Current Issue : April-June Volume : 2011 Issue Number : 2 Articles : 17 Articles
The analysis of marketed coconut oil samples namely A, B and C was carried out to detect the level of adulteration. Various physicochemical parameters were tested to check oils’ purity as per APCC (Asian & Pacific Coconut Community) standards. Moreover the comparative analysis of cream formulations from all the oil samples obtained was carried out to study the effect of different grades of coconut oil on formulation aspects of creams. The saponification values for oil sample C & B were quite comparable which are 258.76 & 251.04 mg of KOH/gm of oil, while acid values for sample A, B and C were 1.11, 0.50, 0.45 mg of KOH/ gm of oil. The polenske value for oil sample B and C were found to be 13.3. The study of formulation aspects of creams showed the most stable cream formed from the oil sample C which complies with all the APCC standards for oil. The pH, mean globule size and centrifugation test value obtained for the most stable emulsion were 6.28+0.07, 30.05+0.92 m, 0.4+0.1 cm respectively....
The increasing research interest surrounding this delivery system has widened the areas of pharmaceutics in particular with many more sub-disciplines expected to coexist in the near future. The purpose of writing this review on pulsatile drug delivery systems (PDDS) is to compile the recent literatures with special focus on the different types and approaches involved in the development of the formulation. Some of the disease conditions wherein PDDS are promising include duodenal ulcer, cardiovascular diseases, arthritis, asthma, diabetes, neurological disorder, cancer, hypertension and hypercholesterolemia. PDDS can be classified into time controlled systems wherein the drug release is controlled primarily by the delivery system, stimuli induced PDDS in which release is controlled by the stimuli, such as the pH or enzymes present in the intestinal tract or enzymes present in the drug delivery system and externally regulated system where release is programmed by external stimuli like magnetism, ultrasound, electrical effect and irradiation. This review also summarizes some current PDDS already available in the market. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form. Thus it is important to develop new drug delivery systems to achieve pulsed delivery of a certain amount of drugs in order to mimic the function of the living systems, while minimizing undesired side effects. With the biological prospective approaches in delivering drugs it is well understood that safer and more realistic approaches in the therapy of diseases will be achieved in the days to come....
Objective: The aim of this research work was to design & evaluate chronomodulated pulsincap drug delivery system of Aceclofenac for arthritis. Material and Method: Aceclofenac Microcapsules prepared by solvent evaporation method using three different drug: polymer ratio (viz., 1:1, 1:2 and 1:3) were subjected to various physico- chemical studies. The optimized formulation MC2 was filled in to formaldehyde treated gelatin capsule using different concentrations (10%, 20% and 30%) of guar gum and methyl cellulose as hydrogel plugs. Further modified capsules were coated with Eudragit S-100 as enteric coating and HPMC as swellable coating by dip coat method. The prepared modified pulsincaps evaluated for physicochemical and release parameters. Key findings: In vitro release studies of all the formulations showed that there was no drug release in simulated gastric fluid (pH 1.2) for 2 hrs, negligible amount (4.48%-14.78%) of drug release was observed in simulated intestinal fluid (pH 6.8 phosphate buffer), drug release occurred in pH 7.4 upto 24 hrs in controlled manner depending upon the quantity of polymer plug. All formulations followed first order release kinetics by diffusion mechanism\r\n Conclusion: The obtained results showed the capability of the system in delaying the drug release for programmable period of time which improves the anti-inflammatory therapy in the management of rheumatoid arthritis....
Dendrimers are a unique class of synthetic macromolecules having highly branched, three dimensional, nanoscale architecture with very low polydispersity and high functionality. These features have made their application in nanotechnology, pharmaceutical and medicinal chemistry particularly attractive. This review briefly discusses the various aspect of dendrimer including properties, preparation of dendrimers types, characterization, dendrimer based products and their use as pharmaceutical, therapeutic, diagnostic agent and their potential for applications in drug delivery. The biocompatibility of dendrimers follows patterns known from other small particles. Cationic surfaces show cytotoxicity; however, derivatization with fatty acid or PEG chains, reducing the overall charge density and minimizing contact between cell surfaces and dendrimers, can reduce toxic effects. This review clearly demonstrates the various application of dendrimer and indeed substantiates the high hopes for future....
Plants have provided us a range of variety materials to aid improve and sustain the health of all living things either directly or indirectly. Gums and mucilages are widely used natural materials for conventional and novel dosage forms. These natural materials have advantages over synthetic ones since they are chemically inert, nontoxic, less expensive, biodegradable and widely available. The Okra (Hibiscus esculentus) mucilage is one of these vital materials. Matrix type transdermal patches containing drug Ketoprofen were prepared by solvent casting method employing a mercury substrate by using the combinations of Okra mucilage, Polyethylene glycol, Methyl and Propyl Paraben, Span-80. The transdermal patches were evaluated for their physicochemical properties like thickness, weight variation, flatness, tensile strength, hardness, folding endurance, drug content, swellability, surface pH, water vapour transmission, and in vitro permeation. IR studies indicated no interaction between drug (Ketoprofen) and Polymer (Okra mucilage). The prepared patches possessed satisfactory pre formulary and formulary characteristics. Hence, it can be concluded that Ketoprofen could be developed as a transdermal delivery system with Hibiscus Esculentus fruit mucilage that is an alternative to intravenous administration and has minimal adverse effects....
The purpose of this research work was to develop and evaluate matrix-type transdermal therapeutic system containing Nicardipine hydrochloride with different ratios of hydrophilic and hydrophobic polymeric combinations by the solvent evaporation technique. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. Seven transdermal patch formulations (F-1, F-2, F-3, F-4, F-5, F-6, F-7) consists of Hydroxypropyl methylcellulose E5 and Ethyl cellulose in the ratios of 8:0, 0:8, 2:6, 3:5, 5:3, 6:2, 4:4 respectively were prepared. All formulations carried dimethyl sulfoxide as penetration enhancer and dibutyl phthalate as plasticizer in acetone and methanol (4:3) as solvent system. The prepared transdermal patches were evaluated for in vitro release, moisture absorption, moisture loss and mechanical properties. The diffusion studies were performed by using modified Franz diffusion cells. The formulation, F-1 (Hydroxypropyl methylcellulose E5 alone) showed maximum release of 97.1887 ± 0.566 % in 7 hrs, where as F-2 (Ethyl cellulose alone) showed maximum release of 66.9393 ± 1.812 % in 24 hrs. The formulation, F-7 with combination of polymers (4:4) showed maximum release of 91.7772 ± 0.780 % in 24 hrs, emerging to be ideal formulations for Nicardipine hydrochloride. The developed transdermal patches increase the efficacy of Nicardipine hydrochloride for the therapy of hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina....
The aim of this study was to develop the formulation of griseofulvin by nanocrystallization for the enhancement of solubility and dissolution property of drug. In the present study the area of interest are drugs belonging to class II of BCS classification. Nanocrystal is a new carrier free colloidal drug delivery system with particle size ranging from 100-1000 nm, and is considered as a viable drug delivery strategy to develop the poorly soluble drugs. In the present work an attempt was made to enhance bioavailability of Griseofulvin by nanocrystallization technique. The drug nanocrystals (NC) were prepared by emulsion solvent diffusion method. Two different solvents and two different stabilizers were evaluated in the process. All formulations were in the size range of 600-900nm and showed marked improvement in dissolution velocity when compared to pure drug (3-4 μm), thus greater bioavailability. Short term stability studies were carried out as per ICH guidelines and all formulations were found to be stable. It was concluded that formulating poorly water soluble drugs in the form of drug NC would be a promising approach in delivery of class II drugs by oral route in much efficacious way....
The objective of this study was to develop and evaluate a floating pulsatile drug delivery system of captopril based on an impermeable cylinder. This drug delivery system comprised of three units: impermeable cylinder, rapidly disintegrating tablets of different disintegrants in different concentration and a erodible plug. It was found that the first pulse released within 30 min. followed by a lag time of 4.5 h and finally second pulse release. Higher concentration of crosspovidone (F3 - 5 %) was responsible for maximum drug release in first and second pulse as compared to other formulation. Low viscosity polymer HPMC E5 with ratio 45:53:2 (HPMC-E5: spray dried lactose: SSG) containing erodible plug was responsible for lag time of 4.5 h. This novel technique can be effective innovation in treatment hypertension....
The present investigation aims to evaluate the transdermal potential of elastic liposomes (Ethosomes) loaded with 5 Fluorouracil (5 FU), an effective antineoplastic agent with poor skin permeation. 5 FU ethosomes were prepared, optimized and characterized for vesicular shape and surface morphology, vesicular size and size distribution, stability, entrapment efficiency, in vitro skin permeation test, skin irritancy test. Transmission electron microscopy, Dynamic light scattering shows spherical vesicles and nanometric size range (140.6 nm). Percent entrapment efficiency of the optimized formulation (Et63/20/40) was found to be 76.6 + 0.52%. Fourier Transformed-Infra Red (FT-IR) data generated to assessed the fluidity of skin after the application of formulation. Further, a better skin tolerability suggested that ethosomes may offer a suitable approach for transdermal drug delivery of 5 FU. These results can be considered as a step forward for the transdermal drug delivery system of certain problematic molecules like 5 FU for various types of skin cancers like Actinic Keratosis (AK), Squamous Cell Carcinoma (SCC), and Basal Cell Carcinoma (BCC) etc....
Drug delivery systems are becoming increasingly sophisticated as pharmaceutical scientists acquire a better understanding of the physicochemical and biochemical parameters pertinent to their performance. Over the past three decades, orally disintegrating tablets (ODTs) have gained considerable attention as a preferred alternative to conventional tablets and capsules due to better patient compliance. ODTs are solid dosage forms containing medicinal substances which disintegrate rapidly, usually in a matter of seconds, when placed on the tongue. An orally disintegrating tablet or orodispersible tablet (ODT) is a drug dosage form available for a limited amount of over-the-counter (OTC) and prescription medications. ODTs differ from traditional tablets in that they are designed to be dissolved on the tongue rather than swallowed whole. The ODT serves as an alternative dosage form for patients who experience dysphasia (difficulty in swallowing). The purpose of the present study was to develop and characterize fast dissolving tablets of Domperidone using direct compression and wet granulation technique. In the present study, Domperidone is the model drug. In this method the different excipients used were microcrystalline cellulose, crosscaramellose sodium, mannitol magnesium stearate. We formulate seven formulations with batch codes F1 to F7 by direct compression method. In-vitro drug release showed that almost drug was release nearer to 97 to 98 % range in 20 minutes. Depending upon cumulative drug release, in-vitro disintegration time, wetting time, there was found that direct compression method is better than wet granulation method. Depending upon cumulative drug release, in-vitro disintegration time, wetting time results, one formulation F7 was selected for further studies....
Malaria has remained a major public health concern in the developing world, caused by a protozoan parasite of the genus Plasmodium. More than 600 million people are infected annually resulting in more than three million deaths, mostly children in Africa. Increased resistance to malaria drugs has made the situation worse and control of the disease will require rapid development of new control methods, so development of vaccines against malaria is one of the most effective modes of treatment available. An effective vaccine against malaria that would protect non-immune individuals from the disease has long been a dream....
The objective of the present study is aiming at the novel methodologies in the development of Chronotherapy and designing accordingly to the chronological behavior of body. Although oral delivery has become a widely accepted route of administration of therapeutic drugs, the gastrointestinal tract presents several formidable barriers to drug delivery. The increasing research interest surrounding chronic drug delivery systems (ChrDDS) may lead to the creation of a new discipline in pharmaceutics known as chronopharmaceutics. Such novel and more biological approaches may lead to safer and more efficient disease therapy in future. This concept has several advantages, notably maximum therapeutic benefit, minimum harm, improved patient convenience and compliance. Pharmacists must realize the need to develop and dispense such medications having potential therapeutic benefit. The current article focuses on the diseases requiring pulsatile drug delivery system (PDDS), methodologies involved for the existing systems, recent update and PDDS products currently available in the market....
Around 70 to 90 million people suffer from glaucoma which results in optic nerve damage and may lead to blindness. Major causes of glaucoma are hypertension, diabetes, low tension, genetically. Glaucoma can be classified into congenital and acquired. Primary and secondary types of glaucoma come under acquired. African Americans and Hispanics in the US, people over 60years old more susceptible to glaucoma. Drug classification in the treatment of glaucoma are �Ÿ-blockers, adrenergics, miotics and systemic carbonic anhydrous inhibitors. Several approaches are surfacing in the treatment and medication for glaucoma which includes inserts. This article gives an overview about glaucoma, types, diagnosis and treatment. Approaches of ophthalmic inserts also are established in the treatment of glaucoma....
The objective of this investigation was to develop solid lipid nanoparticles (SLN) of an antihypertensive drug carvedilol with the help of hot homogenization followed by ultrasonication method. SLN were prepared by using tripalmitin as lipid at various concentrations (1, 2.5 and 5%) and tween 80 as surfactant at various concentrations (1, 1.5 and 2%). The developed SLN were characterized for particle size, polydispersity index, entrapment efficiency of carvedilol and morphology. The physicochemical interaction between carvedilol and lipid was investigated by Fourier transform infrared (FTIR) Spectroscopy. The mean particle size was found to be in the range of 50-220 nm with a narrow particle distribution of polydispersity index, 0.238. The drug entrapment efficiency (EE %) of SLNs was more than 80% and increased as the concentration of lipid was increased and decreased as the concentration of surfactant was increased. The drug release was decreased as the concentration of both lipid and surfactant was increased. In vitro release of carvedilol from SLN followed Higuchi diffusion and first order equation....
The preparation and physico-chemical evaluation of Losartan potassium floating tablet as per 32 Factorial Design is presented. Statistical experimental design and data analysis using response surface plot and Contour plot is also illustrated. A 32 factorial design for the controlled release of Losartan potassium was used with two formulation variables - X1 (Drug: Polymer ratio) and X2 (Viscosity of polymer). Nine formulations were prepared and dissolution studies and floating characteristics were performed on these formulations. The two formulation variables were- found to be significant for the release properties (P < 0.05), while Viscosity of polymer was found to be significant for total floating time as well as % drug release. The quadratic mathematical model developed could be used to further predict formulations with desirable release and floating properties....
A new sustained release microencapsulated drug delivery system for acetazolamide by employing pectin was developed and characterized. The microcapsules were formulated with pectin by orifice ionic gelation technique .Polymers such as HPMC, MC, Sod.CMC, gum karaya, gum kondagogu and gum olibanum were used along with pectin. Microcapsules were evaluated for particle size, flow properties, drug entrapment efficiency, and in vitro drug release studies. . The drug release from the microcapsules was dependent on the curing reagent employed such as calcium chloride, barium chloride, aluminium chloride and zinc chloride (CaCl2, BaCl2, AlCl3 and ZnCl2). The microcapsules formulate with the curing reagent BaCl2 has shown better sustained release. The optimised formulation of microcapsules having the composition pectin: gum kondagogu: drug (0.25: 0.5:1) produced the complete release at the required release rate. The drug release of the formulation followed first order kinetics and the mechanism of drug release followed diffusion....
The objective of the present investigation was to design floating tablets of famotidine. A full 23 factorial design was adopted using hydroxy propyl methylcellulose, sodium bicarbonate and ethyl cellulose as independent variables for the preparation of the famotidine tablets. The prepared floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, in vitro buoyancy and drug release study. Multiple regression analysis was performed for dependent variables floating lag time, percent of drug release with in 1h (Q1), 10h (Q10) and diffusion exponent (n). Polynomial equations and response surface plots were generated for all dependent variables. It was observed that all the factors had significant contribution on all dependent variables studied. The study of analysis of variance revealed that floating lag time was primarily influenced by concentration of sodium bicarbonate. The release of famotidine was influenced by concentration of hydroxy propyl methylcellulose and ethyl cellulose....
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