Current Issue : January-March Volume : 2011 Issue Number : 1 Articles : 23 Articles
Rapid developments in the field of molecular biology and gene technology resulted in generation of many macromolecular drugs/compounds with superior pharmacological efficacy, site specificity and devoid of toxic effects. However, the major problem for the oral delivery of these therapeutic agents is their extensive presystemic metabolism, instability in acidic environment resulting into inadequate and erratic oral absorption. Parenteral route of administration is the only established route that overcomes all these drawbacks associated with these drugs. But, the parenteral formulations are costly, have least patient compliance and require repeated administration. The buccal delivery system found to be most convenient and easily accessible site for the delivery of such therapeutic agents. This route provides direct access to the systemic circulation through the internal jugular vein thus avoiding the hepatic first-pass effect and degradation in the gastrointestinal tract, ease of administration, and the ability to terminate delivery when required. The epithelium that lines the oral mucosa is a very effective barrier that restricts the membrane permeation for many drugs administered via this route, and can be a limiting factor to the absorption of drugs. The use of penetration enhancers is one approach for improving buccal drug delivery. This requisite has fostered the study of penetration enhancers that will safely alter the permeability restrictions of the buccal mucosa. This review concentrates on various classes of transmucosal chemical permeation enhancers such as bile salts, surfactants, fatty acids and their derivatives, chelators, cyclodextrins and chitosan along with their mechanism of action. Even though these enhancers influence drug delivery, further exploration of these compounds is required to understand their modifying action on the properties of buccal mucosa....
The science of drug delivery is always affected by the choice of polymers which act as carriers. Synthetic polymers frequently suffer from the problem of being non-biocompatible, non-biodegradable and expensive. Natural polymers therefore are a promising solution to this problem. Chitosan is fiber-like substance derived from chitin, a homopolymer of �Ÿ-(1?4)-linked N-acetyl-D-glucosamine, infact second most abundant polysaccharides found in nature and it is one of material yet to be utilized to its full potential . Our objective is to appraise the state of the art concerning this polysaccharide and to take a closer look at chitin and chitosan applications. Chitosan, which is soluble in acidic aqueous media, is used in many applications (food, cosmetics, biomedical and pharmaceutical applications) because of their biocompatibility, biodegradability and non-toxicity, apart from their antimicrobial activity and low immunogenicity, which clearly points to an immense potential for future development. These candidate biopolymers can be easily processed into gels, sponges, membranes, beads and scaffolds forms. It has become of great interest not only as an underutilized resource, but also as a new functional material of high potential in various fields, and recent progress in chitin chemistry is quite noteworthy .From the studies reviewed it is concluded that chitosan are promising materials for pharmaceutical industry. It has shown promising properties for formulation of many novel and advanced medicines .The review article presented, explores into various aspects of existing and possible futuristic uses of chitosan in pharmaceutical and allied industries as it is the only multipurpose cationic polymer of natural origin on which worth extensive study and research has been done. Based on current research and existing products, some new and futuristic approaches in this fascinating area are thoroughly discussed....
The purpose of this research was to develop a matrix-type transdermal therapeutic system containing an antihypertensive drug, atenolol (ATL), with different concentrations of hydrophobic polymers like Eudragit RL-100 (ERL-100) and Eudragit RS-100 (ERS-100) by the solvent evaporation technique. Different concentrations of oleic acid (OA) were used to enhance the transdermal permeation of ATL. The physicochemical compatibility of the drug and the polymers was also studied by differential scanning calorimetry (DSC) and infrared (IR) spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, flatness, drug content, folding endurance, % moisture uptake and % moisture content. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. The results followed Higuchi kinetics, and the mechanism of release was diffusion-mediated. Formulation prepared with ERL 100 polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin as compared with all other formulations....
Today pelletization technology represents an efficient pathway for manufacture of drug delivery system. There is different pelletization and granulation techniques available to prepare drug loaded spherical particles or granules. Extrusion Spheronization is one of pelletization techniques and utilized in formulation of beads and pellets. Limitations related to bioavailability and site specific drug delivery can be overcome by this technique. Today this technology has gained attention because of its simple and fast processing. Compared to single-unit dosage forms, oral multiparticulate drug-delivery systems (e.g. pellets, granules) offer biopharmaceutical advantages in terms of a more even and predictable distribution and transportation in the gastro-intestinal tract. Extrusion spheronization is widely utilized in formulation of sustained release, controlled release delivery system or modified release delivery systems. This review article focused on frequently used pelletization techniques for producing pellets for oral drug delivery by extrusion spheronization process, parameters and its application in pharmaceutical industry as well as melt extrusion modified process utilized for formulation of sustained release tablets, transdermal delivery system and transmucosal delivery system in pharmaceutical industry. Each technique has its own advantages and disadvantages. Layering processes have been used over the years for manufacturing of pellets. Most of the scientists have focused research on refining and optimizing existing pelletization techniques and also focused on the development of novel approaches and procedures of manufacturing pellets employing innovative formulation and processing equipment. These pelletization techniques have great impact on the development of different type’s novel drug delivery systems. A number of pelletized products are being designed to maximize the in vivo performance of medications already in the market and to meet all regulatory requirements....
Gastro-retentive floating drug delivery systems have emerged as an efficient means of enhancing the bioavailability and controlled delivery of many drugs. FDDS promises to be a potential approach for gastric retention. The purpose of writing this review on floating drug delivery systems (FDDS) is to compile the recent literature with special focus on the principal mechanism of floatation to achieve gastric retention. The recent developments in FDDS which includes- the approaches in designing of single-unit and multiple-unit floating systems, and their classification, formulation aspects and applications of these systems are also covered in detail. This review also summarizes the in vitro techniques and in vivo studies to evaluate the performance of floating drug delivery systems....
The objective of this research was to prepare and evaluate buccal adhesive controlled release tablets of Diltiazem hydrochloride by direct compression method using Carbopol960p ,Guar gum and Xanthan gum as rate retardant polymers in concentration of 5%,15%,30%w/w. The formulations were evaluated for weight variation ,Hardness, %Friability, %Drug content, Mucoadhesive strength, surface pH and invitro drug release studies. Mucoadhesive strength was determined by the force of detachment in grams and was found to be between 17.67+0.141gm to 56.7+0.14gm and Surface pH was found to be 7. Invitro release studies revealed that as polymer concentration increases from 5% to 30%w/w, rate of drug release was retarded and the data was fitted into pharmacokinetic models. Among all other formulations, formulation (F5) containing 15%w/w of guar gum was found to be best as the release was retarded upto 8 hours and it follows zero order with non-fickian diffusion mechanism....
Metformin hydrochloride is an biguanide class of antidiabetic agent superior to the phenformin, therefore an attempt to extend release of metformin hydrochloride was carried out using Eudragit L100, Eudragit NE 30D and Hydroxy propyl methyl cellulose (HPMC)/ethylcellulose (EC) combination. The technique employed was wet granulation followed by compression. The matrix tablets prepared with different proportions of the retarding polymers were subjected to various physico-chemical characterizations. The in vitro release profiles of the resulting tablets were evaluated in 0.1N Hcl for 2 hrs and pH 6.8 phosphate buffer for remaining hours. Preliminary data suggested that the matrix tablets made with HPMC/EC combination of polymer showed a great promise as a retardant for release. The other in process quality parameters were also studied for the same batch of tablets that gave in vitro profiles in accordance with the theoretical release profiles. The shelf life of the product was determined by subjecting the tablets to various temperatures. The stability of drug in the formulation was determined using Fourier transform infrared spectroscopy. The release kinetics has been examined for the tablets with respect to the in vitro profiles and stability data from the stand point of a diffusion controlled process (Higuchi profile) and that of a first order kinetics. Bioavailability study using rabbits was also performed for the matrix tablets (HPMC/EC) and the pharmacokinetic treatment was given to the in vivo data obtained. The in vitro and the in vivo studies revealed the potential suitability of HPMC/ EC polymers to formulate the matrix tablets for sustaining the release of metformin hydrochloride....
Drug products that provide extended or sustained release first appear as major new class of dosage form since last few years. The extended release dosage forms as one that allows a reduction in dosing frequency from that necessitated by a conventional dosage form. The main objective is to formulate extended release oral tablet by using two types of polymers with opposing nature. These two polymers used were hydroxylpropyl methyl cellulose which is hydrophilic in nature while other was ethyl cellulose which is hydrophobic in nature. The hydrophilic polymer release drug and hydrophobic polymer controls that release by retarding the release thus give the drug in predetermined manner. We develop final formulation with optimized concentration of both polymers. Then after selection of excipients, the preformulation study was carried out like mainly drug polymer incompatibility study there were not any impurities found. Final batch then put for stability study for 1 month under 600 C temperature. Also various evaluation parameters were checked and they are weight variation, assay, hardness, in-vitro dissolution and relative substances. Final results for in-vitro dissolution were matched with marketed formulation and the match was found. The similarity factor was found near to that marketed preparation so we can say that the final batch is pharmaceutically equivalent with marketed preparation. The dose dumping study was also performed to check the release profile in 30% absolute ethanolic condition....
The aim of the present study was designed to develop model controlled release matrix tablet formulations for propranolol hydrochloride. Propranolol hydrochloride tablets were prepared by using different drug: gum ratios of guar gum, gum karaya alone and a mixture of guar gum and karaya gum (in 1: 1 ratios) by wet granulation method. The influence of the proportion of the gum on the release rate of the drug from the tablets was studied. The tablets were analyzed to determine their hardness, friability, dug content and in vitro release profile. The release of the drug is by diffusion and swelling controlled mechanisms exhibiting non-Fickian transport. The matrices containing blend of gums exhibited precise controlled release than the guar gum and karaya gum matrices because of burst effect and fast release in case of guar gum and much slow release in case of karaya gum. The first-pass effect of propranolol can be avoided by using this formulation....
The purpose of this research was to formulate tasteless complex of famotidine with Indion 214 (exchangeable ion is H+) and to evaluate molecular properties of drug complexes. The effect of batch process, complexation time, pH and drug- resin ratio on famotidine loading on Indion is reported. Drug-resin complexe (DRC) was characterized by infrared spectroscopy. The efficient drug loading was evident in batch process using Indion 214 with drug-resin ratio of 1:1.5 in 180 minutes. It was observed that optimum drug loading was achieved at 7.5 pH and was not much increased at pH higher than it. IR spectroscopy revealed complexation of –NH (drug) with Indion 214. In-vitro taste studies of DRC shown that drug release from DRC in salivary pH was insufficient to impart bitter taste. Effective and satisfactory taste masking can be obtained by using Indion 214 as ion-exchange resin this complex can be use for oral formulations....
The objective of the research work was to formulate and optimize the oral sustained release matrix tablets containing tramadol hydrochloride by 32 factorial design. Matrix tablets were prepared by wet granulation method using HPMC K15M as matrixing agent. Polynomial equations and response surface plots were generated for all dependent variables using multiple regression analysis. It was observed that both the factors had significant influence on all dependent variables studied (p<0.05). The results indicating that as the concentration of polymer increases the release rate constant was decreased. Release rate obtained was highest when lactose was employed as filler followed by dicalcium phosphate and starch. In initial stage both concentration of polymer and type of filler governed the drug release while in later stage only concentration of polymer predominates. Hence, major controlling factor for kinetics of drug release was concentration of polymer....
The present study is planned to develop Rosuvastatin calcium into immediate release tablets. Pre-formulation study and drug excipients compatibility study was done initially and the results obtained direct the way and method of formulation. Preformulation and drug excipients compatibility study, prototype formulation carried out for the dose of Rosuvastatin calcium 10 mg and optimized to get the final formula. Rosuvastatin calcium is prone to degradation so compaction and direct compression method is used. All the mentioned batches were taken by the said method. Granules were evaluated for tests such as bulk density, tapped density, compressibility index and Hauser’s ratio and sieve analysis before compression. Tablets were tested for weight variation, thickness, hardness, friability and dissolution. In vitro dissolutions were performed and (F2) values were calculated. Dissolution profile of F8 was matched perfectly with marketed (innovator) formulation and F2 value was found to be excellent. Also the impurity profile and stability result of RF8 was found to be excellent. It can be concluded that the immediate release tablet was effective and stable....
This report explains an investigation on development of fast mouth dissolve tablets of felodipine and comparison of efficiency of disintegrant functions of 3 classes of super disintegrants employing 3 different granulation techniques. In this study fast mouth dissolve tablets of felodipine were prepared using 3 classes of disintegrants like cross carmellose sodium (CCS), crosspovidone (CP) and sodium starch glycolate (SSG) employing 3 granulation techniques viz., wet granulation (WG), intra-extra granulation (IE) and direct compression (DC) techniques. 13 formulae with two levels of concentration of each superdisintegrants incorporated in the preparation of tablets by DC technique and constant concentration level of each superdisintegrant in the preparation of tablets by WG and IE technique. The granules were subjected for precompressional evaluation parameters like bulk density, tap density, and Carr�s index and the tablets were evaluated for postcompressional parameters such as hardness, friability, weight variation, in-vitro disintegration time and in-vitro dissolution study. The results obtained were within the acceptance limits. It was concluded that among the 3 disintegrants and granulation techniques, the tablets prepared with CCS as disintegrant employing with IE granulation technique were found to be superior with respect to disintegration and dissolution....
Granulation may be defined as a size enlargement process which converts small particles into physically stronger & larger agglomerates. This process involves adherence of primary powder particles to form larger, multi particle entities called granules High-shear wet granulation, fluidized-bed granulation, and roller compaction followed by milling are commonly used granulation techniques in the pharmaceutical industry. Primary granule properties of interest are granule size and size distribution, intra granular porosity and granule strength. Bulk properties of interest include bulk density, flowability, and moisture content. Several techniques to observe and control granulation processes are currently being used in the pharmaceutical industry e.g., impeller torque in high-shear mixers. More recently, probes have been used to monitor and control particle size or moisture content of the granulation in high-shear mixers and fluid-bed granulators. Appropriate use of these techniques can provide a more thorough understanding of a formulation and manufacturing process to establish meaningful design space, specifications, and manufacturing controls. Through this review article we are mainly focusing on different method of granulations and innovations in granulation technology....
This study investigated the influence of different dissolution methods on esomeprazole in-vitro release from mini-tablet coated with Eudragit L 100-55, aqueous acrylic enteric system. One of the methods utilized novel sinkers specifically designed to prevent mini-tablet from sticking to each other. This method produced the fastest and most reproducible drug release in buffer compared to USP 1 (baskets), USP 2 (paddles) or USP 2 with conventional sinkers....
There are numerous strategies that can be applied when developing combination products with soluble compounds. However, new strategies will have to be used by considering combinations with soluble and insoluble compounds. Different physical phases will have to be used to achieve the greatest pharmacokinetic profile for a number of such Active Pharmaceutical Ingredients. This will result in the need for multi-phase delivery system to deliver them. Each compartment is sealed to prevent the medicaments from escaping and coming into contact with one another. New capsule technologies: Innercap Technologies, Intestinal pressure-controlled colon delivery capsules, Colonic drug delivery system based on pectin and galactomannan coating, Azo hydrogels, Colon Targeted Delivery System, Implantable insulin pump in form of capsule and Pulsed release capsule device. Evaluation tests of the innovative capsules can be performed by weight variations, content uniformity, compatibility testing, disintegration time, lag time, in-vitro drug release, water uptake studies, rheological analysis, thermal analysis and critical Stability study. The release profile can be modulated with modification in the shell materials or coatings can be applied to target or control the release of medicaments from the compartments. Also release profile can be depended to the active compounds filled into each capsule in a number of ways....
Iontophoretic drug delivery system is viable drug delivery platform technology. Iontophoresis is an effective technique for physically facilitating transport of solutes across skin for both local and systemic effects. The principle distinguishing feature is the control afforded by iontophoresis and the dose can also be titrated for individual patients by adjusting current. It is believed to be future method of choice for the systemic delivery of protein and peptide drugs which normally can only be delivered by parenteral therapy. Iontophoretic drug delivery system is particularly desirable for drug that need prolonged administration at controlled plasma levels that basis make appropriateness to cardiovascular agents for transdermal development. Controlled zero order absorption, easy termination of drug delivery, easy to administration also support for popularity of iontophoretic delivery. This paper reviews the work on iontophoretic studies of cardiovascular agents in tabular form....
After opening up of the economy in most sectors, 1991 onwards, this industry has been no Nanobiotechnology is a recently coined term describing the junction of the two existing but isolated worlds of engineering and molecular biology. It is a combination of three words: “nano” tiny, “bio” is living things, and “technology” is about tools. It refers to the ability to create and manipulate biological and biochemical materials, devices, and systems at atomic and molecular levels. Thus, it is an integration of physical sciences, molecular engineering, biology, chemistry, and biotechnology, and holds considerable promise of advances in pharmaceuticals and health care. Nanomaterials are at the leading edge of the rapidly developing field of nanotechnology. Their unique size-dependent properties make these materials superior, crucial in many areas of human activity, and above all a tiny tool to learn about living things. Consequently it applies the tools and processes of nanofabrication to build devices for studying biosystems. In this review we discussed the role of nanobiotechnology in molecular diagnosis, drug discovery, and development of nanomedicine and personalized medicine. The FDA approval is essential for clinical applications of nanotechnology and substantial regulatory problems could be encountered in the approval of nanotechnology-based products therefore we also discussed about the limitations of use of nanobiotechnology in drug discovery....
The process of mucoadhesion involving a polymeric drug delivery system is a complex one that includes processes such as wetting, adsorption and interpenetration of polymer chains. The success and degree of mucoadhesion bonding is influenced by various polymer-based properties such as the degree of cross-linking, chain length and the presence of various functional groupings. The attractiveness of mucosal-targeted controlled drug delivery of active pharmaceutical ingredients, has led formulation scientists to evaluate numerous polymeric systems for such tasks. Formulation scientists have at their disposal a range of in-vitro and in-vivo mucoadhesion testing setups in order to select candidate adhesive drug delivery system. As such, mucoadhesive systems have found wide use throughout many mucosal covered organelles for active ingredients delivery for local or systemic effect. Evaluation of such mucoadhesive formulations has transgressed from first-generation charged hydrophilic polymer networks to more specific second-generation systems based on lectin, thiol and various other adhesive functional groups....
The potential uses of large number of herbal drugs are limited due to their poor bioavailability and poor absorption. This limitation can be improved by formulating a appropriate drug delivery system, which enhance the rate and the extent of drug. Phytomedicines, complex chemical mixtures prepared from plants, have been used in medicine since ancient times and continue to have widespread popular use. The hydrophilic nature and unique chemical structure of these compounds pose major challenge because of their poor bioavailability through the skin or gut. The use of phytosomes is a novel formulation technology which helps to overcome these problems. Phytosomes are produced by a process whereby the standardized plant extract or its constituents are bound to phospholipids mainly phosphatidycholine producing a lipid compatible molecular complex. This phytosomes resembles a little cell. It is also often known as herbosomes. The phytosomes technology has been enhanced the bioavailability of many popular herbal extracts including milk thistle, Ginkgo biloba, grape seed , green tea, hawthorn, ginseng etc and can be developed for various therapeutic uses or a dietary supplements. Phytosome exhibit better pharmacokinetic and pharmacodynamic profile than conventional herbal extracts....
Together with the permeability, the solubility behaviour of drugs remains one of the most challenging aspects in formulation of a drug and it is a key determinant of its oral bioavailability. There have always been certain drugs for which solubility has presented a challenge to the development of a suitable formulation for oral administration (i.e. Rofecoxib, Itraconazole, Glipizide, Meloxicam, and Piroxicam). Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. They are usually presented as amorphous products, mainly obtained by two major different methods, for example, melting and solvent evaporation. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. In this review, it is intended to discuss the recent advances related on the area of solid dispersions and the methods used for the characterization of solid dispersions....
The poor oral bioavailability of Ranitidine hydrochloride (RHCL) from the conventional tablets can be attenuated by designing it into gastric floating drug delivery systems. The present work is aimed for the development of sustained release floating tablet of RHCL using different viscosity grade polymers. The pre-compression properties of power mixes and post-compression properties of the floating tablets were evaluated. The tablets were prepared by direct compression method using a ten-station rotary tablet compression machine at the hardness of 5 kg/cm2. The presence of different viscosity grade gel forming polymers with gas generating agents and filler modulate the in vitro buoyancy. The formulations H5, C4 and K2 were found to be optimized and can be retained in the stomach to improve peroral sustained delivery of RHCL....
Cancer is life threatening disease causes mortality and morbidity in developed as well as in developing countries. In United States 1.44 million new cases of cancer diagnosed in the year 2008. In India there are nearly 1.5–2 million cancer cases at any given point of time and in Tamilnadu out of one core populations covering six districts such as South Tamilnadu 12,000 cancer cases are recorded every year. Nowadays, there are tremendous improvements in cancer diagnostic producers and treatment which supports the cancer patient recovers. Due to life style changes and intervention may increase the virulence of disease. Early diagnosis and advancement in screening may help the cancer patient effective treatment and monitor during treatment will increase survival rate of the patient. Many alternative medicine and holistic type of management has followed to manage the cancer. The present study reviews the cancer status, early diagnosis methods, treatment and holistic approach for effective monitoring and possible control of various type of cancer....
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