Pulsatile drug delivery system is the most interesting time- and site-specific system. This system is designed for chronopharmacotherapy which is based on circadian rhythm. The principle rationale for the use of pulsatile release is for the drugs where a constant drug release, i.e., a zero-order release is not desired. Pulsatile drug delivery system is defined as the rapid and transient release of certain amount of molecules within a short time period immediately after a predetermined off-release period, i.e., lag time. Various systems like capsular systems, osmotic systems, pulsatile system based on the use of soluble or erodible polymer coating, use of rupturable membranes and pulsatile system based on membrane permeability are summarized in this article. These systems are beneficial for the drugs having chronopharmacological behavior where night time dosing is required and for the drugs having high first-pass effect and having specific site of absorption in gastrointestinal tract.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Terbinafine HCl (Poorly water soluble drug), when prepared as solid dispersion showed improved solubility and dissolution. So the main purpose of this investigation was to increase the solubility and dissolution rate of Terbinafine HCl by the preparation of its solid dispersion with polyvinyl pyrrolidone K30 using solvent evaporation methods. FT- IR spectra revealed no chemical incompatibility between drug and polyvinyl pyrrolidone K30. Drug-polymer interactions were investigated using differential scanning calorimetry (DSC), Powder X-Ray Diffraction (PXRD).

[ABSTRACT]  [FULL TEXT]  [PDF]

Nanoparticle has emerged as a promising strategy for the efficient delivery of drugs used in the treatment of cancer by avoiding the reticuloendothelial system, utilizing the enhanced permeability and retention effect and tumor-specific targeting. Delivery methods using nanoparticle are highlighted including both degradable and non-degradable polymers. The preparation techniques include emulsion polymerization, micelle polymerization, desolvation of macromolecule, and emulsion-solvent evaporation methods. The particle size of the polymeric nanoparticle is in the nanometer range (10-1000 nm) and is dependent on the method of preparation employed.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

The purpose of this review is to give detail insight of pluronic lecithin organogels (PLOs) as a topical and transdermal drug delivery system. Pluronic lecithin organogel is a microemulsion-based gel that has been effectively used by physicians and pharmacists to deliver hydrophilic and lipophilic drugs topically and transdermally across the stratum corneum. It is thermodynamically stable, viscoelastic, and biocompatible gel composed of phospholipids (lecithin), organic solvent, and polar solvent. Various types of therapeutic agents have been easily incorporated in PLO to improve their topical drug delivery. Pluronic lecithin organogel improves the topical administration of drug mainly because of desired drug partitioning, biphasic drug solubility, and the modification of skin barrier system by organogel components. Beside this, it shows low skin irritation, increases patient compliance, reduces side effects, avoids first pass metabolism, and increases efficiency of drug. In addition, PLO has been shown in vivo and in vitro to modulate the release and permeation of drugs applied transdermally. Thus, in future, it has wide range of applications and opportunities to experiment with various drugs in this type of drug delivery system.

[ABSTRACT]  [FULL TEXT]  [PDF]

Metformin hydrochloride is an orally administered antihyperglycemic agent, used in the management of non-insulin-dependant (type-2) diabetes mellitus. Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Unfortunately, a high percentage of patients suffering from type-2 diabetes are elderly people showing dysphagia. In this study, orally disintegrating tablets were prepared using direct compression and wet granulation method. First, the tablets of metformin were prepared using starch RX1500 and microcrystalline cellulose by direct compression. The tablets showed erosion behavior rather than disintegration. Then lactose was incorporated which created pores to cause burst release of drug. But these tablets did not give good mouth feel. Thus, Pearlitol SD 200 (spray dried mannitol) was used to prepare tablets by wet granulation (10% polyvinylpyrrolidone in Isopropyl alcohol as binder). The optimized batches of tablets (LMCT3 and MP13) not only exhibited desired mouth feel but also disintegration time, in vitro dispersion time, water absorption ratio, and in vitro drug release. All the batches contained 15% starch 1500 and 4% of croscarmellose sodium. The optimized batches prepared by direct compression and wet granulation showed 85% drug release at 4 min and 8 min, respectively. The strong saline and slight bitter taste of the drug was masked using nonnutritive sweetener and flavor.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

A simple, rapid, accurate, precise and reproducible simultaneous equation method has been developed for simultaneous estimation of ambroxol hydrochloride and cetirizine hydrochloride in tablets. Ambroxol hydrochloride has absorbance maxima at 243 nm, while cetirizine hydrochloride has absorbance maxima at 229 nm in glass-distilled water. The method developed involves no separation or extraction process. The proposed methods were successfully applied to the determination of ambroxol hydrochloride and cetirizine hydrochloride in tablets, with high percentage of recovery, good accuracy, and acceptable precision. Different analytical performance parameters such as linearity, precision, accuracy, limit of detection, limit of quantitation, and robustness were determined according to International Conference on Harmonization ICH Q2B guidelines. Results of analysis of formulation given as percentage of label claim ± relative standard deviation were found to be 99.27 ± 0.8083 and 102.43 ± 1.5357 for ambroxol hydrochloride and cetirizine hydrochloride respectively. Results of recovery studies given as percentage of label claim ± relative standard deviation were found to be 99.88 ± 0.3811 and 100.36 ± 2.0480 for ambroxol hydrochloride and cetirizine hydrochloride respectively.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Metformin hydrochloride is an orally administered antihyperglycemic agent, used in the management of non-insulin-dependant (type-2) diabetes mellitus. Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Unfortunately, a high percentage of patients suffering from type-2 diabetes are elderly people showing dysphagia. The above problem becomes even more severe due to high dose (500-1000 mg) and need for daily intake of metformin. Thus, the above titled work was undertaken to provide patient friendly dosage form. Not only metformin is poorly compressible (Carr's index 37), but effervescent ingredients are also poorly compressible so, method of wet granulation was used for preparation of tablets using absolute alcohol as binder. Metformin effervescent tablets were prepared using citric acid (CA), tartaric acid (TA), and treated sodium bicarbonate (heating at 120°C for 30 min), glycine, talc, sucralose, and mango flavor. Controlled heating of sodium bicarbonate formed a sheath or desiccant skin of sodium carbonate on bicarbonate nucleus leading to surface passivation which prevents onset effervescent reaction in presence of moisture leading to stability. Of all combinations, CA and TA in the molar ratio 1:2 was found to be most stable as higher amount of least hygroscopic TA protects hygroscopic CA from the attack of moisture. Also, it was found that using treated sodium bicarbonate in stoichiometric ratio gave substantially stable effervescent tablets on short term stability study (room temperature and humidity and 75% relative humidity (RH) and room temperature) as sodium carbonate preferentially absorbs moisture. All the ingredients selected were water soluble.

[ABSTRACT]  [FULL TEXT]  [PDF]

Dionvenience of administration and patient compliance are gaining significant importance in the design of dosage forms. Metformin hydrochloride is an orally administered antihyperglycemic agent, used in the management of non-insulin-dependant (type-2) diabetes mellitus. Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Unfortunately, a high percentage of patients suffering from type-2 diabetes are elderly people showing dysphagia. Persons suffering from dysphagia may get choked when they consume liquid formulation, thus to alleviate such problem liquid formulation of high viscosity was prepared. Formulation of oral soft gel batches of metformin was carried out using hydrophilic polymer gellan gum at concentrations ranging from 0.2-0.4% w/v and sodium citrate at two different concentrations (0.3% and 0.5%). The prepared batches were evaluated for appearance, viscosity, pH, drug content, syneresis, in vitro drug release, and taste masking. The batch with 0.4% w/v gellan gum and 0.5% sodium citrate not only showed 85% drug release at 15 min, but all the desired organoleptic properties. The taste masking was carried out using nonnutritive sugar and flavors. The optimized batch showed substantial stability when subjected to short term stability study (0-8°C and Room temperature). The problem of dose measurement by patients was outweighed as oral medicated gels are to be packed in unit dose container.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]

Hydrotropy is one of the reliable methods to enhance aqueous solubility of poorly soluble drugs. In the present investigation, hydrotropic solution of urea (6 M) was employed as a solubilizing agent to solubilize the poorly water-soluble drug, cefadroxil, in the tablet form and determined with the help of spectrophotometric determination in ultraviolet region. In solubility determination study, it was found that there was more than 10-fold enhancement in solubility of cefadroxil in 6-M urea solution. Cefadroxil showed maximum absorption at 263 nm and obeyed Beer's law in concentration range of 10-80 µg/ml. Results of analysis were validated statistically and by recovery studies. The proposed method is new, simple, eco-friendly, economic, and accurate and can be utilized in routine analysis of cefadroxil tablets.

[ABSTRACT]  [FULL TEXT]  [PDF]

A simple, precise, and economical procedure for the simultaneous estimation of rabeprazole sodium and itopride hydrochloride in tablet formulation has been developed. Rabeprazole sodium belongs to the class of proton pump inhibitor and Itopride hydrochloride belongs to the class of anticholinesterase activity as well as dopamine D2 receptor antagonistic activity, is being used for the symptomatic treatment of various gastrointestinal motility disorders. The present method involves the solving of simultaneous equations (Vierodt's method). Rabeprazole sodium has absorbance maxima at 283 nm in phosphate buffer (pH 7.4) and itopride hydrochloride absorbance maxima at 258 nm in phosphate buffer (pH 7.4). Both these drugs obey Beer's law in the concentration range employed for the present method. The result of analysis has been validated statistically by recovery studies. The slope and intercept for rabeprazole sodium were 0.0407 and 0.02 and for itopride hydrochloride were 0.0214 and 0.168, respectively, as determined by the method of least squares. The results were found satisfactory and reproducible. The method was applied successfully for the estimation of rabeprazole sodium and itopride hydrochloride simultaneously in tablet dosage to form without the interference of common excipients.

[ABSTRACT]  [FULL TEXT]  [PDF]

Diabetes mellitus is a chronic metabolic disorder characterized by elevated blood glucose concentration known as hyperglycemia. Diabetes mellitus covers a wide range of heterogeneous diseases and involves management of its associated acute and chronic complications; thus, there is every possibility of administering other drugs along with the primary anti-diabetic agent, which may be the cause for a drug-drug interaction to occur. In the present study, the possible pharmacodynamic interaction was studied with amlodipine besylate and gliclazide in diabetic rats and healthy rabbits. The animals were divided into three groups. Gliclazide was studied at a dose of 1.44 mg/200 g and 5.6 mg/1.5 kg body weight in rats and rabbits respectively. Amlodipine besylate at a dose of 0.090 mg/200 g and 0.350 mg/1.5 kg body weight was used for the interaction study in rats and rabbits respectively. The drugs were administered orally and the blood samples were collected before and after administration of drug for a period of 16 h in rats and 24 h in rabbits. The serum samples were then subjected to glucose estimation by glucose peroxides method. The percentage reduction in blood glucose levels were calculated with respect to initial levels. Gliclazide showed a significant reduction of elevated and normal blood glucose levels. The extent of blood glucose reduction was comparatively reduced in the case of combination therapy of amlodipine besylate and gliclazide. The study also suggests the necessity to readjust the dose of gliclazide when co-administered with amlodipine besylate.

[ABSTRACT]  [FULL TEXT]  [PDF]

The present study was aimed for the development and evaluation of hydrotropic starch gels of terbinafine hydrochloride which is an allylamine derivative of antifungal agent was formulated by using corn starch and sodium salicylate as hydrotropic salt. The gels were prepared in presence and absence of propylene glycol. The prepared gels were evaluated for in vitro drug release, rheological behavior and microbial studies. The degree of increase in the drug diffusion was found to be in order corn starch gel with propylene glycol was greater than corn starch gel without propylene glycol. The microbial studies were carried out in soya bean casein digest medium with Candida albicans as test organisms and were found to be 22.86 ± 0.58 and 20.22 ± 0.65 mm for TCSG (IV) and TCS (III), respectively. All the gels exhibited shear thinning. The rheogram indicated that the gel systems are pseudoplastic and exhibited thixotropy. The added propylene glycol has not appreciably altered the apparent viscosity values.

[ABSTRACT]  [FULL TEXT]  [PDF]

[FULL TEXT]  [PDF]