FORMULATION AND CHARACTERIZATION OF FLOATING BEADS OF ANTIBIOTIC BY EMULSION GELATION TECHNIQUE

Objective: The study aims at formulation and characterization of floating hydrogel beads of cefdinir for improving its bioavailability. Methods: Cefdinir is broad-spectrum, oral, third-generation cephalosporin antimicrobial agent active against Gram-positive and Gram-negative bacteria. The floating hydrogel beads of cefdinir were formulated with polymers such as sodium alginate and sodium carboxymethyl cellulose by emulsion gelation technique using olive oil/castor oil. The beads were evaluated for surface morphology, bead size, entrapment efficiency, floating characteristics, in vitro swelling, in vitro drug release, and stability studies. Results: On the basis of evaluation, all the beads show good swelling up to 12 h in 0.1 N hydrochloric acid. The swelling was followed by values in order of vegetable oil > mineral oil in case of emulsion gelation method. Scanning electron microscopy study shows that beads were spherical in shape. Comparing all the formulations, formulation FB12 was considered as optimized formulation which shows % yield 94.06±0.11, % floating 87.28±0.90, in vitro drug release 94.68, and also stable in stability studies. Conclusion: From the findings, it may be concluded that cefdinir-loaded floating beads were successfully prepared and proved to be useful for the better bioavailability and patient compliance for enhanced antimicrobial activity

Fabrication and Evaluation of Floating Mucoadhesive Tablets of Cefpodoxime Proxetil Using Factorial Design

The present research work aims to fabricate and optimize gastroretentive floating mucoadhesive tablets of Cefpodoxime Proxetil, so as to remain in the gastric region for appropriate hours and hence significantly prolong the gastric residence time of drugs which improve bioavailability. Floating-Mucoadhesive tablets of Cefpodoxime Proxetil were prepared by direct compression method using various polymers such as HPMC K 200 M, Carbopol 940P. Sodium Bicarbonate & Citric acid was incorporated as a gas-generating agents and HPMC K 200 M, Carbopol 940 P was incorporated as Mucoadhesive agent. Optimization study was carried out by using 32 factorial design. The concentration of polymers was considered as independent variables whereas Floating lag time,Swelling Index, Mucoadhesive Strength, of the tablets were utilized as dependent variables. The floating- Mucoadhesive tablets were evaluated for weight variation, hardness, thickness, friability, drug content, in-vitro buoyancy study, and in-vitro and ex-vivo Mucoadhesive studies, swelling index and in-vitro dissolution studies. The study reveals the significant effect of the amount of polymers on Floating lag time, Swelling Index, Mucoadhesive Strength of the tablets. FTIR, DSC study indicates no drug-excipients interaction in the prepared formulations. The prepared tablets exhibited satisfactory physico-chemical characteristics. All prepared batches shown good in-vitro buoyancy studies and Mucoadhesion studies. The In-vitro dissolution profiles of optimized floating- Mucoadhesive formulation of Cefpodoxime Proxetil were found to sustained the drug release up to 12 hrs and release can be extended for longer period over 12 hrs by increasing the concentration of polymers. The best result from optimized batches is of AT5 which gives floating lag time 21±2, Mucoadhesive strength 16.60 gm & drug release 98.65% in 12 hrs. Floating- Mucoadhesive tablet were prepared and could be a promising approach to deliver  Cefpodoxime Proxetil with improved gastric residence time which improve bioavailability &  effective in the management of the bacterial infection. Keywords: Cefpodoxime Proxetil, , HPMC K200M, Carbopol 940P,Floating-Mucoadhesive, factorial desig

Methodologies and tools for OSS: current state of the practice

Over the years, the Open Source Software (OSS) development has matured and strengthened, building on some established methodologies and tools. An understanding of the current state of the practice, however, is still lacking. This paper presents the results of a survey of the OSS developer community with a view to gain insight of peer review, testing and release management practices, along with the current tool sets used for testing, debugging and, build and release management. Such an insight is important to appreciate the obstacles to overcome to introduce certification and more rigour into the development process. It is hoped that the results of this survey will initiate a useful discussion and allow the community to identify further process improvement opportunities for producing better quality software

FORMULATION AND EVALUATION OF MUCOADHESIVE BUCCAL PATCHES OF PIROXICAM

The main objective of present investigation to formulate and evaluate mucoadhesive buccal patches of Piroxicam, using solvent casting method. HPMC K100 M were used as a mucocoadhesive polymer and PEG 400 used as a plasticizer as well as penetration enhancers. The formulated patches of piroxicam were evaluated for their appearance, weight variation, thickness, folding endurance, surface pH, swelling index, drug content, % elongation, mucoadhesive strength, in vitro drug release, kinetic release study and stability study. Among all formulated batches (S1-S8) of buccl patches batch S6 showing maximum drug release after 8 hours 94.77 % and mucoadhesive strength 10.21±0.35g). The stability study optimized batch S6 doesn’t show any changes with respect to previous evaluation carried out before stability study. It may concluded the mucoadhesive buccal patches of Piroxicam were successfully prepared using HPMC K100 M by solvent casting method, evaluated & it is better alternative to conventional drug delivery for the management of pain and arthititis

FORMULATION AND CHARACTERIZATION OF MUCOADHESIVE MICROSPHERES OF GLICLAZIDE HYDROCHLORIDE

This article illustrates the Formulation and Characterization of Mucoadhesive microspheres of Gliclazide Hydrochloride.The mucoadhesive microspheres were prepared by the Emulsion Solvent Evaporation method by using Eudragit L 100 and Ethyl Cellulose 22 CPS polymers & PEG 4000 added as a pore forming agent . Formulated microspheres were evaluated for various parameters. The characteristics like shape and structure of prepared microspheres were determined by Optical microscopy and scanning electron microscopy respectively. The prepared microspheres exhibited prolonged drug release (12 hrs) the mean particle size increased as the concentration of Eudragit L 100 increased. Decrease in size of microspheres leads to decrease in mucoadhesion time, % drug loading and faster the drug release. The optimized formulation shows following cumulative release after 12 hrs i.e. 96.40%. The microspheres exhibited 80% mucoadhesion and showed good drug entrapment efficiency i.e. 80.13±0.91% as well as drug loading efficiency is 26.70±0.75%.  It can be concluded that the present mucoadhesive microspheres can be an ideal system to deliver the Gliclazide Hydrochloride in the sustained release manner for management of Type II Diabetes Mellitus. Keywords: Mucoadhesive, Gliclazide Hydrochloride, Microspheres, Eudragit L 100, drug entrapment efficiency.Â

DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure

FORMULATION OPTIMIZATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ONDANSETRON HCL

The aim of the work is to design Gastroretentive tablets of Ondansetron HCl for gastric retention by using 32 factorial designs. Floating tablets of Ondansetron HCl were prepared by direct compression method using polymers, sodium alginate and excipient. Gastroretentive tablets of Ondansetron HCl were successfully prepared by effervescent technique using different gel forming polymers- HPMC K200M, and sodium alginate. Formulation was optimized by design expert software. Floating tablets were evaluated for floating time, floating lag time, drug content, raft measurement and in vitro dissolution profile. The lag time is between 17-22 sec and floating time of the formulations for 12 hrs. The best fit model is Korsemeyer Peppas Model. From the study it is proof that the sustain release by floating tablets of Ondansetron HCl can be develop. Optimized batch selected was A3, The prepared gastroretentive test formulation was found to exhibit satisfactory physico-chemical characteristics at the end of 3 months, during the stability studies. The optimized formulation A3 was found to be stable at 400C/ 75% RH. Keywords: Gastric retention time, Ondansetron HCl, HPMC, sodium alginate, measurement of raft, Factorial design, stability studies.Â

Chemical Modification: A unique solutions to Solubility problem

Almost 40% of the new chemical entities at present self find out poorly water soluble drugs. Badly water soluble drugs have solubility and dissolution related bioavailability problems. Solubility is one of the most important parameter to give desired concentration of drug in systemic circulation to get its pharmacological response. Orally administered drugs obtained completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs perform an valuable role in the process of formulation development. Enhancement of solubility of drug is the most challenging job in drug development process. Solubilization may be affected by co solvent water interaction, micellar solubilization, reduction in particle size, inclusion complexes, solid dispersion, and change in polymorph. This review highlight various techniques of solubility enhancement with special emphasis on Chemical modification methods like Salt formation, Co-crystallization, Co-solvency, Hydrotropy, use of novel solubilizer etc along with physical modification techniques. Keywords: Salt formation, Co-crystallization, Solubility, particle technologies, Milling solubility enhancement, Cosolvent, physical and chemical methods

Designing fabrication and evaluation of Oral fast Disintegrating tablet of Ranitidine HCL

The aim of this research work was to design develop & evaluate oral fast disintegrating tablets of Ranitidine HCL. The Orodispersible tablets of Ranitidine HCl were prepared by using direct Compression technique with a Synthetic Superdisintegrant such as Crosspovidone and a natural Superdisintegrant Fenugreek gum in different concentration. 32 factorial designs was applied to study the effect of independent variables,  concentration of Crosspovidone & Fenugreek gum on dependent variables like Cumulative % Drug release and Disintegration time by using design expert software. Prepared oral fast disintegrating tablets evaluated for Pre and Post-compression parameters. The prepared tablets exhibited satisfactory physico-chemical characterise especially fast disintegration & dissolution property. Full factorial design and optimization technique successfully used in the development oral fast disintegrating tablets. Comparing the all the formulations, formulation F9 was considered as optimized formulation which shows excellent fast disintegration, in vitro dissolution, and faster drug release within 6 min in comparison to other batches also stable in stability study. Keywords:  Fast disintegrating, Ranitidine, Crosspovidone, Gum, Optimizations, Water absorption rati

A Novel Derivatization Ultraviolet Spectrophotometric Method for the Determination of Amlodipine Besylate Using Benzoyl Chloride

The present research work aims to develop a novel ultraviolet UV spectrophotometric method for the determination of Amlodipine Besylate using Benzoyl Chloride as a derivatizing agent, which is simple, rapid, sensitive, selective, and accurate method for the spectrophotometric determination of Amlodipine Besylate in powder form.  Synthesis is based upon the Schotten Baumann Reaction. In this method, derivatization of aliphatic amine group of Amlodipine Besylate carried out with benzoyl chloride and aqueous sodium hydroxide (NaOH).The λmax was found to be 237 and 226nm for assay of Amlodipine Besylate and synthesised product respectively. The linearity was found in concentration range of 1-10 μg/ml. The correlation coefficient (r2)was found 0.9985. The regression equation, intercept (a) and slope (b) was found as Y=0.0762x - 0.0077, 0.0077 and 0.0762 respectively. Method was developed and validated as per ICH guidelines for linearity, accuracy, precision, LOD, LOQ, interday and intraday. The LOD and LOQ for estimation of Amlodipine besylate were found as 0.2367, 0.7178 respectively. Recovery of Amlodipine besylate was found to be 93.30%.The proposed method is found to be simple, rapid, selective and highly sensitive than most of the Spectrophotometric methods available in literature. Keywords: Derivatization, Ultraviolet spectrophotometry, Amlodipine besylate, Validation, Synthesis