International Journal of Drug Delivery
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Formulation and evaluation of fast dissolving tablet of aceclofenac
Get PDFFast disintegrating drug delivery system offers a solution for these patients having difficulty in swallowing tablets/ capsules etc. Aceclofenac (anti-inflammatory and analgesic) was selected as the model drug. The poor aqueous solubility of the drug results in variable dissolution rate and hence poor bioavailability. In the present study, an attempt had been made to prepare fast dissolving tablets of the drug using various super disintegrates sodium starch glycolate following by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, disintegration time, water absorption ratio and wetting time, in vitro dissolution studies. All the formulation showed disintegration time in range of 12.2 to 27.5 second along with rapid in vitro dissolution. It was concluded that the fast dissolving tablets of the poor soluble drug can be made by direct compression technique using selective super disintegrantes showing enhanced dissolution, taste masking and hence better patient compliance and effective therapy.Keywords: Aceclofenac; Fast disintegrating; Superdisintegrants; Taste maskin
Paradoxical effect of coating on natural guar gum blended carbomer matrix systems for the neurological depressive disorders
Get PDFOral extended release products offer potential advantages in patient compliance and therapeutic outcomes like sustained blood levels with attenuation of adverse effects. In neuropsychiatric disorders like depression, most of the formulations serve a marketing objective rather than a clinical objective. The present investigation was aimed to develop a once daily sustained release formulation for delivery of an acid-labile, water soluble antidepressant, duloxetine HCl. The formulation was pragmatically designed using blend of natural and synthetic polymeric biomaterials that it releases the drug at alkaline pH in a sustained manner. The basic intention was to develop a tablet formulation with hydrophilic matrix core, using blend of release retarding natural biodegradable polymers such as guar gum, carbopol 71G-NF (a synthetic carbomer) and C-Pharm® gel. Barrier coating using HPMC-E5 was given to retard the initial release followed by enteric coating with HPMC-AS to prevent exposure of drug in acidic mileau of the stomach. The formulation exhibited desired release pattern and was described best-fit by Hixon-Crowell model. Stability analysis under stress conditions up to one month displayed good reproducibility. The matrix tablets successfully decreased the symptoms of depression (significant decrease in immobility time) in a rat forced swimming model. Pharmacokinetic data of the formulation revealed (tmax ~ 6 h, Cmax ~ 1157.58 ng/ml, mean AUCt~11145.04 ng*h/ml, and Ka~1.07h-1) good correlation in all animals.Keywords: Matrix tablets; Duloxetine HCl; Sustained release; Enteric coating; Hixon-crowell mode
Chitosan Microspheres as Potential Vaccine Delivery Systems
Get PDFThe recent advances in controlled delivery systems for protein pharmaceuticals such as microspheres, liposomes, pumps and implants, have provided a new avenue for delivery of vaccine antigens. Adjuvants aimed at increasing the immunogenicity of recombinant antigens remain a focus in vaccine development worldwide, there is currently considerable care for the development of chitosan microspheres as controlled release of vaccines, since the major disadvantage of several currently available vaccines is the need for repeated administration. Microspheres prepared from the biodegradable and biocompatible polymers, chitosan have been shown to be effective adjuvants for a number of antigens. This review mainly focuses on chitosan microspheres adjuvant as vaccine delivery systems by summarizing our and other research groups’ investigation on properties of microspheres formulation encapsulating several kinds of antigens. The results indicate that compared with commonly used PLA and PLGA, chitosan biomaterial has several potentials in vaccine delivery systems. Chitosan microspheres can control the rate of release of entrapped antigens and therefore, offer generation adjuvant to replace or complement existing aluminium salts for vaccine potential. The review mainly aims to promote the investigation of chitosan microspheres adjuvant for antigens for world wide researcher.Keywords: Tetanus toxoid; Chitosan microspheres; Vaccine delivery system; Biodegradable polymers
Development and in vitro evaluation of polar lipid based lipospheres for oral delivery of peptide drugs
Get PDFA 32 factorial design was employed to produce oral sustained release lipospheres prepared by modified double emulsion solvent evaporation technique for Serratiopeptidase (acid-labile enzyme) using wax and polar lipid combination as retardants. The effects of formulation variables selected through preliminary trials namely peptide and stabilizer (Tween® 80) concentration was evaluated by F-test on the drug content and size of lipospheres. The results of analysis of variance tests for both effects indicated that the test is significant (p < 0.05). The effect of Tween® 80 concentration (SSY1- 41.66; SSY2 – 25.30) was found to be higher than peptide amount (SSY1- 3.94; SSY2 – 4.03) on the size and drug content of lipospheres. Characterization was carried out through photomicroscopy, scanning electron microscopy, particle size analysis and in vitro drug release study. The effect of formulation variables on the integrity of enzyme was confirmed by in vitro proteolytic activity. The drug release from lipospheres followed first-order kinetics and was characterized by the Higuchi diffusion and Ritger-Peppas model. Lipospheres having maximum drug content (11.93±0.89) released 3-4% enzyme at pH 1.2 in 4 h. In phosphate buffer, lipospheres showed an initial burst release of 20.89±1.87% to 27.89±2.03% in one hour with additional 73.22±2.36% to 94.75±2.78% in next 12 hours. Thus, peptide loaded lipospheres with desirable characters in terms of maximum peptide content and diffusion release pattern were successfully prepared with formulation optimization approach.Keywords: Cetyl alcohol, Enzyme, factorial design, Lipospheres; Peptide, Serratiopeptidas
Evaluation of KYRON T-314 (Polacrillin Potassium) as a novel super disintegrant
Get PDFOrodispersible tablets (ODTs), also known as fast melt, quick melts, fast disintegrating have the unique property of disintegrating in the mouth in seconds without chewing and the need of water. The purpose of this investigation was to develop mouth dissolving tablets of aceclofenac using KYRON T-314 (Polacrillin Potassium) as a novel superdisintegrant. Mouth dissolving tablets of aceclofenac were prepared by wet granulation technique using KYRON T-314 as superdisintegrant and menthol as subliming agent. The present study demonstrated potentials for rapid absorption, improved bioavailability, effective therapy and patient compliance.Keywords: KYRON T-314, Mouth dissolving tablet, Aceclofenac, Subliming agent, Superdisintegrant
In Vitro and In Vivo evaluation of hydroxypropylmethyl cellulose phthalate capsules
Get PDFThe aim of this study was to develop a novel HPMCP capsule. The HPMCP capsule containing99mTc-DTPA and lactose was evaluated in in vitro and in vivo studies. First of all, the HPMCP capsules were prepared and characterized with lenght and diameter size, brittleness facility, moisture content and microbiological test. In vitro resistance and solubility studies of prepared capsules were tested at pH 1.2 and pH 7.4 buffers. The radiolabeled HPMCP capsules were administrated to fasted volunteers. The disintegration times and positions of capsules were recorded by using gamma scintigraphy. In vitro studies showed that HPMCP capsules were gastro resistant for 2 h at pH 1.2 and dissolved at pH 7.4 in 20-25 minutes. The radiolabeled capsules did not disintegrate in stomach whereas disintegrated in intestines. In conclusion, it was found that, the prepared HPMCP capsules can be an alternative to the hard gelatine capsules and used for intestinal targeting.Keywords: Capsule, hydroxypropylmethylcellulose phthalate (HPMCP), gamma scintigraphy, radiolabelling, technetium-99m
Design and evaluation of sustained release matrix tablets of levofloxacin for effective treatment of microbial infections
Get PDFThe objective of present work was to formulate and evaluate sustained release matrix tablets of levofloxacin for treating microbial infections effectively. Levofloxacin is the active component of the racemate ofloxacin, and used for treating a variety of clinical conditions such as lower respiratory tract infections, acute sinusitis, uncomplicated skin and soft-tissue infections and complicated urinary tract infections. Different formulations were prepared by wet granulation method using various release rate controlling hydrophilic polymers. The formulations were evaluated for hardness, weight variation, friability and drug content uniformity. The in vitro release of drug from the formulations was studied in pH 1.2 acidic buffer and pH 6.8 phosphate buffer, and it was found that the prepared tablets were able to sustain the release of the drug. The release of levofloxacin from the tablets was diffusion controlled and the release mechanism was non-Fickian. For conclusion, the developed formulations may reduce the dosing intervals, reduce the dose related side effects and increase the drug’s efficacy for treating infections.Keywords: Matrix tablets, levofloxacin, HPMC, guar gum, xantham gum, locust bean gum, Amorphophallus starch
Roll Compaction/Dry Granulation (Rcdg): Technologies and Their Applications In Drug Delivery and Development
No full textRecently molecular modelling, high throughput screening, combinatorial and parallel synthesis techniques have increased the number of drug molecules ready for formulation into suitable delivery systems. However, many of these drugs have poor physicochemical properties. Oral route is the most preferred route of drug administration due to its convenience, highest patient compliance and low production cost. However, formulating drugs having inconsistent low densities, with poor flow properties and compressibility in solid dosage forms poses a major challenge for the formulation scientist. Roll Compaction/Dry Granulation (RCDG) is a pressure agglomeration method in which powder(s) is densified by passing between two counter-rotating rolls. The RCDG technique has significant effect on fluidity, compressibility and compactibility of the pharmaceutical active pharmaceutical ingredients and excipients consequently, influencing drug release profile and tablet properties. There is an increasing interest of industry and academia in RCDG technique, since RCDG excludes any liquid solvent or binder solution and is environmentally safe and cost-effective. Various mathematical models for analysis of powder compaction are reported, that allow better understanding of process parameters, leading to its better design and control. However, losses of tabletability/reworkability, high fines fraction, non-homogeneity of compacts are few challenges in formulation development using roll compaction. These can be overcome by judicious optimization of process parameters and selection of appropriate excipients.This article aims at discussing the current technological advancements related to roll compactor devices available for dry granulation, their working principle, benefits and challenges of RCDG technology along with various applications relevant to the pharmaceutical field