DEVELOPMENT AND EVALUATION OF FLOATING TABLET OF METOPROLOL SUCCINATE FOR INCREASED BIOAVAILABILITY VIA IN VIVO STUDY

Objective: This study was performed to formulate a floating tablet using hydrophobic glyceryl behenate (GB) and hydrophilic hydroxypropyl methylcellulose polymers, optimization of the same for retention in stomach and sustained drug delivery over a period of 20 h from upper gastrointestinal tract so as to increase its oral bioavailability.Methods: Granules of GB with the metoprolol succinate (MS) was formulated and compressed with the other ingredients to formulate a floating tablet. Physiochemical parameters of an optimized formulation along with its in vitro buoyancy study, dissolution study, in vivo studies in rabbit, and stability studies were performed.Results: Differential scanning calorimetry data show no interaction between polymers and the drug MS. A 32 factorial design was applied for optimization purpose, and from ANOVA and surface response plot the best formulation (F3) was obtained. In vitro dissolution study shows sustained drug release for 20 h for all the formulations and in vivo studies using rabbit model show increased bioavailability of an optimized formulation F3 as compared to the marketed sustained release formulation of MS (25 mg). Stability study shows no comparable differences in physical parameters and the drug release of initial formulation and the one which is kept for accelerated stability testing.Conclusion: Hence, we can conclude that a floating tablet containing a combination of hydrophilic and hydrophobic polymers can be used for gastric retention for more than 20 h which will increase the oral bioavailability of MS

PREFORMULATION STUDIES USING LACTOSE IN DEVELOPMENT OF SOLID ORAL DOSAGE FORM: A GRAPHICAL REPRESENTATION USING SeDeM METHOD

Objective: The objective of the study is to evaluate and present lactose scientifically as an excipient of choice in formulation development of solid orals dosage form for direct compression method. Present work will establish the ability of lactose as an excipient to be the choice of candidate while developing formulation having poor flow API using direct compression process. In addition to this different type of lactose is processed using secure development method (SeDeM) in order to evaluate best suitable type of lactose amongst its different type.Methods: Lactose anhydrous, lactose monohydrate and Lactose spray dried (SD) were employed for evaluation using SeDeM method, twelve different selected pharmacotechnical parameters were determined experimentally and were treated mathematically and expressed in the graphical representation as SeDeM diagram. Parameter index, parameter profile index and good compression index values were calculated.Results: Good compression index was found to be 6.06,5.72,6.83 parameter index was 0.25, 0.42, 0.17 and parameter profile index found to be 6.36,6.01,7.18 for lactose anhydrous, lactose monohydrate and Lactose SD respectively.Conclusion: This research work reveals that data obtained will be useful for the pharmaceutical industries while formulating the drug product and will reflect the scientific characteristics of this excipient as well. This will enable the availability of values obtained after performing SeDeM studies on lactose to scientific society based on the results researchers can use establised data and statistics in their pre-formulation studies to incorporate lactose with confidence and can be justified scientifically in the development formulation of the direct compression process and API having poor flow. Results indicating good direct compression characteristics of the all 3 type of lactose, and Lactose SD can be preferred amongs these 3 types.Â

DEVELOPMENT AND VALIDATION OF UV-VISIBLE SPECTROSCOPIC METHOD FOR ESTIMATION OF CARBAMAZEPINE IN BULK AND TABLET DOSAGE FORM

Objective: To develop and validate simple, accurate, rapid, precise, reproducible and cost effective spectrophotometric method for the quantitative estimation of carbamazepine in a pharmaceutical formulation.Methods: The developed UV spectrophotometric method for the quantitative estimation of carbamazepine is based on measurement of absorption at maximum wavelength 284 nm using methanol as a solvent. The stock solution of carbamazepine was prepared, and subsequent suitable dilution was prepared in distilled water to obtained standard curve. The standard solution of carbamazepine shows absorption maxima at 284 nm.Results: The drug obeyed beer lambert's law in the concentration range of 2-14 µg/ml with regression 0.9997 at 284 nm. The overall % recovery was found to be 99.99% which reflects that the method was free from the interference of the impurities and other excipients used in the formulation. The low value of % RSD was indicative of accuracy and reproducibility of the method. The % RSD for inter-day and intra-day precision was found to be 0.1568 and 0.1746 respectively which is<2% hence proved that method is precise.Conclusion: The results of analysis have been validated as per International Conference on Harmonization (ICH) guidelines. The developed method can be adopted in routine analysis of carbamazepine in tablet dosage form as well bulk dosage form.Keywords: Carbamazepine, UV Spectrophotometry, Method development, Validation, ICH guidelines, Methanol

THE HEN'S EGG TEST - CHORIO-ALLANTOIC-MEMBRANE (HET -CAM) AND HAEMOLYSIS STUDY AS AN ALTERNATIVE TEST FOR OCCULAR IRRITANCY ANIMAL EXPERIMENTS (Draize Test)

Human eyes are frequently exposed to chemicals accidentally or on purpose due to their external location. Therefore, chemicals are required to undergo the evaluation of the ocular irritancy for their safe handling and use before release into the market. Draize rabbit eye test developed in 1944, has been a gold standard test which was enlisted as OECD TG 404 and OECD TG 405 but it has been criticized with respect to animal welfare due to invasive and cruel procedure. To replace it, diverse alternatives have been developed: (i) Hen Egg Test-Chorio-Allantoic-Membrane (HET-CAM) test (ii) RBC Haemolysis study

DEVELOPMENT AND EVALUATION OF FLOATING TABLET OF METOPROLOL SUCCINATE FOR INCREASED BIOAVAILABILITY VIA IN VIVO STUDY

Objective: This study was performed to formulate a floating tablet using hydrophobic glyceryl behenate (GB) and hydrophilic hydroxypropyl methylcellulose polymers, optimization of the same for retention in stomach and sustained drug delivery over a period of 20 h from upper gastrointestinal tract so as to increase its oral bioavailability. Methods: Granules of GB with the metoprolol succinate (MS) was formulated and compressed with the other ingredients to formulate a floating tablet. Physiochemical parameters of an optimized formulation along with its in vitro buoyancy study, dissolution study, in vivo studies in rabbit, and stability studies were performed. Results: Differential scanning calorimetry data show no interaction between polymers and the drug MS. A 32 factorial design was applied for optimization purpose, and from ANOVA and surface response plot the best formulation (F3) was obtained. In vitro dissolution study shows sustained drug release for 20 h for all the formulations and in vivo studies using rabbit model show increased bioavailability of an optimized formulation F3 as compared to the marketed sustained release formulation of MS (25 mg). Stability study shows no comparable differences in physical parameters and the drug release of initial formulation and the one which is kept for accelerated stability testing. Conclusion: Hence, we can conclude that a floating tablet containing a combination of hydrophilic and hydrophobic polymers can be used for gastric retention for more than 20 h which will increase the oral bioavailability of MS

Recent trends and future of pharmaceutical packaging technology

The pharmaceutical packaging market is constantly advancing and has experienced annual growth of at least five percent per annum in the past few years. The market is now reckoned to be worth over $20 billion a year. As with most other packaged goods, pharmaceuticals need reliable and speedy packaging solutions that deliver a combination of product protection, quality, tamper evidence, patient comfort and security needs. Constant innovations in the pharmaceuticals themselves such as, blow fill seal (BFS) vials, anti-counterfeit measures, plasma impulse chemical vapor deposition (PICVD) coating technology, snap off ampoules, unit dose vials, two-in-one prefilled vial design, prefilled syringes and child-resistant packs have a direct impact on the packaging. The review details several of the recent pharmaceutical packaging trends that are impacting packaging industry, and offers some predictions for the future

Design and development of controlled porosity osmotic tablet of diltiazem hydrochloride.

The present work aims towards the design and development of extended release formulation of freely water-soluble drug diltiazem hydrochloride (DLTZ) based on osmotic technology by using controlled porosity approach. DLTZ is an ideal candidate for a zero-order drug delivery system because it is freely water-soluble and has a short half-life (2-3 h). Sodium chloride (Osmogen) was added to the core tablet to alter the solubility of DLTZ in an aqueous medium. Cellulose acetate (CA) and sorbitol were used as semipermeable membrane and pore former, respectively. The effect of different formulation variables namely concentration of osmogen in the core tablet, % pore former, % weight gain, pH of the dissolution medium and agitation intensity on the in vitro release was studied. DLTZ release was directly proportional to % pore former and inversely proportional to % weight gain. The optimized formulation (F8) delivered DLTZ independent of pH and agitation intensity for 12 h at the upper level concentration of % pore former (25% w/w) and middle level concentration of % weight gain (6% w/w). The comparative study of elementary osmotic pump (EOP) and controlled porosity osmotic pump revealed that it superior than conventional EOP and also easier and cost effective to formulate

Synthesis, and the antioxidant, neuroprotective and P-glycoprotein induction activity of 4-arylquinoline-2-carboxylates

An efficient formic acid catalyzed one-pot synthesis of 4-arylquinoline 2-carboxylates in water via three-component coupling of arylamines, glyoxylates and phenylacetylenes has been described. 4-Arylquinoline 2-carboxylates 1o and 1q displayed significant antioxidant activity as indicated by their Fe-reducing power in the ferric reducing ability of plasma (FRAP) assay. The compounds were found to react directly with hydrogen peroxide, which might be one of the mechanisms of their antioxidant effect. Compounds 1o and 1q effectively quenched H<SUB>2</SUB>O<SUB>2</SUB> and amyloid-β-generated reactive oxygen species (ROS) and also displayed significant protection against H<SUB>2</SUB>O<SUB>2</SUB>-induced neurotoxicity in human neuroblastoma SH-SY5Y cells. Additionally, all compounds exhibited promising P-glycoprotein induction activity in human adenocarcinoma LS-180 cells, indicating their potential to enhance amyloid-β clearance from Alzheimer's brains. Furthermore, all compounds were relatively non-toxic to SH-SY5Y and LS-180 cells (IC₅₀ &#62; 50 μM). The promising antioxidant, ROS quenching, neuroprotective and Pgp-induction activity of these compounds strongly indicate their potential as anti-Alzheimer's agents