Current Issue : April - June Volume : 2011 Issue Number : 2 Articles : 18 Articles
Water soluble polymers are always being in good demand because of their certain advantages over organic solvents with respect to ecological, toxicological and manufacturing safety concerns, including Pollution, Explosion hazards, Risk of operators, High cost of organic solvents, solvent toxicity and many more. Aqueous polymeric dispersions, latexes, or pseudolatexs are all colloidal systems in which high molecular weight polymers are homogeneously dispersed in submicron sizes with the aid of surfactant(s) and other stabilizing agents. There are a wide range of water insoluble polymers includes Acryates: Eudragit, Cellulose: Ethyl cellulose, Vinylics: Polyvinyl acetate phthalate, Cellulosic esters: cellulose acetate phalate (CAP) & many more which provide a great research platform to develop an aqueous polymeric dispersions (APD) with the intention of conferring benefits and properties to the dosage form over the uncoated variety or organic coating. The present article is mainly focused on the theoretical & practical aspects of the development techniques/steps & research scope behind the development of APD....
The gliclazide microcapsules were formulated to extend the hypoglycemic effect for a period of 10-12hrs. The gliclazide microcapsules were formulated by using ionic gelation method with and without mechanical stirring. The effect of various process variables such as curing time, stirring speed, stirring time, volume of curing reagent and concentration of curing reagent on entrapment efficiency and drug release rate was studied. The optimized formulation was selected based on the entrapment efficiency and drug release rate. The optimized formulation of gliclazide microcapsules were subjected to the hypoglycemic activity in healthy albino rabbits (n=5). The blood glucose levels were measured and then percentage glucose reduction was calculated. The data was treated statistically. Compared the mean blood glucose levels observed from gliclazide and its microcapsules. The hypoglycemic activity of pure drug was observed at 2nd -3rd hour and it was extended for a period of 2nd to 10th hour in case of microcapsules....
The present investigation deals with design and development of fast dissolving Celecoxib tablet by solid dispersion and camphor sublimation method using 32 Full Factorial design. The Celecoxib tablet prepared using solid dispersion of drug with carrier (PVP-K30) and different proportion of super disintegrants (Ac-Di-Sol). Drug was evaluated for bulk density, tapped density, Carr’s index and Hausner's Ratio. The different tablet (H1-H9) were prepared using solid dispersion of drug with carrier by direct compression method and evaluated for Compatibility study, Hardness, Thickness, Friability, Disintegration time and Wetting time. In vitro drug release profile of different batches (H1 to H9) was done by using USP type II apparatus. The optimized batch H7 was compared with marketed formulation and shows the better release (88.51%) than marketed formulation (80.71586%). Physical characterization of optimized formulation (H7) was done by FT-IR. Accelerated stability study was done to after 3 month. The Stability data indicate that formulation was stable at environmental condition. Camphor sublimation method was used to evaluate the effect of camphor on in vitro dissolution profile. The different proportion of independent variable (Ac-Di-Sol and Camphor) was used. The prepared formulation was evaluated for Hardness, Friability, Disintegration and drug content. From the different batches F8 shows 92.10% release in one hour. The FTIR spectrum of optimized formulation (F8) was done to check the interaction. It could be revealed that incorporation of camphor in tablet provide beneficial role in improving dissolution of drug....
Ginger (Zingiber officinale) has traditionally been used in delicacy, medicine, or spice. aromatic, pungent, spicy, has been claimed as an antioxidant and also an anti-ulcer agent; Evaluation of in vitro antioxidant activity of ginger extract (GE) in a series of in vitro test systems and its comparison with ascorbic acid showed promising data. In the present study we developed floating beads (FBs) of GE with intent to achieve a localized therapeutic action and a prolonged stay in the stomach. Developed beads were evaluated for ethanol induced gastric ulcers in rats. Latter is a model for oxidative stress induced gastric ulcers. Oxidative stress of the stomach mucosa in terms of malondialdehyde and antioxidant enzymatic parameters showed a significant attenuation with free GE which was further enhanced significantly by the developed FBs of GE. The number and severity of ulcers (ulcer index) significantly reduced by 48% at1 hours post administration with free GE, the value increased to 62.5% at 1 hour & further 83% at 24 hours post administration with developed floating beads of GE....
Domperidone is practically water insoluble drug exhibiting poor dissolution and absorption. The main objective of the present study is to improve the dissolution rate of domperidone by preparation of solid dispersion using polyethylene glycol (PEG 6000) as a carrier at low and high concentration. Solid dispersions were prepared by Fusion method at different polymer ratio. The physical state and drug: polymer interaction were analyzed by Differential scanning calorometry, and infrared spectroscopy, and Scanning electron microscopy. The dissolution rate of Domperidone from solid dispersions was markedly enhanced by increasing polymer concentration. The result shows that dissolution rate of domperidone from all Physical mixture and solid dispersion was significantly higher than that of domperidone alone. The result indicated that solid dispersion 1:9 exhibited more than 90% of drug release after 20 min. DSC study showed that the degree of crystaliinity of domperidone in solid dispersion decreased when the ratio of the polymer increased, suggesting that the drug is present inside the sample in different physical state. The Fourier transform infrared spectroscopy studies showed the stability of domperidone and the absence of well defined drug polymer interaction....
In the present study, solid dispersion (SD) of nitrendipine was prepared to enhance its water solubility. The SD was prepared by using poly-vinyl alcohol (PVA) and poloxamer188 (PXM188) as a carrier. The different drug polymer ratios were prepared by the techniques physical mixing and solvent evaporation. The product was characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and in vitro dissolution rate studies. Phase solubility analysis was performed in aqueous solution for drug polymer interactions. DSC and XRD analysis demonstrated the conversion of nitrendipine to amorphous form with both physical mixture (PM) and SD. SD with PXM188 released 98% of the drug in 100 min as compared with 79% of drug released in 100 min by SD with PVA. Thus, SD with both polymers increased drug release, particularly greater in the case of PXM188 than PVA....
Microspheres loaded with meloxicam were prepared by ionic gelation method without the use of chemical cross–linking agent, glutaraldehyde in order to avoid its toxic reactions and other undesirable effects. Ionotropic gelation was employed by using sodium-tripolyphosphate (Na-TPP) as cross-linking agent and chitosan as the polymer. All the prepared microspheres were subjected to various physico-chemical studies, such as drug-polymer compatibility by Fourier Transform Infrared Spectroscopy (FT-IR), surface morphology by Scanning Electron Microscopy (SEM), particle size distribution, encapsulation efficiency and in-vitro drug release characteristics. The drug release rate decreased with an increase in the cross-linking density. DSC and XRD analysis indicated that the meloxicam trapped in the microspheres existed in an amorphous or disordered crystalline state in the polymer matrix. From the preliminary trials, it may be concluded that drug-loaded microspheres can be prepared by a simple technique which avoids the use of complex apparatus and special precautions....
The present investigation concerns the development of Gastroretentive floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of gastric irritating Diclofenac sodium by using Mango resin i.e., Mangifera indica and to study its release retardant activity in prepared floating formulation. Different concentrations of resin were tried in order to get the desired sustained release profile over a period of 12hr. sodium bicarbonate and citric acid were incorporated as gas generating agents. Various formulations were evaluated for precompression properties like flow of granules, bulk and tapped density, post compression properties like uniformity of weight, hardness, friability, thickness, invitro buoyancy characteristics, drug content, invitro drug release profile and mechanism of drug release. Prepared tablets exhibited satisfactory precompression and post compression properties. All the prepared batches showed good invitro buoyancy. It was also found that invitro drug release rate decreases with increases amount of natural retardant polymer mango resin. The kinetics of drug release from all the formulations followed the zero order by regression analysis and further mechanism of drug release was conformed by Higuchi�s and Korsemeyer�s model showed that non-fickian and anomalous drug releases. Finally optimized formulation F4 was compared with marketed Voveran SR tablet of Diclofenac sodium was showed similar release profile with similarity factor value 90.12....
In the present study, we formulated liposomes of salbutamol sulphate, antiasthamatic drug in order to improve pulmonary delivery by Thin Film Hydration technique, using lipid- Phospholipon�® 90G as a lipid of choice. Sustained release effect of liposomes was found to be extended as long as 10hrs and maximum drug entrapment was found to be 40-50%. Salbutamol sulphate, 0.1 % was incorporated in a ratio of 1:10 with that of lipid. To obtain rigidity and stability to liposomal vesicles, cholesterol and antioxidant Butylated Hydroxy Anisole (BHA) were used. 33 Factorial Design was applied to optimize concentration of cholesterol , BHA and PH of hydration buffer with respect to percentage drug entrapment. Stable liposomes were obtained with 0.25% of cholesterol and hydrating buffer pH, 6.4. In further process variables study, the maximum drug entrapment was found to be about 52-55% at the lowest rotation speed, 30rpm; and at optimum ratio of batch size to rotary flask capacity as 1:5....
The purpose of this research works to develop and optimized the extended release film coated matrix tablet of Divalproex sodium to mask the foul taste of divalproex sodium, improve the product stability and to modulate the release properties. In the present study extended release tablet of Divalproex sodium was prepared by using wet granulation method. Different grades of hydroxypropyl methyl cellulose (K100M CR and HPMC K15M CR) were evaluated for gel forming properties. Preformulation study shows that drug and other excipients are compatible with each other. The tablets were made film coated by using specific coating polymer. The effects of polymers concentration on drug release profile were investigated. All the Prepared formulations were evaluated for the physical characteristics, in vitro dissolution and accelerated stability study was also performed for three months indicated that optimized formulation was stable. Finally, process optimization was carried out to optimize the process parameters like kneading time, mixing time, thickness of the tablet and lubrication time. The release of divalproex sodium from the film coated tablet for a period up to 18 hrs was recorded in controlled manner. \nKeywords: Extended release, epilepsy, Divalproex sodium, Matrix tablet, Kneading time....
Escin is a neutral glycosidic drug with anti-inflammatory, anti-edematous, vasoprotective and venotonic activity used in treatment of chronic venous insufficiency (CVI), hemorrhoids and post-operative oedema.The purpose of this study is to explore the passive and electrically assisted transdermal transport of escin by iontophoresis, the effect of different variables on transdermal transport and iontophoresis efficiency was assessed. These variables are type of iontophoresis (anodal/cathodal), current density (0.25 mA/cm2 & 0.5 mA/cm2), concentration of drug solution (2 mg/ml & 4 mg/ml), mode of current (continuous/pulsed) and type of solvent used (Deionized water/normal saline). In vitro passive and iontophoretic transport experiments of escin were performed in phosphate-buffered medium. Rat skin show a net negative charge at pH 7.4 and in the presence of current, an electroosmotic convective solvent flow in the anode-to-cathode direction takes place. The results of the present study show that transdermal iontophoresis can be useful for enhancing the transport across the skin of high molecular weight compounds, even though neutral....
The concept of mucoadhesion started in early 1980’s. Since, then much advancement took place in designing mucoadhesive drug delivery systems. These delivery systems make an intimate contact with mucosa of the respective site to enhance the drug absorption by sustaining or increasing the residence time of the drug at the respective site. In addition, the physicochemical properties of polymers investigated in designing various delivery systems viz., tablets, microcapsules, films, patches, gels, etc., has affected the process of mucoadhesion invariably. So for better understanding, the review focuses on the nature, theories and sites of mucoadhesion, polymers for mucoadhesion and delivery systems. In this connection, the review enlightens the current new generation polymers explored for mucoadhesion and outlines the research work carried out on this area....
Nanotechnology refers to research and technology development at the atomic, molecular, and macromolecular scale, leading to the controlled manipulation and study of structures and devices with length scales in the 1- to 100-nanometers range. The possibility to manipulate the physical, chemical, and biological properties of these particles affords researchers the capability to rationally design and use nanoparticles for drug delivery, as image contrast agents, and for diagnostic purposes.To achieve efficient drug delivery it is important to understand the interactions of nanomaterials with the biological environment, targeting cell-surface receptors, drug release, multiple drug administration, stability of therapeutic agents and molecular mechanisms of cell signalling involved in pathobiology of the disease under consideration.Anti-cancer drugs including paclitaxel, doxorubicin, 5-fluorouracil and dexamethasone have been successfully formulated using nanotecnology. Quantom dots, chitosan, nanoparticles have also been used for in vitro RNAi delivery and and nasal delivery of vaccines. Anti-cancer drugs such as loperamide and doxorubicin bound to nanomaterials have been shown to cross the intact blood-brain barrier and released at therapeutic concentrations in the brain. The use of nanomaterials including peptide-based nanotubes to target the vascular endothelial growth factor (VEGF) receptor and cell adhesion molecules like integrins, cadherins and selectins, is a new approach to control disease progression. Nanotechnology is of great use for medical diagnosis and various nanoparticles have exhibited tremendous potential for detecting disease markers, pre-cancerous cells, fragment of viruses and other indicators. Recent advances in the field have aimed towards multifunctionalization of nanoparticles to produce therapeutic systems that combine targeted drug therapy with diagnostics, for a more real-time therapeutic approach....
Gamma scintigraphy is a non- invasive method for imaging the behavior of dosage forms in vivo in animals and humans. Gamma scintigraphy requires the presence of γ- emitting radioactive isotope in the dosage form that can be detected in vivo by an external gamma camera. Gamma emitting radionuclide is tagged with the active constituent or the excipients of the formulation. The radioactive dosage form is administered via the intended route of administration and the subject (human/animal) is scanned under a gamma camera. Radionuclide tagged drugs/formulations/devices can provide vital information regarding the extent, rate, site, and mode of drug release and morphology of the drug delivery system during release in humans under ethical norms. Pharmacokinetics and Pharmacodynamics of new drug molecules studied by this technique give qualitative as well as quantitative data....
The rate-limiting step to absorption of drugs from the gastrointestinal tract is often dissolution from the dosage form. Diacerein is used drug in the treatment of Osteoarthritis. One of the major problems with Diacerein is that, it is practically insoluble in water,coming under class-II of biological classification system,, which results in poor bioavailability after oral administration. In the present study, solid dispersions of Diacerein were prepared by solvent evaporation method, Physical mixture and Fusion method to increase its water solubility. In the present study amphiphilic carrier like gelucire 50/13 was used in the ratio of 1:1, 1:3 and 1:5. Prepared solid dispersions were characterized in the liquid state by phase solubility studies and in the solid state by Differential Scanning calorimetric analysis, Powder X-ray diffractometry,Scaning electron microscopy and Fourier Transform Infrared spectroscopy. The aqueous solubility of Diacerein was preferential by the presence polymer with increasing concentration. Solid state characterizations indicated that Diacerein was present as an amorphous material and entrapped in polymer matrix. The release study findings were well supported by the results of wettability, saturation solubility and permeability studies....
In the present investigation, the dissolution rate improvement of glimepiride was carried out by preparing solid dispersions (SDs) using melting technique with poloxamer 188, a copolymer nonionic surfactant. Prepared SDs were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC) and evaluated for solubility, in vitro drug release, dissolution efficiency and in vivo drug absorption by intraperitoneal glucose tolerance test (IPGTT). All the SDs had shown good flow properties. Loss of their individual surface properties during melting and solidification as reveled by SEM studies indicated the formation of effective SDs. X-ray diffraction studies showed decrease in crystallinity of glimepiride in SDs as compared to the pure glimepiride. All the formulations prepared by melting technique have shown significant enhancement of dissolution rate when compared to pure glimepiride. The dissolution rate of glimepiride increases as the amount of polymer (poloxamer 188) increases in SDs. Moreover, IPGTT indicated that the SDs of glimepiride-poloxamer 188 markedly reduces the blood glucose concentration in Swiss Albino mice. Thus, the present study demonstrated that a copolymer nonionic surfactant, poloxamer 188 provides a promising way to prepare solid dispersion with glimepiride which increases the solubility, dissolution rate and oral bioavailabilty of glimepiride....
Dry powder inhalers have been developed as an alternative to Metered dose inhaler (MDI) devices and offer a number of advantages over the latter; principally the reduced need for patient co-ordination since the drug is expelled from the device as a result of the patient’s own aspiratory effort. However, dry powder formulation need to be stable for a period of time and in different climatic conditions such as 25 ºC and 75 % Relative humidity (RH). Therefore the aim of this study was to produce stable Ipratropium Bromide-Multidose dry powder inhaler (IPR-MDPI) using different types of lactose that meets European Pharmacopoeia/United States Pharmcopoeia (EP/USP) requirements after 3 months storage at 25 ºC, 75 % RH. Mixture of α-lactose and micronized ß-lactose were used to prepare two Ipratropium Bromide formulations and they were IPR -01 and IPR -01R. Α-lactose (Foremost Aeroflo 65) was used to prepare two formulations and they were IPR-02 and IPR-02R. All four blends were then tested according to EP/USP guidelines for mass delivery, dose content uniformity, total dose (TD), fine particle dose (FPD) and fine particle fraction (FPF) at time point zero (t=0). These formulations were put on the stability trial at 25 ºC, 75 % RH (unwrapped), 30 ºC, 60 % RH (unwrapped) and 40 ºC, 75 % RH (wrapped) respectively. Batch-to-batch reproducibility between the repeat blends was good, with similar performance data. Both formulation approaches showed similar trends in pharmaceutical performance over the lifetime of the stability trial. Drug per actuations (DPA) were within EP/USP guidelines over the 2/3 months of the stability trials, despite a small rise in DPA over the lifetime of the trial and the lifetime of the device. The average DPAs over all stability conditions and time points were: 21.1 1.7 g (IPR-01 and IPR-01R) and 20.9 1.5 g (IPR-02 and IPR-02R). However, the increases seen in DPA meant that the DPAs did not pass the tougher specifications of the Food and Drug Administration Authority (FDA) (Dose Content Uniformity, DCU limits). FPDs remained stable and high for all formulations (10.5 1.0 g). FPF fell initially between t = 0 and t = 1 month, but the FPF value stabilized reaching an equilibrium value (45–49 %) between t = 1 and t = 2/3 months. Performance appeared independent of stability conditions (including wrapped and unwrapped), although dose consistency was slightly more variable at 25 ºC, 75 %RH for both formulations. The /-lactose IPR-MDPIs showed slightly less variation in DPA and FPD over the lifetime of the stability trials, but the pure -lactose IPR-MDPIs produce higher FPDs. The present research showed that the two lead IPR-MDPI approaches (-Lactose (Borculo) + 2.5 wt. % micronised -lactose + 1 wt. % IPR and -Lactose (Foremost Aeroflo 65) + 1 wt. % IPR) show encouraging stability trends at all three stability conditions on the basis of their pharmaceutical performance....
One of the major steps in formulation development activity is the development of film coating formulation and process. Formulation and development scientist should understand the critical aspects associated with different kind of coating technique and process. The decision regarding the coating technology is very critical. It is very important to use the most optimized coating formulations in order to get the best results. Various film forming polymers are used to form the coat around the drug for different purposes. Fluidized bed processing is widely used as it is ideal for a wide range of both heat sensitive and heat resistant products.. Difficulties arise with the large number of variables involving in the fluidized bed coating process. Various variables affect the quality of drug layering. In our research work, we used Box-Behnken design to statistically optimize the selected processing parameters and evaluate the main effects, interaction effects and quadratic effects of the processing parameters on the drug layering. From our research work we found that as the fluidization pressure was increased, the drug content was also increased. As atomization pressure and feed rate increases, the drug content decreases....
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