A solubility method was used to detect complexation and consisted of observing changes in the solubility of aspirin in the presence of varying urea concentrations at. Solubilisation is the process of preparation of thermodynamically stable isotropic solution of a substance normally insoluble or sparingly soluble in a given solvent by incorporation of an additional amphiphilic components 26. A novel, safe and sensitive method of titrimetric estimation has been developed using 2 m sodium salicylate as a hydrotropic solubilizing. Threedimensionally organized lipid cubic selfassemblies and derived oilinwater emulsions called cubosomes are attractive for various biotechnological applications due to their ability to be loaded with functional molecules and their associated sustained release properties. Some modified versions of aspirin came onto the market in an effort to achieve the benefits of aspirin. Results of analysis by proposed method and phamacopoeial method are very comparable. Patients considered to be at increased risk of a vascular event should also be advised to carry their own aspirin and, if they experience sudden severe chest pain. In the present investigation hydrotropic solubilization technique has been employed to solubilize poorly watersoluble aspirin analgesic and antipyretic drug by 0. Numerous solid dispersion systems have been demonstrated in the pharmaceutical literature to improve the dissolution properties of poorly watersoluble drugs. Aspirin acetylsalicylic acid, asa, which was initially developed as an analgesic antiinflammatory agent, has come to be the basis of antiplatelet.
This means the maximum amount of solute that the pure solvent can hold in solution, at specified environmental conditions. The solubilization of lam in pluronic micelles increased with the increase in temperature. Application of hydrotropic solubilization phenomenon in. Salicylates have been derived from the willow tree bark. Aspirin, enteric coating, extrusionspheronization, hotmelt coating, palmitic acid, stearic. Ph, solubility, ionization affecting absorption pharmatutor. Freezedrying, also known as lyophilisation, lyophilization, or cryodesiccation, is a dehydration process typically used to preserve a perishable material or make the material more convenient for transport. Aspirin, the acetyl derivative of salicylic acid, is. The solubilization of the hydrophobic antiepileptic drug lamotrigine lam in five different pluronic micelles viz. Temperaturedependent solubilization of the hydrophobic. Aspirin acetylsalicylic acid aspirin has a long past. A simple, efficient and new spectrophotometric method has been developed for spectroscopic estimation of terconazole in bulk form. Salicin is the active ingredient from willow bark of salix alba.
Accordingly, the role of caspases in aspirin induced apoptosis was also evaluated. Taking into account the prac assessment report on the psurs for acetylsalicylic acid the scientific conclusions are as follows. We next explored whether aspirin treatment would promote the osteogenic potential of swine bmsc. Aspirin stimulates the osteogenesis of bmsc in vitro and in vivo. It is the incorporation of the compound referred to as solubilisate or substrate within micellar l 1 phase or reverse micellar l 2 phase system. Although salt formation, solubilization and particle size reduction have commonly been used to increase dissolution rate and thereby oral absorption and bioavailability of low water soluble drugs 2. Research articles effect of selected surfactants, above and below the cmc, on aspirin solubility j. The goal of this experiment was to synthesize aspirin. Validating usp aspirin based on the maximum daily dose 3000 mg day are shown in table 4.
Aqueous solubility of inorganic compounds at various temperatures the solubility of over 300 common inorganic compounds in water is tabulated here as a function of temperature. Understand the various types of pharmaceutical solutions. Other methods, such as salt formation, complexation with cyclodextrins, solubilization of drugs in solvents, and particle size reduction have. In the present study, a very slightly soluble drug, terconazole has been solubilize in water using.
This aim of this experiment focuses on the synthesis of pure aspirin acetylsalicylic acid from ethanoic anhydride and salicylic acid while using concentrated sulfuric acid as a catalyst for the. Aspirin has always had excellent pain relief benefits, but it was also recognized that, it could cause digestive problems for some patients when used regularly. There are various approaches for solubilization of poorly water soluble drugs. The multielement crm standards were diluted in millipore 18. Solid dispersion technique for improving solubility of. A study of the interaction of aspirin with urea in water was initiated in an effort to obtain evidence of complex formation between these compounds and to observe possible changes in aspirin stability resulting from complexation. The solubilization study was performed for up to 5 hr in a clark. Since there are similarities between the two problems, some of the same information appears in both problem. The role of platelet and its interaction with aspirin scielo colombia. An overview article pdf available december 2012 with 3,497 reads. It is rapidly biotransformed with a serum half life of 1. Lim, x school of pharmacy, west virginia university, morgantown, wv 26506 school of pharmacy, west virginia university morgantown wv 26506 x school of pharmacy, west virginia university, morgantown, wv 26506 school of pharmacy, west virginia university morgantown wv 26506 c.
Representative classes of surfactants in aqueous solutions, above and below the cmc, were studied for their solubilizing effects on suspensions of aspirin usp crystals. Solubility is defined as the concentration of the compound in a solution that is in equilibrium with a solid phase at the specified temperature. Aspirin induced gg1 cell cycle arrest in hct116 cells. Predisposing factors factors predisposing to attacks include a personal and family history of atopy and aspirin and food ingestion.
All blanks and standards were matrix matched to the samples in 10%hno 3 and 10%hcl. For patients who have undergone revascularization procedures including cabg, ptca, or carotid endarterectomy when there is a preexisting condition for which aspirin is already indicated. The types of exercise preceding the attacks ranged from mild tennis warmups to strenuous exercise, including dancing, sprinting in track events, jogging or running, and playing basketball or soccer or tennis. Development and validation of a dissolution test for 6 mg. Values for ka, and so reported for a p cular drug in the literature are in distilled water.
Salicylic acid 1838 was used for pain relief and fever but its acidity was a major problem. Design of aspirin formulation for rapid pain relief. Hydrotropic solubilization technique is used to increase aqueous solubilities of poorly water soluble drugs using hydrotropic agents. Design and characterization of enteric coated pellets of. Effect of selected surfactants, above and below the cmc. Here, we employed both of these lipidbased systems for the delivery of a model drug, aspirin, under comparable. The role of nitric oxide in aspirin induced thrombolysis in vitro and the purification of aspirin activated nitric oxide synthase from human blood platelets soumendra k. Solubility and dissolution are different concepts, but are related. Pdf crystallization and morphological characteristics of. Solubilization of metronidazole by watermiscible multi. A novel mechanism for aspirinmediated growth inhibition. Company replaced the phenol group with an ester group.
Aspirin is an ester that has high molecular weight and it not soluble in water hence the solid can be separated by crystallization process. Design and characterization of enteric coated pellets of aspirin using hotmelt coating technique s. Methods for measurement of solubility and dissolution rate of sparingly soluble drugs 5 1 introduction the dissolution rate and the release rate of a drug are essential to know for drug characterization. Du journal of undergraduate research and innovation quantitative estimation of aspirin in various drugs. Several studies were done to evaluate the stability. In order to clearly identify the material for the two separate problems, each problem is presented in its entirety within a labeled frame.
Aspirin was administered orally everyday at the dose of 100 mgkg. Du journal of undergraduate research and innovation. Freezedrying works by freezing the material and then reducing the surrounding pressure to allow the frozen water in the material to sublimate directly from the solid phase to the gas phase. A human gastric cell line ags was exposed to physiologic concentrations 3 to 50 mm of aspirin. Aspirin is a drug that is usually used to relieve minor aches and pain and other medical uses such as antiinflammatory medication. Pdf techniques for solubility enhancement of poorly. Methods for measurement of solubility and dissolution rate. This present study describes the development and validation of a simple dissolution test for 6mg def tablets, which was optimized on the basis of solubility and stability. The solubilization of rapamycin, a poorly water soluble investigational immunosuppressive drug, by facilitated hydrotropy is presented.
Extraction of membrane proteins by differential solubilization. Current guidelines should be consulted for use of dual antiplatelet therapy lowdose aspirin plus ticagrelor, clopidogrel, or prasugrel uses. Amoxiciuin dissolves fast, has a high solubility and a good stability if the ph cau be buffered at 8. In the present investigation hydrotropic solution of urea 10m has been used. Antitumor and antiangiogenic effects of aspirinpc in. Hydrophobic drugs like phenacetin, aspirin shows decrease in dissolution rate as they tend to adsorb air at the surface and inhibit their wettability. Therefore, we examined the ability of aspirin to inhibit tumor growth of hepg2 cells in a nude mouse xenograft model. The role of nitric oxide in aspirin induced thrombolysis. International journal of pharmacy and pharmaceutical sciences. Same way for aspirin, phenytoin, penicillin, cephalosporin, etc. Solid dispersion technique for improving solubility of some poorly soluble drugs mogal s. Acetylsalicylic acid was synthesized by gerhardt in 1853 and even put on the market during the 1880s by the firm merck. Download fulltext pdf techniques for solubility enhancement of poorly soluble drugs.
Ibuprofen is supplied as tablets with a potency of 200 to 800 mg. Hydrotropic solubilization technique is one of them. Knowledge of the pka value of a drug and the approximate rule of thumb introduced in chapter 1 allows a prediction of the extent to which each of. Aspirin administration reduces the growth of hepg2 xenografts. What is % purity definition how to do percent purity. Values for ka, and so reported for a p cular drug in the literature are in distilled. The structures of aspirin, methotrexate and furosemide. Article history several techniques are used to increase the aqueous solubility of poorly water soluble drugs.
Capitals indicate lifethreatening, underlines indicate most frequent. We conclude that aspirin acts through coxindependent mechanisms by resulting in an increase in mmr protein expression and subsequent apoptosis, which might serve as an additional means of growth inhibition in aspirin treated human colon cancer cells. Novel application of hydrotropic solubilizing additives in. Selfassembled lipid cubic phase and cubosomes for the. Synthesis and recrystallization of aspirin lab report. Hydrotropy is a solubilization technique in which addition of large amount of a second solute results in an increase in the aqueous solubility of another solute. Both time and concentrationdependent effects on apoptosis were noted, which were effectively prevented by the caspase inhibitor zvadfmk. Partially watermiscible aromatic solutes such as benzyl. Route onset peak duration aspirin pirin po 530min 1. In order to measure the dissolution an instrument called rotating disc is used. Aspirin promotes bone marrow mesenchymal stem cellbased.
An experimental investigation of the interaction of. Using hydrotropy fluvoxamine maleate is analyzed in bulk drug and tablet. Uv vis absorption spectroscopy and colorimetric studies. In the present investigation hydrotropic solution of sodium.