Current Issue : July- September Volume : 2012 Issue Number : 3 Articles : 21 Articles
The concept of research subscribed in this article is directed towards the development of some NDDS for the treatment of various life threatening diseases and disorders. The nanosuspension can be proved as a gift as the poorly water soluble drugs can be easily formulated into nanosuspension. One of the critical problems associated with poorly soluble drugs is too low bioavailability. There are number of formulation approaches to resolve the problems of low solubility and low bioavailability. Nanosuspension not only solves the problems of poor solubility and bioavailability but also alters the pharmacokinetics of drug and thus improves drug safety and efficacy. Nanosuspensions are sub-micron colloidal dispersions of nanosized drug particles stabilized by surfactants....
Wondering through advances in drug development and modification of route of administration. It was seen that many drugs fails to show their action orally and thus the scientist studied and overcome the challenges associated with oral route drug delivery system. And a transdermal was one of the route developed for drug delivery. To develop, transdermal route, the impervious nature of skin was studied and task to cross the various layers lipophilic stratum corneum, and the outermost layer of the skin. It was observed that through transdermal route a systemic effect of a drug was obtained which differs from traditional drug delivery. A new technologies has encouraged manufacturers to develop various formulation of transdermal route. A review article covers, physiology of skin, basic components of transdermal route, methods of preparation, types of transdermal patches, evaluation and future technologies and approaches....
The ultimate goal of any drug delivery system is the successful delivery of the drug to the body; however patient compliance must not be exculpated. Fast dissolving drug delivery systems such as, Oral Thin Strip (OTS), offer a convenient way of dosing medications, to special population groups with swallowing difficulties such as children and the elderly, and also to the general population. OTS is the novel dosage form that disintegrates and dissolves within the oral cavity. Intra-oral absorption permits rapid onset of action and helps by-pass first-pass effects, therefore reducing the unit dose required to produce desired therapeutic effect. The present review provides an overview of various polymers that can be employed in the manufacture of OTS and highlights the effect of polymers and plasticizers on various physico-mechanical properties of OTS. It further gives a brief account of formulation of OTF and its objective is to compile the recent advancements and literature regarding the fast dissolving films and its market prospects....
Co-crystal technology is had recently got rapid popularity in the pharmaceutical field. Co-crystals generally contains two or more molecular components. Among them one is active pharmaceutical ingredient (API) and other is crystal former bonded with each other generally by hydrogen bond. Co-crystallization changes the molecular interactions and composition of API, and is considered better alternative to gate desired drug properties. Co-crystals provide several advantages over original drug molecule. It can overcome several issues of drug molecule such as solubility, stability and bioavailability. Co-crystal is generally formed when it is thermodynamically more stable than the crystals of original API and crystal former. In future vital role can be played by co-crystals in pharmaceutical industry....
The current Ofloxacin therapy is associated with high incidence of side effects seen in about 30% of patients. Ofloxacin is incompletely absorbed from GIT, it has absorption window confined to upper GIT. Its bioavailability was reported about 45%-50%, hence it was considered suitable candidate for formulation as gastro-retentive floating drug delivery system. Therefore Ofloxacin gastro retentive Floating tablets were prepared by wet granulation technique using semi-synthetic polymers like HPMC K4M and HPMC K100M for their gel-forming properties and also with natural polymer like pectin. The compressed Ofloxacin floating tablets were evaluated for physical parameters like Hardness, % Friability, weight variation and content uniformity. The formulation F4 was only formulation which was lies in between Pharmacopeial limits. All formulation is also evaluated for floating lag time and total floating time. Formulations containing HPMC K100M has least floating lag time and remained floated for more than 12 hrs. The HPMC alone polymer or low viscosity grade HPMC along with pectin unable to controlled on release rate it release drug >90% in 8 hrs. while in combination of HPMC K100M with pectin it release less than 55% in 8 hrs. The optimized formulation F4 was selected for in-vivo buoyancy test which carried out on Rabbit by using Barium sulphate as a radio opaque agent instead of active medicament. The results indicate that gas powered gastro-retentive floating Tablets of Ofloxacin containing HPMCK100M and pectin provides a better option for controlled release action, improved bioavailability and remained more than 6 hrs. in upper GI tract....
Lornoxicam, a potent non-steroidal anti-inflammatory drug which has short half life, which formulates the sustained release dosage forms advantages. Therefore the present investigation was concerned with the development of the sustained release matrix tablets using hydrophilic and hydrophobic polymers, which after oral administration were designed to prolong the duration of action. Lornoxicam Sustained release matrix tablet was prepared by wet granulation method using Acrypol 912G and Eudragit RSPO in formulation. FTIR and DSC study showed that there is no change in lornoxicam crystal form. The dissolution profile of the most satisfactory batch was fitted to zero-order, first-order, Higuchi, Hixson Crowell and K-Peppas models to ascertain the kinetic modelling of drug release. From the result it was observed that the combination ratio of Acrypol 912G and Eudragit RSPO have distinct effect on in vitro drug release profile. Release rate of lornoxicam was decrease with increased the total polymer concentration. Mechanism of drug release was explained by K-Peppas equation and found that diffusion-erosion occurs by anomalous transport (non-Fickian) release was predominant....
In the recent years, particularly in the last two decades, a great deal of technological and scientific research has been devoted to the development of rate-controlled oral drug delivery systems to overcome physiological problems, such as short gastric residence times (GRT) and unpredictable gastric emptying times (GET), in order to be able to formulate gastro-retentive dosage forms, which will allow the delivery of restricted ‘absorption window’ drugs which are absorbed in a particular portion of the GI tract . Several approaches are currently being used to prolong the GRT, including floating drug delivery systems (FDDS), also known as hydrodynamically balanced systems (HBS), swelling and expanding systems, high-density systems, and other delayed gastric emptying devices. In this review, the current and recent developments of FDDS, marketed products, are discussed....
Recently, controlled and sustained drug delivery has become the standard in modern Pharmaceutical design and an intensive research have been done in getting much better drug product effectiveness, reliability and safety. This interest has been increased by the advantages shown by in situ forming polymeric delivery systems such as ease of administration and reduced frequency of administration, improved patient compliance and comfort. Among oral dosage form, liquid dosage forms are more prone to low bioavailability because of their faster transit from the stomach. The sustained release of the drug from the oral liquid formulation can be obtained by liquid in situ gelling system. The formation of gels depends on factors like temperature change, pH change, presence of ions and ultra violet irradiation, from which the drug gets released in a sustained and controlled manner. The in situ gel forming polymeric formulations provide several advantages like sustained and prolonged action as compared to conventional drug delivery systems as well as produce patient compliance by reducing dosing frequency. From a view point of manufacturing, the production of such systems is less complex and thereby lowers the investment and manufacturing cost....
Matrix type transdermal drug delivery systems (TDDS) of Hydroxyzine hydrochloride (HHCL) with and without permeation enhancers were prepared by solvent casting method. Mixture of polymers Eudragit RS100, Eudragit RL100, PVP, HPMC E15 LV and ethyl cellulose were employed in the preparation of patches. Dibutylphthalate was used as plasticizer. The prepared patches were evaluated for physicochemical characterization, in vitro and ex vivo diffusion study. In order to reduce the skin barrier property and to enhance the skin permeation of drug, permeation enhances transcutol and propylene glycol were incorporated in polymeric films.\r\n The central composite design was applied to optimize the best permeation enhancer. Formulations (HhLS3 0t) with Eudragit RS100, RL100 at 25% transcutol concentration and formulation (HhLS3 -1P) with Eudragit RS100, RL100 at 15% propylene glycol were found to be the best. Among these two permeation enhancers used, no statistically significant difference (p> 0.05) was observed between transcutol (25%) and propylene glycol (15%). All the optimized formulations had shown zero order kinetics and non fickian type of diffusion. No signs of skin-irritation were observed in testing with rabbit....
The aim of the study was to design controlled porosity osmotic pump (CPOP) tablets of Zolpidem tartrate. The porous osmotic pump contains pore forming agent (PEG-400) in the coating membrane which after coming in contact with water, dissolve, resulting in an in situ formation of microporous structure. Zolpidem tartrate is a nonbenzodiazepine analogue of imidazopyridine of sedative and hypnotic category. The dosage regimen of Zolpidem tartrate is 12.5 mg tablet once in a day. The plasma half-life ranges from 2 to 4 hours. Hence, Zolpidem tartrate was chosen to develop a controlled release system for 4 hours. The effect of different formulation variables, namely, ratio of drug to osmogent, membrane weight gain and level of pore former on the in-vitro release was studied using by different ratio of drug to osmogent and different concentration of pore forming agent. Cellulose acetate (4%) was used as the semipermeable membrane. Drug excipients compatibility was studied by FTIR and it indicated that there was no interaction between drug and excipients. Microporous structure of coating membrane of optimized formulation F4C3 was determined by Scanning Electron Microscope (SEM). Drug release was inversely proportional to membrane weight gain however, directly related to the level of pore former in the membrane. Optimized formulation (F4C3) was found to deliver 50% of total dose within 30 minute and above 90% of drug (Zolpidem tartrate) at the end of 4 hours. Optimized formulation F4C3 showed that tablets were stable at accelerated environment condition, for one month....
The present investigation describes the influence of the hydroxypropyl methayl cellulose (HPMC) and different diluents on release behaviour and kinetics of Itopride HCL sustained release floating tablets using 32 full factorial design. The amounts of HPMC K100M (X1) and type of diluents (X2) were selected as independent variables and buoyancy lag time, drug release at 12hr (Q12), at 18hr (Q18) and T50% were selected as a dependent variable. Itopride HCL tablets were prepared by direct compression method using different proportions of HPMC K100M as release retardant with different diluents. The parameter optimized using 32 factorial designs. The tablets of all batches were evaluated for drug content, hardness, friability, weight variation and in vitro drug release profile. Different dissolution models were applied to drug release data in order to evaluate release mechanisms and kinetics. Regression analysis and response surface analysis were performed for dependent variables. Formulation FD2 was selected as an optimum formulation as it shows more similarity in dissolution profile with innovator profile (Similarity factor, f2= 56.58). It was observed that type of diluents and concentration of polymer had significant influence on BLT, T50%, and Q12 but no significant influence of diluents on Q18. Mathematical treatment of the in vitro drug release data suggests that, the drug release of all the formulations followed Higuchi model, the release exponent n < 0.5 indicate that drug diffuses through the polymeric matrix by a Fickian (case I) diffusion mechanism....
Gold nanoparticles (AuNPs) has been used since Ancient Roman times to colour glass intense shade of yellow, red or mauve, depending on the concentration of gold and in Hindu Chemistry, for various potions. Gold nano particles appear deep red to black in solution colour depends on size of nanopaticles. It exists in the form of colloidal as well as soluble particles. Due to its extremely small size, they are more readily taken up by the human body. Nanogold are able to cross the biological membranes and access cells, tissues and organs that larger size particles are normally cannot. Gold nanoparticles are produced mainly three techniques employing chloroauric acid (H[AuCl4]); a) Turkevich method, b) Brust method and c) Sonolysis. The most common characterization technique of AuNPs is high-resolution transmission electron microscopy (HRTEM), which gives a photograph of the gold core of the AuNPs, but the core dimensions can also be determined using scanning tunneling microscopy (STM), atomic force microscopy (AFM), small angle X-ray scattering (SAXS),a laser desorption ionization mass spectrometry (LDI-MS), and X-ray diffraction. Review suggests its possible biomedical application in cancer and Alzheimer�s disease as both diagnostic kit and in treatment. Scattering property of nano gold particle have made them an ideal tool in the field of analysis. In future much of the research will be diverted to its possible application in the sectors like cosmetic formulations, bacterial detection, florescence assay, alternative to ayurvedic medicine and biosensors....
There are many different approaches to targeted drug delivery which is classified broadly into three categories. (1) Physical or mechanical approach, (2) Biological approach, (3) Chemical approach. The aim of the specific targeting is to enhance the efficiency of drug delivery and at the same time to reduce the toxicity and side effect. Different types of magnetic carriers are magnetoliposomes, magnetic nanoparticles, magnetic release erythrocytes and magnetic emulsions. There are many techniques for synthesis of magnetic nanoparticles including from bacteria, polymerization, salting out, extraction, co-precipitation etc. The application of magnetic nanoparticles in biomedical area. The size and uniformity is critical because it is what their function directly relies on; and an efficient method of producing monodispersed nanoparticles is important. The synthesis magnetic nanoparticles can be characterized by various methods such as transmission electron microscopy and superconducting quantum. Magnetic nanoparticles are mainly used for treatment of cancer, tuberculosis, ocular therapy etc....
Micro-emulsions are clear, thermodynamically stable, isotropic mixtures of oil, water, and surfactant, frequently in combination with a co surfactant. Micro-emulsions have been intensively studied during the last decades by many scientists and technologists because of their great potential in many food and pharmaceutical applications. The use of micro-emulsions is advantageous not only due to the facile and low cost preparation, but also because of the improved bioavailability. The increased absorption of drugs in topical applications is attributed to enhancement of penetration through the skin by the carrier. Saturated and unsaturated fatty acids serving as an oil phase are frequently used as penetration enhancers. The most popular enhancer is oleic acid. Other permeation enhancers commonly used in transdermal formulations are isopropyl myristate, isopropyl palmitate, triacetin, isostearylic isostearate, R (+)-limonene and medium chain triglycerides. The most popular among the enhancing permeability surfactants are phospholipids that have been shown to enhance drug permeation in a different mode. Various potential mechanisms to enhance drug penetration through the skin include directly affecting the skin and modifying the formulation so the partition, diffusion, or solubility is altered. The combination of several enhancement techniques such as the use of iontophoresis with fatty acids leads to synergetic drug penetration and to decrease in skin toxicity. In conclusion, Micro-emulsions were found as an effective vehicle of the solubilization of certain drugs and as protecting medium for then trapped of drugs from degradation, hydrolysis, and oxidation. It can also provide prolonged release of the drug and prevent irritation despite the toxicity of the drug. Yet, in spite of all the advantages the present formulations lack several key important characteristics such as cosmetic permitted surfactants, free dilution in water capabilities, stability in the digestive tracts and sufficient solubilization capacity....
In recent decades, a variety of pharmaceutical research has been conducted to develop new dosage forms. Among the dosage forms developed to facilitate ease of medication, the mouth dissolving tablet (MDT) is one of the most widely employed commercial products. Mouth dissolving tablets have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The development of Fast or mouth dissolving tablets have been formulated for pediatric, geriatric, and bedridden patients and for active patients who are busy and traveling and may not have access to water. Such formulations provide an opportunity for product line extension in the many elderly persons will have difficulties in taking conventional oral dosage forms (viz., solutions, suspensions, tablets, and capsules) because of hand tremors and dysphagia. This article summarizes contents of formulation, various approaches of preparation of MDT like melt granulation, phase transition process, sublimation, three-dimensional printing (3DP), mass extrusion, spray drying, cotton candy process, tablet molding, lyophilization or freeze-drying, direct compression, nanomization, etc., various patented technologies like zydis, orasolv, durasolv, wowtab, flashtab, shearform, ceform, nanocrystal and evaluation parameter in detail....
Systemic bioavailability of many drugs are not being effectively and efficiently achieved using conventional drug delivery approaches due to its complexity. Nasal drug delivery is an alternative approach to the systemic and enteral drug delivery. It avoids presystemic firstpass metabolism and gastric acid hydrolysis of drugs results in increasing the bioavailability. Nasal route gives reduced dosing frequency for bioadhesive controlled release formulations. The nasal mucosa offers direct access to the compartment of the central nervous system via the olfactory route. This review explains the details on anatomy and physiology of nose, mechanism, factors affecting for drug absorption, various approaches, Applications for the nasal dug delivery....
The present investigation concerns the development of Sustained release matrix tablets of Zaleplon, which after oral administration are designed to prolong the duration up to 8 hrs and thereby increase patient compliance, reduced frequency of administration and increase therapeutic efficacy.so as to provide the advantages of improving sleep quality, Prevent Middle-of-the-Night Awakening with No Adverse Effects on Next Day Performance. A 32 full factorial design was used in present study for optimization. Nine batches of tablets were fabricated containing Zaleplon, polymers HPMC K4M, Microcrystalline cellulose, Lactose and other excipients. All the batches were formulated by direct compression. After evaluation of physical properties of tablet, In‐vitro dissolution study was performed by using USP Type II Apparatus (Paddle type) at 75rpm. Deionized water, 900ml was used as dissolution medium which maintained at 37±0.5°C. here deionized water is used because zaleplon has pH independent solubility over the pH range 1.0 to 9.0. The results obtained were satisfactory and complies with the Pharmacopoeial specifications. The formulation containing HPMC K4M (15%) and Microcrystalline cellulose (20%) (F6) showed slower release with required loading dose as compare to other formulations. F6 batch was optimized based on satisfactory retarding release of Zaleplon from matrix to 8 hrs and maximum similarity factor (73.89). The mechanism of drug release of optimized batch was found to be non-Fickian diffusion followed zero order kinetics. Drug excipient compatibility study showed no interaction between drug and excipient. Stability study of optimized formulation showed that tablets were stable at accelerated environment condition....
Colon specific drug delivery system has attracted considerable attention for the past few years in order to develop drug delivery systems that are able to release drugs specifically in the colon in a predictable and reproducible manner. The colon is a site where both local and systemicdelivery of drugs can take place. To achieve successful colon targeted drug delivery, a drug needto be protected from degradation, release and absorption in the upper portion of the gastricintestinal tract (GIT) and then to be ensured abrupt or controlled release in the proximal colon.This review is aimed at understanding recent approaches for dosage forms which is targeting tocolon through pH sensitive system, microbially triggered system i.e., prodrugs and polysaccharidebased system, timed release system, osmotically controlled drug system, pressure dependent release system....
There is considerable interest in the skin as a site of drug application both for local and systemic effect. Skin penetration enhancement techniques have been developed to improve bioavailability and increase the range of drugs for which topical and transdermal delivery is a viable option. The noninvasive route of delivery systems has many advantages over the conventional delivery systems. Althoug its applications are limited by low skin permeability and physicochemical properties of drugs. The permeation of drugs through skin can be enhanced by various methods including physical methods such as iontophoresis, phonophoresis (use of ultrasound energy), eletroporation and by chemical penetration enhancers etc. The transdermal route has been recognized as one of the highly potential routes of systemic drug delivery. However, the major limitation of this route is the difficulty of permeation of drug through the skin. Studies have been carried out to find safe and suitable permeation enhancers to promote the percutaneous absorption of a number of drugs. The present review highlights various categories of penetration enhancers; the involved mechanism leading to a judicious selection of suitable penetration enhancers for improving the transdermal permeation of poorly absorbed drugs....
Solubility enhancement of Albendazole by different approaches. In Physical Mixture method various ratios of solid dispersion were prepared using Albendazole and carriers such as PVP K-30, PEG-6000, β-CD, Sodium Lauryl Sulphate and PEG-4000 by following method. The physical mixtures of drug and carriers in 1:1 and 1:2 were prepared by mixing individual components that was previously sieved (85 #) together with a spatula. The prepared powder was been keep in self seal coven and put in to the desiccators for farther evaluation. In Kneading methodthe physical mixtures of drug and carriers in 1:1 and 1:2 were triturated in a mortar with a small volume of water-acetone (1:1 v/v) solution. The thick slurry was kneaded for 45 minutes and then dried at 45 ºC. The dried mass was pulverized and sieved from 85 # and fraction was collected. The prepared powder was been keep in self seal coven and put in to the desiccators for farther evaluation. In Solvent Evaporation Method the aqueous solution of carrier was added to acetone solution of drug. The resulting mixture was stirred for 1 hour and evaporated at a temperature of 45 ºC until dry. The dried mass was pulverized and sieved from 85# and fraction was collected. The prepared powder was been keep in self seal coven and put in to the desiccators for farther evaluation. In Melt Dispersion Method the different ratio of ABZ: PEG 4000 and ABZ: PEG 6000 are taken in Petridis and heated until dry residue occurs. The dried mass was pulverized and sieved from 85# and fraction was collected. In vitro release data, solubility data of various batches suggests that highest solubility and in vitro drug release was found in β-CD Solvent Evaporation method. These values are higher than that of pure drug and marketed formulations. The studies indicate that the solubility of Albendazole can be enhanced by different approaches, in which β-CD Solvent Evaporation method can enhance the solubility of Albendazole maximum. So, this method can be used to formulate the dosage form....
Today the oral rout is the preferred rout of drug administration because of low cost of therapy and ease of administration. Oral controlled release stomach specific system is a promising delivery system for a drug candidate having limited absorption window, low solubility, local action in stomach, and those drugs which degrades in intestinal fluid. This review covers the detailed scenario related to stomach specific drug delivery system with their advantages over the conventional drug delivery system and also limitation. The term “Gastroretentive Drug Delivery System (GRDDS) may also be used for stomach specific drug delivery system. Various types of techniques are employed for development of such dosages form. This review also focus on formulation aspect of floating drug delivery system and some floating drug delivery system, available in market, are also enlisted. The purpose of this comprehensive review is to provide basic knowledge of GRDDS....
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