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Canagliflozin (CNF) is the newest sodium/glucose cotransporters 2 (SGLT2) inhibitor used for management of type 2 diabetes mellitus having poor aqueous solubility. As very few tablet formulations are available in the market, this study aimed to develop an alternative, cost-effective formulation of CNF with enhanced solubility and dissolution profile. For this purpose, binary (F1-F8) and ternary (F9-F15) solid dispersions of CNF were formulated using polymers such as Soluplus, β-cyclodextrin, Hydroxypropyl β-cyclodextrin, Kolliphor P188 and Affinisol in varying ratios. From saturation solubility study and dissolution study, ternary dispersions F9 (CNF/Soluplus/Kolliphor P188 1:1:1) and F10 (CNF/Soluplus/Affinisol 1:1:1) showed 9.04 and 6.62 fold solubility enhancement and drug release of 100.5% and 100.16% respectively. Thus, F9 and F10 were selected for tablet formulation (namely C1 and C2 respectively) and further analysis. In the comparative dissolution study of C1, C2 and marketed formulation (Invokana), the dissolution profile of C1 was found to be comparable with Invokana having per cent drug release of 100.279% and 100.867% respectively. Thus, with the evidence of improved solubility and dissolution profile of C1, it can be concluded that ternary dispersion of CNF/Soluplus/Kolliphor P188 in 1:1:1 ratio can achieve similar dissolution as that of the marketed formulation. CNF pure drug and optimised ternary formulations were characterized by X-ray powder diffraction, thermal analysis and infrared spectroscopy. Thus, binary and ternary amorphous solid dispersions can be a potential alternative for CNF to improve solubility and dissolution profile. [ABSTRACT FROM AUTHOR]

In the present study, novel environmentally responsive ophthalmic drug delivery system composed of two gelling polymers with different phase transition mechanisms was developed in order to obtain sustained drug release in ocular cavity. Combination of polyacrylic acid (carbopol 934P) and xanthan gum was investigated as ophthalmic vehicle and assessed for its in vitro and in vivo performance. Different ratios of these polymers were used to prepare environmentally responsive ophthalmic drug delivery system by simple mixing procedure. Developed formulation was assessed for physical tests such as appearance/clarity, pH, gelation; and performance characteristics such as drug content, rheological measurement, in vitro release, antimicrobial efficiency, in vivo studies for eye irritation, residence time estimation. Prepared formulation showed agreeable appearance/clarity, acceptable pH and good gelation property. In vitro and in vivo studies demonstrated adequate drug content, desired rheological behavior and reasonable in vitro and in vivo drug release property. In conclusion, the optimum concentration of polymers results in increased residence time and sustained drug release. On the basis of these findings, environmentally responsive system based on combination of carbopol and xanthan gum may be considered as a promising tool for ophthalmic delivery. [ABSTRACT FROM AUTHOR]

The objective of this study was to investigate a novel hydrogel plug using isolated root mucilage of Sterculia urens to obtain a desired lag time for an oral chronotherapeutic colon-specific pulsatile drug delivery of indomethacin. Pulsatile drug delivery was developed using chemically treated hard gelatin capsule bodies filled with eudragit multiparticulates of indomethacin, and sealed with different hydrogel plugs (root mucilage of S. urens, xanthan gum, guar gum, HPMC K4M and combination of maltodextrin with guar gum). Indomethacin multiparticulates were prepared using extrusion spheronization, spray drying and solvent evaporation techniques with Eudragit® L-100 and S-100 (1:2) by varying drug-to-polymer ratio. After oral administration, the water-soluble cap of capsule dissolved in the intestinal fluid and the hydrogel plug swells. After a controlled time, the swollen plug subsequently ejected from the dosage form, releases the contents of the capsule. The formulation factors affecting the drug release were concentration and types of hydrogel plug used. In vivo gamma scintigraphy study in healthy rabbits proved the capability of the system to release drug in lower parts of the gastrointestinal tract after a programmed lag time. This study demonstrates that the indomethacin multiparticulates could be successfully colon-targeted by the design of time and pH-dependent modified chronopharmaceutical formulation. In conclusion, the investigated novel hydrogel plug could be a valuable tool for achieving desired lag time. [ABSTRACT FROM AUTHOR]

The aim of the present study was to formulate a self-emulsifying drug delivery system of atorvastatin calcium and its characterization including in vitro and in vivo potential. The solubility of atorvastatin calcium was determined in various vehicles such as Captex 355, Captex 355 EP/NF, Ethyl oleate, Capmul MCM, Capmul PG-8, Gelucire 44/14, Tween 80, Tween 20, and PEG 400. Pseudoternary phase diagrams were plotted on the basis of solubility data of drug in various components to evaluate the microemulsification region. Formulation development and screening was carried out based on results obtained from phase diagrams and characteristics of resultant microemulsion. Prepared formulations were tested for microemulsifying properties and evaluated for clarity, precipitation, viscosity determination, drug content and in vitro dissolution. The optimized formulation further evaluated for particle size distribution, zeta potential, stability studies and in vivo potential. In vivo performance of the optimized formulation was evaluated using a Triton-induced hypercholesterolemia model in male Albino Wistar rats. The formulation significantly reduced serum lipid levels as compared with atorvastatin calcium. Thus studies illustrated the potential use for the delivery of hydrophobic drug such as atorvastatin calcium by oral route. [ABSTRACT FROM AUTHOR]

Gellan gum-based mucoadhesive microspheres of ondansetron hydrochloride for intranasal systemic delivery were prepared to avoid first pass effect, an alternative route of administration to injection and to enhance systemic bioavailability of ondansetron hydrochloride. The microspheres were prepared using spray method. The evaluation results of microspheres were reported in our previous study. The aim of this work was to study the in vivo performance of mucoadhesive microspheres in comparison with oral and intravenous preparations of ondansetron hydrochloride. The nasal delivery system gave increased AUC0-240 and Cmax as compared to those of oral delivery. In conclusion, the gellan gum-based microsphere formulation of ondansetron hydrochloride with mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption. [ABSTRACT FROM AUTHOR]

The objective of the present study was to correlate the results of the in vitro release of a previously reported pulsatile drug delivery system with the in vivo radio imaging study. The formulated drug delivery system containing pellets of barium sulphate was administered to rabbits after overnight fast. Formulated dosage form, previously evaluated for in vitro drug release study, showed drug release after 6-10 h of lag time depending on the hardness as well as the thickness of the plug. Radio imaging study also showed that the plug in the capsule drug delivery system remains intact for the period of 6 h. Thus, the formulated drug delivery system is capable of delaying release in vitro as well as in rabbits for 6 hours. [ABSTRACT FROM AUTHOR]

The Ayurveda, the ancient Indian system of medicine, has detail mentions of importance of cow's milk, curd, ghee, urine and dung in the treatment of various human aliments. Cow dung ash has many beneficial implications in agriculture, organic farming as good quality natural manure and biopesticides, as alternate energy resources and high medicinal values. Bio-fertilizer and pest repellants obtained from cow mine and dung restores micro-nutrients and fertility of the soil and provides food free from health hazards of chemical fertilizers and pesticides. No other fertilizer in the world is as cheap and harmless as dung fertilizer. Dung and urine also provide valuable alternate source of energy in the form of biogas, fuel and electricity. In current research formulation of medicinal toothpaste from cow dung ash is checked for the improved dental health products. This toothpaste is invented to defuse which illness due to toothache. Therefore, this formulation is done by mixing the compound of toothpaste with the cow dung ash. Formulation is mixing the compound or substances prepared as per a formula. Several formula is made for a particular application and normally are hyperactive than its individual component when it used alone. However, the compound that mixing is do not react in other to get mixture with desired characteristics'. It done by measured liquid by volume and solid by weight. Toothpaste was formulated in different weight of abrasive using two methods. This formulated toothpaste was further evaluated and evaluation test are as per bureau of Indian standards. In this toothpaste cow dung ash is used as abrasive. [ABSTRACT FROM AUTHOR]

The main objective of the present research work was to develop a bilayer tablet of metoclopramide hydrochloride (MTH) and diclofenac sodium (DS) in separate layers to avoid incompatibility and thus to maximize the efficacy of both drugs in combination for the effective treatment of migraine headaches. MTH and DS were formulated as immediate and sustained release layers respectively. In vitro dissolution kinetic studies of an optimized (D10) batch of DS in both sustained release layer and bilayer tablet forms show good linearity of regression coefficient 0.9773 (first order equation). The results reveal that an optimized immediate release layer (M5) of MTH and a sustained release layer (D10) of DS might be suitable for the treatment of migraine by sequential release of the two drugs in a bilayer tablet., Lay Abstract: Migraine is a type of recurring headache of moderate to severe intensity associated with gastrointestinal, neurological, and autonomic symptoms. In migraine, a combination of pretreatment with antiemetics is required for symptomatic treatment, when nausea and vomiting are severe. In our present research, we have selected the metoclopramide hydrochloride (MTH) active ingredient for study because it has an antiemetic effect and is a prokinetic agent. MTH is more effective to counteract gastric stasis associated with migraine, and it enhances the rate of absorption of non-steroidal anti-inflammatory drugs (NSAIDs). In the present investigation we combine MTH and a second active ingredient, diclofenac sodium, as a formulated bilayer tablet to prevent degradation of MTH.