M.PHARM PHARMACEUTICS

The objective of this study was to design a dual retard technique of once daily Inlay tablet of Atorvastatin calcium as Immediate Release (IR) formulation with Matrix tablet of Metoprolol tartarate as Sustained release (SR) formulation for Hypertension and Atherosclerosis. The Inlay tablet was prepared by Wet granulation method. The Compatibility of the drug with various excipients was studied by Differential scanning calorimetry (DSC). The formulations were developed by using polymers like Guar gum, Eudragit, HPMC for sustained release layer and Sodium starch glycolate, Cross povidone, Cross carmellose sodium as Super disintegrants for immediate release layer. Six formulations (F1-F6) were prepared and evaluated for various parameters like Thickness, Hardness, Weight variation, Disintegration, Swelling Erosion behavior, Simultaneous analysis by both UV and HPLC, In vitro release and Stability studies at 40º±2ºC, RH 70±5%. Among the six formulations (F1-F6), F4 possess expected release pattern in both immediate release layer and sustained release layer. Further from the Release kinetics it was revealed that the drug release for formulation F4 follows Zero order. Thus the study concludes that the formulation can overcome the disadvantages of other multilayered tablets and can be used to treat the patients having high blood pressure with Hyperlipidemia that plays major risk factors for CHD.

The aim of the present work was to prepare and investigate the valsartan nanoparticles. nanoparticles were prepared by nanoprecipitation method and the various formulations were prepared by optimizing. The prepared nanoparticles were characterized by FTIR, DSC, SEM, particle size analysis, In vitro diffusion and in vivo studies are been performed. The particle sizes of the prepared nanoparticles were ranging from 175 to 232 nm. From three formulations, F2 formulation showed best release of 60.38 % at the end of 24 th h. In vivo studies revealed that in case of free drug, 40.9 mcg/ml drug of maximum dose was recovered but in case of nanoparticles the dose recovered in serum was 16.02 mcg/ml after 6 th h. The formulation stored at 4 o ± 1 o C was more stable compared to the other temperatures. These studies suggest that the feasibility of formulating valsartan loaded Eudragit L 100 nanoparticles for the treatment of hypertension by enhancing the bioavailability.

A Novel drug delivery system for the treatment of Periodontitis was developed for site specific delivery of Aceclofenac sodium which has excellent anti inflammatory activity. Dental Implants are pharmaceutical devices in the form of strip with very small drug loading capacity and it can be formulated in the size of 0.8 x 0.4 square cm. The objective of the present study was to formulate and evaluate controlled release dosage form of Aceclofenac sodium for the topical treatment of inflammation in periodontitis. It is a site specific delivery device with once daily continuous delivery of Aceclofenac sodium as an anti inflammatory compound with excellent activity against the Inflammation. Dental Implants was prepared by Solvent casting technique, using polymers like HPMC K 100 , HPMC K 4 M, Gelatin and Ethyl cellulose with Dibutyl phthalate as Plasticizer. The physicochemical parameters like Thickness, Weight variation, Content uniformity and in vitro Release studies were evaluated and the drug release was found to follows Non-Fickian diffusion mechanism. Formulation F2 shows 20.93 % of drug at the end of 12 th hr and was considered as best formulation for further controlled release. The drug release data shows a best fit for korsermayer -Peppas fitting curve and obeys Zero order release kinetics.

The objective of the present study was to prepare and evaluate microbeads for the controlled release of lamivudine from the prepared microbeads using different polymers. The microbeads were prepared by ionic gelation method. The prepared microbeads were characterized for FTIR, scanning electron microscopy (SEM), the percentage drug content, entrapment efficiency, and in vitro dissolution studies. Accelerated stability studies were also carried out for the formulations. The microbeads were spherical in shape and free flowing. The entrapment efficiency was varying from 76 to 86%. The release of drug from the microbeads was extended up to 8 to 12 hours. FTIR studies showed the stable character of lamivudine in the microbeads. SEM studies revealed that the microbeads were porous in nature. The release kinetics studies revealed that the prepared microbeads were best fitted to the zero order for all eight formulations and peppa's model. The release kinetics data and characterization studies indicated that the drug release from microbeads was diffusion -controlled and the microbeads were stable in nature.

The objective of the present study was to improve the therapeutic efficacy of a formulation which contains two drugs i.e. Isoniazid and Salbutamol sulphate. The present invention is to provide a dosage form comprising of an active ingredient (Isoniazid) as modified release and another active ingredient (Salbutamol sulphate) as immediate release, wherein the modified release active ingredient is selected for tuberculosis and the immediate release active ingredient is selected with low dose for asthma. Once-daily sustained release matrix tablets of Isoniazid with Inlay Salbutamol sulphate tablet as an immediate release formulation, were prepared by using hydroxyl propyl methyl cellulose (HPMC) and superdisintegrants, with different polymer ratios modified release dosage form has been formulated by wet granulation method. The drugexcipients incompatibility studies were performed by Fourier Transform Infrared spectrophotometer (FTIR).The granules showed satisfactory flow properties and compressibility Index. In vitro dissolution test was carried for 12 hours and formulation F4 attained the expected release pattern in both immediate release layer (i.e. 95.20% at the end of 30 mins) and in sustained release layer (i.e. 54.22% at the end of 12 hours). Release kinetics studies revealed that the drug release from formulation F4 (12%) followed zero order kinetics with release exponent value (n) 0.806, which shows that release pattern of tablet follows Non -fickian diffusion mechanism while fitting the drug release data to Korsermeyer-Peppas fitting curve.

A reverse phase high performance liquid chromatographic method has been developed for the simultaneous estimation of valsartan and hydrochlorothiazide in bulk and in pharmaceutical formulation using RP -C18 column. The mobile phase (acetonitrile: methanol: 50 mM phosphate buffer adjusted to pH 3 with orthophosphoric acid) was pumped at a flow rate of 1.0 ml/ min in the ratio of 20: 50: 30%v/v and the eluents were monitored at 250 nm. Linearity was obtained in the concentration range of 4 -40 µg/ ml for valsartan and 1 -10 µg/ ml for hydrochlorothiazide. The method was statistically validated and RSD was found to be less than 2% indicating high degree of accuracy and precision of the proposed HPLC method. Due to its simplicity, rapidness, high precision and accuracy, the proposed HPLC method can be applied for determining valsartan and hydrochlorothiazide in bulk and in pharmaceutical dosage form.

There is an increasing demand for more patient compliant dosage form and a novel method is the development orally disintegrating tablets which dissolve or disintegrates instantly on the patient tongue or buccal mucosa. Prednisolone is a naturally occurring glucocorticoids (hydrocortisone), it targets to corticosteroid binding globulin (it regulates Enzyme regulatory activity, Enzyme inhibitory activity and protease inhibitor activity. Used in treatment of severe inflammatory conditions including allergies, arthritis, asthma, or skin reactions.Its metabolizing enzyme is Cytochrome P450 3A4 (CYP 3A40). Hence the main objective of the study was to formulate orally disintegrating tablets of Prednisolone to achieve a better dissolution rate and further improving the bioavailability of the drug. Orally disintegrating tablets prepared by direct compression and using super disintegrate like crospovidone, croscarmellose sodium and sodium starch glycolate designate, designated as three different groups of formulation (F-1 to F-13) respectively were prepared and evaluated for the pre-compression parameters such as bulk density, compressibility, angle of repose etc. The prepared batches of tablets were evaluated for hardness, weight variation, friability, drug content, disintegration time and in-vitro dissolution profile and found satisfactory. In present work wet granulation technique was employed to prepare tablets. Microcrystalline cellulose is used as diluents. Aspartame and mannitol is used as sweetening agents. Crospovidone XL10 as disintegrant. Prednisolone Sodium Phosphate was having bitter taste and to mask the bitter taste flavoring agent like mint flavor and taste masking agents like PEG4000, Ethyl cellulose 4cps, Eudrait EPO and Eudragit L100. Post compressional parameters hardness, friability, weight variation, disintegration time, drug content and dissolution studies are studied. All three groups of formulations released the drug at faster rates than that of marketed conventional tablets of Prednisolone.

Diabetes mellitus generally accompanied with major complications like Hypertension, Cardio myopathy, Stroke, Hyperlipidemia, Ischemic cerebrovascular disease, and Peripheral vascular disease. These conditions account for most morbidity and mortality among middle-aged and older people. The drug of choice for type2 diabetes mellitus is Metformin hydrochloride and for Hypertension is Metoprolol tartarate, to reduce the prevention of cardiac problems in diabetic patients. The objective of this research work was to overcome the above complication and to establish Bilayer tablet of Metformin hydrochloride (SR) with Metoprolol tartarate (IR) as a once daily formulation. The formulations of tablets (B1-B10) were prepared by using release retarding agents like HPMC K100, Eudragit S 100 for sustained release (SR) layer and super disintegrants like Crosspovidone, Sodium starch glycolate (SSG) for immediate release (IR) layer. Both sustained and immediate release granules were evaluated for flow property. Bilayer tablets were evaluated for weight variation, hardness, thickness, swelling index and in-vitro drug release for 12 hours. All the formulations obey Zero order release kinetics and the mechanism of drug release was found to be nonfickian diffusion by fitting the data to peppas equation. The result suggest that the developed Bilayer tablet of Metformin hydrochloride (SR) with Metoprolol tartarate (IR) could perform therapeutically better and improve efficacy than conventional dosage forms, and also it trounce the severe diabetic complication especially hypertension.

The present research is focused to formulate, optimize and evaluate a Nanostructured Lipid Carrier (NLC) containing Anti-hypertensive drug by hot homogenization technique followed by ultrasonication method, by altering formulation and process variables. Nine formulation of NLC was formulated based on formulation variable like different concentration of phospholipid and surfactant and also process variables like Homogenization time and Ultra-sonication time. The objective of this research is to optimize the formulation based on Particle Size, PDI, Zeta potential , Drug content, Entrapment efficiency and to select the best formulation for in vitro studies. The particle size analysis revealed that among the nine formulations, the size of F7 formulation was found to be 10.7nm which is approximately between the ranges of (10-500 nm) of NLC. The stability of the F7 formulation was evaluated by measuring the zeta potential and polydispersity index (PDI) of the NLCs by Horiba particle size analyzer and found to be-41.2mV and 0.187 respectively, thus showing uniformity in surface charge distribution and also good dis-persibility of the particles in phase and it was concluded that the F7 formulation was found to be a good and stable formulation. The percentage drug content, entrapment efficiency was found to be very high in F7 formulation viz 85.80 ± 1.64% and 89.46 ± 2.16% respectively. Thus, it was concluded that hot homogenization technique method followed by Ultrasonication was an optimized technique for the preparation of NLC nanoparticle containing Anti-Hypertensive drug like Carvedilol.

The aim of present study was to formulate and evaluate of Solid lipid particles contain Convoline. Convoline was extracted from Convolvulus pluricaulis whole plant by using hydro alcoholic extraction process and Convoline was dried by using Rotary Flash Evaporator. Convoline, an essential of Convolvulus pluricaulis with anti-epileptic activity. It is a water insoluble drug, so the oral delivery of Convoline is very difficult due to variable dissolution and low bioavailability. So they encapsulated into SLN, which enhance the penetration through lipoidal membrane and enhance bioavailability. An optimized SLN formulation consisting of Convoline, Acconon C-44 EP/NF, Span20 and PEG-200 was successfully developed with an increased dissolution rate and bioavailability. Drug kept constant for all formulations and characterizations for surface morphology (SEM), Particle size analysis, poly dispersibility index (PI), zeta potential measurement, % drug content, drug entrapment efficiency and Invitro drug release. From the results obtained it was concluded that, Convoline-Solid lipid nanoparticles (CSLN) was successfully prepared and SLN S8 formulation prepared by Acconon C-44 EP/NF showed best physicochemical and release characteristics.

The objective of this research is to formulate and evaluate Solid Lipid Nanoparticles containing Acyclovir by various phospholipids and surfactants using hot homogenization technique. Totally nine batches of SLN was formulated by hot homogenization technique and evaluates for PS,ZP,PI,Drug content, Entrapment efficiency, Invitro drug release studies and Invitro release kinetics studies. From the data's, it was concluded that hot homogenization technique method followed by ultrasonication was an optimized technique for the preparation of SLN nanoparticles containing Acyclovir, which lead to better results like high entrapment efficiency, high drug content and SLS was a better choice of surfactant to reduce the particle size and leads to uniform distribution of SLN in its phase. So, SLN will be an alternative drug delivery system for acyclovir to enhance the bioavailability and therapeutic response of drug.

Agreeable of bioavailability poorly water-soluble drugs present one of the greatest challenges in drug formulation. Nano structured lipid carrier's drug (NLC) are the most advanced and commercially viable formulation approaches. The aim of present study is to develop and compare the pharmacokinetic profile drug in NLC oral suspension form of poorly water soluble drug Carvedilol by using formulation variables like campritol-188, captex-200, as lipid, polaxomer-188, Tween-40 as surfactants, soyalecithin as co-surfactants and homogenization speed, ultra sonoication time as process variables respectively. NLC are colloidal mixture of solid lipid: liquid lipid: surfactant: co-surfactant: solvent with incorporated drug (7:3:7:0.9). Carvedilol drug under gone solubility studies in various surfactants, co-surfactants, and lipids. Optimization of formulation was, done by 2 3 factorial design by using design expert software based on variations in surfactant, co-surfactant, Homogenization speed and lipids. By optimization of the formulation in 2 3 factorial design NLC formulation region is, identified. Prepared NLC was, evaluated for thermodynamic stability (Stable), Visual assessment (clear), Drug content (29.08% ± 0.079, 29.19% ± 0.132), Entrapment Efficacy (95.01% ± 0.653, 98.12% ± 0.069), SEM (10-20µ), Particle size distribution (0.5 nm, 1.4 nm), Zeta potential (14.9 Mv,-35.6 Mv), Poly dispersity (0.429), in-vitro, drug release (78.44% ± 0.262, 78.08% ± 0.03) and invitro pharmacokinetic studies (0.979, 0.956 Zero order values).

The aim of the present study was to prepare and evaluate Solid lipid nanoparticles containing Ropinirole Hydrochloride to improve the therapeutic efficacy and reducing the frequent dosing. Double emulsion method was employed using palmitic acid as a lipid with various drug-lipid ratios for the preparation of solid lipid nanoparticles. The formulated solid lipid nanoparticles were evaluated for chemical compatibility study, percentage yield, drug content, entrapment efficiency, particle size analysis, morphology, in vitro drug release and kinetic study. It was found that there was no chemical interaction between drug and polymers used as per FTIR results. The druglipid ratio showed remarkable impact on drug content, entrapment efficiency. SEM analysis revealed that solid lipid nanoparticles are Circular in shape with smooth surface. The solid lipid nanoparticles were then loaded in capsules followed by invitro drug release study; which depicted that solid lipid nanoparticle with drug -lipid ratio 1:9 was more proficient to give controlled release at the end of 12 h. The kinetics analysis of the drug release from the solid lipid nanoparticles follows Zero order and anomalous (non-Fickian) transport mechanism.