Current Issue : October - December Volume : 2012 Issue Number : 4 Articles : 11 Articles
The purpose of this research was to formulate and systematically evaluate In vitro performances of biodegradable microspheres of Metformin HCl, an oral hypoglycemic agent for treatment of Type-II diabetes. The present study consisted of a three-level three-factorial (33) design- Box Behnken design for experimentation. A 3-factor, 3-level Box-Behnken design was used to derive a second order polynomial equation and construct contour plots to predict responses. Response surface graphics were used to show the factor interaction between the considered variables. Selected independent variables studied were the Drug: Polymer Ratio (X1); Agitation Speed (rpm) (X2); and Surfactant Ratio (X3) added to the formulation. The selected dependent variables investigated were particle size (μm), percentage drug entrapment efficiency and percentage of drug released at 12 hrs. Batch P1 exhibited excellent results in terms of particle size (32.78μm), percentage drug entrapment efficiency (75.25) and percentage of drug released (82.24) at 12 hrs....
In the present work, fast disintegrating tablets of Telmisartan were prepared using novel co-processed superdisintegrants consisting of Croscarmellose sodium (CCS) and Crospovidone (CP) in different ratios (1:1, 1:2, 1:3, 1:4 & 1:1, 2:1, 3:1, 4:1). The developed superdisintegrants were evaluated for angle of repose, carr’s index and the type of flow. The angle of repose of the developed excipients was found to be <30°C, Carr’s index in the range of 12-21 %and the type of flow was good for all. Fast disintegrating tablets of Telmisartan were prepared using above co-processed superdisintegrants and evaluated for pre-compression and post-compression parameters. Based on the disintegration time (15 secs) , wetting time (8 secs), water absorption ratio (approx 86 %) and In-vitro dissolution time (within 2 mins), batch T8 was found to be the most promising batch. Stability (40°C/75%RH) and drug- excipients interaction (FT-IR & DSC) were also studied and no interaction between drug and excipients were revealed. Amongst all eight designed formulation, the formulation T8 containing 5% of co-processed superdisintegrants (4:1 i.e., 4 parts of CCS and 1 part of CP) emerged as the overall best formulation as compared to other ratios....
The ultimate goal of any drug delivery system is the successful delivery of the drug to the body; however, patient compliance must not be overlooked. Fast dissolving oral drug delivery systems, such as, fast dissolving oral films, offer a convenient way of dosing medications, not only to special population groups with swallowing difficulties such as pediatric and geriatric patients, but also to the general population. Fast dissolving oral Films are the novel dosage forms that disintegrate and dissolve within the oral cavity within a minute, without needing water or chewing. A novel fast release oral film drug delivery system for the treatment of emesis in pediatrics and geriatric patients was developed for immediate oral delivery of Domperidone which is an excellent antiemetic drug. Domperidone films were prepared by solvent casting technique using two water soluble polymers, Pullulan and Sodium carboxy methyl cellulose in different concentration. Infrared analysis revealed no interaction between Domperidone and polymers. The prepared films were evaluated for their thickness uniformity, folding endurance, content uniformity, surface pH, In-vitro disintegration time and In-vitro drug release. Formulation F1 released 99.27% of drug within 12 sec and was considered as best formulation. This case study showed that Pullulan was the most suitable film-forming material for domperidone-loaded films, providing fast dissolution films that were not sticky and were easy to handle....
The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming ophthalmic systems that are instilled as drops into the eye and undergo a sol–gel transition in the cul-de-sac. The present work describes development of an ophthalmic gel forming solution system of an agent brimonidine tartrate used in the treatment of glaucoma. Polyox WSR 301 was used as the gelling agent in combination with HPMC E50LV as a viscosity enhancing agent. The developed gel forming solution evaluated for Appearance, Clarity, pH and drug content, Rheological evaluation, In vitro drug release, Test for sterility, Stability study, Ocular irritation study and In vivo efficacy study (the elimination of brimonidine tartrate in tear and intraocular pressure-lowering effect). The developed formulation was therapeutically efficacious, stable, non-irritant and provide sustained release of the drug over an 8 hour. The developed system is thus a viable alternative to conventional brimonidine tartrate eye drops....
Transdermal drug delivery system (TDDS) is emerging system as compared to oral and parentral. In TDDS, patch system was developed to control the release of drug and achieved advantages over the oral and parenteral. However, TDDS has limited market success due to the barrier properties of the Stratum Corneum and stability of formulation. Then after, the number of vesicular drug delivery systems such as liposomes, ethosomes, niosomes were developed as Novel transdermal drug delivery system (NTTDS). It delivers the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it channel the active entity to the site of action. Ethosome is better achievement in vesicular drug delivery system, helpful to achieve goal needed by NTDDS. Ethosomes are soft, malleable and noninvasive delivery carriers that enable drugs to reach the deep skin layers and/or the systemic circulation. Also, the ethosomal systems are conceptually sophisticated, characterized by simplicity in their preparation, safety and efficacy—a combination that can highly expand their application. It provides a number of important benefits including improving the drug's efficacy, enhancing patient compliance and reducing the total cost of treatment. Because of their unique structure, ethosomes are able to encapsulate and deliver the highly lipophilic molecules such as minoxidil as well as cationic drugs such as trihexyphenidil through the skin. Enhanced delivery of bioactive molecules through the skin by means of an ethosomal carrier opens numerous challenges and opportunities for the research and future development of novel improved therapies....
In recent years scientific and technological advances have been made in development of ocular controlled drug delivery system (OCDDS) to overcome physiological adversities such as short residency time, rapid elimination of drug, lower bioavailability of drug. The present investigation was focused to prepare resinate of drug (moxifloxacin) and ion exchange resign (INDION 254) to increase the residence time and decrease the solubility of drug in ocular site and incorporated in ocular insert. Ocular insert was prepared by solvent casting method. Nine formulations of OCDDS were prepared with different concentration of polymer (HPMC, MC, and PVA). Prepared formulation was subjected to physicochemical evaluation test like thickness, surface pH, swelling index, folding endurance, In vivorelease test, antimicrobial test, sterility test, In vivo release and accelerated stability study test. In vivorelease of formulation BRF6 was shown 98.87 % at the end of 12th hrs. In vivorelease of all the formulation was computed with release kinetic model to predict release rate. Higuchi matrix model suggested all the formulation was followed diffusion release mechanism. Korsmeyer Peppa’s equation suggested that all formulation was followed anomalous diffusion mechanism. Optimized formulation (BRF6) was subjected to antimicrobial test and sterility test. Result clearly showed it was passed. Accelerated stability study indicated optimized formulation was stable for longer period of time....
The aim of present work was to formulate Mucoadhesive buccal patches of Omeprazole .The buccal region of the oral cavity is an attractive target for administration of the drug of Choice for increase bioavailability and prevent first pass metabolism of drug and also to prevent degradation in stomach. Omeprazole patches were prepared using HPMC K15 M, HPMC K4M, PVP K30, Sodium Alginate, Eudragit L 100, Eudragit S100 and Carbopol 934. The patches were evaluated for their thickness, Uniformity content, folding endurance, weight uniformity, Swelling index, tensile strength and surface pH. In vitro loaded studies of Omeprazole was done in phosphate buffer (pH 6.8)....
For the past few decades, there has been a considerable research interest in the area of drug delivery using particulate delivery systems. Colloidal carriers like Lipospheres have been used as a physical approach to alter and improve the pharmacokinetic properties of various types of drug molecules. Lipospheres are solid microparticles composed of fat core stabilized by phospholipids layer represent promising carrier system for the delivery of highly challenging, labile and unstable substances. Lipospheres introduced in 1990 represent an alternative carrier system to traditional colloidal carriers, such as emulsions, liposomes and polymeric micro- and nanoparticles, it possess excellent drug delivery system and has broad prospects in the pharmaceutical field. This paper basicly reviews the types of Lipospheres, preparation, characterization and their applications in the delivery of drug molecules and therapeutic genes The future direction of research and clinical implications of Lipospheres is also considered....
Pectin pellet loaded with highly hydrophilic drug, levetiracetam were prepared by powder layering technique. Pectin and starch powder was used as release retarding material. Eudragit L100 and S100 were act as the shell material. Both, the powder mixture and drug was sieved through a 400 µm screen and mixed with Polyvinyl pyrolidone (kollidon 25) in water as binder. The resultant pellets by this technique were evaluated for physiochemical properties like micromeritic properties, particle size, percentage yield, sphericity index, entrapment efficiency, % mucoadhesion, drug release pattern, scanning electron microscopy, release kinetics and stability. The pellet size measured by sieving method was ranged from 699.11-840.9µm. The enhancement of pectin content in pellet resulted in increasing pellet size. From the study it was found that formulation containing middle level polymer ratio had high % yield and encapsulation efficiency. Percentage mucoadhesion were increased from 57 % to 82 % due to increases of pectin. The drug release study was performed using USP XXIV basket apparatus. The study of drug release showed that in SGF % release of drug was found to be less for all formulations. In SIF, at the end of 6th h release rate was 36.03 ± 1.05% for LPP1 and 22.05 ± 0.66% for LPP4. In SCF, at the 8th h the release was 102.15 ± 0.30% for LPP1. In conclusion, pectin pellet loaded with levetiracetam obtained with desirable size, shape, % yield, sphericity index, entrapment efficiency and drug release profile....
Traditionally, drugs are released in an immediate or extended fashion. However, in recent years, pulsatile drug release systems are gaining growing interest. A pulsatile drug release, where the drug is released rapidly after a well defined lag-time, could be advantageous for many drugs or therapies. Pulsatile drug delivery systems (PDDS) are gaining importance as these systems deliver the drug at specific time as per the pathophysiological need of the disease, resulting in improved patient therapeutic efficacy and compliance. This system is designed for chronopharmacotherapy, which is based on circadian rhythm. The principle basis for the use of pulsatile release is for the drugs where a constant drug release, i.e., a zero-order release is not preferred. Ideally, with a pulsatile system, the drug is released rapidly and transient after a defined lag time of no drug release. Diseases wherein PDDS are promising include asthma, peptic ulcer cardiovascular diseases, arthritis attention deficit syndrome in children. Marketed product like Pulsicap®, Ritalin® and Pulsys® are based on pulsatile release system....
The new chemical entities (NCE’s) discovered by medicinal chemist have good pharmacological action but have poor pharmacokinetic properties. Therapeutic effectiveness of a drug depends upon the bioavailability and ultimately upon the solubility of drug molecules. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response. Hence, enhancement of solubility becomes prime requisite for formulation scientist. Various methods are used for enhancement of solubility. The current review enlists various methods for enhancement for solubility with special emphasis on Solid dispersion. It focuses on in detail on methods of preparation, evaluation, types of carriers and applications of solid dispersion....
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