Current Issue : January - March Volume : 2013 Issue Number : 1 Articles : 11 Articles
The purpose of the present study was to formulate and evaluate the controlled release mucoadhesive microbeads of pantoprazole sodium for intestinal delivery. Microencapsulation is an accepted process, used to achieve controlled release and targeting of drugs. Intestinal residence time of the dosage form can be prolonged by mucoadhesion, which increases bioavailability by facilitating the intimate contact of the dosage form with the underlying absorption surface. Pantoprazole is a proton pump inhibitor used in the treatment of gastric ulcers and gastro-esophageal diseases. Pantoprazole is to be made absorbed in the intestine as it is unstable under the acidic gastric environment, thus mandating enteric delivery. Pantoprazole has a short biological half-life of 1h, which makes it a suitable candidate for sustained delivery so as to achieve prolonged therapeutic action and to reduce peak and valley effect in plasma drug concentration. Pantoprazole microbeads were prepared using Sodium Alginate and mucoadhesive polymers like Carboxymethylcellulose Sodium, Methylcellulose and Hydroxypropylmethylcellulose by orifice-ionic gelation method followed by coating with Eudragit S-100. The prepared microbeads were characterized in terms of their morphology, particle size, encapsulation efficiency, swelling ratio, in-vitro wash-off mucoadhesion test and ability of the formulation to withstand acidic media during its transit in stomach. Different formulation variables like polymer-polymer ratio, drug-polymer ratio and coating concentration were considered. Dissolution study was carried in phosphate buffer (pH 7.4). Most of the beads formulated were spherical with sufficient swelling, mucoadhesive and acid resistant properties. The drug release was also found to be slow and extended upto 12h....
In the present study, an attempt has been made to evaluate and compare the effect of different HPMC grade of hydrophilic polymers on the release profile of drug from matrix system. Salbutamol sulphate, an anti-asthmatic agent, was used as a model drug to evaluate and compare of its release characteristics from different matrices. Matrix tablets of salbutamol sulphate were prepared by direct compression process using methocel K15M CR, methocel K100M CR polymer. Release kinetics of salbutamol sulphate from these sustained release matrices in distilled water using USP paddle method with sinker for 8 hours was studied. Analysis of salbutamol sulphate is done by UV visible spectrophotomer using wavelength 277nm. Statistically significant differences were found among the drug release profile from different formulations. Higher polymer content (70%) in the matrix decreased the rate of the drug due to increased tortuosity and decreased porosity. At lower polymeric level (30%), the rate of drug release was elevated. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer equations. The results generated in this study showed that the profile and kinetics of drug release were functions of polymer type, polymer level and physico-chemical properties of the drug....
The major drawbacks associated with the conventional administration of ondansetron hydrochloride can be attenuated using the skin as a route of administration. However, the effective transdermal delivery is limited by the skin barrier properties. The main objective of the present work was the mechanistic investigation on penetration enhancing effect of different natural essential oils on the transdermal permeation of ondansetron hydrochloride using different analytical tools like scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FT-IR). The enhancing effects of citronella oil, lemon oil and nutmeg oil were investigated across enhancer pretreated pig skin in Keshary-Chien glass diffusion cell. The target flux of ondansetron hydrochloride was achieved with 15 % v/v lemon oil. The in vitro permeation data was best fitted with the zero order kinetic model indicating that the mechanism of drug permeation was diffusion controlled. The FT-IR, SEM and DSC study confirmed that the permeation enhancement effect of the investigated enhancers was caused by the stratum corneum lipid extraction mechanism. A higher enhancement value was observed with lemon oil followed by nutmeg oil and citronella oil....
Fast dissolving tablets were dissolved/disintegrated in the mouth within a matter of few seconds without need of water. Fenofibrate is a fibric acid derivative drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease. It reduces both LDL and low VLDL levels and enhance the level of HDL levels .The purpose of this research was to develop fast dissolving tablets of fenofibrate were prepared by sublimation method and direct compression method. In the Sublimation method, different sublimating agent like camphor, thymol and menthol were used while in direct compression method Crosspovidone, KyronT314, Sodium Starch glycolate as superdisintegrating agents were used in different concentration. The prepared batches of tablets were evaluated for thickness, hardness, weigh variation, friability, drug content uniformity, wetting time, disintegration time and in-vitro dissolution study. From these, fenofibrate fast dissolving tablet prepared by sublimation method gives better release profile as well as wetting and disintegration time as compared to direct compression method. Optimized batch was F9 with 15 % menthol as a sublimating agent having better disintegration time (18 sec), wetting time (23 sec) and t90 % was 12 min....
The purpose of this investigation was to identify a best method for developing fast dissolving tablets (FDTs) of Naproxen sodium. Techniques like effervescent, superdisintegrants addition, sublimation were used. Different trails were designed and prepared. Effervescent agents citric acid and sodium bicarbonate; superdisintegrant crospovidone and subliming agent camphor were used for effervescent, superdisintegrants addition and sublimation methods respectively. The blend and compressed tablets were evaluated. The results showed that superdisintegrants addition method was the best one for formulating naproxen fast dissolving tablets....
The aim of the current investigation is to develop oral once daily sustained release matrix tablets of risperidone, that match with theoretical drug release profile. The interaction studies of polymer and drug with FTIR revealed no interference, this made an account for usage of both hydrophilic and hydrophobic polymers in different combinations for direct compression of tablet. The evaluation of physical properties like angle of repose, bulk density, compressibility index, hausner ratio and appearance, dimensions, weight variation, hardness, friability, drug content, in vitro drug release were carried out for both powdered blend and compressed tablet respectively, and are in acceptable limit. Results of dissolution studies indicated that formulation containing 50% HPMC K100 and 27% sodium carboxy methylcellulose was the most successful formulation which was evidenced by similarity (f2) and dissimilarity (f1) factors. The formulated risperidone tablets followed first order release kinetics and Higuchi diffusion was the dominant mechanism of drug release, resulting in regulated and complete release within 24 hours. Swelling studies supported the mechanism of drug release. Risperidone is an atypical antipsychotic drug available in market as 0.5,1,4,6 and 8mg as conventional tablet with 16mg maximum dose per day. Very less number of sustain release formulations are not working out with dosage regimen provided. so in this work a novel approach to provide similar invitro release profile to that of developed theoretical drug release after oral administration is been targetted....
The aim of presented research work was to develop prolong release tablets of Pramipexole dihydrochloride using systemic scientific approach. Pramipexole dihydrochloride, dopamine receptor agonist used in treatment of Parkinsonism is fall under biopharmaceutical classification system class 1. Dosing frequency of Pramipexole dihydrochloride can be reducing from three times to once a day by developed prolong release formulation. This is a breakthrough in regard to minimizing pill burden and enhancing patient compliance. Furthermore, 24 hour continuous drug release of the once-daily prolong release formulation results in fewer fluctuation in plasma concentrations over time compared to immediate-release Pramipexole dihydrochloride, given three times daily. Predetermine logical release profiles of prepared 1.05 mg Pramipexole (equivalent to 1.50 mg Pramipexole dihydrochloride monohydrate) prolonged release formulation was tailored by implementation of design of experiment tool which was used to optimize concentration of intragranular hypromellose, extragranular hypromellose and extragranular carbomer homopolymer type B which were added as controlled release polymers in range of 30 to 40%, 10 to 20% and 1.0 to 2.0% respectively while Q2hour, Q12hour and Q24hour were fixed as responses. Value of Q2hour, Q12hour and Q24hour in optimized formulation was 39.43%, 69.38% and 91.38% respectively at 36.44% intragranular hypromellose, 15.56% extragranular hypromellose and 1.22% extragranular carbomer homopolymer type B....
Increase in solubility, dissolution rate and bioavailability of new chemical entity (Drugs) is a very tough and essential task in drug development process, approximately 40% of the new chemical entities which are being discovered are poorly water soluble or practically insoluble drugs. Solubility of any therapeutically active substance in aqueous media is a key property as it governs dissolution, absorption and thus the in vivo efficacy. Drugs which are administered orally get completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs play an important role in the process of formulation development. Problem of solubility is a major challenge for formulation scientist which can be solved by different technological approaches during the pharmaceutical product development work. The present review deals in detail about the different nanotechnology based techniques used to improvement of the solubility and dissolution rate of poorly water soluble drugs and application of nanoparticle and there dosage form....
In the recent years, many new excipients and modified preparations of existing excipients have been developed and introduced to the pharmaceutical field. These new excipients are found to be very useful for the formulation of various drug delivery systems. The main aim of the present investigation is to provide new sustained release excipient which, when incorporated into a final product, produces controlled release of active ingredient over an extended period of 12 hrs or more when the dosage form is exposed to G.I fluids in gastric environment. Okra pods are fruits of the plant Abelmoschus esculentus L. moench, family Malvaceae. Okra gum, which is a natural polymer, has advantage over synthetic and semi-synthetic polymers, in that it is cheap and easily available, non-irritant, biodegradable, biocompatible, and eco-friendly. In the present investigation the physico chemical, microbial and rheological properties of Okra gum powder are evaluated. Further Okra gum was subjected to accelerated stability studies according to ICH guidelines. Physico chemical properties like particle size distribution, surface characteristics, bulk density, tapped density, compressibility, flow properties, moisture content, PH, volatile acidity, swelling and water absorption properties are carried out. DSC and Infrared spectroscopy are performed on Okra gum powder....
The objective of this study was to improve therapeutic activity of gliclazide by improving its aqueous solubility through preparation of inclusion complex between gliclazide and β-cyclodextrin. Gliclazide β-cyclodextrin solid complex was prepared with equimolar ratio of both gliclazide and β-cyclodextrin in presence or absence of water soluble polymers (PVP-K15 and HPMC) using co-evaporation, spray drying and freeze drying techniques. The prepared solid complexes were characterized by DSC, IR, XRD and dissolution testing in comparison with the pure gliclazide powder. The solid complexes prepared by spray drying, freeze drying and co-evaporation in presence of hydrophilic polymers showed a prompt drug release compared to pure gliclazide (P < 0.05). The spry dried complex in presence of PVP-K15 showed the highest drug release after 5 and 90 min and significantly increased the % dissolution efficiency (P < 0.05) compared to the pure drug. Moreover, in vivo assessment of the hypoglycemic activity of this complex in comparison with a commercial drug product was studied in diabetic rats. Statistical analysis of the pharmacodynamic parameters including maximum % reduction in blood glucose level (BGL) and area under % reduction in BGL versus time curve (AUC0-24) data obtained for gliclazide -cyclodextrin complex showed significantly (P<0.05) higher values compared to the commercial drug product. These results suggest that spry dried gliclazide -cyclodextrin complex in presence of PVP-K15 is useful for improving the hypoglycemic effect of gliclazide in diabetic rats....
For the effective treatment of various skin and soft tissue diseases, cloxacillin medicated cream were prepared. The formulations were subjected to various physicochemical studies like pH, spreadability, extrudability, drug content, in vitro drug release, and stability studies. The preparations were non-Newtonian and exhibited pseudoplastic behavior. In vitro drug release studies were carried out using a pH 6 phosphate buffer as a receptor medium. Formulations exhibited an extended release of the drug for over a period of 3 hours and the release depended on the type of base used. Stability studies showed no significant variations (P > 0.05) in pH, spreadability, extrudability, and drug content. An in vitro release study concluded that oil-in-water cream based preparation appeared to probably extend the release of cloxacillin....
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