DESIGN AND EVALUATION OF BILAYER FLOATING TABLETS OF DILTIAZEM HCL

The present investigation concerns design and evaluation of bilayer floating tablets of Diltiazem HCl Diltiazem HCl is Class I drug, though its reported bioavailability is only 40 %. It is having very short half life of 3 to 4 hrs. Hence many sustained release formulations were developed for Diltiazem HCl. A direct compression method was used to formulate all batches. 32 factorial design was applied to study % cumulative drug release and hardness. Super disintigrants like Sodium starch glycolate was used for immediate release layer and HPMC K200 M, Xanthan gum like polymers were used in floating layer for sustain release layer.Optimisation study was performed by using design expert software. Successful formulation was developed having floating lag time as low as 14 sec and drug release was sustained up to 12 hrs. A biphasic drug release can be obtained by using bilayer tableting technology which involved compression of immediate and sustained release layer together. The variables HPMC K200M and Xanthan Gum evaluated in this study exhibited significant affected the release profile. Keywords: Bilayer floating tablets, Diltiazem HCl, HPMC K 200 M, Xanthan gum, % drug release

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

INSIGHT IN TO APPLICATIONS OF THERMAL SINTERING TECHNIQUE IN NDDS SPECIALLY GRDDS

Oral route the most popular route of administration for systemic action .Oral conventional drug delivery has following limitation of unpredictable gastric emptying rate, short gastro intestinal transit time, and inter subject variability leads in to less bioavailability so goal of drug delivery were not properly achieved by conventional dosage forms. So there is need of sustained drug delivery. The sustained drug delivery can be achieved by matrix tablet wherein a solid drug is dispersed in an insoluble matrix. The matrix tablets can be prepared by wet granulation method or modern thermal sintering technique. Sintering concept in the pharmaceuticals technology is very novel. The term sintering means fusion of particles or formation of welded bonds between particles of polymer. Sintering is a method of heating the material in a sintering furnace below its melting point (solid-state sintering) until its particles adhere to each other. In this process, polymer particles undergo fusion or formation of welded bonds between the each particle. Controlled release oral dosage forms were developed by sintering the polymer matrix to its glass transition temperature. The use of sintering technique adds to the effectiveness of polymers to extend the release of drug from formulation depending upon the duration and temperature of sintering. Sintering technique enhanced the extent of drug retardation from the systems studied is short enough for it to be a suitable candidate for SR formulation. The term sintering means fusion of particles or formation of welded bonds between particles of polymer. The SR oral dosage forms can be developed by sintering the polymer Gastroretentive drug delivery system is facing many challenges which can be overcome by upcoming newly sintered technique.   This review article explains about various aspects of sintering technique also highlighted some research work on sintered technology. Keywords: Oral route, sintering, sustain, thermal, drug delivery, research workÂ

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

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

Pharmacological Effects of Asiatic acid in Glioblastoma Cells under Hypoxia

Glioblastoma multiforme (GBM) is the most common and malignant primary brain tumor in adults. Despite current treatment options including surgery followed by radiation and chemotherapy with temozolomide (TMZ) and cisplatin, the median survival rate remains low (<16 months). Combined with increasing drug resistance and the inability of some compounds to cross the blood brain barrier (BBB), novel compounds are being sought for the treatment of this disease. Here, we aimed to examine the pharmacological effect of Asiatic acid (AA) in glioblastoma under hypoxia. To investigate the effects of AA on cell viability, proliferation, apoptosis and wound healing, SVG p12 fetal glia and U87-MG grade IV glioblastoma cells were cultured under normoxic (21% O2) and hypoxic (1% O2) conditions. In normoxia, AA reduced cell viability in U87-MG cells in a time and concentration-dependent manner. A significant decrease in viability, compared to cisplatin, was observed following 2hrs of AA treatment with no significant changes in cell proliferation or cell cycle progression observed. Under hypoxia, a significantly greater number of cells underwent apoptosis in comparison to cisplatin. While cisplatin showed a reduction in wound healing in normoxia, a significantly greater reduction was observed following AA treatment. An overall reduction in wound healing was observed under hypoxia. The results of this study show that AA has cytotoxic effects on glioma cell lines and has the potential to become an alternative treatment for glioblastoma

Design and characterization of orodispersible tablets of Aceclofenac

The aim of this investigation was to prepare orodispersible tablets of Aceclofenac using various concentrations of superdisintegrant agents like croscarmellose sodium, sodium starch glycolate and polyplsadone xl-10 by direct compression method. Seven formulations having superdisintegrants at different concentration levels were prepared. These tablets were evaluated for drug content, weight variation, friability, hardness, wetting time and invitro disintegration time. Formulation (F4) which shows rapid disintegration contained equal proportion of cross carmellose sodium and polyplasdone xl-10. It was concluded that superdisintegrants addition technique is a useful method for preparing orodispersible tablets by direct compression method.Keywords: Aceclofenac, Orodispersible tablets, Ac-Di-Sol, Crospovidone, Sodium starch glycolate