Current Issue : April - June Volume : 2012 Issue Number : 2 Articles : 13 Articles
Solubility plays an important role in drug disposition, since the maximum rate of passive drug transport across a biological membrane, is the product of permeability and solubility. Thus improvement of aqueous solubility in such case is valuable goal to effectively formulate them into bioavailable dosage forms. The complexation with cyclodextrins is most frequently used. Cyclodextrins are cyclic oligosaccharides which have recently been recognized as useful pharmaceutical excipients. The molecular structure of these glucose derivatives generates a hydrophilic exterior surface and a non polar cavity interior. Such cyclodextrins can interact with appropriate size drug molecules which lead to the formation of inclusion complexes. A critical review of the literature was carried out to characterize the formation of inclusion complexes by different techniques in the solid and in the solution state. The characterization of inclusion complexes was done with a purpose to determine the interaction of drug molecules with cyclodextrins which confirm the formation of inclusion complexes....
Cimetidine is an H2 – anti histaminic drug that has been widely used in the treatment of gastric ulcers. It is suitable drug for gastro-retentive floating tablets due to its short half life and poor absorption in lower gastro intestinal tract. In the present research work Box – Behnken Design was used for optimization of level of independent variables (sodium bicarbonate, bees’ wax and ethyl cellulose) on dependent variables (floating lag time and percent release at the end of 24 hrs) in the formulation of Cimetidine gastro retentive floating tablets with less experimentation. Based on the polynomial equations and from the results it was concluded that sodium bicarbonate (10%), bees’ wax (10%) and ethyl cellulose (15%) were favourable for formulation of gastro – retentive floating tablets employing HPMC K4 as release retardant....
Many elderly persons face difficulties in administering conventional oral dosage forms because of hand tremors and disphagia. To fulfill these medical needs, a variety of dosage forms for oral administration known as intra-oral fast dissolving dosage forms were developed. Fast dissolving capsules are solid dosage forms which disintegrate or dissolve rapidly in the mouth without chewing and water. Novel fast dissolving capsules of amlodepine besylate were developed. Two preparation techniques were adopted namely laser perforation and vaccum drying. Nine formulae of amlodepine capsules were prepared, the powder blends of the drug and different excipients used were evaluated with respect to bulk density, tapped density and angle of repose. The prepared capsules were evaluated regarding their physical characteristics. In –vivo disintegration time was determined and in-vitro release study was also carried out to confirm that our goal was achieved. The prepared powder blends fulfilled the pharmacopeial limits. The two techniques proved to be promising and the in –vivo disintegration time of the prepared formulae ranged between 26- 37 seconds....
The present investigation was carried out to evaluate the ability of Eudragit S-100 based enteric coated capsules to target embelin to small intestine. Embelin mainly shows its anthelmintic activity against tapeworms which are mainly found in small intestine. Embelin was extracted successfully from Embelia ribes burm F. by cold maceration technique. Solid dispersion of embelin with PVP (1:1) was prepared using solvent evaporation method. Since prepared solid dispersion was very fluffy, its granules were prepared in order to improve its flow properties by wet granulation method using isopropyl alcohol as a granulating agent. The prepared granules of solid dispersion were filled in HPMC capsules. Capsules were coated using 3, 5 & 7% w/v Eudragit S-100 aqueous dispersion for 5, 10 & 15% weight gain. Enteric coated capsules were evaluated for various parameters like coating defect, drug content, acid uptake and in vitro drug release. None of the capsule was disintegrated in pH 1.2 within two hours. Since all the capsules remained intact in acidic pH 1.2, it was concluded that enteric coating was achieved successfully. In-vitro dissolution test of enteric coated HPMC capsules showed maximum release of Embelin in phosphate buffer pH 7.4. Thus it was concluded that the formulation E4 (5% Eudragit S-100 with 5% weight gain) is suitable for successful targeting of Embelin to small intestine....
This research work was done to design oral controlled release matrix pellets of water insoluble drug Propafenone Hydrochloride (PHC), using blend of sodium alginate (SA) and glyceryl palmito stearate (GPS) as matrix polymers, methyl crystalline cellulose (MCC) as spheronizer enhancer, sodium lauryl sulphate (SLS) as pore forming agent. PHC formulations have been developed by the pellitization technique by drug loaded pellets were further characterize with regard to the drug content, size distribution, and pellets were further characterize by Scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy ( FTIR) and X-ray Diffraction study ( XRD ). Stability studies were carried out on the optimized formulation for a period of 90 days at 40 ± 2 oC and 75 ± 5% relative humidity (RH).The drug content was in the range of 92.47 – 97.38 %. The mean particle size of drug loaded pellets was in the range 1035 to 1210 mm. SEM photographs and calculated sphericity factor confirms that the prepared formulations were spherical in nature. The drug loaded pellets were stable, compatible, as confirmed by DSC and FTIR studies. XRD patterns revealed the crystalline nature of pure PHC. Loose surface crystal study indicated that crystalline PHC was observed in all formulation and more clear in formulation F3. Drug release was controlled for more than 24 h and mechanism of drug release followed Fickian diffusion. It can be conclude that F3 is an ideal formulation for once a day administration....
The objective of the present study was to increase the solubility and dissolution rate of poorly soluble drug ritonavir. Ritonavir is having low aqueous solubility and high permeability which can be considered as drug belonging to class-II according to BCS. In this study nanosuspension technology was tailored to increase solubility and dissolution rate of ritonavir and to transfer into dry powder which is suitable for filling into capsules. Ritonavir nanosuspension was prepared by pearl milling technique using zirconium beads as a milling media and poloxamer407 as a stabilizer. The prepared nanosuspension was characterized by particle size analysis, zeta potential, DSC and XRD studies. Ritonavir nanosuspension was dried using vacuum tray drier, the dried mass was filled into capsules by adding polyplasdone XL-10, span-20 and magnesium stearate. The capsules were evaluated for drug release, assay and stability. The nano sized crystalline ritonavir alone and in capsule dosage form showed dramatic increase in solubility and dissolution rate when compared to the micronized ritonavir....
The aim of present work is to provide transdermal delivery of acetyl cholinesterase inhibitor provides more beneficial drug delivery over oral drug delivery system. Transdermal patch offer the advantages such as maintenance of controlled and prolong drug level, reduced frequency of dosing, minimization of inter and intrapatient variability, self administration, and easy termination of medication during treatment due to side effects observed leading to patient compliance, directly systemic delivery prevent drug related side effects. Rivastigmine transdermal patch made from different types of pressure sensitive polymers like acrylic adhesive, polyisobutylene adhesive and silicon adhesives. Rivastigmine salt and free base forms were evaluated for In vitro permeation study. Formulations were evaluated for skin permeation study, physical properties. Free base form has significantly higher permeation than salt form. Drug permeation profiles form different PSAs (pressure sensitive adhesives) were evaluated for model dependent release kinetics. It was found that acrylic type PSA formulation has zero order release pattern. PIB (polyisobutylene) and silicone type PSAs indicate peppas model fitting with supercase II type of release pattern. Physical properties of different formulations were evaluated in terms of peel, tack and shear. All formulations were stable during 28 days study and reflects physical stability of formulations. Acrylic type pressure sensitive adhesive has better peel, tack and shear properties. Acrylic pressure sensitive adhesive can be use to prepare stable formulation of rivastigmine with zero order controlled release profile....
Despite phenomenal advances in injectables, transdermals, inhalable, nasal and other routes of administration oral route of administration remains well ahead as the most preferred delivery route, with tablets emerging as the most popular solid oral dosage form used today. However various factors like difficulty in swallowing, unavailability of water etc lead to high incidence of patient non compliance which in turn can lead to ineffective therapy and increased health care cost. Methods to improve patient’s compliance have always attracted scientists towards the development of fancy oral drug delivery systems. Among them, mouth dissolving drug delivery systems (MDDDS) have acquired an important position in the market by overcoming previously encountered administration problems and contributing to extension of patent life. Mouth dissolving tablet are solid unit dosage forms, which dissolve rapidly in mouth without chewing and water. Within the patient population Mouth dissolving tablets has applications in some increasingly important demographic groups such as pediatric and geriatric patient who have either difficulty or disliking for swallowing conventional tablet and capsules. In this article various aspects of mouth dissolving tablets are covered including: formulation aspects, evaluation techniques, technologies available and the advances made so far in the field of fabrication of mouth dissolving tablets....
This article mainly focuses on the development of Nano particle systems and methods for delivering anti-tubercular drugs directly to the lungs via the respiratory route. The main advantages of inhaled drug delivery include direct drug delivery to the diseased organ, targeting to alveolar macrophages, reduced risk of systemic toxicity and improved patient compliance. Researchers have demonstrated the possibility of various drug delivery systems using lipids, polymers and proteins to serve as inhalable anti-tubercular drug carriers. In recent years, encapsulation of antimicrobial drugs in Nano particle systems has emerged as an innovative and promising alternative that enhances therapeutic effectiveness and minimizes undesirable side effects of the drugs. Beginning with the respiratory delivery of a single anti-tubercular drug, it is now possible to deliver multiple drugs simultaneously with a greater therapeutic efficacy. Several key issues such as patient education, cost of treatment, stability and large scale production of drug formulations, etc. need to be addressed before anti-tubercular inhaled therapy finds its way from theory to clinical reality...
There is a constant need for new delivery systems that can provide increased therapeutic benefits to the patients. Pulsatile drug delivery is one such system that, by delivering drug at the right time, right place, and in right amounts, holds good promises of benefit to the patients suffering from chronic problems like arthritis, asthma, hypertension, etc.Sustained release formulations are not efficient in treating the diseases especially diseases with chronological pathopysiology, for which, pulsatile drug delivery is beneficial. Various methodologies are employed for developing pulsatile drug delivery like time controlled PDDS which includes delivery systems with rupturable coating layer or with erodible coating layers or with release plug controlling, stimuli induced PDDS less temperature induced and chemical stimuli induced systems and externally regulated system. Multiparticulate systems are useful for treatment of patients; due to their resulting high efficiency and robustness. There are various technologies present in the market based on the various methodologies. Pulsatile release systems should be promising in the future....
Microsponges delivery systems (MDS) composed of tiny sponge like spherical particles that consist of a myriad of interconnecting voids of particle size range 10-25µm within a non collapsible structure with a large porous surface. Microsponge is a versatile drug delivery vehicle and can suspend or entrap a wide variety of substances. The outer surface is typically porous, allowing a sustained flow of substances out of the sphere. It offers numerous advantages over other technologies like reduced side effects, improved stability, increased elegance and enhanced formulation flexibility. Microsponges are porous, polymeric microspheres that are used mostly for topical and recently for oral administration as well as for biopharmaceuticals (peptides, proteins and DNA-based therapeutics) drug delivery. Specifically, microsponges lessen the irritation usually associated with powerful therapeutic agents used topically like retinoids or benzoyl peroxide. They can be incorporated into conventional dosage forms such as creams, lotions, gels, ointment, tablet and powder and share a broad package of benefits & thus provides formulation flexibility. MDS technology is being used currently in cosmetics, over-the-counter (OTC) skin care, sunscreens and prescription products. This review article covers methods of preparation, release mechanism, characterization and applications of Microsponge delivery system with patent information and marketed topical formulations....
Nanotechnology is a field of research at the intersection of science; Biology, chemistry, physics, engineering and medicine. It designs different type and functions of nanoparticles, and they are capable of targeting cancer cells, this targeted delivery system of drug molecules to tumor tissue and cancer cell, is one of the most attractive and challenging activities faced in pharmaceutical field, due to the significant and pharmacokinetically specific atmosphere that lives in tumor nanoparticles show much guarantee in cancer treatment by selectively in advance access to tumor due to their small size and modifiability. Target-specific drug therapy and methods for early diagnosis of pathologies are the priority research areas in which nanotechnology would play a vital part. In this review we focused on nonmaterial, nanocarrier and Biomarkers of cancer having general principle of targeting drug to the cancer cell by intracellular mechanism; we also cover the marketed formulation of Nanoparticles, having recent application in cancer therapy. The basic approach of review to design the feature prediction and breakthrough in cancer therapy....
The aim of present study was to develop Microballoons of Ciprofloxacin hydrochloride to treat H.pylori infections and gastro-intestinal anthrax caused by B.anthracis. in order to achieve, Materials and method: Microballoons of ciprofloxacin hydrochloride were prepared by emulsion solvent diffusion method using polymer such as ethyl cellulose (EC) and eudragit S100 (EU) in different ratios (drug: polymer 1:1, 1:2, 1:3). The microballoons were characterized for their shape and surface morphology by optical and scanning electron microscopy, drug loading, buoyancy time and infrared spectroscopy (FT-IR) for the compatibility study. Key findings: The micromeritic properties of microballoons were found to be much improved .The in-vitro drug release were studied by USPXXIII (basket type). The prepared microballoons exhibited prolonged drug release (>12 hrs) and remained buoyant for > 12 hrs. The mean particle size increased and drug release rate decreased at higher polymer concentration. The release kinetics studies were fit into zero order and Fickian diffusion controlled mechanism was observed. Conclusion: from the obtained results we can achieve an extended retention in the upper GIT, which may result in enhanced absorption, decreased dosing interval and improved bioavailability....
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