DEVELOPMENT AND OPTIMIZATION OF ORODISPERSIBLE TABLETS OF CARVEDILOL BY COMBINATION OF SUPER-DISINTEGRANTS ADDITION AND SUBLIMATION TECHNIQUES

Objective: Objective of the present research work was to prepare orodispersible tablets of carvedilol (CDL) for dysphagic patients.Methods: Carvedilol, an anti-hypertensive drug, was chosen as a model drug in this study. Orodispersible tablets of carvedilol were prepared using different super-disintegrating agents such as crospovidone, croscarmellose sodium and sodium starch glycolate at different concentrations. The best formulation was selected based on disintegration and dissolution profile that was further taken for sublimation studies using camphor, menthol and thymol. Drug-excipients interaction studies were carried out by fourier transform infra-red (FTIR) spectrophotometer with pure drug sample and optimized formulation.Results: The orodispersible tablet formulation having 4% croscarmellose sodium disintegrated in 92 sec. Hence this formulation was considered best formulation and taken further for sublimation studies. A formulation containing 10% w/w of menthol showed disintegration time of 16 sec with more than 96.64% drug release within 15 min. Menthol leaves the porous structure as it sublimates from the tablet. This might have contributed to the decrease in disintegration time. Hence, this formulation was considered optimized.Conclusion: From this study, it can be concluded that orodispersible tablets of carvedilol may prove to be more efficacious in the treatment of hypertension particularly in dysphagic patients

DEVELOPMENT, CHARACTERIZATION AND EVALUATION OF SOFT ORAL EDIBLE GEL USING GELLAN GUM

Objective: The objective of present research work was to formulate and evaluate a novel oral edible gel dosage form using gellan gum as gelling agent and carvedilol as a model drug to ease the administration to dysphagic and geriatric patients. Methods: Oral edible gels were prepared using gelling agent low acetylated gellan gum and sodium citrate in different concentrations. The prepared edible gel formulations were evaluated for gelation time, appearance, texture, viscosity, pH, syneresis, drug-excipient compatibility studies by fourier transform infrared FTIR and percentage of drug release from the gel formulation. Results: Formulation containing gellan gum (0.4 % w/v) and sodium citrate (0.3 % w/v)) was found to be spoon thick†in consistency that is accepted for dysphagic patients as per national dysphagia diet task force. This formulation showed more than 95 % drug release within 12 min and found to be stable for 6 mo. All other parameters tested were optimal. Hence, this formulation was considered optimized. Conclusion: From this study, it can be concluded that the novel edible gel dosage form containing Carvedilol can be formulated and this dosage form may prove to be more efficacious in the treatment of hypertension in dysphagic patients

PERFORMANCE STUDY OF FLEXIBLE PAVEMENTS ON NON EXPANSIVE SOILS

As part of infrastructure development   huge investment is being made on expansion of National highways and important roads across the country.  For improvement of Highways two types of Pavements are commonly used in India viz., Flexible Pavements (Bituminous) and rigid pavements (Concrete). Flexible pavements are widely used in this country from the considerations of economy The performance of Flexible pavements depends largely on properties of original ground on which the pavement rests, the quality of materials used in the construction of various layers of pavement and quality assurance as per relevant specifications. In general any road after construction is basically evaluated by the performance in terms of unevenness index and structural stability over a period of time. The evaluation of these two important parameters will facilitate the clear understanding of performance of various materials used in the construction and to undertake suitable rehabilitation measures if necessary. Keywords: Expansive Soil, Flexible Pavement

NOVEL PYRAZOLINES: SYNTHESIS AND EVALUATION OF THEIR DERIVATIVES WITH ANTICANCER AND ANTI-INFLAMMATORY ACTIVITIES

Objective: Synthesis of novel pyrazolines (P2-P4 & P7-P9) from the chalcones (C2-C10) obtained by condensing different aldehydes with 2-acetyl- 5-bromothiophene and evaluates them for in vitro anticancer and anti-inflammatory activities.Methods: The synthesized pyrazolines and chalcones were screened for anticancer activity against human breast cancer cell lines-MCF-7 and MDA-MB-468 in the range of 100 nm to 100 µm. Inhibition of bovine albumin denaturation and heat-induced hemolysis in vitro methods were followed to screen for anti-inflammatory activity. The structures of synthesized compounds were confirmed based on the IR, 1H NMR and mass spectral data.Results: Among the synthesized compounds, methoxy trisubstituted pyrazoline derivative (P6) exhibited an interesting profile of anticancer activity against MCF-7 cell line with GI50<0.1 μ M. similar to that of the standard drug doxorubicin. Compounds C8, P8, P3 have moderate anti-inflammatory activity in bovine denaturation and heat induced hemolytic method.Conclusion: Novel pyrazolines and chalcones were synthesized and evaluated for anticancer and anti-inflammatory activity. The methoxy containing compounds one of which P6 found to be active against MCF-7 breast cancer cell line. The chloro-substituted compounds found to show anti-inflammatory activity.Â

VALIDATED STABILITY INDICATING HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC METHOD FOR THE QUANTIFICATION OF ASENAPINE MALEATE

Objective: A stability indicating high performance liquid chromatography method using the photodiode array detector is developed and validated for the analysis of asenapine in bulk and in its tablet formulation. Methods: The method utilized a BDS Y Persil C18 (250 x 4.6 mm, 5 µm) column with 0.1% orthophosphoric acid and methanol (65:35 v/v) as mobile phase. The analysis was performed at 30 oC column temperature with a flow rate of 1 ml/min and detection at 227 nm. The method was validated for specificity, sensitivity, precision, linearity, accuracy and robustness. Asenapine was subjected to stress degradation studies under acidic, basic, oxidative, thermal and photolytic conditions. Results: Under optimized experimental conditions, asenapine was eluted from the column at a retention time of 6.781 min. The method was linear in the range of 100-300 µg/ml. The linear regression data showed good relationship (correlation coefficient (R2) = 0.9999). The relative standard deviation and mean recovery values were within limits. The analytical performance of the method was not affected when small variations in the experimental parameters were made. Degradation products resulting from stress degradation studies did not interfere with the detection of asenapine. Conclusion: The proposed stability indicting high performance liquid chromatography method is sensitive, precise, accurate, robust and specific. This method can be used for quantification of asenapine in bulk drug and in tablet dosage form in the presence of its stress degradation products

INDICATING UPLC METHOD FORQUANTIFICATION OF RELATED COMPOUNDS OF ACETYLSALICYLIC ACID IN IT`S SOLID DOSAGE FORM

A simple, sensitive and specific UPLC method was developed for the identification and quantification of related compounds of aspirin from its solid dosage forms. The chromatographic separation employs the gradient elution using C18 column with the length of 100 mm x 2.1mm dimensions by using the solvent-A (containing mixture of water and orthophosphoric acid), solution-B (containing mixture of acetonitrile and methanol) with the flow rate of 0.4mL/min. All the analytes were detected and quantified at the wavelength of 237nm by using photo diode array detector. The method was validated as per ICH guidelines and found to be specific, precise, linear and accurate. This method has very lower limit of detection and limit of quantification. The peak purity obtained with all related compounds with the aid of photo diode array detector was satisfactory. Hence this method was concluded that stability indicating method.Key Words: Aceylsalicylic acid, Aspirin, Stability indicating UPLC method

Simultaneous Estimation and Validation for Determination of Lamivudine and Zidovudine in Human Plasma By LCMS/MS Method

A high performance liquid chromatographic method with mass detection was developed for determination of Lamivudine and Zidovudine in human plasma. Lamivudine and Zidovudine were extracted from an aliquot of human plasma using Solid Phase Extraction technique, and then injected into a liquid chromatograph equipped with a tandem mass spectrometry detector; quantitation was done by peak area ratio method. A weighted (1/Conc2) linear regression was performed to determine the concentration of analyte. This method demonstrates acceptable performance and is suitable for the determination of Lamivudine and Zidovudine in human plasma over the range of 25.291 to 4046.621 ng/mL and 23.357 to 4057.l4lng/mL respectively using Solid Phase Extraction Procedure. As all the values obtained were within the limits as specified, the method has been successfully used to analyse the human plasma containing Lamivudine and Zidovudine with good recoveries and proved to be robust

Development and Validation of a Spectrophotometric Method for Quantification and Dissolution Studies of Glimepiride in Tablets

The objective of present study was to develop and validate an analytical method for quantitative determination and dissolution studies of glimepiride in tablets. The glimepiride shows absorption maxima at 225 nm and obeyed Beer's law in the range of 6.0 – 14.0 µg/mL. The limit of detection and limit of quantitation were 0.06, and 0.17 µg/mL respectively. Percentage recovery of glimepiride for the proposed method ranged from 99.32 to 100.98% indicating no interference of the tablet excipients. It was concluded that the proposed method is simple, easy to apply, economical and used as an alternative to the existing spectrophotometric and non-spectrophotometric methods for the routine analysis of glimepiride in pharmaceutical formulations and in vitro dissolution studies