Review on estimating emtricitabine and tenofovir in bulk/pharma.

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Journal name: World Journal of Pharmaceutical Research
Original article title: A review on estimation of emtricitabine and tenofovir disoproxil fumarate in bulk and in pharmaceutical dosage form
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Original source:

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Author:

Ankita V. Deodhe, Dr. N. S. Dighe, Prof. S. D. Magar, Prof. G. S. Shinde and Jyoti J. Vikhe


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: A review on estimation of emtricitabine and tenofovir disoproxil fumarate in bulk and in pharmaceutical dosage form

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Doi: 10.20959/wjpr20192-14086


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Summary of article contents:

Introduction

Antiretroviral therapy (ART) is a critical component in managing HIV infection, as it can significantly increase the CD4+ cell count. Among the various medications used in ART, Emtricitabine (EMT) and Tenofovir Disoproxil Fumarate (TDF) stand out as prominent choices. Emtricitabine is classified as a nucleoside reverse transcriptase inhibitor (NRTI), while Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor (NtRTI). Both medications are essential in treating not only HIV-1 but also hepatitis B, with a combined mechanism of action that prevents the virus from altering the genetic material of healthy cells. This paper reviews the methods for estimating these drugs in bulk and pharmaceutical dosage forms, highlighting various analytical techniques validated according to International Council for Harmonisation (ICH) guidelines.

Importance of Antiretroviral Therapy

The significance of ART in treating HIV infection cannot be overstated. Through a combination of antiretroviral drugs, ART helps control HIV replication, thereby increasing the CD4+ cell count and reducing viral load. This not only extends the asymptomatic phase of the infection but also lowers the risk of transmission to others. Treatment modalities include multiple routes of transmission such as sexual contact, blood transfusion, and maternal transfer during childbirth. The effective management of HIV can lead to significant health improvements, emphasizing the critical role of drugs like Emtricitabine and Tenofovir Disoproxil Fumarate in ART regimens.

Mechanism of Action of Emtricitabine and Tenofovir Disoproxil Fumarate

Emtricitabine works by mimicking the natural substrates of reverse transcriptase, ultimately inhibiting the enzyme responsible for converting viral RNA into DNA. Through phosphorylation by cellular enzymes, it forms emtricitabine-5’-triphosphate, which competes with deoxycytidine-5’-triphosphate, leading to premature termination of viral DNA synthesis. Similarly, Tenofovir Disoproxil Fumarate serves as a nucleotide analog that obstructs reverse transcriptase in HIV-infected individuals. Together, the combination of these drugs not only suppresses viral replication but also promotes a healthier immune response, making them beneficial components of ART.

Analytical Methods for Estimating Emtricitabine and Tenofovir Disoproxil Fumarate

Several analytical methods have been documented for estimating Emtricitabine and Tenofovir Disoproxil Fumarate in pharmaceutical formulations. These include techniques such as Reverse Phase High-Performance Liquid Chromatography (RP-HPLC), Ultraviolet (UV) Spectrophotometry, and Ultra-Performance Liquid Chromatography (UPLC). The methodologies vary in the specifics of the mobile phases, flow rates, and retention times, addressing efficiency and accuracy in the drug estimation process. Importantly, the optimization of these methods ensures that analysis meets regulatory standards, paving the way for reliable quality control in pharmaceutical formulations.

Conclusion

In summary, Emtricitabine and Tenofovir Disoproxil Fumarate are vital in the fight against HIV, demonstrating both potency and reduced side effects compared to traditional treatments. This review elucidates the importance of these drugs in antiretroviral therapy while also presenting various validated analytical methods to ensure precise estimation in bulk and in medicinal formulations. With the advancement of analytical techniques, healthcare providers can better monitor the quality and efficacy of these essential medications, ultimately contributing to improved patient outcomes in HIV treatment.

FAQ section (important questions/answers):

What is the primary use of Emtricitabine and Tenofovir Disoproxil fumarate?

Emtricitabine and Tenofovir Disoproxil fumarate are primarily used in antiretroviral therapy to treat HIV-1 infection and also active against hepatitis B by increasing CD4+ cell counts and lowering viral loads.

What are the mechanisms of action of Emtricitabine and Tenofovir?

Emtricitabine inhibits reverse transcriptase, preventing HIV from replicating. Tenofovir, a nucleotide analogue, blocks the function of reverse transcriptase, also halting HIV replication, thereby fighting infection effectively.

What analytical methods are used for estimating these drugs?

Common methods for analysis include RP-HPLC, UPLC, and UV-Spectrophotometric techniques. These allow for effective quantification of Emtricitabine and Tenofovir Disoproxil fumarate in pharmaceutical formulations.

What are the key pharmacokinetic properties of Emtricitabine?

Emtricitabine is administered orally, has 93% bioavailability, low protein binding, and is primarily eliminated via renal excretion, with a half-life of approximately 10 hours.

What is the importance of the fixed drug combination of these medications?

The fixed drug combination simplifies dosing, decreases pill burden, and enhances patient adherence to therapy, making it convenient for managing HIV infection effectively.

How do the side effects of these drugs compare to traditional treatments?

Emtricitabine and Tenofovir Disoproxil fumarate generally have fewer side effects compared to traditional antiretroviral drugs, making them preferable options for many patients under therapy.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Review on estimating emtricitabine and tenofovir in bulk/pharma.”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.

1) Drug:
Drugs are substances that can alter biological functions and are used primarily for treating diseases. In HIV therapy, drugs like Emtricitabine and Tenofovir Disoproxil fumarate are key components. Effective antiretroviral regimens can lower viral loads and help maintain immune function, critical for prolonging the lives of HIV-infected individuals.

2) Transmission:
Transmission refers to the process by which an infectious disease is spread from one individual to another. In the context of HIV, common routes include sexual contact, sharing of needles, and maternal transmission to infants. Understanding transmission dynamics is essential for developing effective prevention strategies and treatment protocols.

3) Water:
Water is a vital solvent in biological systems, necessary for life processes, chemical reactions, and drug solubility. Many pharmaceutical formulations and biochemical processes depend on water as a medium. In the context of drug formulation, water solubility affects absorption, bioavailability, and overall efficacy of drug therapies.

4) Ahmednagar:
Ahmednagar is a city in Maharashtra, India, known for its educational institutions, including Pravara Rural College of Pharmacy. It plays a significant role in pharmaceutical education and research, contributing to advances in healthcare, drug development, and community health initiatives, especially in managing diseases like HIV.

5) Pravara:
Pravara is a locality in Ahmednagar, significant for housing various educational and research institutions, particularly the Pravara Rural College of Pharmacy. This college contributes to pharmaceutical education, focusing on drug development, formulation, and research, which are vital in advancing treatment options for diseases such as HIV.

6) Powder:
Powder refers to the physical form of a substance consisting of small particles. Many medications, including antiretroviral drugs, may be formulated as powders for direct use or as intermediates in tablet dosage forms. The powder form affects drug dissolution, stability, and bioavailability, ultimately influencing therapeutic outcomes.

7) Blood:
Blood is a bodily fluid that carries oxygen, nutrients, and immune cells throughout the body. Regarding HIV, blood is a primary medium through which the virus is transmitted. Monitoring blood for viral loads and CD4+ cell counts is essential in managing and assessing the progression of HIV infection.

8) Salt (Salty):
In chemistry and pharmacology, a salt is a compound formed from the reaction of an acid and a base. Tenofovir Disoproxil fumarate is a salt used to enhance drug stability and absorption. The formulation as a salt often improves the solubility of a drug, leading to better therapeutic efficacy.

9) Viru:
The term 'viru' is likely a shortened reference to 'virus,' which is a microscopic infectious agent that can replicate only inside living host cells. HIV is a retrovirus that targets CD4+ T-cells, important for adaptive immunity, leading to the complications of AIDS. Addressing viral infections is crucial in healthcare.

10) Substance:
A substance is a specific kind of matter with uniform properties. In drug formulation, substances can refer to active ingredients (like Emtricitabine) or inert materials. The selection of suitable substances affects the efficacy, safety, and stability of pharmaceutical products, critical for effective disease management and patient care.

11) Activity:
Activity in pharmacology refers to the biological effect or action of a drug on a living organism. Emtricitabine and Tenofovir have antiviral activity, inhibiting the multiplication of HIV. Understanding a drug's activity helps healthcare professionals select appropriate treatments and monitor therapeutic effectiveness in patients.

12) Disease:
A disease is a pathological condition of a bodily part, an organ, or system resulting from various causes, including infection. HIV is a communicable disease affecting the immune system. Managing diseases like HIV involves a combination of drug therapy, patient education, and lifestyle modifications to improve health outcomes.

13) Methane:
Methane is a chemical compound (CH4) and not directly related to the pharmaceutical context. However, it can be relevant in discussions about drug formulations, where organic compounds may interact with various chemical processes. Despite its primary use as an energy source, its implications may arise in pharmacological research.

14) Study (Studying):
A study refers to a detailed examination and analysis of a subject within a structured format. In the pharmaceutical context, studies often focus on drug efficacy, safety, and pharmacokinetics. Clinical studies provide insights into how drugs like Emtricitabine and Tenofovir affect HIV treatment outcomes, guiding therapeutic decisions.

15) Life:
Life refers to the condition distinguishing living organisms from inorganic matter, characterized by capacity for growth, reproduction, and response to stimuli. In the context of HIV, effective antiretroviral treatments aim to enhance the quality and length of life for infected individuals, highlighting the critical intersection of healthcare and longevity.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Review on estimating emtricitabine and tenofovir in bulk/pharma.’. Further sources in the context of Science might help you critically compare this page with similair documents:

Analytical method, Bioavailability, HIV infection, Mechanism of action, Route of administration, Chromatographic parameters, Pharmaceutical dosage form, Serological test.

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