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. Some modified versions of aspirin came onto the market in an effort to achieve the benefits of aspirin. 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. The solubilization of rapamycin, a poorly water soluble investigational immunosuppressive drug, by facilitated hydrotropy is presented. 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. Design of aspirin formulation for rapid pain relief. Salicylic acid 1838 was used for pain relief and fever but its acidity was a major problem. There are various approaches for solubilization of poorly water soluble drugs. Other methods, such as salt formation, complexation with cyclodextrins, solubilization of drugs in solvents, and particle size reduction have.
In order to measure the dissolution an instrument called rotating disc is used. Aspirin, enteric coating, extrusionspheronization, hotmelt coating, palmitic acid, stearic. In order to clearly identify the material for the two separate problems, each problem is presented in its entirety within a labeled frame. Our in vitro observation suggested a potential role of aspirin in the treatment of liver cancer. In the present investigation hydrotropic solubilization technique has been employed to solubilize poorly watersoluble aspirin analgesic and antipyretic drug by 0. Current guidelines should be consulted for use of dual antiplatelet therapy lowdose aspirin plus ticagrelor, clopidogrel, or prasugrel uses. Representative classes of surfactants in aqueous solutions, above and below the cmc, were studied for their solubilizing effects on suspensions of aspirin usp crystals. 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. Results of analysis by proposed method and phamacopoeial method are very comparable. Accordingly, the role of caspases in aspirin induced apoptosis was also evaluated. The role of nitric oxide in aspirin induced thrombolysis. Temperaturedependent solubilization of the hydrophobic. Therefore, we examined the ability of aspirin to inhibit tumor growth of hepg2 cells in a nude mouse xenograft model.
Aspirin promotes bone marrow mesenchymal stem cellbased. 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. 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. An experimental investigation of the interaction of. Salicin is the active ingredient from willow bark of salix alba. Solubility is defined as the concentration of the compound in a solution that is in equilibrium with a solid phase at the specified temperature. All blanks and standards were matrix matched to the samples in 10%hno 3 and 10%hcl.
Experimental analysis of aspirin bulk sample by proposed method aspirin bulk sample 0. Solid dispersion technique for improving solubility of. Company replaced the phenol group with an ester group. Capitals indicate lifethreatening, underlines indicate most frequent. Aspirin, the acetyl derivative of salicylic acid, is. Understand the various types of pharmaceutical solutions.
Route onset peak duration aspirin pirin po 530min 1. Values for ka, and so reported for a p cular drug in the literature are in distilled water. Aspirin acetylsalicylic acid aspirin has a long past. In the present investigation hydrotropic solution of sodium. The goal of this experiment was to synthesize aspirin.
Same way for aspirin, phenytoin, penicillin, cephalosporin, etc. 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. Ibuprofen is supplied as tablets with a potency of 200 to 800 mg. The solubilization study was performed for up to 5 hr in a clark. Du journal of undergraduate research and innovation. Aspirin was administered orally everyday at the dose of 100 mgkg. Aspirin induced gg1 cell cycle arrest in hct116 cells. Ph, solubility, ionization affecting absorption pharmatutor.
The solubilization of the hydrophobic antiepileptic drug lamotrigine lam in five different pluronic micelles viz. Several studies were done to evaluate the stability. Amoxiciuin dissolves fast, has a high solubility and a good stability if the ph cau be buffered at 8. Partially watermiscible aromatic solutes such as benzyl. Solubility and dissolution are different concepts, but are related. A novel, safe and sensitive method of titrimetric estimation has been developed using 2 m sodium salicylate as a hydrotropic solubilizing. 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. 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. 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. Aspirin administration reduces the growth of hepg2 xenografts. In the present study, a very slightly soluble drug, terconazole has been solubilize in water using. Uv vis absorption spectroscopy and colorimetric studies. Since there are similarities between the two problems, some of the same information appears in both problem. Aspirin is an ester that has high molecular weight and it not soluble in water hence the solid can be separated by crystallization process.
The role of platelet and its interaction with aspirin scielo colombia. 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. Extraction of membrane proteins by differential solubilization. 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. The solubilization of lam in pluronic micelles increased with the increase in temperature. Selfassembled lipid cubic phase and cubosomes for the. 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. We next explored whether aspirin treatment would promote the osteogenic potential of swine bmsc. Article history several techniques are used to increase the aqueous solubility of poorly water soluble drugs. Aspirin stimulates the osteogenesis of bmsc in vitro and in vivo. An overview article pdf available december 2012 with 3,497 reads.
Numerous solid dispersion systems have been demonstrated in the pharmaceutical literature to improve the dissolution properties of poorly watersoluble drugs. Antitumor and antiangiogenic effects of aspirinpc in. It is rapidly biotransformed with a serum half life of 1. 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. 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. Taking into account the prac assessment report on the psurs for acetylsalicylic acid the scientific conclusions are as follows. Both time and concentrationdependent effects on apoptosis were noted, which were effectively prevented by the caspase inhibitor zvadfmk. A simple, efficient and new spectrophotometric method has been developed for spectroscopic estimation of terconazole in bulk form. Application of hydrotropic solubilization phenomenon in. The structures of aspirin, methotrexate and furosemide. 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. A novel mechanism for aspirinmediated growth inhibition. 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. Physicochemical properties of drugs pharmaceutical press.
Solid dispersion technique for improving solubility of some poorly soluble drugs mogal s. What is % purity definition how to do percent purity. Aspirin acetylsalicylic acid, asa, which was initially developed as an analgesic antiinflammatory agent, has come to be the basis of antiplatelet. 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. Research articles effect of selected surfactants, above and below the cmc, on aspirin solubility j. 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. In the present investigation hydrotropic solution of urea 10m has been used. Hydrotropic solubilization technique is used to increase aqueous solubilities of poorly water soluble drugs using hydrotropic agents.
Validating usp aspirin based on the maximum daily dose 3000 mg day are shown in table 4. Synthesis and recrystallization of aspirin lab report. Hydrophobic drugs like phenacetin, aspirin shows decrease in dissolution rate as they tend to adsorb air at the surface and inhibit their wettability. This means the maximum amount of solute that the pure solvent can hold in solution, at specified environmental conditions. Download fulltext pdf techniques for solubility enhancement of poorly soluble drugs. 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. Du journal of undergraduate research and innovation quantitative estimation of aspirin in various drugs. 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. 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.
Design and characterization of enteric coated pellets of aspirin using hotmelt coating technique s. Acetylsalicylic acid was synthesized by gerhardt in 1853 and even put on the market during the 1880s by the firm merck. 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. Solubilization of metronidazole by watermiscible multi. 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. A human gastric cell line ags was exposed to physiologic concentrations 3 to 50 mm of aspirin. Novel application of hydrotropic solubilizing additives in.
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