Formulation and characterization of modified release tablets containing ionizid using swellable polymers

The aim of this work was to develop swellable modified release (MR) isoniazid tablets using different combinations of polyvinyl acetate (PVAc) and sodium-carboxymethylcellulose (Na-CMC). Granules were prepared by moist granulation technique and then compressed into tablets. In vitro release studies for 12 hr were carried out in dissolution media of varying pH i.e. pH 1.2, 4.5, 7.0 and 7.5. Tablets of all formulations were found to be of good physical quality with respect to appearance (width and thickness), content uniformity, hardness, weight variation and friability. In vitro release data showed that increasing total polymer content resulted in more retarding effect. Formulation with 35% polymer content exhibited zero order release profile and it released 35% of the drug in first hr, later on, controlled drug release was observed upto the 12th hour. Formulations with PVAc to Na-CMC ratio 20:80 exhibited zero order release pattern at levels of studied concentrations, which suggested that this combination can be used to formulate zero order release tablets of water soluble drugs like isoniazid. Korsmeyer-Peppas modeling of drug release showed that non-Fickian transport is the primary mechanism of isoniazid release from PVAc and Na-CMC based tablets. The value of mean dissolution time decreased with the increase in the release rate of drug clearly showing the retarding behavior of the swellable polymers. The application of a mixture of PVAc to Na-CMC in a specific ratio may be feasible to formulate zero order release tablets of water soluble drugs like isoniazid.Keywords: Isoniazid, Polyvinyl acetate, Sodium-carboxymethylcellulose, Modified release tablets

Comparative Analgesic and Anti-inflammatory Activities of Two Polyherbal Tablet Formulations (Aujaie and Surangeen) in Rats

Purpose: To investigate the analgesic and anti-inflammatory activities of two herbal polymedicines - Aujaie and Surangeen to ascertain their therapeutic claims.Methods: A total of 96 rats were divided into two equal groups; one for determination of antiinflammatory activity and the other for analgesic activity. Anti-inflammatory and analgesic activities were evaluated by carrageenan-induced paw edema and formalin-induced paw licking test, respectively. For both studies, group I (untreated control) received 1 ml/kg, (po) of gum suspension 1 h before carrageenan injection. Aspirin (100 mg/kg, po) was given to group II (treated control) before injection. Groups III, IV and V were administered orally aujaie (3, 4 and 5 mg/kg, po, respectively), while surangeen tablets (10, 20 and 40 mg/kg, po) were given to groups VI, VII and VIII, respectively. Pain was experimentally induced by injecting 0.1 ml of 2.5 % formalin (40 % formaldehyde in distilled water) via the subplantar region of the left hind paw.Results: Significant (p < 0.05) anti-inflammatory activity for aspirin (group II as well as for groups III - VIII with paw edema inhibition (PDI) ranging from 24.6 - 90.2 %, There was significant ((p < 0.05) analgesic activity in group II, VI and VII while in groups III - V and VIII the activity was insignificant (p < 0.05).Conclusion: Aujaie and surangeen tablets exhibited pronounced analgesic and anti-inflammatory activities in rats depending on the dose employed.Keywords: Aujaie, Surangeen, Anti-inflammatory, Analgesic

Screening of various botanical extracts for antioxidant activity using DPPH free radical method

Aiming at the exploration of herbal use by society, crude extracts of the seeds of some commonly used medicinal plants (Vitis vinifera, Tamarindus indica and Glycin max) were screened for their free radical scavenging  properties using ascorbic acid as standard antioxidant. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The overall antioxidant activity of grape seeds (Vitis vinifera) was the strongest, followed in descending order by soybean (Glycin max) and tamarind (Tamarindus indica). The seeds extract of Vitis vinifera, Glycin max and Tamarindus indica showed 85.61%, 83.45% and 79.26%, DPPH  scavenging activity respectively.Key words: Antioxidant activity, DPPH, free-radical, Vitis vinifera, Glycin max, Tamarindus indica

In vivo Evaluation of a Cosmetic Emulsion Containing Soybean Extract for Anti-Aging

Purpose: To develop and assess the anti-aging potential of a cosmetic W/O emulsion containing an extract of soybean, Glycine max (L.) Merr. Fabaceae.Methods: This single-blind placebo-controlled study was performed in 11 healthy male human volunteers. A formulation comprising of 4 % of concentrated extract of soybean was prepared by loading the extract in the internal aqueous phase of the emulsion. A control (base), consisting of theemulsion without the extract, was also prepared. Both formulations were applied to the cheeks of all volunteers for 12 weeks and their effect on different skin parameters, i.e., moisture contents, elasticity and surface evaluation of living skin (SELS) were assessed.Results: The formulation containing 4 % soybean extract showed significant (p ≤ 0.05) effects on skin elasticity and moisture contents but the base showed insignificant effect (p ≤ 0.05). There was significant (p . 0.05) decline in SELS, i.e., SEsc (skin scaliness, from 1.73 } 0.05 to 1.66 } 0.06), SEw (skin wrinkles, from 71.74 ± 1.52 to 68.51 ± 1.64), SEsm (skin smoothness, from 109.01 ± 4.77 to 102.03 ± 4.23), and SEr (skin roughness, from 4.04 ±0.09 to 3.82± 0.08) parameters after applicationof the extract formulation for 12 weeks.Conclusion: Topical application of the cosmetic emulsion containing soybean extract exerts potential skin anti-aging effects.Keywords: Glycine max, Soybean, Anti-aging, Skin elasticity, Cosmetic emulsion, Surface evaluation of living skin (SELS), Skin moisture conten

Fabrication of novel gastro-retentive Floating microcapsules by utilizing a combination of HPMC and EC and their physicochemical assessment

The project was aimed to develop floating microcapsules (FMs) using combination of a hydrophobic (ethyl cellulose, EC) and hydrophilic polymer (hydroxy propyl methyl cellulose, HPMC), and to evaluate them. An easy and novel phase separation method was adopted to prepare FMs. Chloroform and paraffin oil were employed as solvent and non-solvent respectively. Five kinetic models were applied to assess and describe the mechanism and pattern of tramadol hydrochloride (TmH) release from FMs and they were subjected to FTIR and XRD to evaluate TmH-HPMC-EC interaction. As EC concentration was increased the retardation in drug release, improvement in flow characteristics and decrease in floating time were observed. Kinetics of drug release was followed by Korsmeyer-Peppas kinetic model. It was concluded that the floating microcapsules of TmH can be produced using phase separation method and they have no drug-polymer interaction. The accelerated stability studies also ensured the physicochemical integrity of FMs.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Effect of cream formulation of fenugreek seed extract on some mechanical parameters of human skin

Purpose: To determine the effect of an emulsion formulation of fenugreek (Trigonella Foneum-Graecum L) seed extract on some mechanical parameters of the skin of healthy human volunteersMethods: A water-in-oil emulsion cream base without fenugreek seed extract which served as control, and a similar formulation containing 4 %w/v of the extract in the internal (aqueous) phase were prepared. Each of the formulations was applied to the cheeks of 10 human volunteers for a period of 4 weeks and some mechanical parameters (R0, R1, R2, R3, R4, R5, R6, R7, R8 and R9) of the skin were measured weekly using Cutometer MPA 580. Results: The results indicate that the effects of the creams on skin mechanical properties were significant (p < 0.05) with respect to time, except for R4 and R9. The extract-containing cream substantially increased skin elasticity, hydration and the ability of skin to resist photo-aging when compared to the base. Conclusion: Both the cream base and the cream containing fenugreek extract demonstrated significant (p < 0.05) improvement in all mechanical parameters related to skin elasticity, ageing, hydration and fatigue but the effect of the extract cream was more pronounced in some cases

Dual coated microparticles for intestinal delivery of nimesulide

Nimesulide was formulated as novel dual coated microparticles using chitosan (CTN) and ethyl cellulose (EC) as encapsulating materials for its improved delivery to the intestine and to prevent gastric irritation and increase patient compliance. The first coating was applied by chitosan using pH change method followed by second coating of ethyl cellulose using thermal change method. This process was analysed for its capability to produce microparticles of uniform size, good flowability, uniform drug loading and maximum entrapment efficacy and the absence of interaction between drug and process parameters as well as the polymers confirmed by XRD and FTIR analysis. In vitro release study was carried out in simulated gastric fluid (SGF) for first 2 h and simulated intestinal fluid (SIF) for next 6 h. The formulation M7 and M8 that contained chitosan and ethyl cellulose in the concentration of 1:1 and 1:2 (M1:EC) were found to achieve the targets of the present study such as uniform intestinal release of acidic drug and thus improves the patient compliance.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Study of nimesulide release from ethylcellulose microparticles and drug-polymer compatibility analysis

The aim of this study was to formulate ethyl cellulose (EC) microparticles for sustained release of nimesulide and study the effect of processing variables, drug to polymer ratio and also study the drug polymer compatibility. The microparticles were prepared by coacervation (temperature change) technique. Physical properties, such as particle size, entrapment efficiency, release pattern and morphological characteristics were investigated by in vitro dissolution, SEM, FTIR, XRD, DSC and TGA in order to optimize the formulation of the microparticles. With the increase of polymer concentration there was an increase in size and drug entrapment efficiency of microparticles. There was a decrease in size and nonlinear change in entrapment efficiency with the increase of stirring speed and time. The release of drug from microparticles was anomalous diffusion. It was confirmed that there is no strong chemical interaction between drug and polymer except the change in crystal habit and polymorphism. Ethyl cellulose microparticles containing nimesulide are suitable for controlled release devising.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Synthesis of biodegradable microspheres of tramadol by simple phase separation technique and their in vitro evaluation

Biodegradable microspheres of Tramadol Hydrochloride (TmH) were developed using simple phase separation technique. Poly lactide-co-glycolide (PLGA) was employed as a release controlling polymer. Simple phase separation method was adopted to prepare microspheres; Dichloromethane (DCM) and Liquid Paraffin (LP) were employed as solvent and non-solvent respectively. Five kinetic models were applied to assess and describe the mechanism and pattern of TmH release from biodegradable microspheres. Biodegradable microspheres were subjected to FTIR, DSC and XRD, to evaluate TmH-PLGA interaction. Retardation in the release of TmH was observed as PLGA concentration was increased. Kinetics of drug release was following higuchi model. The microspheres exhibited no interaction between TmH and PLGA. Biodegradable microspheres of TmH can be produced using phase separation method. Microspheres were stable with no drug-polymer interaction. The accelerated stability studies also ensured the physicochemical integrity as differences of release profile over the period of three months were insignificant.Colegio de Farmacéuticos de la Provincia de Buenos Aire