From the drug release studies, it can be clearly seen. Formulation design and evaluation of self micro emulsifying. Preparation and in vitroin vivo evaluation of puerarin. The dissolution characteristics of solid smedds and commercial formulation librium were indicated statistically significant drug release in. Selfmicroemulsifying drug delivery system wikipedia. Martin, popularly known as uncle bob these principles, when combined together, make it easy for a programmer to develop software. In this formulation emulsifying ingredients are incorporated into powder to make solid dosage form such as tablets. Formulation and evaluation of selfemulsifying drug. The phase diagram was constructed by using chemix software.
Formulation and evaluation of solid self micro emulsifying drug. Pdf formulation and evaluation of selfemulsifying drug. Zeta potential value of pitavastatin smedds showed a negative surface charge 23. The present investigations was aimed to improve the solubility, dissolution rate and ultimately the.
Ternaryphase diagram was plotted using chemix school 3. Liquidfilled hard shell capsules consist of a pair of hard gelatin capsule halves that are joined together after filling with a dose of liquid of semisolid fill formulation. Results the optimized liquid smedds formulation contained 10% lauroglycol fcc as an oil, 60% cremophor rh, and 30% peg polyethylene glycol 400 as a surfactant and cosurfactant. Smedds showed excellent oil adsorption capacity, low bulk density and good flow properties. 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. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of dissolution rate limited absorption. Development of selfmicroemulsifying drug delivery system and. Preparation and in vitroin vivo evaluation of puerarin solid. It is not related to the grasp software design principles. Formulation and invitro evaluation of liquid and solid self. Solid formulation of a supersaturable selfmicroemulsifying drug delivery system for valsartan with improved dissolution and bioavailability dong woo yeom, 1, bo ram chae. The mean droplet size of the homogeneous microemulsion was 37. Selfmicroemulsifying drug delivery system smedds for. Formulation and evaluation of selfemulsifying drug delivery system for nimodipine, a bcs class ii drug.
Solid smedds containing aerosil 300 showed good flow properties and uniform drug content. Design and development of solid self emulsifying osmotic delivery system of nifedipine. A number of lipid carriers are currently available, including solid lipid nanoparticles sln 8, selfmicroemulsifying drug delivery systems smedds 9, nanostructured lipid carriers nlc. The crystalline state of the formulation was altered according to the xrpd analysis. The oral bioavailability of carbamazepine from smeds is higher than the release of carbamazepine from conventional tablet. Formulation and characterization of pioglitazone hcl self emulsifying drug delivery system darna bhikshapathi1. In addition, the solid smedds formulation was in a more stable state than liquid smedds in ph 1. Up to 70% of nces in current pipelines suffer from poor aqueous solubility bcs class ii as depicted in figure 1. Optimized formulation of solid selfmicroemulsifying. Salvia extract figure 5a appeared as irregular shape particles. Formulation and evaluation of solid self micro emulsifying drug delivery system. That is, by an intrinsic property of the drug formulation, rather than by special mixing and handling.
Development and optimization of piroxicamloaded solid. Nov 07, 2017 in the ssusmedds formulation, compression force was shown to have little influence on disintegration performance and drug dissolution. The formulation strategy included selection of oil phase based on saturated solubility studies and surfactant and cosurfactant screening. Shah college of pharmaceutical education and research, modasa, 2 kalol institute of pharmacy, kalol, india. The solid selfmicroemulsifying drug delivery system ssmedds of tacrolimus was prepared as follows. Design and evaluation of a selfemulsifying drug delivery. First, sirolimus was dissolved in appropriate amounts of a mixture of oil and cosolvent. Patel2 1 departments ofpharmaceutics, malibacollege pharmacy, veer narmad southgujaratuniversity, surat 394350, india, 2 department. Formulation design of selfmicroemulsifying drug delivery.
However, smedds is a liquid formulation and has several limitations including low stability and portability during the manufacturing process and interaction of filling the capsule shell 24. D is an acronym for the first five objectoriented designood principles by robert c. Ex vivo stability of the formulation was also evaluated. Smedds is dependent upon the particular physicochemical compatibility of the drugsystem 11. The solubilisation capacity for was to investigate smedds for piroxicam. Mar 30, 2016 the optimized smedds formulation was transferred on to the inert adsorbent i. Thus it can be inferred that the prepared solid smedds with the porous carrier have the ability to be processed into solid dosage form.
Various techniques are known for converting lsmedds to ssmed, which include a adsorption onto solid carriers, b melt granulation melt extrusionextrusion spheronization and c spray drying. The porosity of solid carriers may be mostly negated due to absorption of the liquid formulation, leading to the diminished effect of compression force. The optimized smedds formulation was transferred on to the inert adsorbent i. The stability of the formulation was assessed by analyzing concentration of bortezomib with the. Formulation and invitro evaluation of liquid and solid. Drug solubility in the lipid adjuvants is an important parameter in the lsmedds development, so carv solubility in pure transcutol and in a 3. To address these limitations, more approaches were committed, such as adsorbing, lyophilization, and spray drying, which can combine the advantages. Preparation and pharmacokinetics evaluation of oral self. In the present study, a stable smedds formulation for different drugs in smedds is different due to various intermolecular forces between drug and smedds components12. Thermodynamically stable liquid smedd was converted to solid smedds to get the advantage of the solid dosage form. Ease of administration and painless approach made oral route the most preferred. Preparation of a solid selfmicroemulsifying drug delivery. Pdf design and optimization of chlordiazepoxide solid self.
Agilent technologies, usa consisting of the chem station software. Incorporation of a liquid selfemulsifying formulation into a solid dosage form may combine the advantages of sedds with those of a solid dosage form and overcome the disadvantages of liquid formulations described above 20. Swadeep 1, ranjit prasad swain 1 1maharajahs college of pharmacy, vizianagaram535002, andhra pradesh, india 2royal college of pharmacy and health sciences, berhampur760002. Albendazole is an anthelmintic agent with poor solubility and absorption. Smedds are mostly prepared in liquid dosage form in soft and hard gelatine capsules which have some manufacturing and leakage problems. Development and evaluation of liquid and solid self. An update from formulation development to therapeutic strategies anjan kumar mahapatra 1, p. Pharmaceutics free fulltext formulation development of. Preparation of a solid selfmicroemulsifying drug delivery system by. Nov 05, 2017 for the love of physics walter lewin may 16, 2011 duration.
The present work aimed at formulating a solid self micro emulsifying drug delivery system solidsmedds for olmesartan medoxomil with the objective of improving the. Approaches to development of solid self micron emulsifying drug delivery system. The solid smedds was formulated by spray drying liquid smedds with the solid carrier calcium silicate. It employs the familiar ouzo effect displayed by anethole in many aniseflavored liquors. Preparation and in vivo evaluation of a dutasterideloaded. However, lipid formulation may interact with the capsule, resulting in either brittleness or softness of the shell. Particle size analyzer, scanning electron microscopy sem, differential scanning calorimetry dsc, powder xray diffraction pxrd, and fourier transform infrared ftir spectroscopy experiments characterized the physiochemical properties of the mtxloaded solid smedds.
Pdf formulation and evaluation of solid self micro emulsifying. Phase diagram was constructed using chemix software version 3. The solid smedds formulation was prepared by dissolving 1 mg sirolimus in a 100 mg mixture of oil, cosolvent, and surfactant. The smedds formulation showed complete release in 15 min.
Health, general carbonates citric acid lactose nifedipine phthalates silica silicon dioxide sodium bicarbonate. For the love of physics walter lewin may 16, 2011 duration. The ssmedds formulation was reconstituted 250 times with distilled water under gentle stirring and the globule size, size distribution and zeta potential were analysed by zeta sizer nano. The emulsion was developed using sesame and soybean oils along with surfactantcosurfactants, and the tablets were prepared by wet granulation using. The optimized liquid and solid smedds showed higher drug release than the marketed capsule and pure api active pharmaceutical ingredient powder. The principles are a subset of many principles promoted by american software. Solidstate microemulsion preconcentrate for the delivery of cyclosporine is prepared by. Vpa smedds successfully withstood the stability testing. The principles are a subset of many principles promoted by american software engineer and instructor robert c. The solid smedds was formulated by spray drying liquid smedds with. Morphological analysis of solid smedds sem the outer macroscopic structure of the solid smedds was investigated by s4100 scanning electron microscope. Smedds l smedds are encapsulated either in hard or in soft gelatin capsules. The mixture was agitated until a uniform, freeflowing powder was obtained.
Preparation of lx solid smedds ssmedds formulations the lx ssmedds was prepared by a lyophilization. A selfmicroemulsifying drug delivery system smedds is a drug delivery system that uses a microemulsion achieved by chemical rather than mechanical means. The rate and extent of drug dissolution from solid smedds was significantly higher than pure drug and commercial tablet formulation. Design and development of solid self emulsifying osmotic. A series of lx lsmedds were prepared in the formulation with varying concentrations of labrafil m 1944cs and labrafac lipophile wl 49 1030% ww, and the k. Solid selfmicroemulsifying formulation for candesartan. We developed a chewable tablet 200 mg drug equivalent, containing a selfmicroemulsifying drug delivery system smedds, with oral disintegrating properties. The optimized formulation of both liquid and solid smedds showed maximum 80% release. The optimized liquid smedds formulation c7iib was converted into free flowing powder by adsorption of liquid onto solid carriers that provided a high surface area with good disintegration characteristic the soild carriers used includes aerosil 200 pharma a1, aeropearl 300 pharma a2 and fujicalin sg f1. In objectoriented computer programming, solid is a mnemonic acronym for five design principles intended to make software designs more understandable, flexible and maintainable. The results of the pharmacokinetic study indicate that the smedds formulation shows significantly greater bioavailability than the raw sirolimus powder or commercial product rapamune oral solution. The solid smedds are new approach to overcome above mention problems.
Though they apply to any objectoriented design, the solid principles can also form a core philosophy for methodologies such as agile development or adaptive software development. From figure 3b,c, in the soybean oil or sesame oilpeg400 or cremophor rh40tween80 system, we observed that the liquid smedds formulation of 20% of soybean oil or sesame oil, 30%. Formulation and evaluation of a selfmicroemulsifying drug. Bakhle, jasmine g avari department of pharmaceutical sciences, division of pharmaceutics, r. Solid selfmicroemulsifying drug delivery system of lovastatin suparna s. The solid smedds exhibited good flow characteristics with carrs index value as 12. Various types of solid carriers have been extensively investigated to solidify smedds, including silicabased waterinsoluble adsorbents e.
Formulation and characterization of pioglitazone hcl self. The s smedds formulation was reconstituted 250 times with distilled water under gentle stirring and the globule size, size distribution and zeta potential were analysed by zeta sizer nano. Smedds is system with droplet size ranging from 20 200 nm10,11. Approaches to development of solid self micron emulsifying. Phase diagrams were constructed using chemix school software, version 3. Smedds was optimized using simplex lattice mixture design. Pharmaceutical product formulation development freethink. Development and optimization of piroxicamloaded solid self. A serious of smedds formulation with the 20mg drug, oil. The formulation containing telmisartan 20 mg, castor oil 30% ww, tween 20 55% ww, propylene glycol 15% ww was concluded to be optimized.
The scanning electron micrographs of salvia extract and solid smedds formulation are shown in figure 5. Martin, popularly known as uncle bob these principles, when combined together, make it easy for a programmer to develop software that are easy to maintain and extend. Vpa loaded smedds were subjected to various conditions of storage as per ich guidelines for 3 months. For this purpose, quality by design qbd approach employing doptimal mixture design was used to prepare smedds of nfm. Similarly, this optimal solid smedds formulation composed of 75 mg silicon dioxide, 20 mg peceol, 30 mg cremophor rh60 and 50 mg transcutol hp was chosen for.
The samples were mixed thoroughly to dissolve the drug in methanol, centrifuged at 3000 rpm for 15 min using 12c microcentrifuge remi motors, mumbai, india to separate the undissolved excipients. The optimized smedds and solidsmedds exhibited 100% in vitro drug release up to 120 min, which was significantly higher p smedds is defined as isotropic mixture of natural or synthetic oils, solid or liquid surfactants and hydrophilic co solventssurfactants that have unique ability of forming fine oil in water ow micro emulsion upon mild agitation followed by dilution in aqueous media such as in gi fluid 1. Liquid and semisolid formulation technologies bioavailability. Solid formulation of a supersaturable selfmicroemulsifying. Adsorption on solid carrier is easy and reliable method to convert liquid smedds into solid smedds agarwal et al. To overcome these problems, lipid formulations could show a solid state by using suitable adsorbents. Oral drug delivery systems also being the most costeffective to manufacture, have always lead the worldwide drug delivery market. Research article formulation and evaluation of self micro emulsifying system of candesartan cilexetil jill 1,b. 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. Jan 27, 20 in addition, the solid smedds formulation was in a more stable state than liquid smedds in ph 1.
Spraguedawley rats were fasted for 12 h prior to sacrifice. Smedds have recently been described and they surmount. Development and optimization of self microemulsifying drug. Optimization of selfmicroemulsifying drug delivery system. So, preformulation solubility and phase diagram studies are required in order to obtain an. Formulation and evaluation of solid selfmicroemulsifying. The composition of optimized formulation c7iib consist of capryol 90 as oil, labrasol as surfactant and captex 500 as cosurfactant, containing 32 mg of candesartan cilexetil showing drug release for liquid smedds formulation 99. Neusilin us2, to formed a solid self emulsifying drug delivery system ssmedds. The prepared liquid formulation of eprosartan mesylate was dropwise on a solid carrier in a glass mortar.
Further, the software generated numerically optimized smedds were developed by utilizing desirability. Poor oral bioavailability is pronounced with the majority of recent active ingredients because of. Comparison of pure drug, selfmicroemulsifying drug delivery system and solidselfmicroemulsifying drug delivery system. The outer macroscopic structures of salvia extract and solid smedds formulation were examined using a scanning electron microscope s3400n, hitachi, tokyo, japan. The solid carriers used for adsorption comprised of materials that provided a high surface area with good disintegration characteristics.
Development of solid smedds formulation of poorly water soluble drugs. Request pdf formulation and evaluation of solid selfmicroemulsifying drug delivery system for azilsartan medoxomil this study aimed to develop solid selfmicroemulsifying drug delivery system. Preparation and characterization of selfmicroemulsifying. Neusilin us2, to formed a solid self emulsifying drug delivery system s smedds.
Cationic solid self micro emulsifying drug delivery system. Liquid smedds were developed, and carvedilol was used as a class ii model drug. We developed a chewable tablet 200 mg drug equivalent, containing a selfmicroemulsifying drug delivery. The in vitro dissolution studies indicate that formulation of olm in the form of smedds formulation enhances the dissolution properties. Pharmaceutics free fulltext formulation development.
At definite time intervals, samples were analyzed and found no signs of drug crystallization in ssmed formulation. The stability of the formulation was assessed by analyzing concentration of bortezomib with the hplc method. Olmesartan medoxomil olm is an angiotensin ii receptor blocker arb antihypertensive agent administered orally that has absolute bioavailability of only 26% due to. The powders were fixed to an aluminium stub using doublesided adhesive tape made electrically conductive. Failure to attain intended therapeutic effect of the poor water soluble drugs by this route led to development of novel drug delivery systems which will fulfill therapeutic needs. Selfmicroemulsifying drug delivery system smedds and solid smedds of telmisartan was aimed at overcoming the problems of poor solubility and bioavailability. Liquid smedds and solidsmedds containing olm, each equivalent to 20 mg was dispersed in suitable quantity of methanol. This study sought to prepare enteric s smedds by hme and evaluate the effects of the process and formulation variables on s smedds properties via boxbehnken design. Mean size, polydispersity index pdi and zeta potential of the resulting microemulsions were. Bortezomib smedds filled in hard gelatin capsules was placed at room temperature for 24 h. Results the optimized liquid smedds formulation contained 10% lauroglycol fcc as an oil, 60% cremophor rh, and 30% peg polyethylene glycol 400 as a surfactant and cosurfactant respectively.
The droplet size of solid smedds formulation after reconstitution with distilled water 10 times dilution was seen to be 119. The optimized liquid smedds formulation was converted into free flowing powder by adsorption of liquid smedds onto solid carriers. Formulation and characterization of pioglitazone hcl self emulsifying drug delivery system darna bhikshapathi1, posala madhukar 1, bevara dilip kumar 2 and gurram aravind kumar 1 1department of pharmaceutics, vijaya college of pharmacy, munaganoor, hyderabad 2zenon labs, 15, industrial development area, balanagar, hyderabad. But adsorption process is simple and involves addition of the liquid formulation to solid carriers by mixing in a blender 26.
Request pdf formulation and evaluation of solid selfmicroemulsifying drug delivery system for azilsartan medoxomil this study aimed to develop solid selfmicroemulsifying drug delivery. M nagpur university, maharashtra, india abstract aim. The smedds formulation was filled in hard gelatin capsules 1 size and used for drug release studies to compared with plain fur. Sep 24, 2012 the dissolution studies were conducted for 1 hr to observe the variation or occurrence of precipitation over a time. To improve the solubility and bioavailability of nfm, the self microemulsifying drug delivery system smedds was developed.
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