Editor(s)
Dr. M. V. N. L. Chaitanya
Assistant Professor,
Dilla University, College of Health Sciences, Pharmacy (Pharmacognosy), Dilla, Ethiopia.

ISBN 978-93-5547-035-5 (Print)
ISBN 978-93-5547-095-9 (eBook)
DOI: 10.9734/bpi/caprd/v4

This book covers key areas of Pharmaceutical Research and Development. The contributions by the authors include spectrophotometric method, ion-pair complex, hydrocortisone, Tretenoin, stability indicating RP-HPLC, Acquired Immunodeficiency Syndrome, Antiretroviral Therapy, Combined Antiretroviral Therapy, Human Immunodeficiency Virus, phytochemical constituents, pharmacological studies, COVID-19, obesity, inflammation, oxidative stress, immune response, genetic disorders, ayurvedic concepts, pharmacy education, Pseudocholinesterase enzyme, diazinon poisoning, alcoholism, therapeutic index, prognostic value, castrative agent, epigallocatechin, sperm motility, labeo rohita fingerlings, histopathology, gill and liver, heavy metal stress, Anti-cardiovascular, antioxidant, baby, functional food, nano polyphenol, pharmaceuticals, callus and cell suspension cultures, culture medium. This book contains various materials suitable for students, researchers and academicians in the field of Pharmaceutical Research and Development.

Media Promotion:

### Content

##### Study on the Development and Validation of Direct Spectrophotometric Method for the Estimation of Glimepiride

Dilip M. Chafle

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 1-11
https://doi.org/10.9734/bpi/caprd/v4/2866E

Aims and Objectives: To develop simple, sensitive and direct spectrophotometric methods for the estimation of widely prescribed antidiabetic hypoglycemic agent Glimepiride in pure and pharmaceutical dosage form.

Application of spectrophotometric technique for development of methods. Optimization of reaction parameters and spectral characteristics for developed methods. To propose possible reaction mechanism for developed methods. Application of the developed methods for quantification of the drug in formulations. Validation of the developed method as per ICH guidelines.

Methodology: Two spectrophotometric methods were developed based on ion-pair formation of drug with Cresol Red dye (Method A) and Bromophenol Blue dye (Method B) in methanol and chloroform. The possible reaction mechanism was proposed with evaluation of statistical parameters. The methods were validated for its application to determine Glimepiride in bulk as well as in pharmaceutical formulations

Results: The Beer's law was found linear in the range 10 - 60 µgml-1 at 450 nm for method and 2 - 20 µgml-1 at 578 nm for method B, respectively. The linear regression equation obtained by applying least square regression analysis for glimepiride were found to be Absorbance = 0.0136 x Concentration in µgml-1 + 0.028; R2 = 0.9965 for method A and Absorbance = 0.0428 x Concentration in µgml-1 + 0.0722; R2 = 0.9949 for method B. The Sandell's sensitivity was found to be 0.0696 and 0.0177 for method A and B respectively. The apparent molar absorptivity calculated to be for both methods were 6.6724 x10 and 2.0999 x104 l mol-1 cm-1.

Conclusion: Two direct spectrophotometric methods for determination of Glimepiride have been developed successfully and validated for sensitivity, accuracy, precision, repeatability and robustness as per ICH guidelines. The developed methods are suitable for the routine estimation of Glimepiride in pure and dosage form. The developed methods can act as a tool for quality control of drug in analytical laboratories.

##### A Stability Indicating Reverse Phase High Performance Liquid Chromatography Method for Simultaneous Estimation of Hydroquinone, Hydrocortisone and Tretenoin in Cream Formulation: A Recent Study

Raksha Shilu, Pankaj Kapupara, Meghna Patel

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 12-26
https://doi.org/10.9734/bpi/caprd/v4/2869E

##### Impact of Highly Active Antiretroviral Therapy (HAART) on Some Immunological Indices and Quality of Life of HIV Positive Patients in Africa

M. M. Abduljalil, R. A. Umar, M. G. Abubakar

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 27-45
https://doi.org/10.9734/bpi/caprd/v4/13551D

The HIV infection is one of the most global pandemic with current global estimate of 79.3 million people infected. Due to its high mortality and morbidity it threatened the existence of mankind. This was before the discovery of effective therapy which inhibits replication of the virus. Potent combination therapy called HAART is a great therapeutic advancement for management of HIV positive individuals. The combination therapy has impacted on the lives of individuals by enhancing their quality of lives. The study evaluated the impact of HAART on some immunological indices (CD4 T-cells and WBC count) and the quality of lives of HIV positive (patients) cohort in Sokoto, Nigeria. A total of 200 samples comprising 50 controls, 50 HAART naïve, 50 on HAART for 1-6 months, and 50 on HAART for 7-12 months were enrolled into the study. CD4 T-cell was quantified using flow cytometry via the method developed by Cassens et al. (2004) whereas WBC count was done using the method of Cheesbrough (2010). The HIV positive patient groups have significantly (P<0.05) lower levels of CD T-cells and WBC count compared to the control subjects. The 2 parameters were significantly higher in those on treatment for 7-12 months compared to other two HIV positive groups. The increases in the level of the 2 parameters are related to the duration of treatment. The result suggests that, HAART exerts a positive impact on the lives of people living with HIV by improving the levels of CD4 T-cell and WBC count. Therefore, sustained HAART treatment by the HIV positive subjects may elevate the levels of the two immunological indices to normal levels which will improve physical, psychological, social and spiritual aspects of their lives.

##### Pharmacological Studies on Amomum compactum

Maulana Yusuf Alkandahri

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 46-55
https://doi.org/10.9734/bpi/caprd/v4/2775E

This review article will discuss details on the future pharmacological potential of A. compactum. The herb Amomum compactum, also known as cooking spices, belongs to the Zingiberaceae family. Many research now show that A. compactum serves as a medicinal plant with a wide range of pharmacological activity. A wide range of pharmacological activities in traditional medicine are recorded for sections of this herb, particularly thefruits, leaves and seeds, such as antifungal, antibacterial, antioxidant, gastroprotective, anti-inflammatory, immunomodulatory, anti-cancer, anti-asthmatic, and acute renal failure. The majority of this plant's phytochemical constituents are flavonoids, saponins, essential oils, steroids, and triterpenoids. Information about the current A. compactum can serve as the basic data for further research, to discover new compounds and properties. Therefore, more research on A. compactum can be done to explore newer and complete therapeutic activities.

##### Investigating the Collision between Two Pandemics: Obesity and COVID-19 Viral Infection

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 56-68
https://doi.org/10.9734/bpi/caprd/v4/2833E

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes the novel coronavirus disease 2019 (COVID-19). The principle risk factor for the development of serious forms of COVID-19 was found to be the precarious metabolic health. There are several mechanisms that implicated in the seriousness of COVID-19 ranging from attenuation of immune system function to chronic inflammation. It is important to keep in mind that obesity is a complex disease when discussing the relation between obesity and the severity of COVID-19. An increasing body of proof links obesity to COVID-19. Obesity has an obvious role in the high incidence, symptoms severity and mortality rates of viral infections seen in obese patients. Adipose tissue shows a high expression of the angiotensin-converting enzyme 2 (ACE2), the receptor for entry of SARS-CoV-2 into host cells, so obese population exhibit higher vulnerability to COVID-19. The primary immune response is offered mainly by type-I interferon (IFN-I) that is suppressed in COVID-19. The pro-inflammatory state associated with obesity produces imbalance of the inflammatory response to COVID-19, as the cytokine storm found in subjects with serious disease form. Obesity is considered as chronic inflammation of low degree, so it shows a capacity for pathogenic immune amplification. In this review, the effect of obesity on the immune system and their possible interrelations is described, with emphasis on the role of dysfunctional adipose tissue on immunity within the scope of COVID-19 infection. The authors described the dysfunctional immune responses caused by obesity that lead to organ injury in COVID-19 infection and impair the ability of patient to combat the virus. Obese patients have a longer period of stay in the hospital as well as a more severe clinical picture when compared with lean patients.  Further research is required to assess the impact of obesity control, immunonutrition and physical exercise in SARS-CoV-2 infection.

##### Exploration of Ancient Wisdom of Clinical Genetics in Ayurvedic Classics

Shyny Thankachan, Bhagavan G. Kulkarni

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 69-78
https://doi.org/10.9734/bpi/caprd/v4/2836E

Present generation is anxious about lifestyle disorders and ways to lead a healthy wellbeing. Modern science emphasizes the role of genetic factors in physical appearance, mental characteristics and disease formation of individuals. Human genome studies reveal that most of the diseases have a genetic component.  Genetic mutations occur either randomly or by the influence of an environmental factor.   Genetic disorders may or may not be hereditary. WHO data illustrate, the congenital anomalies are the reason for 17%–43% of infant mortality. Even though physical structure, appearance and behavior of every individual is different, there are some common traits transferred from parents to offspring which is explained in terms of genetics. If a parent's genetic configuration is vulnerable to some diseases, their children and grandchildren are more susceptible to such illness.  In Ayurveda the concept of genetics is spread all over the samhitas especially in shaareerasthaana in a hidden form. Ancient ayurvedic scholars had the idea that the genetic materials are transmitted from generation to generation. The expression of these can be understood with regard to prakriti. An individual’s unique physical characteristics and psychic behaviors (phenotype) depends on the prakriti(genotype).  Genetics emerged in the mid to late 19th Century. But centuries before itself, ancient Ayurvedic literature documented the union of sukra and shonita(sperm and ovum), concept of beeja, beejabhaga and beejabhagavayava, inheritance, congenital anomalies, and genetic disorders.Ayurveda also gave importance to personalized or individualized concepts of understanding and treating diseases. Ayurvedic concepts like garbhasambhavasamagri (factors necessary for formation of garbha) and garbhotpadaka bhava (six procreating factors), dinacharya, ritucharya, sadvritha, dharaneeya, adharaneeyavega, ritumaticharya, &garbhinicharya assures the regulation of gene sequencing and gene expression and thus can-do wonders to the challenging issues. Ayurvedic science not only gives importance to anatomical, physiological and pathological aspects of genetics but also emphasizes the measures to prevent it. The genetics in Ayurveda is hence given much importance as the occurrences of genetic disorders are increasing day by day. So here an attempt is made to understand the concepts which was explained in ancient Ayurvedic books from the perspective of modern genetics

##### Effectiveness of Theoretical and Practical Courses in the Pharmacy Program: Feedback of Pharmacy Undergraduate Students

Mohammad Javed Ansari, Nehad J. Ahmed, Mohd Faiyaz Khan

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 79-86
https://doi.org/10.9734/bpi/caprd/v4/2855E

Background: The practical courses are considered critical for the development of skills and competency in the students taking professional programs such as bachelor in pharmaceutical sciences.  The curriculum of pharmacy needs continuing revision and assessment to effectively equip the students with the required skills and with the human values that are needed to become effective and responsible professionals. The feedback of stakeholders including students remain central to revision and updation of professional programs.

Objective: The objective of the present study was to investigate pharmacy undergraduate students' views regarding the effectiveness of theoretical and practical courses in the pharmacy program in Al Kharj, Saudi Arabia.

Methods: This study included a survey that was developed based on a literature review related to effectiveness of theoretical and practical courses. The data was collected using google form and the descriptive data were represented as a numbers and percentages.

Results: Over 71% students agreed that the courses with practical were comparatively more interesting than the courses that include only theoretical part. Additionally, more than 73% of the students agreed that the practical part helped them to understand the concepts of the course in better way. Only 26.53% of the students agreed that if the course containing theoretical only, it will be difficult to understand effectively and only 22.45% agreed that the courses containing practical only were difficult to understand effectively.

Conclusion: The study showed that pharmacy students had more interest in the practical learning as compared to theoretical learning. Pharmacy schools should ensure that their undergraduate pharmacy programs include enough credit hours of practical courses.

##### Determining the Serum Psedocholinesterase Levels Following Diazinon Poisoning in Relation to Liver Function-Prognostic and Therapeutic Value

K. Swarnalatha, B. Surya Prakasa Rao, S. Sharon Sonia

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 87-94
https://doi.org/10.9734/bpi/caprd/v4/14041D

Background: Study of serum pseudo-cholinesterase (PChE) levels gives the knowledge of the therapeutic efficacy and severity of liver dysfunction & serves as a prognostic & therapeutic index of liver injury in individuals with Diazinon poisoning with or without alcoholism.

Methods: Blood samples were collected from normal male adults as control and PChE is estimated. Blood samples were taken on the 1st day and on 5th day for pseudocholinesterase estimation, from diazinon poisoning patients with or without alcoholism,attending  local hospitals. Serum PChE was estimated.

Results: Serum PChE was estimated among the normal healthy male adults & taken as the normal value. Among 30 normal adults, the control value of PChE ranged between 125 and 321 $$\mu$$mol/ml with 212 as the mean. Following the treatment with atropine, PAM(Pyridine-2-Aldoxime) and blood transfusion, blood samples were estimated on 5th day, among patients with diazinon poisoning. Their mean value was found to be 200 $$\mu$$mol/ml. There is a tendency of rise of level of serum PChE in the non-alcoholics with diazinon poisoning. Recovery of serum PChE levels towards normal value is satisfactory. Among individuals with alcohol and diazinon poisoning, on 1st day, the serum PChE is comparatively lower. The value is 100 $$\mu$$mol/ml. This unsatisfactory response is probably due to additional hepatotoxicity of alcohol and diazinon poisoning.

Conclusions: In diazinon poisoning without alcoholism, the drugs' prognostic and therapeutic efficacy is superior to that of alcoholics. As a result, there is a possibility of requiring hepatoprotective measures.

##### Influential Study of Green Tea Leaf Extracts (Camellia sinensis L.) on Male Reproductive System of Albino Rats

Shyamal Kanti Das, Soumendra Nath Karmakar

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 95-104
https://doi.org/10.9734/bpi/caprd/v4/14442D

Present study has been undertaken to observe the efficacy of herbal product- Green tea leaf extract (GTLE). The objective of this study is also to determine the simple possible way out of male castration parallel to surgical method. This herbal agent used in this experiment, has shown great influence on male reproductive system functionally as well as morphologically. The extract was made using the method of Wei. H. et al.  During a 26-day period, the extract was given to two different experimental animal groups at two different doses. Following treatment, it was discovered that the weight of the testis was significantly reduced, as opposed to the normal weight gain of all the animals. When compared to the control animal group, the treated groups had lower sperm count and motility. In comparison to the control group, enzymes such as SGPT and SGOT were normal, as were other blood parameters such as glucose and protein. Testosterone levels were reduced in the treated groups. In the treated groups, FSH and LH levels were also altered. Histological examination revealed that spermatogenesis was inhibited, as evidenced by the disintegration of testicular seminiferous tubules. According to the findings of this study, GTLE has a potent castrative effect on the male reproductive system in a dose-dependent manner.

##### Toxicity of Chromium on the Histopathological Changes in Gill and Liver of Fresh Water Fish Labeo rohita Fingerlings

P. Naga Jyothi, P. Sreenivasulu

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 105-111
https://doi.org/10.9734/bpi/caprd/v4/13419D

The present study is aimed to assessing the toxicity of the heavy metal chromium on the histology of labeo rohita fingerlings was studied. The fingerlings were exposed for 10,20 and 30 days in 10% sublethal concentration of 96 hrs Lc5o of chromium (3.5ppm). During this period fishes were fed with artificially prepared food (on the 10th, 20th, 30th day fishes) were taken out, sacrificed and the tissues of gill and liver were excised out. The Gill exposed to sub lethal concentration of chromium showed mild histological study during 10 days, of exposure. After 30 days fusion of gill lamellae, hypertrophy and degeneration of epithelium is prominent. Liver lesions consisted of vacuolation, degeneration of hepatocytes and degeneration of cell boundaries of hepatocytes. These result showed that the degree of distortion of the gill concentration of the metals was found to be dose and time dependent. Effect of chromium on various biochemical and metabolic enzymes of gill and liver of fresh water fish Labeo rohita were observed. Histopathological changes in gill and liver of fresh water fish Labeo rohita  undergoes heavy metal stress.

##### Study about Nano Polyphenol: Biomaterial in Functional Food and Its Preparation

Pham Thanh Thuan, Pham Van Thinh, Pham Thi Thanh Thao, Truong Ngoc Minh

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 112-131
https://doi.org/10.9734/bpi/caprd/v4/2915E

Polyphenols are diverse in structure and bioactivities, found in all plants and some animals, and include lignin, flavonoids, polyphenols, phenolic acid, and stilbenes. They are appreciated in antioxidant, anti-cardiovascular and application of them for humans, wherein polyphenol use for baby and pregnant woman still have numerous questions, simultaneously nano polyphenols are of great interest in recently. Hence, the chapter focused on polyphenols (define, classification, structure, and resources), their activity and mechanisms (antioxidant and anti-cardiovascular), use for baby and pregnant women, and the preparation methods of nano polyphenols (ten extraction methods of polyphenols and eleven methods of nano polyphenol preparations). Nanopolyphenols are necessary for future functional foods and medicine, for humans against disease and aging, but limited to use in pregnant-trimester women and children under 18 years old.

##### In vitro Production of Secondary Metabolites Reserpine and Ajmalicine in Rauvolfia Serpentina (L.) Benth.

Gyanendra Tiwari, M. K. Tripathi, Sushma Tiwari, Niraj Tripathi, Devi Singh Uikey, R. P. Patel

Current Aspects in Pharmaceutical Research and Development Vol. 4, 2 November 2021, Page 132-152
https://doi.org/10.9734/bpi/caprd/v4/2136C

Rauvolfia serpentina is an erect evergreen, woody perennial shrub and usually recognized as Sarpgandha Main institutes of sarpgandha roots are reserpine, rescinnamine, deserpidine and yohimbine and the root part of the plant is employed in several Ayurvedic polyherbal formations viz., sarpgandha vati. When efficient and reproducible plant regeneration systems are available, in vitro culture is an important experimental tool in medicinal and aromatic crops. Experiments were carried out to quantify secondary metabolite production in Rauvolfia serpentina from filtrate of callus and cell suspension cultures. Reserpine and ajmalicine were found infiltrate of both one-month-old callus and cell suspension cultures.  The culture medium MSD.5IB (MS+1.0 mgl-1 2,4-D + 0.5 mgl-1 IBA) recovers the most reserpine content in both callus and cell suspension cultures after one month. The amount of reserpine in a liquid medium decreased dramatically as the concentration of 2,4-D in the medium increased. When the concentration of 2,4-D was increased, the concentration of Ajmalicine in both callus and cell suspension cultures decreased linearly. These products may be further produced in commercial scale in bioreactor by using raw biomolecules for commercial purposes.