Table (9): Chromatographic Conditions for Zolmitriptan HPLCAssay
Mobile phase 70% 10 mM ammonium acetate : 30 % Methanol pH. 4.0
Temperature. 25○C
Flow rate. 1 ml/min
Injection volume. 10 µL
Detection wave length. 225 nm
Elution type. Isocratic
2.3.11.5 Preparation of Standard Curve
To a 0.5 ml of blank plasma, 100 µl of Zolmitriptan standard solutions at concentrations of 0.5, 2, 5,.10, 20,.40 ng/ml and 100 µl of internal standard (IS) Sumatriptan (500 ng/ml) were added and. vortexed for 60 seconds. After that, 50 µl 10 N NaOH solution was added and vortexed for 60 seconds. Afterward, 2 ml of diethyl ether was added and vortexed for 60 seconds. The solution was centrifuged for 20 minutes, at 4000 rpm. Organic layer was filtered by 0.45µm millipore filter paper, then evaporated to dryness under the effect of heat of the water bath, then reconstituted with 500 µl of mobile phase. The standard calibration curve for Zolmitriptan was assembled by using the analyte/IS peak-area ratios versus the concentrations of the analytes (100).
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Zolmitriptan was extracted by protein precipitation method. The plasma samples were firstly permited to thaw at room temperature. The sample preparation involves the following: 100 µl internal standard of Sumatriptan at a concentration of 500 ng/mL was added to 0.5 ml serum sample in a glass tube , the drug was extracted by the same method mentioned previously.
2.3.11.7 Pharmacokinetic Data Analysis
Pharmacokinetic parameters, including half life t1/2 (h) was calculated as 0.693/Kelim.. The maximum drug concentration (Cmax, ng/ml) and the time to reach Cmax (Tmax, h) were got from the individual plasma concentration-time curves. The area under the curve AUC0–12 (ng h/ml) was calculated as the area under the plasma concentration-time curve up to the final measured sampling time and calculated by the linear trapezoidal rule ( 101)
In experiment two, the drug Panacetin was separated by a series of chemical reactions into its three components: sucrose, aspirin, and an unknown active ingredient, either acetanilide or phenacetin. The purpose of this lab was to determine what percentages of each component is present in the pain-killer. The initial step was to dissolve Panacetin in dichloromethane. However, sucrose is insoluble in dichloromethane because organic molecules are soluble in organic solvents, and dichloromethane is an inorganic solvent, so only aspirin and the unknown dissolved. By using gravity filtration, sucrose was filtered from the solution and 0.30g of solid was collected.
The purpose of experiment three was to identify the unknown component in the drug Panacetin. The use of physical properties can help identify unknown compounds and estimate the degree of their purities. In this experiment, solubility in boiling water and melting point were used to determine if the unknown was acetanilide or phenacetin. Since both compounds are soluble in boiling water and insoluble in cold water, recrystallization was used to remove any impurities from the solid.
During Phase 1, sufficient information about the drug’s pharmacokinetics and pharmacological effects should be obtained to permit the design of well-controlled, scientifically valid, Phase 2 studies.
Dosages of the drug vary from one extreme to another based upon the patients needs.
The purpose of this lab is to investigate the composition of a compound suspected to be Panacetin, a type of pain-killer. Panacetin is typically made up of sucrose, aspirin, and acetaminophen, but the third component in this experiment is unknown. The unknown component is suspected to be a chemical relative of acetaminophen, either acetanilide or phenacetin. Using techniques such as extraction, evaporation, and filtration, the three components will be isolated based on their solubilities and acid-base properties. Then, the percent composition of Panacetin can be deduced based on the masses of the three dried components. The
The purpose of this lab was to synthesize aspirin, determine the theoretical yield, compare the percent yield to the theoretical yield and test the purity of aspirin by adding Iron (III) chloride to the product.
The National Prescribing Centre recognize some fundamental differences in the absorption, distribution and excretion of medicines between adults and children. The differences are published in the National Prescribing Centre’s bulletin, produced by
Pharmacokinetics: Oral dosing up to twelve hours for a majority of patients, also a 24-hour dosing interval for selected patients. Extended- release tablet for administered orally could contain up to 450mg.
Running the chloroform extracts and diluted sample together with two positive controls and a negative control on a single chromatographic plate simultaneously, the retention factor(Rf) of five different samples were determined. The RF value of the chloroform extract(0.75) tallied with that of the codeine positive control and that of diluted sample(1.00) with the paracetamol positive control.
They design the drug therapy protocol and indicate the appropriate dosage to use so that patients get the optimal outcome of the medication. Clinical assessments are vital to test the efficiency and the safety of an existing medication specifically through therapeutic drug monitoring. This practice is known to provide effective pharmacologic therapy though producing the maximum benefit of a drug which can remain longer period of time within the patients and have almost no toxicity that could cause harm to patients. This is why therapeutic drug monitoring in the field of pharmacy is essential enough to figure out an effective medication against a disease without any dangerous toxic actions involved to improve patients’ quality of life and hopefully find exceptional cures which is one of the pharmacists’
Pharmacokinetics (PK): Well absorbed in the gastrointestinal tract, metabolised in the liver and excreted in the urine. 1-2,4 The average PK parameters of DVS with once-daily dosing are1,4:
Figure 9 Plasma concentration of a conventional immediate release (IR) dosage form, a sustained release (SR) dosage form, and an idealized zero-order controlled release (ZOCR) dosage form[38].
Half life is a term used to determine how long it will take for a drug to be eliminated from the body (Preston, O’Neal & Talaga, 2017). However the term steady states is used when the medication reaches at period where the amount still in the body is the same as being removed (Preston et al., 2017). The steady state typically is reached after four half-lives once it has been given (Preston et al., 2017). Therefore a drug that has a half life of six hours it would roughly take 24 hours to be eliminated once it was taken. This is determined by the example given in the text, Handbook of clinical psychopharmacology for therapist (Preston, et al., 2017). “If half-life is twenty-four hours, then the steady state is usually reached in four days”
A prodrug in order to elicit required pharmacological effect, must be converted enzymatically or chemically to the parent drug in vivo. The prodrug approach was widely used to overcome various problems associated with absorption, tumor targeting, distribution, pharmacokinetics, premature metabolism, occurrence of side effects, and patient compliance46-51. The concept of the prodrug was first applied to steroids in ophthalmology to improve the corneal absorption, aqueous solubility and patient compliance 52. The first prodrug dipivefrin (a prodrug of epinephrine) for ophthalmic use was formally introduced in the late 1970s for enhancing ocular bioavailability of epinephrine 53.
The lowest amount of analyte in the drug, which can be quantitatively determined with suitable precision and accuracy, indicates the limit of quantification (LOQ). The limit of quantification (LOQ) and limit of detection (LOD) were determined based on the slope and the standard deviation of the response using the signal-to-noise ratio (S/N) as per ICH guidelines Q2(R1) 2005. The LODs for Lamivudine, Abacavir and Dolutegravir were found to be 0.021, 0.330 and 0.038 µg/mL, respectively and the LOQs for Lamivudine, Abacavir and Dolutegravir were 0.056, 1.320 and 0.095 µg/mL respectively (Table 6.7). The LOD and LOQ chromatograms were shown in Figure 6.7 and Figure