Effervescent Form Research Articles

Analytical Method Development and Validation Of Stability Indicating RP-HPLC Method For Assay and Related Substances of Paracetamol and Caffeine Effervescent Tablets: Review

he ongoing, interdependent tasks related to the departments of research and development, quality control, and quality assurance are the creation and validation of analytical methods. Analytical methods are essential for risk management and equivalency assessments. It aids in the development of acceptability standards unique to a product and the consistency of outcomes. Validations establish whether the analytical process is appropriate for the goal for which it was designed. A review of the literature indicates that paracetamol and caffeine can be determined individually or in combination with other medications using analytical techniques based on UV spectroscopy, RP-HPLC, and HPTLC. The parameters were checked for correctness, precision, robustness, and other aspects of analytical validation in accordance with ICH guidelines. The discovered techniques can be applied to the bulk and tablet dosage form analysis of paracetamol and caffeine in effervescent form since they are straight forward, sensitive, and repeatable. The review also outlines the applicability and constraints of numerous published analytical techniques for paracetamol and caffeine analysis. Stability studies have to be conducted on time and in compliance with the standards issued by the World Health Organization, International Conference of Harmonization, and other bodies. The capacity of a pharmaceutical product to meet the physical, chemical, microbiological, toxicological, protective, and informational requirements of a specific formulation in a particular container-closure system is known as its stability. It also ensures that a pharmaceutical product's effectiveness, safety, and performance will be maintained for the duration of its shelf life, which is seen as a need for approval and acceptability. The requirement for ongoing quality and purity monitoring of medications and products gave rise to various stability test techniques. This review covers the various drug substance stability categories as well as the applicability of various techniques for drug substances that are stable, the applicability of various methods used to test the pharmaceutical product's stability, guidelines released to test the pharmaceutical product's stability, protocols for stability testing that outline the essential elements of a well-managed and regulated stability test, and other aspects of stability are all covered in this review. The researcher working on paracetamol and caffeine in effervescent form will greatly benefit from this thorough review study.

Comparison of oral bioavailability of acetaminophen tablets, capsules and effervescent dosage forms in healthy volunteers

Abstract A wide variety of acetaminophen dosage forms have been administered to relieve mild to moderate pain and fever, so far. The purpose of this study was to compare the oral bioavailability in healthy volunteers, of three of these dosage forms. We included healthy volunteers in our study and divided replace with placed them into three groups: tablet, capsule and effervescent. Each dosage form contained 500 mg of acetaminophen as active material. Blood samples were taken at 0.5, 1, 2, 4 and 8-hour intervals after receiving the dose. Acetaminophen blood levels were measured using HPLC method. Data were fit in a “one-compartment PK model”, using P-Pharm 1.5 software and analyzed under statistical tests. The maximum concentrations of acetaminophen in blood samples were measured at 1h after taking the drug (6.61±3.19 μg/ml, 11.29±3.94 μg/ml and 15.25±2.54 μg/ml in groups receiving capsule, tablet and effervescent, respectively). Pharmacokinetic (PK) data analysis & modeling from the three groups showed that the half-life of acetaminophen was 140.72 min in the tablet group, 140.29 min in capsule and 132.08 min in effervescent. The area under the blood levels curve were 47.04, 40.62 and 53.11 μgmin/ml, in tablet, capsule, and effervescent groups, respectively. Statistically significant differences in PK parameters were recorded as the study replace with we compared effervescent with tablets and capsule dosage forms (p < 0.05). According to the results, the effervescent form creates better PK parameters compared with tablet and capsule forms, therefore, it is suggested replace with we suggested that this form should be administer in cases of pain and fever to achieve quick drug efficacy.

Blood pressure reduction in hypertensive patients after withdrawal of effervescent medication

Raised blood pressure associated with the sodium excipient content of soluble or effervescent analgesic has been previously reported. However, the influence of other anions associated with sodium on blood pressure is still controversial. Observational study of elderly hypertensive patients with uncontrolled blood pressure treated with effervescent paracetamol (3 g/day) for osteoarthritis. Blood pressure was measured before and after (4 weeks or more) switching paracetamol from an effervescent format to a tablet form in 34 patients. Blood pressure was recorded by community pharmacists during a pharmacotherapeutic follow-up service. Sodium intake in an effervescent form was 74 mmol/day (mainly associated with sodium bicarbonate and carbonate excipients). Initial blood pressure was high (range: 153-168 mmHg systolic and 92-99 mmHg diastolic). Switching to paracetamol tablets (no sodium content) was associated with both lowered systolic pressure of 13.1 mmHg (95%CI: 11.9-14.3, p < 0.0001) and a moderate reduction of diastolic pressure of 2.5 mmHg (95%CI: 2.1-2.9, p < 0.0001). No changes in medication in the study period took place, and weight and lifestyles remained stable. A detailed review of pharmacotherapy and lifestyle reveals no other causes for blood pressure to lower. A relationship of causality between the intake of high sodium excipients and high blood pressure in elderly hypertensive individuals, without chloride ions, was found. Clinicians should be aware of possible raised blood pressure when effervescent formulations are prescribed to hypertensive patients.

Formation and Stability of Effervescent Sodium Perborate

Sodium perborate in its effervescent form (ESP) has the ability to release both gaseous and active oxygen in aqueous solution. Gravimetric analysis and direct measurement of gaseous oxygen have been used to investigate the ideal conditions for the formation of ESP from sodium perborate monohydrate (PBS1). A dehydration temperature of 125 °C gave the maximum yield of effervescent oxygen, with the mass loss corresponding closely to 1 mol of water/mol of PBS1. In stability studies, freshly formed ESP was capable of generating 10.1 wt % effervescent oxygen. However, this value fell to only 1.35% of its initial value after exposure to ambient air (26 °C and 36% relative humidity), confirming the unstable nature of this material. ESP stability was improved by screening its surface with a coating of fine boric acid powder. Further work on the coating of ESP is recommended in order to further improve its stability.

Migraine — Treatment of Acute Attack

The treatment of an acute attack of classical or common migraine is sleep, an antinauseant such as metoclopramide, an analgesic, either aspirin or paracetamol, and in some patients 1 or 2 mg of ergotamine tartrate. Treatment should be given as early in the attack as possible and all drugs should, if possible, be given in a soluble or effervescent form. When vomiting occurs early in the attack, treatment is best given by suppository, inhalation or intramuscular injection. Ergotamine tartrate is only necessary in about one third of attacks and when used is best given by suppository or inhalation. Doses of ergotamine tartrate higher than 2 mg per attack or 6 mgs per week may cause toxic symptoms as may the abuse of analgesics.

Treatment of the acute migraine attack--current status.

The main treatment of the acute migraine attack remains sleep, sedation, an anti-nauseant and analgesics, and in some patients 1 or 2 mg of ergotamine tartrate. Drugs containing large amounts of caffeine should not be used. Absorption of drugs may be impaired in a migraine attack. Metoclopramide is probably the anti-emetic of choice because it is an effective anti-nauseant and promotes normal gastrointestinal activity. Domperidone has a similar action but is said not to go through the blood-brain barrier, so is less likely to cause extrapyramidal reactions. All drugs, including analgesics such as aspirin and paracetamol, are best given in a soluble or effervescent form. Where vomiting occurs early in the attack, suppositories may be indicated. Ergotamine tartrate is necessary in about one third of attacks and is best given by suppository or by inhalation. Doses higher than 2 mg per attack or 6 mg in one week may cause toxic symptoms, the early signs of which are headache, nausea, vomiting and a feeling of not being very well. The non-drug treatments of an acute attack include pressing on the temporal artery, hot and cold compresses and relaxation.

Bioavailability and antimigraine efficacy of effervescent ergotamine.

SYNOPSISIn about 20% of migraine patients treatment with enterally administrated ergotamine tartrate proves unsuccessful. One of the causes for this might be a poor systemic availability of the drug from the ordinary solid tablets. The present study aimed to investigate the bioavailability and the therapeutic value of ergotamine tartrate in effervescent form.In twenty volunteers the plasma ergotamine levels were measured by using a radioimmunoassay after oral administration of 2.0 mg ergotamine tartrate combined with 50.0 mg caffeine in effervescent form. Measurable plasma drug levels were found in 14 (70%) of the subjects and the mean maximum plasma ergotamine level of 0.45 ng/ml was achieved at 30 minutes.In the clinical part of the study 25 migraine patients treated their migraine attacks with effervescent ergotamine. The therapeutic value of it was considered as good by 9, moderate by 11 and poor by 5 of the patients. Among 18 of them the therapeutic effect seemed to be equal to their earlier ergotamine medications. The results indicate that the plasma pharmacokinetics of ergotamine tartrate in effervescent form is similar to and possibly faster on the absorptive phase than that reported earlier after enteral administration. In patients who do not gain benefit from the usual ergotamine tablets or suppositories, effervescent ergotamine would appear to be an alternative worth consideration.

Migraine--treatment of acute attack.

The treatment of an acute attack of classical or common migraine is sleep, an antinauseant such as metoclopramide, an analgesic, either aspirin or paracetamol, and in some patients 1 or 2 mg of ergotamine tartrate. Treatment should be given as early in the attack as possible and all drugs should, if possible, be given in a soluble or effervescent form. When vomiting occurs early in the attack, treatment is best given by suppository, inhalation or intramuscular injection. Ergotamine tartrate is only necessary in about one third of attacks and when used is best given by suppository or inhalation. Doses of ergotamine tartrate higher than 2 mg per attack or 6 mgs per week may cause toxic symptoms as may the abuse of analgesics.