13 research outputs found

    Formulation and Evaluation of Mesalamine Nanosphere Tablet

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    Nanospheres are the particles having the size range between 10-200 nm in diameter. Nanospheres can be amorphous or crystalline in nature and also they have the ability to protect the drug from enzymatic and chemical degradation. For the preparation of standard calibration curve of Mesalamine with Phosphate buffer pH 6.8 and Absorbance of µg/ml solution was measured between 200-400nm by using Shimadzu 1601 UV/Vis double beam spectrophotometer. Nanosphare containing Mesalamine were prepared using nanoprecipitation method. 200 mg of polymer (Eudragit RS and L) was dissolve in 50 ml water. Drug was dissolve in 20 ml of methanol. Both solution were mixed and add 50 ml of water and stirred for half an hour. Methanol and water was evaporated under reduced pressure using rotary flash evaporator until 10 ml of solution was remaining. Than this suspension was centrifuge at 15000 rpm at 40C for half an hour. The supernatant was discarded and remaining portion was washed with distilled water. The nano-sphares was dried over night at 600C and stored in desiccators. The surface morphology (roundness, smoothness, and formation of aggregates) and particle size was studied by scanning electron microscopy (SEM). Zeta potential of the best formulation (F4) was determined by zeta potential probe model DT- 300. Mesalamimne, Dextrose and Lactose were taken in required quantities mixed and granulating agent (Starch past) was added and passed through #40 sieves, then lubricant magnesium stearate and talc was added then compressed into tablets by rotary tablet punching machine. Then film coating is done by 6% w/v solution of Cellulose acetate Phthalate in isopropyl alcohol using 2% tween-80 as plasticizer in coating pan. The weight of tablet was kept constant for all formulations. Nanosphare tablet formulation F-2 Showed maximum drug (97.75%) released and formulation F-4 showed 92.58% drug release. The In-vitro drug released study result showed that formulation F-2 96.58% drug was released after 17 hours which is highest drug release amongst all other tablet formulation. &nbsp

    Quality by Design based formulation and evaluation of acyclovir microsponges

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    Objective: The proposed study is focussed at developing acyclovir microsponges for oral drug delivery systems.  QbD was applied for better understanding of the process and to generate design space, using quality target product profile, critical quality attributes, and risk assessment. The aim of the experiment is to prepare a safe, efficacious, stable and patient compliant microsponge dosage form of Acyclovir. Materials and methods: Pre-formulation studies were carried out which helped in developing a suitable dosage form. UV, FTIR, DSC, and SEM studies were done for pre-formulation and post-formulation evaluations. QbD was applied to generate design space, using QTPP, CQA, and risk assessment. Microsponges of acyclovir were developed by 23 factorial designs. Three variables Drug: Polymer ratio (X1), Concentration of surfactant (X2) and Stirring speed (RPM) (X3) at two levels low and high were selected and response surface plots were generated. The microsponges were prepared by Quassi-emulsion solvent diffusion method. Various characterizations that were carried out include entrapment efficiency, percentage yield, particle size determination, in-vitro drug release studies and kinetic modelling of drug release. Statistical analyses of batches and surface response studies were done to understand the effect of various independent variables on the dependent variables. Results and Discussions: The λmax was confirmed at 251 nm by UV spectroscopy. The melting point was determined experimentally to be 2460C which confirms the drug to be Acyclovir. FTIR and DSC studies confirmed that the drug is Acyclovir. Eight trials were taken as per the by 23 factorial designs.  Conclusion: The study indicates that microsponges of Acyclovir by QbD approach were successfully developed. Keywords: Microsponge, Acyclovir, DoE, Qb

    Formulation and characterization of acyclovir based topical microemulsions by QBD approach

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    Objective: The proposed study is focussed at developing acyclovir microemulsions for topical drug delivery systems.  QbD was applied for better understanding of the process and to generate design space, using quality target product profile, critical quality attributes, and risk assessment. The aim of the experiment is to prepare a safe, efficacious, stable and patient compliant microemulsion dosage form of Acyclovir. Materials and methods: Pre-formulation studies were carried out which helped in developing a suitable dosage form. UV, FTIR and DSC studies were done for pre-formulation and post-formulation evaluations. QbD was applied to generate design space, using QTPP, CQA, and risk assessment. Microemulsions of acyclovir were developed by using 32 factorial designs. Pseudo terneary phase diagrams were constructed to screen various surfactants and co-surfactants for the preparation of microemulsions. Two independent variables Oil Concentration (X1) and Smix Concentration (X2) at three levels low, medium and high were selected and response surface plots were generated. The microemulsions were prepared by plotting pseudo terneary phase diagrams. Various characterizations that were carried out include % transmittance, Viscosity and % drug release. Statistical analyses of batches and surface response studies were done to understand the effect of various independent variables on the dependent variables. Results and Discussions: The λmax was confirmed at 251 nm by UV spectroscopy. The melting point was determined experimentally to be 2460C which confirms the drug to be Acyclovir. FTIR and DSC studies confirmed that the drug is Acyclovir.  Conclusion: The study indicates that microemulsions of Acyclovir by QbD approach were successfully developed. Keywords: Microemulsion, Acyclovir, DoE, Qb

    Pharmaceutical Considerations of Microemulsion as a Drug Delivery System

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    Microemulsions were recognized after the work of Hoar and Schulman in 1943, which revealed the use of strong surface-active agent leading to spontaneous emulsification; however, it was in 1959 when Schulman first used the term “microemulsion” for such emulsion system. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10–100 nm diameters that form spontaneously upon mixing of oil, water, and emulsifier. After its discovery in 1943 to till date, more than 1200 publications have been reported and development of O/W type of microemulsions has been the priority for the researchers, mostly using non-ionic surfactants. Although microemulsions seem to be one of the most promising candidates in pharmaceuticals because of relative ease in the formulation and distinct characteristics when compared to other dispersion systems, its commercial success as a drug delivery system has been very little. Much of the time after its discovery has been exhausted in failure to understand correct formulation requisites or confusing it with other similar systems. In the face of increasing the number of publication year after year, its formulation has been generally based on trial-and-error. Efficient strategies for excipient selection and detailed understanding of microstructures contributing to its formulation is still required which may serve as the foundation for attaining greater success in this field. Keywords: Microemulsion, Surfactants. Spontaneous emulsification, Solubilization

    AN ETHNO-PHARMACOLOGICAL EVALUATION OF CATUNAREGAM SPINOSA (THUMB.) TIRVENG FOR ANTIOXIDANT ACTIVITY

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    Catunaregam spinosa (Thumb.) Tirveng have been reported in studies to possess antioxidant property. Therefore, present study was undertaken to validate different extracts of C. spinosa for antioxidant activity along with safety margin, according to OECD guidelines for toxicity. The extracts of different solvents, such as, distilled water, ethanol, methanol, acetone, chloroform; petroleum ether and benzene were subjected to phytochemical screening and characterization was done by using UV-Visible spectrophotometer. The toxicity studies displayed considerable margin of safety and no adverse effects observed upto 2gm/kg of administration of extract. The antioxidant property of extract of C. spinosa was evaluated for DPPH and FRAP activity. The IC50 value for DPPH activity was found to be 85% and the FRAP was found to be 2.5 μg/ml. These results when compared to standard values indicate towards superior antioxidant potential of C. spinosa extract

    Anti-Inflammatory, Analgesic and Antipyretic Activity of Catunaregam spinosa (Thumb.) Tirveng Extracts

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    Catunaregam spinosa leaves have been ethnopharmacologically accounted for acquiring various pharmacological properties. The present study was undertaken to evaluate anti-inflammatory, analgesic and antipyretic potential of leaves of C. spinosa.The ethanolic extract was selected for this purpose based on phytochemical screening. Inflammation was inhibited at the dose of 200 mg/kg with percent inhibition of inflammation 32.06, 37.28 and 43.16 %, respectively, at 1, 3 and 5 h, while in egg albumin model % inhibition was found to be 47.81%. There was no significant analgesic activity seen in acetic acid induced writhing response method while significant effects were observed in the doses of 25 and 100 mg/kg on hot plate test. No antipyretic activity was shown by ethanolic extracts(25, 100 and 200 mg/kg) against Brewer’s yeast induced pyrexia in rats. Keywords: Catunaregam spinosa, Anti-inflammatory activity, Phytochemical screening, Ethanolic extract

    Optimization of Superdisintegrants Concentration in Designing of Mouth Dissolving Tablets of Solid Dispersion of Domperidone by Using response surface methodology

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    This research involves preparation of mouth dissolving tablets of solid dispersions of Domperidone by direct compression method using various concentrations of superdisintegrants in combination i.e. Croscarmellose Sodium and crospovidone. For optimization, a 32 (two-factor three-level) factorial design is being used in which 2 factors were evaluated, each at 3 levels and experimental trials were performed at all 9 possible combinations for every four selected solid dispersion batches (9x4=36 formulations + one blank). The amount of Croscarmellose Sodium (X1) and crospovidone (X2) was selected as independent variables. The disintegration time, percentage friability and percent drug release were selected as dependent variables. All the active powder blends were evaluated for precompression parameters (viz. angle of repose, Carr’s index, Hausner ratio, etc.) and the tablets were evaluated for post-compression parameters (viz. weight variation, hardness, and friability, wetting time, disintegration time, water absorption ratio, and in vitro drug release studies). Optimization was done using the software (Design Expert® 11.0.4), predicted responses of which were validated

    Non-HIV Related Non-Communicable Diseases in HIV Patients

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    Authors examined the impact of additional factors on fatalities in Chronic HIV patient populations and should have remained on highly active antiretroviral therapy (HAART) for the at least 1 year: Inadequate response to HAART and the existence of AIDS-defining illnesses, depression, and drug and alcohol abuse, and especially in comparison the fatalities to that of the overall demographic. The enhanced rates of mortality in HIV-infected people are primarily impact on risk variables that can be recognized just before to or during the introductory phase of antiretroviral treatment. The fatality rate in patient populations without risk variables who are on effective HAART is virtually identical to something like the non-HIV-infected inhabitants. The significance of a holistic solution for lipid accumulation, cardiovascular, and glomerular comorbidity supervisors in the lengthy effective monitoring of chronic HIV old patients cannot be exaggerated

    Silica-Coated Liposomes for Insulin Delivery

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    Liposomes coated with silica were explored as protein delivery vehicles for their enhanced stability and improved encapsulation efficiency. Insulin was encapsulated within the fluidic phosphatidylcholine lipid vesicles by thin film hydration at pH 2.5, and layer of silica was formed above lipid bilayer by acid catalysis. The presence of silica coating and encapsulated insulin was identified using confocal and electron microscopy. The native state of insulin present in the formulation was evident from Confocal Micro-Raman spectroscopy. Silica coat enhances the stability of insulin-loaded delivery vehicles. In vivo study shows that these silica coated formulations were biologically active in reducing glucose levels

    Formulation of Mouth Dissolving Tablets Using Solid Dispersion Technique: A Review

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    Mouth-dissolving tablets are also called as fast disintegrating tablets, melt-in mouth tablets, orodispersible tablets, quick dissolving etc. Mouth dissolving tablets are those when put on tongue disintegrate rapidly thereby releasing the drug, which dissolve or disperses in the saliva. The faster the drug dissolved into solution, quick will be the absorption and onset of clinical effect. Mouth dissolving tablet containing solid dispersion was developed to improve the solubility of drug and stability of solid dispersion. Such tablets are disintegrate and/or dissolve rapidly in the saliva without the need for water. Hence it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. The later portion of the article focus on the progress in methods of manufacturing, evaluation and various latest technologies involved in the development of Mouth dissolving tablets. Solid dispersion is basically a drug with polymer two-component system; hence the drug–polymer interaction should be determined first in order to ensure the stability of the formulation. This review is intended to discuss the recent advances related on the area of solid dispersion technology. Since different methods are used for the preparation of solid dispersions such as fusion method, solvent method, melting solvent method, melt extrusion method, lyophilisation technique, melt agglomeration process, use of surfactant, electro spinning and super Critical Fluid Technology, of them which method is good and suitable for which type of drug. The use of Mouth dissolving dosage forms has solved various problems noted in administration of drugs to the pediatric and elderly patient, which constitutes a large proportion of the world's population. The initial focus of this review article is based on solid dispersion mainly advantages, disadvantages, types, the method of preparation, and characterization of the solid dispersion at laboratory and industrial level
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