Current Issue : April - June Volume : 2013 Issue Number : 2 Articles : 10 Articles
The vagina remains to be an unexplored route of drug delivery. As a site of drug delivery it offers certain unique features which made vagina an excellent route of drug delivery for both local and systemic effect. Gels are semi-solid systems form a three-dimensional, polymeric matrix in which a high degree of physical/chemical reticulation has been comprised. Gels can present several advantages over other vaginal drug delivery systems such as higher bioavailability, safety, versatility, and economical savings. They are mainly used for topical delivery of contraceptives, anti bacterial, antifungal, antiprotozoal, antiviral, labor-inducing and spermicidal agents, prostaglandins, steroids and also used as an “empty” gel for moisturizing of dry vaginal mucosa. vaginal gels possess a higher biocompatibility and bioadhesivity and can be rapidly eliminated through normal catabolic pathways which decreases the risk for irritative or allergic host reaction at the application site. Mucoadhesive polymer is being used to improve performance of gel and it will be retained at the site and release the drug in a controlled and prolonged manner, so that the drug can be continuously supplied to the absorption sites and reduces dosing frequency. Here, discussed and summarized use and research being done on gel as vaginal drug delivery....
The aim of present investigation was to compare the ionotropic gelation techniques for entrapping Aceclofenac in mucoadhesive microparticulate system. Aceclofenac microcapsules with a coat consisting of alginate and a mucoadhesive polymer sodium carboxymethylcellulose, methyl cellulose, carbopol and hydroxypropylmethylcellulose were prepared by two methods namely orifice-ionic gelation process and emulsification ionic gelation process. The resulting microcapsules were discrete, large, spherical and free flowing. Microencapsulation efficiency was in the range of 88.56-99.2% in case of Orifice ionic gelation method and 93.52-99.03% in case of emulsification method. The microcapsules exhibited good mucoadhesive property in the in vitro wash-off test. Aceclofenac release from these mucoadhesive microcapsules was slow and extended over longer periods of time depending on the composition of coat of the microcapsules. Drug release follows first order kinetics and non-Fickian type of diffusion. With all the mucoadhesive polymers, microcapsules prepared by Orifice method gave more slow release of the contained drug when compared to those prepared by Emulsification method. Alginate-sodium CMC and alginate-methyl cellulose microcapsules of Aceclofenac prepared by Orifice method sustained the drug release over a period of 20-24 h. These mucoadhesive microcapsules are thus, suitable for oral controlled release of Aceclofenac....
Colchicine is used in the therapy of gout, but recent studies indicate that colchicine may have therapeutic effect in the treatment of Alopecia Areata, a common, non-scarring reversible disorder of hair loss. In the present study a topical delivery system in the form of film was developed to minimize the undesired side effects of systemic colchicine. The components used in the formulations, such as polymers and plasticizers were screened and their concentrations were optimized in order to obtain a film with in vitro release rate suitable for sustained drug release and with optimal physical properties such as short drying time, low outward stickiness, high cosmetic attractiveness, high folding endurance, low moisture content, low moisture uptake and suitable swelling index. Further optimization was made to select a film formula which exhibited good flow properties required for spraying and was non-irritant to the skin. The optimized film formula was employed to conduct clinical studies using patients suffering from Alopecia Areata. The results showed that the polymeric film composed of Eudragits, RSPO+RL100 (4:1) exhibited higher therapeutic efficacy of colchicine in the majority of the patients vis-à-vis the ethanol solution of the drug and the placebo. In conclusion the selected film provided more effective carrier for colchicine than the solution, exhibited a controlled drug release, improved the cosmetic attractiveness and led to better patient compliance. The selected film formulation developed in this study can represent a novel topical delivery of the drug for treatment of Alopecia Areata...
The main objective of the present investigation was to formulate and evaluate the pulsatile drug delivery system for anti-diabetic drug miglitol to control the increased blood glucose level after food consumption in diabetic patient by allowing the drug to release immediately after meals. Press coated tablets of miglitol were prepared by compression coating immediate release miglitol core tablets with hydrophilic and hydrophobic polymer in different ratios. The ideal concentration of hydrophilic and hydrophobic polymers were selected based on the invitro drug release profile and desired lag time of 4 hrs. The Invitro release studies were carried out for the formulated miglitol press coated tablets using different buffer solutions such as pH 1.2,7.4 and 6.8.The invitro drug release profile of miglitol press coated tablets containing 25mg of glyceryl behenate and 175 mg of L-HPC exhibited a time period of 4 hrs without drug release (lag time) followed by a rapid release of drug. Hence the developed formulation was found to be suitable for the diabetic patient to manage the blood glucose levels which are high after food consumption....
Cefexime is a drug of choice in the treatment of susceptible infections including gonorrhoea, otitis media, pharyngitis, bronchitis and urinary tract infections. The present work was carried out to improve the solubility, dissolution rate, oral bioavailability, stability and palatability of the drug Cefixime by forming it as a reconstitutable oral suspension especially for pediatric use. The poorly soluble drug, Cefixime is formulated as reconstitutable suspension using xanthan gum, olibanum gum, karaya gum, HPMC E5, compound tragacanth powder (CTP) as suspending agents employing various techniques like physical mixing, solvent evaporation and co-grinding. The reconstitutable suspensions were evaluated for flow properties, particle size, pH, viscosity, sedimentation volume, redispersibility and drug release by in vitro dissolution studies. The drug excipients interaction and crystal morphology of optimized reconstitutable suspensions were evaluated by Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD) studies, respectively. The results indicated that the release of the cefixime was rapid from all formulations than the pure drug. The drug release from the suspensions followed first order kinetics. Among all formulations the formulation prepared by kneading method released the drug rapidly than the pure drug and other formulations....
The aim of the present investigation is to develop a time and pH-dependent system for colon specific drug delivery of Tizanidine Hydrochloride. The colon specific drug delivery system (CDDS) is designed such that the innermost part consists of a core tablet of Tizanidine Hydrochloride which is then compressed with hydrophobic polymer (Sodium starch glycolate and microcrystalline cellulose). This is then coated with a pH-dependent methacrylic acid copolymer (Eudragit�® S100 and Eudragit�® L100). The concentration (coating level) of Eudragit�® S100 and Eudragit�® L100 was optimized to provide an enteric coat that allows the tablet to pass intact through the stomach and is targeted to the colon. The coating thicknesses were optimized to set a desired lag time in the intestine. From the in vitro evaluation it can revealed that the developed CDDS can exhibit site-specific drug targeting to the colon....
According to the Biopharmaceutical Classification System (BCS), Etodolac belongs to class II drugs; that is, characterized by low solubility and high permeability therefore, the enhancement of its solubility and dissolution profile is expected to significantly improve its bioavailability and reduce its side effects. Aiming at achieving this goal, five water soluble polymers were assessed as solid dispersion (SD) carriers to enhance the solubility and dissolution profile of Etodolac, each in three ratios. PEG 4000 and 6000 were used to produce 2nd generation solid dispersions, while carriers possessing surface activity or self-emulsifying properties such as Pluronic F-127 and Gelucire 44/14 or 50/13 were used for production of 3rd generation SDs. Saturate solubility studies revealed higher Etodolac solubility in alkaline rather than acidic environments due to its acidic nature, also, amphiphilic polymers (Gelucires and Pluronic F127) showed higher solubility of Etodolac in both media. XRD and DSC studies revealed that the enhanced dissolution might be due to either amorphization of the drug or due to the increased surface area of the drug crystallites after formation of the solid dispersions leading to better wettability and higher dissolution. Etodolac dissolution profiles showed two distinct phases of drug dissolution. SDs exhibited faster dissolution rates than the intact drug and the corresponding PMs, and, increasing the ratio of the solubilzing carrier to drug, resulted in corresponding enhancement in the drug dissolution rate. Accordingly, solid dispersion technique can be assertively considered as a promising procedure for preparing Etodolac in an enhanced solubility and dissolution form....
Glibenclamide (GBM) is an oral hypoglycemic agent belonging to the second generation of sulfonylurea’s commonly employed in the treatment of type II non insulin-dependent diabetes. Its hypoglycemic effect is mainly due to stimulation of insulin release from pancreatic beta cells and sensitization of the peripheral tissues to insulin. GBM is highly lipophilic and minimally soluble in aqueous media. Guar gum has gained immense importance because of its constructive role of releasing sugars and absorbing sugars slowly in the intestinal tract; consequently, reduce the severity of diabetes mellitus and also act as a prospective hydrophilic matrix carrier for oral controlled delivery of drugs. In this study, an approach to possible physical interaction between Glibenclamide and guar gum is presented. For the investigative purpose; molecular level property, particulate level property and thermal methods of analysis have been assessed. Results of FTIR, PXRD, DSC and TGA studies indicated that Guar gum had compatibility with Glibenclamide....
Mefenamic acid is a potent prostaglandin synthetase inhibitor that is used widely as a non-steriodal anti-inflammatory and analgesic-antipyretic drug. It is used in the mild to moderate pain including headache, dental pain, postoperative and postpartum pain, dysmenorrheal, osteoarthritis. However, its oral bioavailability is very low, probably due to poor solubility in water and insufficient dissolution rate. The purpose of the current study is to improve the solubility and dissolution rate of the poorly soluble drug, Mefenamic acid by solid dispersions using hydrophilic carriers like PEG (poly ethylene glycol) and PVP (Polyvinylpyrrolidine) by different methods of preparation of solid dispersions....
The problem of bitter and obnoxious taste of drug in pediatric and geriatric formulations is a challenge to the pharmaceutical industry in the present scenario. In order to ensure patient compliance bitterness masking becomes fundamental. Masking of bitter or objectionable taste of such formulations is highly desirable since it provides commercial gains to pharmaceutical industries due to higher market demand of products, patent protection to novel taste masked formulations and also in some cases extended marketing exclusivity rights. The main objective of present review is to explore different method, technologies and evaluations to mask the obnoxious taste of drugs, so that patients can use these drugs without hesitation of taste....
Loading....