Current Issue : April-June Volume : 2011 Issue Number : 2 Articles : 27 Articles
Drug delivery via the buccal route using bioadhesive dosage forms offers such a novel route of drug administration via systemic drug delivery. The oral mucosa has a rich blood supply and it is relatively permeable. Buccal drug delivery across mucosal lining of the cheek offers a clear advantage over the peroral dosing route by avoidance of extensive first-pass metabolism and drug degradation in the harsh gastrointestinal environment can be circumvented by administering the drug via buccal route. Buccal route provides one of the potential routes for typically large, hydrophilic and unstable proteins, oligonucleotides and polysaccharides as well as conventional small drug molecules. This review article includes permeation through oral mucosa, overview of oral cavity, histology of mucosal layer, mucoadhesive mucosa interaction.. Theories of adhesion, method to study buccal adhesion, evaluation of buccal drug delivery includes surface pH study, permeation through buccal mucosa, mucoadhesive strength, and swelling index....
The dried leaves powder of Adhathoda vasica Family; Acanthaceae was formulated into tablets using the wet granulation method of massing and screening. The leaves powder and granules were subjected to determination of various micromeritic properties of granules indicated a significant improvement in the flowability. Adhathoda vasica leaves powder and granules gave a linear relationship at all applied properties and parameters. The Compressibility index, Carr's index, Hausners ratio, Kawakita equation like parameters explains the properties of granules and powder. The formulated Adhathoda vasica leaves tablets passes the quality control tests for tablet....
This study concerns the evaluation of natural polymers gum Tiruman and Tamarind seed kernel powder as sustained release matrix forming materials in tablet formulation. The matrix tablets of Diclofenac sodium were prepared by wet granulation technique. Different concentrations (5%, 10%, 15%, 20% w/w with respect to total tablet weight) of both the gums were examined to know their effect on in vitro drug release profile. Tablet weight (200mg) and diameter (8mm) was kept constant. The tablets were evaluated for their hardness, friability, drug content and in vitro drug release. Matrix tablets with 15% w/w tamarind seed kernel powder showed sustained drug delivery beyond 8h. Drug release from the polymers followed first order and the release of the drug from the matrix tablets is by diffusion mechanism. It is concluded that both the gums possess substantial matrix forming property that could be used for sustained drug delivery....
Today about 74% of drugs are taken orally and are found not to be as effective as desired. To improve such characters transdermal drug delivery system was emerged. Drug delivery through the skin to achieve a systemic effect of a drug is commonly known as transdermal drug delivery and differs from traditional topical drug delivery. Transdermal drug delivery systems (TDDS) are dosage forms involves drug transport to viable epidermal and or dermal tissues of the skin for local therapeutic effect while a very major fraction of drug is transported into the systemic blood circulation. The adhesive of the transdermal drug delivery system is critical to the safety, efficacy and quality of the product. Topical administration of therapeutic agents offers many advantages over conventional oral and invasive methods of drug delivery. Several important advantages of transdermal drug delivery are limitation of hepatic first pass metabolism, enhancement of therapeutic efficiency and maintenance of steady plasma level of the drug. This article provides an overview of types of Transdermal patches, methods of preparation and its physicochemical methods of evaluation....
In the nanotechnological development, carbon nanotubes (CNTs) have attracted a great deal of attention due to their unique structural, electrical and mechanical properties. Some of the properties of CNTs for example, superior strength; flexibility, electrical conductivity and easy chemical functionalization have been exploited for the biological application both at the cellular and molecular level. Chemical modification of CNT tips has allowed for applications such as conducting measurements as a function of pH, imaging based on specific molecular interactions, and measuring single molecule protein-protein interactions, This review highlights the various preparation methods, types, and other information regarding carbon nanotubes to a pharmaceutical scientist, hence a systemic exploration may provide a lead in establishing possible application of CNTs in this challenging and of nanotechnology based drug delivery....
Four Indian Brands (coded as A,B,C,D) of 500 mg Paracetamol tablets were evaluated for various In vitro parameters, i.e. size and shape, uniformity of weight, hardness, friability, content, disintegration time and dissolution profile. All the products met the requirements of Indian Pharmacopoeia for tablet formulation. The hardness of all the brands was found to be in the range of 3.2-5.2 kg/cm2, while friability was less than 1 %. The disintegration time of all brands was found to be in the range of 1min 30 sec to 3 min 57 sec. All brands comply the I.P. weight variation test and dissolution test. Formulation additives in the tablet, physical form of the drug used in the tablet and manufacturing process vary from manufacturer to manufacturer which is responsible for the variation in the observed dissolution profiles....
Cellulose derivatives are most widely used in the development of formulations. Different cellulose derivatives serves different functions such as disintegrant, binding agent, gelling agent, film forming polymer. It is necessary to know the micromeritical properties such as particle size and size distribution, shape and surface area which ultimately affect formulations stability, uniformity, dissolution and drug release. Hence micromeritics is helpful in evaluation of powders and granules for IPQC and QC parameters. Flow properties such as compressibility index, angle of repose affects greatly the flow properties of powders. In our present research work we studied the micromeritical and flow properties of different cellulose derivatives and from compressibility index and hausner ration we found that ethyl cellulose , methyl cellulose and carboxymethyl cellulose shows fair, passable flow properties whereas Carbopol 940 shows very poor flow properties. From porosity values it was found that ethyl cellulose, carboxyl methyl cellulose and methyl cellulose shows close packing arrangement....
Coprocessing of the excipients is done for the production of the higher quality excipients. The aim of present work is the development of the Tramadol (Opioid analgesic) oro-dispersible tablets by using co-processing excipients. Oro-dispersible tablets are easier for the administration in pediatrics, geriatrics, and bedridden, nauseous or non-compliant patients. Coprocessed excipients were prepared by using spray dryer. Prepared coprocessed were utilized for the formulation of the oro-dispersible tablats. Prepared coprocessed excipients show better flow properties than the conventional excipients. Tablets formulated by using coprocessed excipients were compared with marketed formulations and it is concluded that tablets prepared from the coprocessing of the excipients show better drug release profile than the marketed one....
Ethosomes are provides a number of important benefits including improving the drug's efficacy, enhancing patient compliance and comfort and reducing the total cost of treatment. The Ethosomes were found to be suitable for various applications within the pharmaceutical, biotechnology, veterinary, cosmetic, and nutraceutical markets. Preliminary studies with plasmids and insulin revealed that the ethosomal carrier may be used for enhanced delivery of these agents. In further work, the ethosomal technology was broadened to introduce agents into cultured cells and microorganisms. Enhanced delivery of bioactive molecules through the skin and cellular membranes by means of an ethosomal carrier opens numerous challenges and opportunities for the research and future development of novel improved therapies....
Abstract:. The available conventional vaginal preparations of Benzydamine like vaginal douche and cream have drawbacks like less contact time, messy to apply, uncomfortable for patient, chances of inaccurate drug dosing in semisolid formulations due to non-uniform distribution in the vaginal cavity, poor retention at the site of action due to the self-cleansing action of the vaginal tract. In present study Bioadhesive Tablets were prepared using Carbopol 934 and HPMC. Benzydamine hydrochloride vaginal tablets were evaluated for various parameters like thickness(mm), Hardness (kg/cm2),Average weight (mg), % Drug Content, , % Friability, Effect on pH of medium, Swelling study, in- vitro bioadhesion study, in-vitro benzidamine release study and data treatment thereof. All the physical parameters were found to be satisfactory within the specified limits. It is shown that with the developed formulations, the Benzydamine release, % Swelling and bioadhesion properties of bioadhesive tablets can be controlled by changing polymer concentration and effervescent content. The best fit dissolution kinetic model for release of Benzydamine were found to be zero order kinetic model and Higuchi square root kinetic model. Former revelead that the mechanism of drug release does not depend on concentration of drug and same amount of drug is released per unit time. While Higuchi square root kinetic model showed that drug release occurs by diffusion from Carbopol 934 and HPMC polymer matrix. Bioadhesion of the developed formulations would provide a longer period of residence time. Drug polymer compatibility studies FTIR, DSC, were also carried out indicating no incompatibility between drug and polymers used....
A study was made of the effects of physical and release properties of Zaleplon rectal suppositories with a view to providing more information for the optimization of the rectal formulation of Zaleplon. Suppositories were prepared by using water soluble PEG bases. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content, hardness, melting point, disintegration test. In-vitro release study was performed by using USP type I apparatus using phosphate buffer pH 7.4 as dissolution media. In vitro drug released from water soluble base PEG400:PEG4000 (1:1) was found faster than that from PEG400:PEG6000 (hydrous and anhydrous) bases....
In the present work fast dissolving tablets of Promethazine hydrochloride were prepared by direct compression with a view to enhance patient compliance. Three different superdisintegrants crosscarmellose, tulsion 414 and crospovidone in three different concentrations (2%, 3% and 5%) and nine formulations were made. The granules were examined for pre-compression parameters. The prepared formulations were evaluated for weight variation, friability and hardness, disintegration time, wetting time, % drug content and in vitro drug release. All the formulations showed low weight variation with disintegration time of less than 60 seconds. Tablets containing 3%, 5% crospovidone showed excellent in vitro dispersion time and in vitro drug release as compared to other formulations....
Acyclovir is an antiviral drug, used for treatment of herpes simplex virus infections with an oral bioavailability of only 10 to 20 % (limiting absorption in GIT to duodenum and jejunum), half life about 3h, soluble only at acidic pH (pKa 2.27). Mucoadhesive polymeric nanodrug delivery systems of acyclovir have been designed and optimized using 23 full factorial design. Poly (lactic-co-glycolic acid) (PLGA) (50:50) was used as polymer along with polycarbophil (Noveon AA-1) as mucoadhesive polymer and Pluronic F68 as stabilizer.From the preliminary trials, the constraints for independent variables X1 (amount of Poly (lactic-co-glycolic acid), X2 (amount of Pluronic F68) and X3 (amount of polycarbophil) have been fixed. The dependent variables that were selected for study were, particle size (Y1), % drug entrapment (Y2) and %drug release in 12h (Y3). The derived polynomial equations were verified by check point formulation. The application of factorial design gave a statistically systematic approach for the formulation and optimization of nanoparticles with desired particle size, % drug release and high entrapment efficiency. Drug:polymer ratio and concentration of stabilizer were found to influence the particle size and entrapment efficiency of acyclovir loaded Poly (lactic-co-glycolic acid) nanoparticles. The release was found to follow fickian as well as non- fickian diffusion mechanism with zero order drug release for all batches. In vitro intestinal mucoadhesion of nanoparticles increased with increasing concentration of polycarbophil.These preliminary results indicate that acyclovir loaded mucoadhesive poly (lactic-co-glycolic acid) nanoparticles could be effective in sustaining drug release for a prolonged period....
Shampooing is the most common form of hair treatment. Shampoos are primarily been products aimed at cleansing the hair and scalp. All shampoos are basically water and detergent mixtures. The main objective of this study was to eliminate harmful materials from shampoo formulation and substitute them with a safe natural product. Formulators must play an active role in educating the consumers about the potential harmful effects of synthetic detergents and other chemical additives present in shampoos. A more radical approach in popularizing herbal shampoo would be to change the consumer expectations from a shampoo, with emphasis on safety and efficacy. We had taken three plants extract to formulate the herbal shampoo. Defatted air-dried plants powders were extracted with methanol in soxhlet apparatus set at 600C for 24 hours. The solvent was evaporated at 500C using rotary vacuum. We have used the physico-chemical approach to preservation and by formulating a self preserving shampoo, have avoided this risk posed by chemical preservatives....
Primary concern of GRDDS is the programmability. They programmed/designed to retain the drug in stomach for a prolonged period time and release the drug in a controlled manner, so that the drug could be supplied continuously to its absorption sites in the GIT (on-site drug release). The major advantages with this novel approach includes- enhanced bioavailability, reduced frequency of dosing, targeted therapy, reduced counter-activity of the body, minimized adverse activity at the colon, and reduced fluctuations of plasma drug concentration. Number of techniques has been used to increase the gastric retention time (GRT) of dosage forms by employing a variety of concepts like floating, swelling, inflation, adhesion, high density, and magnetic systems. All these technical approaches and the drug selection criteria were discussed briefly in this review along with various formulation considerations, requirements, methods to asses gastroretentivity of gatroretentive dosage forms (GRDFs), and the factors controlling gastric retention of dosage forms....
Nanoscaffolds can play a central role in organ regeneration as they act as templates and guides for cell proliferation, differentiation and tissue growth. It is also important to protect these fragile cells from the harsh environment in which they are transplanted. The research team created the scaffold to provide a substrate for cell adhesion and migration and to influence the survival of transplanted cells or the invasion of cells from surrounding tissue. The SAPNS they developed appear to slow the growth rate and differentiation of the cells, allowing the cells time to acclimate to their new environment. That delay is very important when the immune system tries attacking cells when they are placed in vivo....
Nanoparticles hold tremendous potential as an effective drug delivery system. In this review we discussed recent developments in nanotechnology for drug delivery. To overcome the problems of gene and drug delivery, nanotechnology has gained interest in recent years. Nanosystems with different compositions and biological properties have been extensively investigated for drug and gene delivery applications. To achieve efficient drug delivery it is important to understand the interactions of nanomaterials with the biological environment, targeting cell-surface receptors, drug release, multiple drug administration, stability of therapeutic agents and molecular mechanisms of cell signalling involved in pathobiology of the disease under consideration. Several anti-cancer drugs including paclitaxel, doxorubicin, 5-fluorouracil and dexamethasone have been successfully formulated using nanomaterials. Quantom dots, chitosan, Polylactic/glycolic acid (PLGA) and PLGA-based nanoparticles have also been used for in vitro RNAi delivery. Brain cancer is one of the most difficult malignancies to detect and treat mainly because of the difficulty in getting imaging and therapeutic agents past the blood-brain barrier and into the brain. Anti-cancer drugs such as loperamide and doxorubicin bound to nanomaterials have been shown to cross the intact blood-brain barrier and released at therapeutic concentrations in the brain. The use of nanomaterials including peptide-based nanotubes to target the vascular endothelial growth factor (VEGF) receptor and cell adhesion molecules like integrins, cadherins and selectins, is a new approach to control disease progression....
Nasal drug delivery has been widely used as an alternative route for the systemic delivery of drugs. This is due to the large surface area, high total blood flow, the avoidance of first-pass metabolism, and ease of application. In recent years the nasal administration of drugs, include various peptide and protein drugs, These drug delivery systems have the ability to control the rate of drug clearance ,In addition, absorption of drug at the olfactory region of the nose provides a potential for a pharmaceutical compound to be available to the central nervous system. The nasal mucosa is an attractive area to deliver medications because the procedure is painless and needleless, which eliminates the risk of needle-stick injuries and reduces patient discomfort. Drug delivery through the nasal route has been used for the treatment of local diseases such as nasal congestion, allergies, infections and CNS disorder. The purpose of this review is to provide an overview of the anatomical and physiological considerations of the nose, mechanism of nasal drug absorption, drug metabolism and. factors that will affect formulation development and design of nasal products. Now the world market has seen an increasing number of systemically acting drugs being marketed as nasal formulations....
The aim of this study was to prepare Spherical crystals of Lactose monohydrate by Solvent change method (SCM) with Distilled Water-Ethanol-Ethyl Acetate System. The prepared crystals were evaluated for flowability, compressibility. Blend were prepared by using lactose crystals and poorly flowing API�s i.e. Paracetamol, Furosemide to check retention of flow property by replacing with poorly flowing APIs. Tablets were prepared by direct compression technique then evaluated for tensile strength, weight variation, hardness, friability, disintegration time. The prepared crystals were white, free flowing and spherical in shape. The yield of spherical crystals was 75%. Prepared crystals were also improved in compressibility and flowability. The tablet dosage form prepared from crystals showed better hardness, friability, disintegration time. The study revealed that this is a simple method and can be adopted in an academic lab for conversion of lactose to directly compressible form. The shift in tablet technique opened new arenas for excipients industries. In such demanding situation spherical crystallization proves better technique....
Pellets are the agglomerated fine powders or granules of drugs and other excipients into small free flowing, spherical particles. As drug-delivery systems become more sophisticated, the role of pellets in the design and development of dosage forms is increasing. Pellets having lots of advantages over their disadvantages. Formulation of pellets is done by different techniques like agitation, compaction, layering and globulation. According to the release profile, we can prepare that type of pellets like immediate release, sustained release and site specific release. Pellets can be used as separate dosage form or it can be compressed to form tablet or can be filled in capsule. Pellets having applications like having good flow property, give high yeild, for formulation of sustained release, immediate release, controlled release and also for tabletting purpose....
Natural gums are economic, easily available and found useful as tablet binder. Significant work was not reported on azadirachta indica gum to use in pharmaceuticals. Objective of the present work was to evaluate and characterized the azadirachta indica gum as a binder in tablet formulation. Tablets were prepared by using azadirachta indica gum as a binder and diclofenac sodium as a model drug. The concentration of the binder was varied from 2 to 12 % w/v in tablet formulations and was compared with the starch (10% w/v) as a standard binder. The evaluation granules prepared showed angle of repose of ranges from 29.21 to 34.27, friability 2.23 to 3.55 %. The hardness of tablet ranges from 4.2 to 4.6 kg/cm2 , disintegration time 7min to 18min., and maximum drug release 96.79 to 98.13 %. Useful concentration of azadirachta indica gum was found to be 8% with compare to starch (10%)....
Nifedipine (NFP) is the prototype nitro-dihydropyridine calcium channel antagonist that is used to treat a variety of cardiovascular disorders. NFP is a BCS class II drug having low solubility in water which leads to low dissolution rate, slow onset of action and variable oral bioavailability. To improve the dissolution rate of NFP by preparing binary and ternary solid dispersions. Binary and ternary solid dispersions were prepared using polyvinyl pyrrolidone K30 (PVPK30) and poloxamer 407 (PLX407) in different weight ratios. The drug and the formulations were characterized by FTIR, DSC and XRD. Solubility analysis and In-vitro dissolution of NFP solid dispersions (binary and ternary) were carried out and then compared. In contrast to the very slow dissolution rate of pure NFP, the solid dispersions showed enhanced dissolution rate. The solubility and dissolution were increased in the order; NFP (Pure drug) < binary solid dispersions < ternary solid dispersions. The fraction of NFP dissolved after 1 hr was approximately 70% and 90% from binary (NFP: PVPK30; 1:8) and ternary solid dispersions (NFP: PVPK30:PLX407; 1:8:2) respectively in comparison to the pure NFP, which was found to be approximately 2% in 1 hr. From this study, it was concluded that NFP showed significant improvement (statistically analyzed using ANOVA) in dissolution rate in case of ternary dispersions as compared to the binary dispersions as well as pure NFP....
To screen and isolate the microorganism that is capable of producing the extra cellular enzyme amylase, from the soil. Isolation of the microorganism, Obtaining pure cultures of starch degrading microbes, Determination of enzyme activities, Carbon assimilation test, Preparation of the media based on the carbon utilization test, Production of enzyme by the fermentation process, Isolation of enzyme amylase from the fermentation media, Demonstration of Enzyme Activity.This paper dealt with the isolation of starch degrading bacteria in pure culture from the soil using a starch laden agar medium and also to measure the amylase enzyme activity and the Amylase enzyme activity was found to be 0.75 IU/ml and it was demonstrated by the analytical techniques. As the isolated soil isolates had the potent amount of the enzyme, it can be tested with various stained cloths and vessels to find out the potency of the enzyme to be used as a detergent in washing and cleaning the vessels....
Oral route is the main route of drug administration in many diseases. Major problem in oral route of drug administration is bioavailability which mainly results from poor aqueous solubility. This leads to lack of dose uniformity and high intrasubject/intersubject variability. It is found that 40% of active substances are poorly water-soluble. Various technologies are developed to overcome this problem, like solid dispersion or cyclodextrin complex formation. Much attention has been given to Self-Micro Emulsifying Drug Delivery System (SMEDDS). SMEDDS appears to be a unique and industrially feasible approach to overcome the problem of low oral bioavailability associated with the lipophillic drugs. It requires small amount of dose and also drugs can be protected from hostile environment in gut. The digestive motility of the stomach and intestine provide the agitation necessary for self-emulsification in vivo. Self micro emulsifying drug delivery systems are specialized form of delivery system in which drug is encapsulated in a lipid base with or without pharmaceutical acceptable surfactant. This review describes SMEDDS as one of the important approaches to overcome the formulation difficulties of potent poorly water soluble drugs....
Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Poorly watersoluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities. Any drug to be absorbed must be present in the form of an aqueous solution at the site of absorption. Water is the solvent of choice for liquid pharmaceutical formulations. Most of drugs weakly acidic and weakly basic with poor aqueous solubility. Hence various techniques are used for the improvement of the solubility of poorly water-soluble drugs include micronization, chemical modification, pH adjustment, solid dispersion, complexation, co-solvency, micellar solubilization, hydrotropy etc. The purpose of this review article is to describe the techniques of solubilizaton for the attainment of effective absorption and improved bioavailability....
The aim of the present investigation was to prepare a hydrophobic matrix, investigate the drug release kinetics and statistically optimize the formulation for sustained release drug delivery of venlafaxine hydrochloride. A novel combination of carnauba wax and Eudragit E 100 was used to prepare the hydrophobic matrix. A simplex centroid design was constructed using the amount of carnauba wax, Eudragit E 100 and lactose as formulation variables. Drug release after 12 hrs and time required for 50% release of the drug were evaluated as response parameters. It was observed that EudragitL 100 had more pronounced effect on retarding the release at the end of 12 hrs whereas carnauba wax was more effective in prolonging the time required for 50% release of the drug. Lactose had least effect on both of these parameters. It was also observed that a combination of all these factors resulted in optimum results for both response parameters. Statistical models and response surface technologies were used to optimize the formulations and these models were found to be valid for predicting the values of response parameters....
Quality is always an imperative prerequisite when we consider any product. It becomes prime when it relates to life saving products like pharmaceuticals. Although it is mandatory from the government and regulatory bodies but it is also a fact that quality of a pharmaceutical product can not be adequately controlled solely by pharmacopoeia analysis of the final product. Today quality has to be built in to the product right from its inception and rigorous international environmental, safety and regulatory standards need to be followed. Validation had proven to be an important tool for quality management of pharmaceuticals. According to ISO 9000:2000 Validation is defined as \"Confirmation, through the provision of objective evidence, that the requirements for a specific intended use or application have been fulfilled\". In contrast with Verification, Validation rather focuses on the question whether a system can perform its desired functions. This review is an attempt to prove it as essential tool for quality management in pharmaceutical industry....
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