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Palanisamy Vishnu
Asst. Professor, Dept. of Pharmaceutics, Vinayaka Mission's College of Pharmacy, Salem
Medicine & Pharmacology

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Pharmacokinetic Modification of Controlled Release Tablets of Antihypertensive Drug Palanisamy Vishnu
Journal of Global Pharma Technology Volume 10 Issue 12.
Publisher : Journal of Global Pharma Technology

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The objective of the study was to pharmacokinetic modification of controlled release tablets  of Isradipine tablets designed to provide 24 hours drug release profile using varying proportion of Eudragit L – 100 and HPMC Phthalate; Lactose monohydrate as matrix-forming material. The prepared matrix tablets showed satisfactory physicochemical properties where drug content was 99.19 % to 103.78 %, thickness was 3.23 mm to 3.36 mm, hardness was 3.37±0.13 to 3.51±0.20 kg/cm2 , friability was less than 1% and % weight variation was within the standard pharmacopoeial limits of ±10% of the weight. Mathematical analysis of the release kinetics of the optimized formulation (F15) was best fitted in zero order kinetics (R2 = 0.982). The dissolution profiles of formulation FI4 and innovator product in multi media were compared in Phosphate buffer pH 6.8.Several kinetic models respectively. The stability data reveals that the FI4 showed a negligible change in drug content thickness, weight variation, hardness, friability and in vitro drug release for three months according to ICH guidelines.
Impact of Pharmacokinetic Parameters Modifications of Tamsulosin Hydrochloride Controlled Release Pellets Palanisamy Vishnu
Journal of Global Pharma Technology Volume 10 Issue 12.
Publisher : Journal of Global Pharma Technology

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Abstract

In recent years scientific and technological advancements have been made in the research and development of controlled release oral drug delivery systems by overcoming physiological adversities. There are so many oral delivery systems in that one of the advance techniques is Pellatization. Tamsulosin  controlled  release pellets prepared by pellatization method that the Tamsulosin is coated on inert suger spheres by using non perial seeds as a binder solutions and Hydroxypropylmethylcellose, Ethyl cellose, Eudragit, Triethyl citrate coating agents used for controlled release action. The prepared pellets were evaluated for Moisture content, Acid resistance Assay, and In-vitro drug release study. All the formulation exhibited assay, Moisture content with in the range given in USP. Dissolution studies revealed that formulations containing Eudragit 0.287gms coating agent Hydroxypropylmethylcellose, 0.00312gm of ethyl cellose 0.138gm Showed 100% of drug release, at the 8th hour. The concentration of coating agents Hydroxtpropylmethycellose and Ethyl cellose had an effect on in-vitro drug release had the same drug release profile when compare with US dissolution parameters, and innovator drug release. Thus, the pellets apart from fulfilling all official and other specifications and exhibited higher rate of drug release.
Pharmacokinetic Modification of Controlled Release Matrix Tablets of Balsalazide Palanisamy Vishnu
Journal of Global Pharma Technology Volume 10 Issue 12.
Publisher : Journal of Global Pharma Technology

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Abstract

Balsalazide is used to treat a certain bowel disease (ulcerative colitis) and it also helps to reduce symptoms of ulcerative colitis such as diarrheal, rectal bleeding and stomach pain.  It has a short half life and under goes extensive first pass metabolism. In the present study, balsalazide  600mg controlled release matrices were prepared by wet granulation method and in vitro drug dissolution studies were performed to find out the drug release rate and patterns. Eudragit L-100, Eudragit RSpo, lactose and their combination were used as rate controlling polymer. Tablets were formulated using different polymers ratios. As In vitro drug releaser was carried out using USP type II (paddle method ) at 50 rpm in 900ml of acetic dissolution medium(pH 1.2) for 2 hrs, followed by 900ml alkaline dissolution medium (Ph7.4) upto 12 hrs. Mean dissolution time is used to characterize drug release rate from a dosage form and indicates the drug retarding efficiency of polymer. When Eudragit L 100 and Eudragit RSpo were used alone as the only retarding polymer, a sustained drug release pattern were not absorbed while, combination in the matrix almost doubled the time required for releasing the drug. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics.
Isradipine Loaded Solid Lipid Microparticles for improved Oral Drug Delivery: preparation, solid state characterization and pharmacokinetic evaluation PALANISAMY VISHNU
Journal of Global Pharma Technology Volume 11 Issue 04 (2019) April 2019
Publisher : Journal of Global Pharma Technology

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Purpose: The objective of the study was to develop and evaluate the isradipine (ID) loaded solid lipid microparticles (SLMs) for enhanced oral delivery. ID is a dihydropyridine calcium channel blocker, having low oral bio-availability (15-24%) due to poor aqueous solubility and also hepatic first-pass metabolism.Methods: ID-SLMs were developed by hot homogenization coupled with ultrasonication method followed by lyophilized. The prepared SLMs were optimized. Solid state characterization and surface morphology of SLMs were analyzed using FTIR, DSC, XRD and SEM, respectively. The physical stability of optimized formulation was studied at refrigerated and room temperature for 6 months. Further, single dose oral bioavailability study was conducted in male Wistar rats compared to suspension at a dose of 5 mg/kg body weight.Results: ID-SLMs prepared with Dynasan-114 (ID8) having particle size, PDI, ZP and entrapment efficiency (EE) of 618.2±4.01 nm, 0.408±0.020, -25.9 mV and 94.85±3.61%, respectively and was physically stable for 6 months. Formulation ID8 SLM showed faster release, has less particle size and more zeta potential. FTIR and DSC, XRD studies revealed that no interaction between the drug and lipids, and conversion of drug to amorphous form. SEM studies showed nearly spherical shaped particles. From in vivo studies, indicated that 2.69-folds enhancement in the bioavailability of SLM compared with control.Conclusion: Thus, the results conclusively demonstrated the role of SLMs for significant enhancement in vivo effect of ID. 
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