloride were prepared by using combination of hydrophilic (HPMC E15) and hydrophobic (ERS100 and ERL 100) polymers in 1:5, 2:4, 3:3, 4:2, 5:1 ratios by solvent casting technique with 15 % v/w propylene glycol as plasticizer. The drug permeation studies revealed that drug permeation increased proportionally with increasing HPMC ratio where ERS 100 as hydrophobic polymer but in case of ERL 100 as hydrophobic polymer proportional increase was not obtained this may be due to increased diffusion path length. The drug permeation kinetics followed zero order profile with diffusion mechanism. The average steady state flux obtained with HPMC: ERL 100 (3:3) was 193.2 μg/cm2 /h and the same was increased to 257 μg/cm2 /h with the incorporation of 5 % v/w of dimethyl sulfoxide as permeation enhancer that was 3 fold of target flux (86 μg/cm2 /h). The FTIR studies showed drug-polymer compatibility.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Studies on ion-exchange resin complex of Dextromethorphan Hydrobromide

The objective of present work was to assess ion exchange resins for taste masking of Dextromethorphan Hydrobromide (DM) - a highly bitter drug. A strong cationic exchange resin (Amberlite® IRP-69) and weak cationic exchange resin (Amberlite® IRP-64) were evaluated. Based on drug loading efficiency, Amberlite® IRP-69 was selected for further evaluation. The effect of different methods of drug loading, drug: resin ratios and particle size on drug complexation was evaluated. The formation of a resinate was confirmed based on Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier transmission infra-red spectroscopy (FT-IR). The results from loading studies at different drug: resin ratios, 1:1, 2:1 and 3:1, indicated that, the drug loading achieved were 78%, 49% and 25% w/w, respectively. For a defined drug:resin ratio, resin particle size of 45-63μm showed highest drug loading whereas, resins with higher particle size, 125-150 μm showed the lower drug loading. The X-ray diffraction spectra showed absence of crystalline peaks indicating formation of resinates. DSC and XRPD showed that the molecular state of the entrapped drug in resinates changed from crystalline to amorphous state regardless of drug loading. The complexes were evaluated for bulk density, angle of repose, taste masking and in vitro drug release. In vitro drug release studies showed more than 80% drug release from resinate prepared with Amberlite IRP 69 within 30 min. Based on the studies we can conclude that taste masking of Dextromethorphan Hydrobromide could be accomplished using a strong cationic ion exchange resin with a particle size 45-63 μm at a 1:1 Drug: Resin ratioColegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and pharmacodynamic evaluation of meloxicam liquisolid compacts

The purpose of this study was to improve the meloxicam dissolution rate through its formulation into liquisolid compacts and then to evaluate the in vitro and in vivo performance of the prepared liquisolid compacts. Dissolution efficiency, mean dissolution time and relative dissolution rate of liquisolid compacts were calculated and compared to marketed formulation. The degree of interaction between the ME and excipients was studied by differential scanning calorimetry and X-ray diffraction were used and results revealed that, there was a loss of meloxicam crystallanity upon liquisolid formulation and almost molecularly dispersed state, which contributed to the enhanced drug dissolution properties. The optimized liquisolid compact showed higher dissolution rates and dissolution efficiency compared to commercial product. The analgesic and anti inflammatory response of optimized liquisolid compact in Swiss albino mice and Wistar rats was found to be superior compared to the marketed formulation.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Genomic Designing of Pearl Millet:A Resilient Crop for Arid and Semi-arid Environments

Pearl millet [Pennisetum glaucum (L.) R. Br.; Syn. Cenchrus americanus (L.) Morrone] is the sixth most important cereal in the world. Today, pearl millet is grown on more than 30 million ha mainly in West and Central Africa and the Indian sub-continent as a staple food for more than 90 million people in agriculturally marginal areas. It is rich in proteins and minerals and has numerous health benefits such as being gluten-free and having slow-digesting starch. It is grown as a forage crop in temperate areas. It is drought and heat tolerant, and a climate-smart crop that can withstand unpredictable variability in climate. However, research on pearl millet improvement is lagging behind other major cereals mainly due to limited investment in terms of man and money power. So far breeding achievements include the development of cytoplasmic male sterility (CMS), maintenance counterparts (rf) system and nuclear fertility restoration genes (Rf) for hybrid breeding, dwarfing genes for reduced height, improved input responsiveness, photoperiod neutrality for short growing season, and resistance to important diseases. Further improvement of pearl millet for genetic yield potential, stress tolerance, and nutritional quality traits would enhance food and nutrition security for people living in agriculturally dissolute environments. Application of molecular technology in the pearl millet breeding program has a promise in enhancing the selection efficiency while shortening the lengthy phenotypic selection process ultimately improving the rate of genetic gains. Linkage analysis and genome-wide association studies based on different marker systems in detecting quantitative trait loci (QTLs) for important agronomic traits are well demonstrated. Genetic resources including wild relatives have been categorized into primary, secondary and tertiary gene pools based on the level of genetic barriers and ease of gene introgression into pearl millet. A draft on pearl millet whole genome sequence was recently published with an estimated 38,579 genes annotated to establish genomic-assisted breeding. Resequencing a large number of germplasm lines and several population genomic studies provided a valuable insight into population structure, genetic diversity and domestication history of the crop. Successful improvement in combination with modern genomic/genetic resources, tools and technologies and adoption of pearl millet will not only improve the resilience of global food system through on-farm diversification but also dietary intake which depends on diminishingly fewer crops