American Journal of Advanced Drug Delivery

Online ISSN: 2321-547X

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Publisher: TIba Pharmaceuticals Pvt. Ltd.
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Development and Optimization of Paracetamol Immediate Release and Aceclofenac Controlled Release Bilayer Tablets

Author(s): M. Sudhakar, Vinay Umesh Rao, Nagraju Samalla
Abstract
| Pages: 93-101
The objective of the study was to formulate bilayer tablets consisting of Paracetamol (PM) and Aceclofenac (AC). 100% of the dose of PM and 50% of the dose of AC was formulated as a fast disintegrating and rapidly dissolving layer which was overlaid with a controlled release layer containing the balance 50% of the dose of AC. The IRlayer was designed in a way to achieve complete release of the dose within a 30 min and SR-layer was designed to deliver the dose at a constant rate of 4 to 5 mg % /hour. To optimize the composition of the IR layer the level of Croscarmellose sodium (CCS) in the formulation was optimized. For optimizing the SR layer, HPMC K4M, K15M and K100M at different levels were evaluated and the type and concentration of HPMC was finalized. These results indicated that release of the drug from the tablet was influenced by content of super disintegrant and polymer grade and concentration. Formulation containing 1.5 % w/w of CCS in IR-layer and 6 % w/w of HPMC K100M in SR-layer showed desired drug release. Thus bilayer tablets could be a potential dosage form for delivering Paracetamol as immediate release and Aceclofenac in a controlled release manner.

Effect of Combination of Methocel K4M, K15M And K100M on the In Vitro Release of Aripiprazole from Controlled Release Tablets Using Full Factorial Design of Experiments

Author(s): Vinay Umesh Rao, E. Sangeetha, M. Sudhakar
Abstract
| Pages: 102-112
The effect of three different viscosity grades on the in vitro dissolution profile of Aripiprazole controlled release tablets was studied. The study was carried out using full factorial design of experiments. The release rate of 5 to 6 mg%/ hour was targeted and the effect of the polymers on drug release over 24 hours was evaluated at the total polymer level between 30% and 45%. The DOE experiments have shown that when the combination of polymer is used, the total polymer concentration should be in a narrow range of 32.4% w/w to 37.5% w/w in order to achieve the target dissolution profile.

Design, Synthesis and Antimicrobial, Antifungal and Anti-Inflammatory Evaluation of Some (4-Substituted Phenyl)[5-(4- Substituted Phenyl)-3-Phenyl- 4,5-Dihydro-1H-Pyrazol-1-yl]-Methanone Derivatives

Author(s): Arpita R. Patel, R. Badmanaban, Dhrubo Jyoti Sen, Chhaganbhai N. Patel
Abstract
| Pages: 113-127
It is evident from reported articles that bacterial infections often produce pain & inflammation. In normal practice, two groups of agents (chemotherapeutics & NSAID’s) are prescribed simultaneously. Unfortunately, none of the drugs available to possesses these activities in a single molecule. Therefore, our aim is to find a compound having dual effect of anti-inflammatory & antimicrobial activitiy (twin drug concept). Pyrazole and its derivatives have been reported for these dual activities. Here an attempt has been made to synthesize eight (4-substituted phenyl)[5- (4-substituted phenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1- yl]methanone derivatives. The synthesized derivatives were assessed for their in-vitro anti-microbial and anti-inflammatory activity. Chalcone derivative was synthesized by Claisen Schmidt condensation between acetophenone and substituted benzaldehyde. It was refluxed with hydrazine hydrate to form pyrazole ring which on reaction with substituted benzoyl chloride in acetone and triethylamine to form to get the parent compound from which the final derivatives has been synthesized. The structures of newly synthesized compounds so obtained were confirmed by using IR, HNMR, MS spectral data.

Safety Measure: COSHH as Laboratory Safety Measures in Control of Substances Hazardous to Health and for Environment

Author(s): Viraj P. Jatakiya, Nadim M. R. Chhipa, Piyush A. Gediya, Sachin M. Patel, Dr. Dhrubo Jyoti Sen
Abstract
| Pages: 128-140
COSHH is the law that requires employers to control substances that are hazardous to health. You can prevent or reduce workers exposure to hazardous substances by: finding out what the health hazards are, deciding how to prevent harm to health, providing control measures to reduce harm to health, making sure they are used, keeping all control measures in good working order, providing information, instruction and training for employees and others, providing monitoring and health surveillance in appropriate cases, planning for emergencies. Most businesses use substances, or products that are mixtures of substances. Some processes create substances. These could cause harm to employees, contractors and other people. Sometimes substances are easily recognised as harmful. Common substances such as paint, bleach or dust from natural materials may also be harmful. Laboratory Safety Standards are in use in clinical and chemical labs, testing labs and research and development labs in industry and educational facilities. Lab safety standards pertain to clothing and equipment as well as procedures and lab design. Standards are obtained from International Organization of Standardization (ISO); International Safety Equipment Association (ISEA); ASTM International (ASTM); International Electro technical Commission (IEC); British Standards Institution (BSI); Laser Institute of America (LIA); Clinical and Laboratory Standards Institute (CLSI); Standards Australia (SAI); and American Industrial Hygiene Association (AIHA). There are many new laboratory safety standards introduced each year. Many important laboratory safety standards have been categorized below. There are many other laboratory safety standards that can be found by using a keyword or document number search: Protective Clothing, Hand/Eye Protection, Equipment Safety, Laser Safety, Laboratory Testing and Management and Laboratory Design and Procedures.

Synthesis and Biological Evaluation of Some Novel Coumarin and Guanidine Derivatives by Oral Glucose Tolerance Test

Author(s): Vahan G. Prajapati, Dr. Dhrubo Jyoti Sen
Abstract
| Pages: 141-148
Objective: The major drawback of current treatment of diabetes is challenging due to resistance to antidiabetic agents their side effects. Chromenes occurs naturally in plants and plays role of anticoagulant activity. Guanidine plays role of antidiabetic activity. 2H-chromenes are the heterocyclic compounds with considerable therapeutic and pharmacological properties. Guanidine is compounds with considerable therapeutic and pharmacological properties. In this view, it has been planned to combine both guanidine and coumarin derivatives. Biological activity for antidiabetic activity has been performed for guanidine derivatives. Experimental and Computational work done: 2H-chromene was synthesized by Pechmann condensation of resorcinol, ethyl acetoacetate and sulphuric acid. Then coumarin was combined with guanidine. This combined compound was substituted by different substituted benzaldehyde and in other series by oxidation, chlorination and Schotten Baumann reaction. The purity of the compounds was checked by TLC monitoring and all the synthesized compounds were characterized by UV, IR, Mass and some of by 1H-NMR spectroscopy. The antidiabetic activities of synthesized compounds were tested by oral glucose tolerance test (OGTT). Results and discussion: In antidiabetic activity, compounds 9-b have shown highest antidiabetic activity while compounds 9-a and 11-a have shown also antidiabetic activity against metformin as standard. Conclusion: Evaluation of antidiabetic revealed that compounds with substituted benzaldehyde at the 4-position of the phenyl ring of 2H-chromenes and at oxidation, chlorination and Schotten Baumann reaction of synthesized intermediate i.e., 9-a is most active antidiabetic agent.

Complexation: Effect of Metal on Microbiological Activity of Sulfanilamide Derivatives

Author(s): Pratik R. Chaudhary, Dr. Dhrubo Jyoti Sen
Abstract
| Pages: 149-156
Resistance strain which outgrows current therapeutics. As new drug development either against resistance strain or any new disease is neither easier nor cheap. Modification of the available entity generally called “sulfonamide” with metal. Sulphonamides and metal duos are promising for their antimicrobial activity. Sulfanilamide metal complexes were synthesized. Coordination complexes of sulfonamide with metal such as Copper, Barium, Zinc, Ferric, Aluminum, Cadmium, Manganese, Magnesium and Calcium were prepared by complexation reaction under stirring and control environmental conditions. The purity of complexes was checked by TLC monitoring and all synthesized complexes were characterized using I.R., Mass, Atomic Absorption Spectroscopy. The antibacterial activity of synthesized complex was tested by Agar plate method.

Synthesis of Substituted 7-Methyl-2,8- Dihydropyrazolo-[1,5-α][1,3,5]-Triazine Derivatives for Anti-Inflammatory and Anti- Microbial Screening

Author(s): Niraj V. Patel, Dr. Dhrubo Jyoti Sen
Abstract
| Pages: 157-173
A series of condensed pyrazolo and triazine derivatives have been synthesized to their physical property melting point, % yield, retention factor (Rf) have been evaluated. Structure is confirmed by UV, IR, NMR and Mass. All synthesized compounds are screened for two biological activities (Anti-inflammatory and Anti-microbial). Anti-inflammatory activity has been carried out by rat paw edema method while anti-microbial activity has been carried out by filter paper disc method. MIC (minimum inhibitory concentration) for antimicrobial screening has been carried out by tube dilution method.

Biological Synthesis of Gold and Silver Nanoparticles by Nitraria schoberi Fruits

Author(s): Majid Sharifi Rad, Javad Sharifi Rad, Gholam Ali Heshmati, Abdolhossein Miri, Dhrubo Jyoti Sen
Abstract
| Pages: 174-179
Biological synthesis of nanoparticles by the use of natural solvents and it’s natural protecting method was compared with physical and chemical methods. Among of biological synthesis of nanoparticles methods, using of plant and particularly medical plants are more important. Synthesis of silver and gold nanoparticles may be influenced directly or indirectly by phytochemicals in plants such as flavonoids, diosgenin and phenolics compounds. In this study the extracts of dry fruit was used for biological synthesis of gold and silver nanoparticles as a reducing agent. Salt of these elements was added to extract with 1mM concentration and the reaction was performed at room temperature. Change color in plant extract after its reaction with gold and silver salts and peak absorption in 550 and 450nm for gold and silver respectively using spectrophotometer showed that gold and silver nanoparticles was produced. Then size and morphology of these nanoparticles was determined by electronic microscope. The shape of particles was circle and the average particle size was 20-30 and 70-100nm for gold and silver respectively.