6. Results and Discussion:
6.1 Preformulation Studies:
6.1.1 Selection of drug:
Carvedilol Phosphate is a non-selective β-adrenergic blocking agent with α-1 blocking activity. It is widely used in clinical practice for the treatment of cardio vascular diseases like hypertension, congestive heart failure, myocardial infarction, etc. Treatment with the β-adrenoceptor blocking agents, metoprolol and carvedilol, has been shown to improve symptoms and left ventricular ejection fraction and to reduce mortality in patients with heart failure. However, a recent clinical study showed that carvedilol had a more favourable effect on the survival rate of patients with heart failure in comparison with metoprolol. Carvedilol is used as a racemic mixture clinically. S-carvedilol has
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Mean values (n=3) of drug dissolution profiles are as shown in table 36. Standard deviation was not more than 2 in any case. It was observed that after storage of three months in stability chamber, drug release was decreased approximately by 5% while lag time was unaffected. Also for pellets stored at ambient conditions lag time was unaffected and drug release was lowered approximately by 5%.
Final formulation (T1) contains formulations C2 and C7, 209 and 211 mg respectively and each contains 20 mg of the drug. Formulation T1 is used for in vivo
The USP/NF generally expresses the solubility in terms of the volume of solvent required to dissolve 1 gram of the drug at a specified temperature. There is also the Biopharmaceuticals Classification System (BCS), which is a scientific classification of a drug substance based on its aqueous solubility and intestinal permeability that correlates in vitro dissolution and in vivo bioavailability of drug products. BCS takes into account two major factors: solubility and permeability, which control the rate and extent of drug absorption from solid dosage forms, and its bioavailability. A drug is considered highly soluble when the highest strength is soluble in 250 ml (this volume is typical study protocols) or less of aqueous media over the pH range of 1.0–7.5; otherwise the drug substance is considered poorly
What if the density of the pill affects the dissolving time in the hydrochloric acid? During this experiment, this question will be answered. The denser the pill, then the longer dissolving rate when time is a function of the dissolving rate. Tablets, coated tablets, gel capsules, and hard capsules will be tested, and all of these each have a different densities.
In evaluating M.T.’s medication regimen it is noted she is currently taking metoprolol 50mg twice daily and it is proven to be ineffective in managing her blood pressure which is currently noted as 174/94 with a pulse of 90. The metoprolol is a beta blocker and is not a first choice for a monotherapy to treat hypertension. The regimen is twice daily and creates complications for the M.T. to remember to take the medication. In addition, there is no documented history of heart failure or MI in M.T.’s medical history but there is
There are different classes of medications used in the treatment of heart failure. While all these classes work differently, the main goal is to reduce the blood pressure of the patient as well as ease respiration that in most cases is compromised due to pulmonary congestion. Among these medications, beta adrenergic blockers, Angiotensin Converting Enzyme (ACE) inhibitors, and diuretics
• Weekly acidic and basic drugs show good solubility when they are ionized and they also decompose faster when they are ionized.
The writing on the role of Beta-blockers in the treatment of heart failure is elaborative and absorbing. The brief explanation about the mechanism Beta blocker is illuminating. Beta blocker use can help to manage heart failure. Beta blockers blocks the effects of the epinephrine (adrenaline). When beta blockers are taken, then the heart rate gets slow and heart demand of oxygen decreases, consequently the blood pressure is reduced (Staff, 2016). Beta blockers have different kinds of with slight differences. Depending on the circumstances, different beta blockers are utilized. The beta blockers can vary in terms of side-effects, as well as in term of the amount that a patient need to take per day. Depending upon the patient condition and treatment
Mineralocorticoid-receptor antagonists such as eplerenone and spironolactone have shown efficacy in improving mortality and morbidity in patients with reduced left ventricular ejection fraction (LVEF ≤ 40%). The TOPCAT study (Treatment of Preserved Cardiac Function Heart Failure with an Aldosterone Antagonist) aims to see if this class of agents is also effective in improving the outcomes for symptomatic patients with preserved
Carvedilol (CAR, Figure 1) is a racemic mixture in which nonselective β-adrenoreceptor blocking action resides in the (-) enantiomer whereas blocking α1-adrenergic receptors is due to both (+) and (-) enantiomers at the same potency. The (-) isomer of CAR is administered in congestive heart failure in combination with diuretic therapy and ACE inhibitors. (-) CAR reduces lipid peroxidation level, as is
There are many different types of pills that humans use for various reasons, and each one is designed to cure or contain a certain problem or pain. This form of medication is usually compacted in a small tablet, sometimes with a coating on top, and meant for the user to swallow as a whole without allowing it to dissolve before entering the stomach. However, considering that people seem to want the fastest relief possible that they can get from their bodily ailments, the research question of this experiment was: Which class of pills dissolve the fastest?
More than 100 years ago, Mackenzie noted the therapeutic effect of digitalis by slowing the heart rate in atrial fibrillation patients (1). Digoxin was the cornerstone for atrial fibrillation until verapamil was discovered in1967; which shown to be effective in slowing the ventricular rate in atrial fibrillation by Bender and colleagues (2). Klein and colleagues wrote a letter to the editor, in 1980, to report his experience with verapamil-digoxin interaction to result in increased serum digoxin concentrations (SCD) by 58% (3).
For elderly people the pharmacokinetics varies. A study was conducted that included evaluating 22 elderly volunteers (>65 years old) receiving a 50 mg oral dose of the drug (4). The peak plasma concentration was 1.54 mcg/mL and it took place 1.3 hours after the dose. The area under the curve (AUC) for the elderly volunteers was 76.4 mcg*h/mL. Compared to young individuals the AUC was much greater for the elderly, suggesting that the ability to clear out the drug decreases in elderly patients thus more of it is absorbed in the body (4). Furthermore, creatinine clearance and the amount of drug recovered in the urine were also much lower in the elderly because of the reduced renal function (4). In normal volunteers, the drug was mainly cleared by the kidneys with around 80% of the drug that was administered appearing in the urine as unchanged (1).
Patterson et al. used three poorly water soluble drugs (carbamazepine, dipyridamole and indomethacin) with a polymer polyvinyl pyrrolidone K30 (PVP K30) at a 1:2 drug polymer ratio to prepare glass solutions of the drugs. The glass solution was referring to an amorphous solid in which the solute will disperse in the solid solvent on a molecular level. (Patterson et al., 2007).
Propranolol was quickly found to reduce morbidity and mortality in angina patients, causing a decrease in anginal attack frequency. After three years, propranolol users were found to have a “death rate due to myocardial infarction four times less than those who had not received the
Intermediate precision was measured on a sample of Trazodone hydrochloride from the same lot used for repeatability measurements. Six preparations of 1000 ppm Trazodone hydrochloride raw material was prepared by analyst A (Eyup Zengin). Analyst A injected the six solutions of Trazodone hydrochloride raw material into Instrument 1 (S/N: XXXXX) on September 20, 2014 at 9:00 a.m. Six preparations of 1000 ppm Trazodone hydrochloride raw material was prepared by analyst B (Syed S). Analyst B injected the six solutions of Trazodone hydrochloride raw material into Instrument 2 (S/N: XXXXXX) on September 27, 2014 at 9:00
Both carrageenan types yielded near zero-order profiles in drug release tablet formulations. The tablet compression pressures had little to no effect on the profiles from 70 to 175 MPa. It was found out that while drug loading increased from 5% to 20%, the exponent of diffusion decreased from 1.056 to 0.678. From zero-order release, the breakup of tablets during the dissolution and departure were the result of 30% drug loading. To predict the time for 50% release as a function of the concentration of both types of carrageenan, the researchers used multiple regression analysis, which was also used for microcrystalline cellulose, a third filler material used in the setup. They concluded that the observed values and the predicted values of the research were in good agreement and the R2 for the final cubic model was 0.9984. (Hariharan M, Wheatley TA, & Price JC., 1997)