Current Issue : April - June Volume : 2017 Issue Number : 2 Articles : 5 Articles
The objective of present work was to develop microencapsulated chitosan microspheres for colon specific drug\ndelivery of capecitabine. As reported initially, in-vitro drug release studies showed more drug release through chitosan\nmicrospheres demanded microencapsulation. The system consists of developed chitosan microsphere entrapped within\neudragit FS30D polymer which combines pH dependent solubility of eudragit FS30D polymer and specific biodegradability of\nchitosan microspheres. The microencapsulation was done for optimized formulation CMF9 with eudragit FS 30D by solvent\nevaporation technique at different ratio. The obtained formulations were characterized for particle size, entrapment efficiency\nand surface morphology. The size of eudragit encapsulated microspheres was between 125 and 164 �¼m and the entrapment\nefficiency of microencapsulated formulations varied between 88 to 94% with increasing core-coat ratio. The SEM study showed\nthat microencapsulated chitosan microspheres exhibited smooth surface and spherical shape. In-vitro drug release behavior was\nstudied in different pH medium and the obtained data were subjected to kinetic equations. Less drug release was observed from\nencapsulated microspheres when the medium pH below 7, which is 5 to 10 % after 2 hrs and 12 to 20% after 5 hrs, while when\nthe pH reached 7.4, the coating layer of eudragit began to dissolve and a controlled release of capecitabine was observed. In\nconclusion, this work presents new approach as well as a new system with a great potential for colonic drug delivery....
The present study involves the formulation and evaluation of buccal films of ondansetron HCl using HPMC K15M, eudragit RL-100 and chitosan in various proportions and combination. The films were fabricated by solvent casting method using. Ondansetron hydrochloride, an antiemetic drug has oral bioavailability of 60% due to hepatic first metabolism and a short half-life of 5 hrs. Buccal route is an excellent alternative method for the systemic delivery that can improve the bioavailability. A significant reduction in dose and dosing frequency can be achieved with prolonged duration of action, thereby improving the patient compliances. The formulations F1-F11 were evaluated for physicochemical parameter like weight variation, thickness, folding endurance, drug content uniformity, swelling index, surface pH and mucoadhesion time in addition to in-vitro drug release and in-vitro permeation studies. All the formulations sustained the release upto 12 hrs with F2 exhibiting best release pattern. The investigation concluded that F2 containing Eudragit RL-100 and HPMC K15M was best formulation which follows the zero order kinetic with R2 value 0.970. Treatment via buccal route offer many advantages in comparison to traditional treatments and can be proposed as a new therapeutic tool....
This research work was an attempt to increase the solubility dissolution rate of rifampicin by solid dispersion as the poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T. fluid often leads to insufficient bioavailability, this low bioavailability leads to less therapeutic effect of particular drug. Rifampicin belongs to BCS class II, which is slightly soluble in water. The carrier or hydrotropic agent used here for preparation of solid dispersion is urea. The hydrotrophy method or solvent evaporation method is very economic, easy and less time consuming and also less harmful as distilled water is used for preparation of solid dispersion. Evaluation of prepared solid dispersion reveals that solubility profile of rifampicin has increased to some extent and hence, bioavailability also increased....
Despite the rapid development of medical technologies, chemotherapy treatment still\noccupies an important place in clinical oncology. In this regard, the current research in this area\nfocuses on the synthesis of new highly effective antitumor substances that have minimal side effects\nand the development of stable pharmaceutical formulations (PF) on their basis. In order to solve this\nproblem, the I. Ya. Postovsky Institute of Organic Synthesis of the Ural Branch of the Russian Academy\nof Sciences actively sought for original substances, namely, nitrosourea (NU) derivatives, one of the\nmost promising classes of anticancer drugs. As a result of this research, a novel NU derivative was\nsynthesized, namely ormustine, which showed high antitumor activity in preliminary preclinical\ntrials. It is now crucial to develop an ormustine pharmaceutical formulation. Conducted technological\nstudies showed that the most suitable solvent for the drug substance is 0.1Mhydrochloric acid, which\nensures its rapid dissolution by ultrasonic treatment. A significant reduction in the concentration\nof the active ingredient during the storage of the solution required the development of a technique\nof its lyophilization and the selection of a shaper such as a Kollidon 17 PF. Upon completion of the\ndevelopment of a pharmaceutical formulation of ormustine, its stability after lyophilization was\ndemonstrated, and a sufficient amount of the drug has been acquired for preclinical research....
The aim of this project was to examine the effect of microneedle rollers on the percutaneous\npenetration of tiagabine hydrochloride and carbamazepine across porcine skin in vitro. Liquid\nchromatography-mass spectrometric analysis was carried out using an Agilent 1200 Series HPLC\nsystem coupled to an Agilent G1969A TOF-MS system. Transdermal flux values of the drugs\nwere determined from the steady-state portion of the cumulative amount versus time curves.\nFollowing twelve hours of microneedle roller application, there was a 6.74-fold increase in the\npercutaneous penetration of tiagabine hydrochloride (86.42 �± 25.66 �¼g/cm2/h) compared to passive\ndelivery (12.83 �± 6.30 �¼g/cm2/h). For carbamazepine in 20% ethanol, passive transdermal flux of\n7.85 �± 0.60 �¼g/cm2/h was observed compared to 10.85 �± 0.11 �¼g/cm2/h after microneedle treatment.\nCarbamazepine reconstituted in 30% ethanol resulted in only a 1.19-fold increase in drug permeation\nacross porcine skin (36.73 �± 1.83 �¼g/cm2/h versus 30.74 �± 1.32 �¼g/cm2/h). Differences in flux values\nof untreated and microneedle-treated porcine skin using solid microneedles for the transdermal\ndelivery of tiagabine were statistically significant. Although there were 1.38- and 1.19-fold increases\nin transdermal flux values of carbamazepine when applied as 20% and 30% ethanol solutions across\nmicroneedle-treated porcine skin, respectively, the increases were not statistically significant....
Loading....