The cephalosporin antibiotic cefuroxime axetil is a prodrug primarily absorbed from the upper part of the GIT and degraded in presence of intestinal esterases. The purpose of this investigation was to apply Box behnken response surface methodology for the development of a gastro retentive floating tablets of cefuroxime axetil and to inspect the effect of formulation variables on drug release and the buoyancy properties of the delivery system.
The amount of methocel K4M, cetyl alcohol and sodium bicarbonate were taken as independent variables and floating lag time, Q12h and t50% were taken as dependent variables. Tablets were prepared by the direct compression method and evaluated for physical properties, swelling, floating lag time, drug release. In vivo floating study also done on statistically optimized formulation in healthy male rabbit.
The duration of floating time were principally >24 hours and floating lag times <29 seconds. FTIR, DSC and diastereomeric ratio of the SOF revealed there was no chemical interaction between drug and polymer. The statistically optimized formulation (SOF) released drug according to zero order kinetics with a fickian diffusion mechanism. The in vivo evaluation of SOF in healthy rabbit showed that the tablet was buoyant in gastric fluid with change in its swelling.
Key words: Box behnken design (BBD), Response surface methodology, Cefuroxime axetil, Gastroretentive drug delivery, Optimization, Independent Variables, Dependent Variables.
1.0. Introduction
Conventional oral dosage forms present no control over drug delivery leading to fluctuations in plasma drug concentration (Dhole et al., 2011). Oral controlled drug delivery is the majority preferable route of drug delivery ...
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...rmulation and evaluation of gastroretentive floating drug delivery system of Ofloxacin. Drug. Inv. Today. 3, 7–9.
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17). Dowieko (2015) points out that “methods of administration and routes of administration are important factors that affect the user experience” (p.17). There are thirteen different ways that a compound can be introduced to the body (Kamienski and Keogy (2006), Doweiko, 2015, p. 17). Compounds administered by the “enteral method enter the body by the gastrointestinal tract ”(Brody, 1994, Dowieko ,2015, p. 17). “Compounds administered by the parenteral method of drug administration involves the injection of a compound directly into the body” (Dowieko, 2015,
In October of 1982, Tylenol, the leading pain-killer in the United States at the time faced a crisis. Seven people in Chicago were reported dead after taking Tylenol. 12-year-old Mary Kellerdman of Elk Grove Village, Illinois, Adam Janus of Arlington Heights, Illinois, his brother Stanley Janus, and his wife Theresa Janus, Mary Reiner of Winfield, Paula Price, and Mary McFarland of Elmhurst Illinois was the last victim of the cyanide-laced Tylenol capsules. This happened bﴱᄃecause there was Extra-Strength Tylenol capsules that had been distributed and tampered with. The capsules contained 65 milligrams of cyanide. The amount necessary to kill a human is five to seven micrograms, which means that the person used 10,000 times more poison that what was needed.. The tampering had occurred when the products reached the shelves. The connection between the deaths and the Tylenol was discovered within days by two off-duty firemen who were listing to their police radios. Phillip Cappitelli and Richard Keyworth were the men to make the connection and tell there superiors.
The molecular formula is C23H27FN4O2, with a molecular weight of 410.49 (Ereshefsky & Mascarena, 2003). Route of administration is oral. Once the drug passes the esophagus and stomach, it makes its way into the small intestines. There are beds of capillaries within the intestine walls.
Sterile compounding is the preparation of products that should be free from all viable forms of life. There are more stringent requirements for sterile compounding than there are for non-sterile compounding. Staff must be trained and tested on their aseptic processing abilities, cleaner aseptic facilities are required, the quality of air entering the aseptic facility must be evaluated and maintained, sterilisation processes must be effective, knowledge of solution stability is needed and sterility testing of the products is required. The most common type of compounded sterile preparations (CSP) used clinically are aqueous injections. These CSPs require greater attention when being prepared as they pose the greatest risk to the patient if they are non-sterile or contain the wrong ingredients and/or wrong concentrations of ingredients if they are given intravenously. The main objective of sterile compounding is to prevent both morbidity and mortality of patients, which can be caused by non-sterility of preparations, high bacterial endotoxin content and errors associated with ingredients of the preparation, as mentioned earlier.
Rohypnol comes in a pill or tablet form as a solution to be injected. The pill or tablet is swallowed, chewed, or put under the tongue to dissolve slowly. Less commonly, it is crushed and snorted or dissolved and injected. It is also sometimes added to marijuana and smoked. Rohypnol usually comes in doses of 1 or 2 milligrams. The affects start very quick within fifteen to twenty minutes and sometimes the effects can last anywhere between eight and eighteen hours.
In this case study, our concern goes for the chitosan nanoparticles; firstly nanoparticles are able to adsorb and/or encapsulate a drug, thus protecting it against chemical and enzymatic degradation. Furthermore the encapsulated drug may be prevented from crystallization, thus forming a solid solution. Depending on drug solubility in the carrier, a drug load varying from only a few percent up to 50%] Secondly, chitosan is ...
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Discuss the possible drug and excipient-related constrains of the formulation (no identity of the drug was given to you at this
In the late 1800’s it was discovered that papa-amino-phenol, could reduce fever, but the drug was too toxic to use. A less toxic extract called phenacetin was later found to be just as effective but also had pain-relieving properties. In 1949, it was learned that phenacetin was metabolized into an active but also less toxic drug, acetaminophen. Since then, acetaminophen has been sold under many over the counter brand names, most popular being Tylenol.
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To continue, compounding would be needed if a patient wants to change something about the medicine such as flavor or strength. It is vital that s...
As we discussed above that pharmacokinetic and pharmacodynamics can be seen as two sides of the same coin in order to gain better understanding of their efficacy and safety profiles.” Generally it is possible to make fairly robust predictions of the pharmacokinetic profile in man using in vitro systems and preclinical pharmacokinetic studies. A previously published survey on the causes of failure in drug development indicated that inappropriate pharmacokinetics were a major cause such as; factors as low bioavailability due to high extraction or poor absorption characteristics, short elimination half-life leading to short duration of action and excessive variability due to genetic or environmental factors. This observation has led to an increased emphasis on pharmacokinetic input to the drug discovery process throughout the pharmaceutical industry. However, it is important to realise that this may only permit the rejection of compounds to b...