The smedds formulation of hl235 was successfully optimized by using the doptimal mixture design. Conclusions this study demonstrates a strategy for the development of a supersaturated smedds formulation of a drug with low aqueous solubility. T1 inclusion of digestible surfactants in solid smedds formulation removes lag time and influences the formation of structured particles during digestion. Approaches to development of solid self micron emulsifying. Solubility of candesartan cilexetil was evaluated in various nonaqueous. The optimized smedds used for curcumin formulations in liquid and pellet forms contained 70% mixtures of two.
Review on self micro emulsifying drug delivery systems. Smedds formulation showed faster drug dissolution rate and higher bioavailability than tms powder. A selfmicroemulsifying drug delivery system smedds for a. Selection of oil, surfactant and cosolvent based on the solubility of. Preparation and characterization of smedds a previously developed smedds formulation showing a permeation enhancing effect via tight junction opening was employed. Formulation and evaluation of solid self microemulsifying drug delivery system a thesis submitted to gujarat technological university for the award of doctor of philosophy in pharmacy pharmaceutics by miss jill bhadreshkumar shukla 119997290015 under supervision of dr. The objectives of this study were to develop smedds formulation containing bortezomib. Download highres image 3kb download fullsize image. Development and oral bioavailability assessment of a. Smedds was placed in dialysis bag during release period to compare the release pattern with conventional tablet. Bortezomib smedds filled in hard gelatin capsules was placed at room temperature for 24 h.
Solubility of the drug in different oil, surfactants and co solvents. Sep 24, 2012 the dissolution studies were conducted for 1 hr to observe the variation or occurrence of precipitation over a time. The dissolution of the drug was enhanced significantly from the smedds formulation as compared to pure drug. In vivo evaluation of an oral selfmicroemulsifying drug. Formulation design of selfmicroemulsifying drug delivery. Dec 15, 2009 sparingly, watersoluble drugs such as candesartan cilexetil offer challenges in developing a drug product with adequate bioavailability. Comparative in vivo antimalarial performance of the developed smedds was evaluated against the larither in swiss male mice infected with lethal anka strain of plasmodium berghei. Smedds were characterized with respect to mean globule size and in vitro drug release pro. Formulation design of selfmicroemulsifying drug delivery systems for improved oral bioavailability of celecoxib. Patel institute of pharmaceutical education and research, shirpur, dist.
In the preliminary study with both oils, capryol 90based smedds formulation showed a larger area of selfmicroemulsifying region than that of capmul mcmbased smedds formulation. Pdf formulation and evaluation of self microemulsifying. Development of dual drug loaded solid self microemulsifying drug. Evaluation of carbamazepine cbz supersaturatable self. It employs the familiar ouzo effect displayed by anethole in many aniseflavored liquors. The ssmedds formulations can result in enhanced oral absorption as compared with the related selfemulsifying drug delivery systems smedds formulation. Smedds formulation was diluted with purified distilled water and was centrifuged at rpm for 15 min at 0. Solid selfmicroemulsifying formulation for candesartan cilexetil. Preparation of smedds formulation by dissolving the drug in mixture of oil. The optimized liquid smedds formulation was converted into free flowing powder by adsorbing onto a solid carrier for encapsulation. Qbd based fmea aided in assessment and control of risk in solid smedds development.
The oral bio availabilities of tacrolimus is poor and exhibits high intra and intersubject variability 489%, average 25% in the liver and the kidney transplant recipients and in patients with renal impairment. Pharmaceutics free fulltext formulation development of. Our results suggest that response surface methodology using bbd and desirability function is a promising approach to understand the effect of smedds variables and to optimize the formulation. The aim of the study was to develop selfmicroemulsifying drug delivery system smedds of a poorly water soluble drug, pioglitazone.
The prepared smedds was the concentrate of drug, oil, surfactant, cosurfactant. The supersaturatable selfmicroemulsifying drug delivery system ssmedds represents a new thermodynamically stable formulation approach wherein it is. Jan 23, 2017 solid selfmicroemulsifying drug delivery systems smedds have received considerable attention in recent times attempting to overcome the drawbacks of liquid smedds. Earlier literature reports on solid smedds have focussed on formulation development. The formulation was evaluated for various tests like solubility, drug surfactant compatibility. Development of selfmicroemulsifying drug delivery system and. Formulation development, characterization, and applications. Spraguedawley rats were fasted for 12 h prior to sacrifice. Formulation and evaluation of a selfmicroemulsifying drug delivery. Inclusion of digestible surfactants in solid smedds. Oct 14, 2012 the selfmicroemulsification properties, droplet size, and zeta potential of these formulations were studied upon dilution with water. The optimized smedds formulation significantly enhanced the oral bioavailability of hl235 in a pharmacokinetic study in rats. Selfmicro emulsifying drug delivery system smedds sagar kishor savale department of pharmaceutics, north maharashtra university, college of r. Selection of the oil component is a crucial step for smedds formulation because it acts as a main excipient for solubilizing the hydrophobic drug molecules.
Therefore, our study put emphasis on the enhancement of oral absorption of bortezomib by formulation of smedds of the drug. The precipitated pellet was freezedried at 30 c and 0. Labrasol was chosen as the vehicle for the smedds considering its. Smedds was higher than those obtained with the commercial suspension by 56% and 52%, respectively.
Lauroglycol fcc as an oil, 60% cremophor rh, and 30% peg polyethylene glycol 400 as a. Formulation and development of microemulsion and smedds akshay r. Optimization of selfmicroemulsifying drug delivery system. The permeability behavior of ibuprofen over three different concentrations 20, 30, and 40. Thus the study confirmed that the smedds formulation can be used as a possible. The present study demonstrated the suitability of mixture design to optimize the compositions for smedds. Approaches to development of solid self micron emulsifying drug delivery system. Pharmaceutical nanotechnology development of smedds using. Formulation and characterisation of selfmicroemulsifying. The in vitro dissolution studies indicate that formulation of olm in the form of smedds formulation enhances the dissolution properties. Development and evaluation of selfmicroemulsifying liquid and. The emulsion was developed using sesame and soybean oils along with surfactantcosurfactants, and the tablets were prepared by wet granulation using.
That is, by an intrinsic property of the drug formulation, rather than by special mixing and handling. Formulation and evaluation of solid selfmicroemulsifying drug delivery system of chlorthalidone by spray drying technology. The relative bioavailability of the smedds formulation to the conventional capsule was 2%. In another study done on rats, the oral bioavailability of the antiinflammatory drug ontazolast was substantially improved when this lipophilic drug was administered in a lipid based formulation, such as. It was washed with water for 1 s twice, and the excess was removed with a filter paper. Formulation and evaluation of self microemulsifying drug delivery system of carbamazepine. The objective of the present study was to develop and characterize selfmicroemulsifying drug delivery system smedds of candesartan cilexetil for filling into hard gelatin capsules. They optimized smedds formulation for telmisartan using boxbehnken design. Feb 06, 2015 the smedds formulation for ajs, a novel medicative compound against depression that is one of the bcs class ii drugs, was prepared successfully, and its microemulsion droplets were less than 30 nm with a narrow size distribution. Nov 05, 2017 for the love of physics walter lewin may 16, 2011 duration. Thus, the formulation of smedds optimized by doptimal mixture design could be a promising approach to improve the oral bioavailability of hl235. The supersaturatable selfmicroemulsifying drug delivery system s smedds represents a new thermodynamically stable formulation approach wherein it is designed to contain a reduced amount of surfactant and a watersoluble polymer precipitation inhibitor or supersaturated promoter to prevent precipitation of the drug by generating and. Selfmicroemulsifying drug delivery system wikipedia.
Composition of smedds formulation typically, a smedds formulation comprises of drug, oil, surfactant and cosurfactant drug lipophilicity and dose of the drug are the main criteria to be considered before development of smedds formulation. Download pdf 175k download meta ris compatible with endnote, reference manager, procite, refworks. Download highres image 3kb download full size image. The area under the curve auc 024h and the peak plasma concentration c max of abz. The efficiency of oral absorption of the drug compound from the smedds depends on many formulation. The optimized liquid smedds formulation contained 10%. Considerations in formulation of a smedds the solubility of the drug in different oils, surfactants and cosolvents. Jan, 2014 contents of the powerpoint on self emulsifying drug delivery systems sedds include. Introduction definition and advantages formulation of sedds preparation of sedds mechanism of self emulsification in vitro evaluation of sedds improvement of oral absorption by sedds applications of sedds solid sedds recent approaches in sedds conclusion references download the powerpoint by liking us on. Download pdf 1886k download meta ris compatible with endnote, reference manager, procite, refworks bib tex compatible with bibdesk, latex text. Albendazole is an anthelmintic agent with poor solubility and absorption. Formulation and development of microemulsion and smedds. Pdf a selfmicroemulsifying drug delivery system smedds has been developed to enhance diffusion rate and oral bioavailability of flurbiprofen. Preparation and characterization of selfmicroemulsifying.
Formulation and evaluation of solid selfmicroemulsifying. The stability of the formulation was assessed by analyzing concentration of bortezomib with the hplc method. Approximately 40% of new drug candidates have poor water solubility and the oral delivery of such drugs is frequently associated with implications of low bioavailability, high intra and intersubject variability and lack of dose proportionality. Thus, statistical experimental design is a useful tool to optimize smedds formulation.
A selfmicroemulsifying drug delivery system smedds is a drug delivery system that uses a microemulsion achieved by chemical rather than mechanical means. Formulation and evaluation of a selfmicroemulsifying drug. Ibuprofen loaded smedds ismedds was developed and was characterized. The study was aimed at developing a selfmicroemulsifying drug delivery system smedds of ibuprofen for investigating its intestinal transport behavior using the singlepass intestinal perfusion spip method in rat. Self microemulsifying drug delivery system of tacrolimus. Formulation of selfmicroemulsifying drug delivery system. Sep 14, 2015 self micro emulsifying drug delivery system smedds 1. Studies on preparation of carbamazepine cbz supersaturatable selfmicroemulsifying s smedds formulation and relative bioavailability in beagle dogs. Similarly the drug exhibited enhanced absorption from the smedds formulation through rat intestinal segment compared to its suspension. Ideally, drug should have low dose, log p 2 and should not possess extensive first pass metabolism. Ex vivo stability of the formulation was also evaluated. In vitro release profiles of smedds of gly, pure gly powder, and marketed gly formulation euglucon tablets, nicholspiramal india, mumbai, india were studied using united states pharmacopeia usp xxiii apparatus i at 37 0. May 15, 2017 download fulltext pdf download fulltext pdf. We developed a chewable tablet 200 mg drug equivalent, containing a selfmicroemulsifying drug delivery system smedds, with oral disintegrating properties.
Design and development of solid self micro emulsifying drug. Girish k jani principal, ssr college of pharmacy silvassa. The selection of oil, surfactant and cosolvent based on solubility of drug and preparation of phase diagram. Smedds of telmisartan are also studied by bhagwat and dsouza 2012. The sample was subsequently stained with uranyl acetate solution for 10 s. Tacrolimus has poor solubility in water ranging from 4 to 12.
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