Novel vitamin enzymes: development, characterization, preclinical eval.

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Journal name: World Journal of Pharmaceutical Research
Original article title: Development, characterisation and preclinical evaluation of some novel enzymes with vitamin
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:

Amol S.Rakte, Dr. Basavaraj K.Nanjwade


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Development, characterisation and preclinical evaluation of some novel enzymes with vitamin

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

Copyright (license): WJPR: All rights reserved


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Summary of article contents:

Introduction

The research presented focuses on the development, characterization, and preclinical evaluation of a novel effervescent tablet formulation containing enzymes (Bromelain, Papain, and Bacterial Protease) along with Vitamin C. The objective was to create a stable, palatable, and mechanically strong product suitable for production under normal environmental conditions. Various tablet formulation methods, including direct compression, dry granulation, and wet granulation, were employed and evaluated based on several physical parameters. The study also assessed the safety and anti-inflammatory efficacy of the tablet using preclinical models in laboratory rats.

Novel Effervescent Tablet Formulation

An essential aspect of the research was the formulation of the effervescent tablet containing multiple enzymes and Vitamin C. The process involved several preformulation studies, including the identification of enzymes through MALDI-TOF mass spectrometry and compatibility evaluation with excipients using Infrared spectroscopy. Three main formulation techniques were used: direct compression, dry granulation, and wet granulation, which were each explored through multiple trials. The formulations produced were systematically evaluated for mechanical integrity, effervescent time, hardness, friability, and pH. The study identified that the wet granulation method produced the most satisfactory formulation characteristics among the methods tested.

Preclinical Evaluation of Anti-Inflammatory Activity

In addition to formulation development, the study evaluated the anti-inflammatory activity of the tablets using the carrageenan-induced paw edema model in rats. The results demonstrated significant dose-dependent anti-inflammatory effects in treated rats compared to the control group. The study measured paw volume before and after treatment and calculated the percent inhibition of edema over time. The standard drug indomethacin showed a maximum inhibition of inflammation at a dose of 10 mg/kg body weight, while the test drug also exhibited substantial activity, with the highest dose (40 mg/kg) achieving a 47.56% inhibition at the 3-hour mark.

Toxicity Assessment

The safety of the enzyme blend was assessed through OECD guidelines for repeated-dose toxicity studies in rats over a 28-day period. The study monitored general health, body weight changes, and various biochemical and hematological parameters, alongside histopathological examinations of vital organs. None of the animals exhibited severe adverse effects, although some biochemical parameters showed non-significant increases, indicating potential mild effects on liver and kidney function. Notably, mild degeneration was observed in liver and kidney tissues, while the overall histological examination indicated that the lesions found in the spleen might suggest mild immune suppression, unrelated to active drug administration.

Conclusion

The research successfully developed a stable and effective effervescent tablet formulation combining enzymes and Vitamin C, assessed through various methods of tablet preparation. The wet granulation method yielded the most promising physical and stability characteristics. The preclinical evaluations underscored the formulation's significant anti-inflammatory effects while indicating a favorable safety profile in laboratory rats, notwithstanding some mild histopathological changes. Overall, the study provided a comprehensive framework for further exploration and development of effervescent tablet formulations incorporating active enzyme ingredients.

FAQ section (important questions/answers):

What was the aim of Amol S. Rakte's research on enzymes and vitamin C?

The research aimed to formulate and evaluate a multienzyme effervescent tablet containing Bromelain, Papain, Bacterial Protease, and Rutin with Vitamin C, ensuring good stability, palatability, and mechanical integrity.

What methods were used for tablet preparation in the study?

The study utilized three methods for tablet preparation: direct compression, dry granulation (slugging), and wet granulation, to compare physical parameters and stability outcomes of the formulations.

How was the compatibility of enzymes and excipients evaluated?

Compatibility was evaluated using Infrared spectroscopy and MALDI-TOF, identifying the enzyme peaks and confirming there were no significant incompatibilities between excipients and active ingredients.

What were the main findings related to anti-inflammatory activity?

The test drug showed significant anti-inflammatory activity in the carrageenan-induced paw edema model, with treatment at higher doses resulting in greater percent inhibition compared to controls.

What were the toxicity study results in rats after drug administration?

The toxicity study showed no deaths or severe adverse effects in rats, with minor increases in biochemical and hematological parameters indicating potential mild liver and spleen changes.

Which formulation method yielded the best stability results?

The wet granulation method (WG-8) demonstrated superior stability, with no significant changes in physical parameters after two months compared to the direct and dry granulation formulations.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Novel vitamin enzymes: development, characterization, preclinical eval.”. 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) Study (Studying):
The term 'Study' in this context refers to a systematic investigation aimed at understanding and evaluating the properties and effects of the formulated effervescent enzyme tablets. It encompasses experimental methods, analysis of physical and chemical properties, and assessments of biological activity, such as anti-inflammatory effects in preclinical models.

2) Amol:
Amol is likely a reference to Amol S. Rakte, the lead author of the research described in the document. His name represents not only his contributions to the study but also the academic and practical insights he brings as part of the collaborative research effort in pharmaceutical formulation development.

3) Drug:
The word 'Drug' pertains to the active components used in the formulation, specifically the enzyme premix combined with Vitamin C used for developing effervescent tablets. The drug's efficacy, safety, and compatibility with other excipients are critical aspects evaluated during the study and analysis.

4) Table:
In the context of this research, 'Table' refers to both the physical form of the drug product being developed and the organized presentation of data. It includes the presentation of various formulations, physical parameters, and stability testing results, essential for understanding the formulation outcomes.

5) Animal:
The term 'Animal' refers to the laboratory rats used in the preclinical evaluation of the formulated effervescent tablets. These animals are crucial for assessing safety, efficacy, and potential side effects, allowing researchers to extrapolate data relevant to human health outcomes and pharmacological effects.

6) Activity:
'Activity' in this study context refers to the biological effect or action exhibited by the formulated tablets, particularly focusing on anti-inflammatory activity observed in the carrageenan-induced paw edema model. The measurement of this activity is key to establishing the therapeutic potential of the drug formulation.

7) Arrow:
The mention of 'Arrow' in the text likely pertains to graphical representations used in figures showing the results of histopathological observations or results. Arrows indicate specific observations, changes, or points of interest within microscopic images that help to illustrate the findings of the study clearly.

8) Toxicity:
'Toxicity' addresses the safety profile of the enzyme formulation, particularly assessing adverse effects in animal models. The study involved evaluation under OECD guidelines to measure potential harmful effects, including organ function impacts, aimed to ensure the formulation is safe for potential human use.

9) Powder:
'Powder' relates to the physical state of the various active and excipient ingredients used in the formulation process. It underscores the importance of powder characteristics, such as flowability and particle size, that influence the tablet manufacturing process, stability, and overall therapeutic performance.

10) Edema (Oedema):
'Edema' refers to the swelling resulting from inflammation, particularly the experimental model used to study the anti-inflammatory effects of the developed tablets. The carrageenan-induced paw edema model gives critical insights into the efficacy of the product in reducing inflammation in vivo.

11) Inflammation:
The term 'Inflammation' denotes the biological response that is assessed in the study to establish the therapeutic potential of the effervescent tablets. It examines how the developed formulation can affect inflammatory pathways and help alleviate conditions related to swelling and pain.

12) Water:
The term 'Water' is significant as it serves as a solvent for the effervescent reaction in the tablets. It plays a role in manufacturing and determining the functioning of effervescent formulations, which rely on hydration to produce carbon dioxide and thus facilitate disintegration.

13) Observation:
Observation refers to the systematic monitoring and assessment conducted during the research to evaluate both physical attributes and biological effects of the enzyme formulation. It covers various aspects such as tablet characteristics and animal responses, essential for deriving reliable conclusions.

14) Glass:
The word 'Glass' likely indicates the equipment used in the experiments, such as beakers or other laboratory glassware utilized for measuring and observing results. Proper use of glass labware is critical for accuracy and integrity in scientific experiments and analytical procedures.

15) Blood:
Blood is central to the toxicity studies where various biochemical and hematological parameters were measured to assess the safety and physiological effect of the drug formulation. Changes in blood composition can indicate potential adverse effects and alterations in organ functionality.

16) India:
India is significant in the context as it is the country where the study was conducted, specifically at Pacific University in Udaipur, Rajasthan. The geographical context may influence the regulatory environment and standards under which pharmaceutical research and development occurs.

17) Rajasthan:
Rajasthan is a state in India where the research was based. It provides a regional context for the study, potentially influencing local pharmaceutical practices, educational institutions involved in the study, and available resources for conducting high-quality pharmaceutical research.

18) Udaipur (Udaypur):
Udaipur is a city in Rajasthan that hosts the Pacific University, the institution involved in the research. The city’s academic infrastructure and focus on pharmacy education contribute to the development of innovative pharmaceutical products and research initiatives.

19) Filling (Filled):
The term 'Filled' may pertain to the process of filling the tablet formulations with specific active ingredients and excipients. Alternatively, it could relate to observations regarding the density or composition of the final product, crucial for understanding formulation characteristics.

20) Pharmacological:
The word 'Pharmacological' ties into the study of drugs and their actions within biological systems, highlighting the research's focus on understanding the therapeutic effects of the enzyme formulation. It encompasses the analysis of how the formulation interacts at cellular and systemic levels.

21) Pharmacology:
Pharmacology, as a discipline, relates to the study of drug interactions, effects, and mechanisms within living organisms. This study belongs to the realm of pharmacology, as it investigates the actions and properties of the formulated drugs in a biological context.

22) Measurement:
'Measurement' refers to the various quantitative assessments conducted throughout the study to evaluate tablet characteristics and biological effects, such as tablet hardness, dissolution times, and anti-inflammatory activity, which are fundamental for ensuring product efficacy and safety.

23) Discussion:
Discussion refers to the section of the research paper where results are interpreted in relation to existing literature and existing knowledge. It is a critical component as it contextualizes the findings of the study within the broader field of pharmaceutical research.

24) Toxicology:
'Toxicology' is relevant as it encompasses the study of adverse effects caused by drugs in living systems, underscoring the importance of safety testing in pharmacological research. This study included toxicity assessments to lead to potential human applications of the formulations.

25) Science (Scientific):
Science refers to the systematic enterprise that builds and organizes knowledge in the form of testable explanations and predictions about the universe. The research exemplifies the application of scientific methodologies in exploring drug formulation and evaluation.

26) Fragrance:
'Fragrance' in this context likely pertains to the sensory attributes of the formulated tablets, particularly the incorporation of orange flavor. The addition of fragrance is essential for enhancing palatability, which is important for patient compliance and acceptance.

27) Thomas:
'Thomas' is a reference to Thomas Baker, a supplier based in Mumbai, where various excipients were procured for the study. The supplier's background emphasizes the importance of sourcing quality materials, which is critical for the success of pharmaceutical formulation development.

28) Nashik:
Nashik is a city in Maharashtra, India, that may relate to the research's context, possibly as a location for procurement or collaboration. It enriches the geographic and socio-economic dimension relevant to the pharmaceutical research environment.

29) Nature:
In this context, 'Nature' might be a reference to the inherent characteristics of the materials involved in the study, including their chemical and physical properties which govern the formulation processes and the subsequent biological effects in the studied dosage forms.

30) Hind:
Hind likely refers to the cultural and regional significance within the Indian context, possibly relating to traditional Indian medicine practices. The inclusion of local context underscores the relevance of the research within the broader scope of traditional and modern medicinal practices.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Novel vitamin enzymes: development, characterization, preclinical eval.’. Further sources in the context of Science might help you critically compare this page with similair documents:

Vital organ, Experimental method, Oral administration, Research Institute, Statistical Significance, Anti-inflammatory activity, Toxicity studies, Stability study, Vitamin C, Hematological Parameters, Histopathological study, Test drug, Weight variation, Carrageenan-induced paw edema, Toxicity study, Carrageenan-induced inflammation, Acute oral toxicity, Compressibility index, Mean corpuscular volume, Mean corpuscular hemoglobin, Hematocrit, Nutritional analysis, Infrared spectroscopy, Standard deviation, Microbiological analysis, Toxic effect, Coefficient of Variation, Mean corpuscular hemoglobin concentration, Total protein, Immune Suppression, Stability Studies, Bio availability, Congestion, Good palatability, Blood Urea Nitrogen, Wet granulation method, Direct compression, Wet granulation, Sodium Benzoate, Dry granulation, Department of Pharmaceutics, Mechanical integrity, Biochemical parameter, Effervescent tablet, OECD Guideline, Albumin level.

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