LIST OF TABLES Sl. Table Title of the table 1 3.01 List of US Patents for FDDS 27 2 3.02 List of drugs explored for various floating dosage forms 35 3 3.03 Gastroretentive products available in the market 36 4 4.01 Standard plot data for Verapamil hydrochloride in ph 1.2 71 5 4.02 Standard plot data for Rosiglitazone maleate in ph 1.2 73 6 4.03 Standard plot data for Losartan potassium in ph 1.2 75 7 4.04 Formulation chart of non-effervescent floating Losartan potassium tablets 76 8 4.05 Formulation chart of effervescent floating Verapamil hydrochloride tablets 77 9 4.06 Formulation chart of Rosiglitazone maleate hollow 78 10 4.07 Relationship between angle of repose and powder flow 87 11 4.08 Relationship between powder flowability & % compressibility 88 12 4.09 Number of animals required for the in vivo evaluation studies 92 13 5.01 Physical properties of non-effervescent floating tablets of Losartan potassium 99 14 5.02 FT-IR spectral data of Losartan potassium and floating matrix tablet formulation G-VI 100 15 5.03 DSC thermograms data of Losartan potassium & its floating matrix tablet formulation G- VI 102 16 5.04 % Swelling data of non effervescent floating matrix tablet formulations in ph 1.2 HCl buffer 105 17 5.05 In vitro release data of Losartan potassium from floating matrix tablet formulations 109 18 5.06 Data of various parameters of model fitting for non effervescent floating matrix tablet formulations 112 19 5.07 Stability study data of non effervescent floating tablet (G- VI) of Losartan potassium 115 20 6.01 Physical properties of effervescent floating tablets of Verapamil hydrochloride 119 FT-IR Spectral data of effervescent floating tablet of 21 6.02 Verapamil hydrochloride (B1) and Verapamil 120 22 6.03 DSC thermogram data of effervescent floating tablet of Verapamil hydrochloride (B1) and Verapamil 123 V
Table 23 6.04 24 6.05 25 6.06 26 6.07 27 6.08 28 6.09 29 7.01 30 7.02 31 7.03 32 7.04 33 7.05 34 7.06 Title of the table Effect of Sodium bicarbonate on onset and duration of floatation of effervescent floating tablet of Verapamil hydrochloride (B1) % Water uptake of effervescent floating tablets of Verapamil hydrochloride formulations in ph 1.2 In vitro drug release data of effervescent floating tablets of Verapamil hydrochloride in ph 1.2 Hydrochloric acid buffer(b1-b6) In vitro drug release data of effervescent floating tablets of Verapamil hydrochloride in ph 1.2 Hydrochloric acid buffer (B7-B13) Kinetic treatment of dissolution profile of tablets (Values of R 2, k, and n for tablets) and mechanism of drug release Stability study data of effervescent floating tablet formulation (B1) of Verapamil hydrochloride Percentage yield of Rosiglitazone maleate hollow Drug loading and encapsulation efficiency of prepared hollow of Rosiglitazone maleate FT-IR spectral data of Rosiglitazone maleate and hollow (F3) DSC thermograms data of Rosiglitazone maleate and hollow (F3) Sphericity values of Rosiglitazone maleate hollow Micromeritic properties of Rosiglitazone maleate hollow 35 7.07 In vitro % floating ability data of hollow 163 36 7.08 In vitro dissolution data of Rosiglitazone maleate hollow 168 37 7.09 Data of various parameters of model fitting of dissolution profiles of hollow (values of R 2, k and n) and mechanism of drug release 171 38 7.10 Stability study for drug content of Rosiglitazone maleate hollow (F3) 125 129 132 133 136 140 147 149 152 154 157 160 174 VI
LIST OF FIGURES Sl.. Title of the. 1 3.01 Diagrammatic representation of internal view of 8 stomach 2 3.02 Pictorial representation of the typical GI motility pattern 9 in fasting state 3 3.03 Picturisation of various gastroretentive formulations 12 location in the stomach 4 3.04 Schematic localization of an intragastric floating system 18 in the stomach 5 3.05 Hydrodynamically balanced system (HBS) showing 19 gelatinous polymer barrier formation and drug release 6 3.06 Improvement in HBS 19 7 3.07 Swellable drug delivery systems 20 8 3.08 Different geometric forms of unfoldable systems 21 9 3.09 Different unfoldabe systems and Gastroretentive dosage 22 form before and after folding 10 3.10 Schematic localization of a high density system in the 22 stomach 11 3.11 SEM photographs of microballoon and microparticle 23 12 3.12 Schematic presentation of the structure of low-density, 24 floating matrix tablets 13 3.13 Intragastric floating drug delivery device 25 14 3.14 Intragastric floating tablet 26 15 3.15 Intragastric floating bilayer tablet 26 16 3.16 Schematic representation of gas-generating systems as 29 monolayer drug delivery system 17 3.17 Schematic illustration of the barrier formed by a raftforming system 30 18 3.18 Diagrammatic sketch of the device representing its 31 operation mechanism(a,b,c,d) 19 3.19 Gas generating systems 32 20 3.20 Floating pills a) The penetration of water into effervescent layer leads to a CO 2 generation and makes the system to float (b) Mechanism of floatation 34 21 4.01 UV-Spectra of Verapamil hydrochloride in ph 1.2 70 22 4.02 Standard plot for Verapamil hydrochloride in ph 1.2 71 23 4.03 UV-Spectra of Rosiglitazone maleate in ph 1.2 72 24 4.04 Standard plot for Rosiglitazone maleate in ph 1.2 73 UV-Spectra of Losartan potassium in ph 1.2 74 25 4.05 VII
. Title of the. 26 4.06 Standard plot of Losartan potassium in ph 1.2 75 27 4.07 Diagrammatic representation of preparation of hollow 79 by Quassi-emulsion technique 28 4.08 Administration of alloxan by I.P route 93 29 4.09 Administration of by oral gauze in 93 suspension form 30 4.10 Blood collection from rat tail vein 94 31 5.01 FT-IR spectra of Losartan potassium & its floating 101 matrix tablet formulation G-VI 32 5.02 DSC thermograms of Losartan potassium & its floating 102 matrix tablet formulation G-VI 33 5.03 Photographs of in vitro floating behavior and 103 dimensional changes of matrix tablet formulation 34 5.04 Photographs showing swelling of floating matrix tablet 106 formulation in ph 1.2 HCl buffer 35 5.05 Swelling profile of floating matrix tablet formulations in 107 ph 1.2 HCl buffer 36 5.06 In vitro drug release profile of Losartan potassium from 110 floating matrix tablet formulations X-ray images showing gastric retention of floating 114 37 5.07 matrix tablet formulation G-VI in a rabbit model at different time intervals % Drug content in the non effervescent floating tablet of 116 38 5.08 Losartan potassium G-VI when stored at 25 ± 2 C & 60 ± 5 % RH for 12 months % Drug content in the non effervescent floating tablet of 116 39 5.09 Losartan potassium G-VI when stored at 30 ± 2 o C/65 ± 5 % RH for 12 months % Drug content in the non effervescent floating tablet of 117 40 5.10 Losartan potassium G-VI when stored at 40 ± 2 C & 75 ± 5 % RH for 6 months FT-IR Spectra of effervescent floating tablet of 121 41 6.01 Verapamil Hydrochloride (B1) and Verapamil DSC thermograms of effervescent floating tablet of 123 42 6.02 Verapamil hydrochloride (B1) and Verapamil Effect of amount Sodium bicarbonate on floating lag 125 43 6.03 time of effervescent floating tablet of Verapamil hydrochloride (B1) 44 6.04 Photographs of in vitro floating behavior of effervescent 126 floating tablet at different time intervals Effect of various concentrations of ingredients on 130 45 6.05 swelling index of floating tablets of Verapamil hydrochloride at the end of 8 h VIII
. 46 6.06 47 6.07 48 6.08 49 6.09 50 6.10 51 6.11 52 6.12 Title of the Swelling behavior of effervescent floating tablet of Verapamil hydrochloride subjected to dissolution testing from 0-8h In vitro drug release profiles of Verapamil hydrochloride effervescent floating tablets (B1-B6) In vitro drug release profiles of Verapamil hydrochloride effervescent floating tablets (B7-B13) X-ray images showing gastric retention of effervescent floating tablet (B1) in a rabbit model at different time intervals % Drug content in the effervescent floating tablet of Verapamil hydrochloride (B-1) when stored at 25 ± 2 C & 60 ± 5 % RH for 12 months % Drug content in the effervescent floating tablet of Verapamil hydrochloride (B-1) when stored at 30 ± 2 o C/65 ± 5 % RH for 12 months % Drug content in the effervescent floating tablet of Verapamil hydrochloride (B-1) when stored at 40 ± 2 o C/75 ± 5 % RH for 06 months. 130 53 7.01 Prepared Rosiglitazone maleate hollow 144 54 7.02 Bar graph of % encapsulation efficiency 150 55 7.03 Bar graph of % drug loading 150 56 7.04 FT-IR spectra of Rosiglitazone maleate and hollow 152 (F3) 57 7.05 DSC thermograms of Rosiglitazone maleate pure drug 154 and hollow (F3) 58 7.06 Scanning electron microscopic photograph of 155 at different magnifications 59 7.07 Image using camera lucida showing sphericity of hollow 156 microsphere at 10x magnification 60 7.08 Bar graph of particle size distribution of hollow 161 61 7.09 Particle size distribution curve of F3 161 62 7.10 Bar graph of in vitro % floating hollow 163 63 7.11 X-ray images showing floating ability of hollow 165 at different time intervals in rabbits 64 7.12 In vitro drug release profile of Rosiglitazone maleate 169 hollow microsphere (F1-F6) 65 7.13 In vitro drug release profile of Rosiglitazone maleate 169 hollow microsphere (F7-F11) Comparison of in vivo plasma glucose levels in alloxaninduced 173 diabetic albino rat following oral administration of pure drug (group III) and 66 7.14 Rosiglitazone maleate hollow microsphere F3 (group IV), with plasma glucose levels of normal rat (group I) and alloxan-induced diabetic rat without drug (group II) 134 134 138 140 141 141 IX
. 67 7.15 68 7.16 69 7.17 Title of the % Drug content in the hollow microsphere of Rosiglitazone maleate (F3) when stored at 25 ± 2 C & 60 ± 5 % RH for 12 months % Drug content in the hollow microsphere of Rosiglitazone maleate (F3) when stored at 30 ± 2 C & 65 ± 5 % RH for 12 months % Drug content in the hollow microsphere of Rosiglitazone maleate (F3) when stored at 40 ± 2 C & 75 ± 5 % RH for 12 months. 175 175 176 X