IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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SEPTEMBER 2019
1

“LIQUID PHASE SYNTHESIS OF COUMARINO BENZIMIDAZOLES FOR ANTIMICROBIAL ACTIVITY”

Singh Mukesh*, Kurmi Mukesh
Birgunj Pratimachowk, Ward No-18, District:-Parsa, Zone:- Narayani (Nepal).

The chemistry which is used to peptide synthesis that replaces insoluble cross-linked resins with soluble polymer supports in a strategy termed as liquid-phase organic synthesis (LPOS).This advance recent approach has been modified sufficiently that reagents and catalyst are now being bound to soluble polymer supports for use in solution-phase combinatorial synthesis. Several different types of polymers have been investigated as supports in LPOS and also incorporated for the synthesis of peptide oligosaccharide and oligonucleotide synthesis. The most commonly used soluble polymer support is polyethylene glycol (PEG). The wide acceptability of PEG is directly linked to its broad solubility profile: soluble in dimethylformamide, dichloromethane, toluene, acetonitrile, water, and methanol .Coumarino benzimidazole derivatives were found to possess various activities which includes anti bacterial, anti protozoal , antifungal, anti inflammatory , anti allergic agents, anthelmentic activity , anti-parasitic activity, cytotoxicity and DNA topoisomerase I inhibitors activity . More ever many research groups have synthesized various benzimidazole compounds and tested for antiviral anti neoplastic and anti filarial agents.Based on these findings, we have synthesized various coumarino benzimidazole and screened for anti microbial activity. It was found that the derivatives S1, S2, S3 and S4 have shown significant antimicrobial activity against gram –ve bacteria with zone of inhibition high as compared to S5 - S8 and the derivatives S1-S8 do not show any significant activity against gram +ve organism which shown in table no.1. 


 


2

DEVELOPMENT OF NOVEL CO-PROCESSED EXCIPIENTS FOR THE DESIGN OF FAST DISSOLVING TABLETS

Sunil Aute, S B Shirsand, Shailashri, Amruta and S A Baig
Department of Pharmaceutical Technology, H.K.E. Society’s College of Pharmacy, Sedam Road, Gulbarga- 585 105, India.

Co-processed excipients were prepared by Spray drying. In Spray drying method, MCC: Mannitol: Aerosil in different ratios (26:70:4, 28:70:2 and 30:70:0) were used. The developed excipients were evaluated for compressibility index (Carr’s index), Hausner’s ratio and flow properties (angle of repose) in comparison with physical mixture of the excipients. The angle of repose of Co-processed excipients was found to be <30o which indicate good flow in comparison to physical mixture of the excipients, due to micronization, a very regular particle size is achieved, Carr’s index in the range of 8.00-12.00% and Hausner’s ratio in the range of 1.00-1.13. Fast dissolving tablets of Repaglinide were prepared using the above Novel co- processed excipients and evaluated for pre-compression and post-compression parameters. Among the tablets prepared, the Novel Co-processed formulations MCC: Mannitol: Aerosil in (26:70:4) ratio was found to be promising and displayed a dispersion time of approximately 30.66 s. Wetting time was found to be 29.66 s. which facilities its faster dispersion in the mouth. Stability studies of promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time. IR-spectroscopic studies indicated that there are no drug-excipient interactions. It can be concluded from the present work that co-processed excipients used in Repaglinide fast dissolving tablets were found to be superior in flow characteristics in comparison with the physical mixture of same excipients. 


 


3

FORMULATION AND EVALUATION OF FAST DISSOLVING TELMISARTAN TABLET BY INCLUSION COMPLEXATION KNEADING METHOD

Sandeep.Ashokrao Wathore*
MUPS College of Pharmacy (B.Pharm), Degaon-444506, Dist.Washim (MS), India.

Telmisartan is a potent, long?lasting, nonpeptide antagonist of the angiotensin II type?1 (AT1) receptor that is indicated for the treatment of essential hypertension. It selectively and insurmountably inhibits stimulation of the AT1 receptor by angiotensin II without affecting other receptor systems involved in cardiovascular regulation. Poor water solubility is the main constant for its oral bioavailability. The rationale of this study to enhance solubility and dissolution of the drug by preparing its complex with ? cyclodextrin. In the present study attempt has been made to prepare, formulate and characterize inclusion complex of Telmisartan with ? cyclodextrin. The inclusion complex prepared by kneading method. The inclusion complex containing Telmisartan:? cyclodextrin (1:5) was further formulated into fast dissolving tablet by direct compression technique using superdisintegrant like sodium starch glycolate. The prepared complex were characterize using FT-IR, DSC and finally fast dissolving tablet were evaluated for various pharmaceutical characteristics viz. Hardness, % Friability, Weight variation, Wetting time, Drug content and in-vitro dissolution profiles. 


 


4

UNDERSTANDING OF KNOWLEDGE, ATTITUDE AND PRACTICE ABOUT ANTIBIOTIC USE AMONG MEDICAL STUDENTS AND GENERAL PUBLIC

Dr. Sadiksha Shrestha, Dr. Puja Das, Dr. Akhila Sivaraj, Dr. Anju Sugathan, Dr. Geetha Jayaprakash
RR College of Pharmacy, Chikkabanavara, Bangalore, 560090/RGUHS.

Antibiotics are among the most widely used class of drugs in hospitals, and they are really important to be used optimally otherwise emerging resistant pathogens will interfere with treatment outcomes. The study was conducted for a period of six months. An Institutional and community based cross-sectional and prospective study. Out of 135 participants, 66(48.9%) were males and 69(51.1%) were females. Analysis of knowledge about antibiotics and attitude towards it among age group (26-33) and (34-42) showed 50-50 results, indicating more awareness about antibiotic is necessary for this age group people. More number of participants were from pharmacy faculty which were 60 (44.4%). Students were participated in more number which was 105 (77.8%) . Survey on knowledge and attitude of participants based on gender, we found both more good knowledge(72.2%) as well as more positive attitude(63.6%) in male. Pharmacy students had more good knowledge (85%) and positive attitude (70%). Students had more good knowledge (68.6%) and positive attitude (57.1%). Age group of 18-25 years was found to have more good knowledge (76.7%) and positive attitude (70%) regarding antibiotics .The intended correct response to knowledge related questions was given correctly by students. Attitude towards usage of antibiotics is clearer among students of medical background. However, students show better attitude regarding antibiotic usage. Students and service people showed good understanding regarding antibiotic usages. Medical students showed better understanding, more good knowledge; as the mean value for each domain was slightly higher for medical background students. 


 


5

IMPORTANCE OF PHARMACOVIGILANCE AND OUTCOMES OF CLINICAL PHARMACY SERVICES IN INDIAN HEALTH CARE SYSTEM

Lavanya Ravi1, Varanasi Vasanthi Krishna Priya1, Navya Devi reddy1, Dr. A. Meenakumari2, Dr. Venkata Rama Rao1, Prof. Rama Rao Nadendla1, Dr. K. Pavan Kumar3
1Chalapathi Institite of Pharmaceutical Sciences, Lam, Guntur.
2AMC Coordinator, Guntur Medical College, Guntur.
3ADR Monitoring Centre, Govt General Hospital, Guntur.

BACKGROUND: The main aim was to collect information about the adverse effects of medicines in the tertiary care hospital, to create awareness of the need for Pharmacovigilance and how this contributes to protect patients from harm, to help patients as well as health professionals to make smart therapeutic decisions. Promoting Proper awareness about the clinical Pharmacy services is needed. In future we hope that these services will promote the better patient care in India. METHODOLOGY: Observational cross sectional study was conducted to assess the Adverse drug reactions, for a period of six months in a tertiary care hospital in south India. For promoting better medication use, ensuring that patients receive appropriate pharmacotherapy, thus minimizing the risk of unfavorable outcomes of pharmacotherapy. Adverse drug reaction forms were collected from all health care professionals i.e., (nurses, graduates, under graduates (UG,PG), general practioners and specialists. RESULTS:- In Our total number of 226 Adverse drug reactions were reported by health care providers. Most of ADRs occurred with oral drugs (56.1%), followed by IV routes (13.7%) and the most common affected organ system was Integumentry system (50.6%), followed by Gastro Enterology (46%), CNS(28%). The most serious drug reactions were due to hospitalization/prolonged (68.75%), followed by life threatening (31.25%) and majority of diverse drug reactions were due to Antibiotics (19.9%), Anti-psychotics (16.8%), Chemotherapy (9.73%).Level of participation of different health-care providers Most of the reports were generated by nurses (n= 100,44.24 % of all reports), followed by under graduate students (n= 60, 26.5% of all reports),General practioners and specialists (n= 20, 8.84%). CONCLUSION: In our study we observe that due to inadequate knowledge gaps with regard to ADR reporting still exist among nurses, under graduate medical practioners, General practioners and specialists especially in our country where the role of pharmacists is still in transition from being product oriented to patient oriented. The study concludes that involving clinical pharmacist services in patients care can significantly helps to identify, resolve and prevent the ADRS in the hospital thereby enhancing the patient’s safety. 


 


6

DEVELOPMENT AND VALIDATION OF RP-HPLC AND TLC METHODS FOR SIMULTANEOUS ESTIMATION OF PARACETAMOL, THIOCOLCHICOSIDE AND ACECLOFENAC IN BULK AND COMBINED PHARMACEUTICAL DOSAGE FORM

Ramzya I. Elbagary¹,2, Ehab F. Elkady2, Magda M. Ibrahim3 and Shaymaa M. Goubran3*
1Pharmaceutical Chemistry Department, Future University in Egypt, Cairo 12311, Egypt.
2Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr el Aini Street, 11562 Cairo, Egypt.

3Department of Analytical Chemistry, National Organization for Drug Control and Research (NODCAR), Cairo, Egypt.

Two accurate, precise, and sensitive methods were developed for the simultaneous determination of ternary mixtures containing paracetamol (PAR), thiocolchicoside (THIO) and aceclofenac (ACE) in bulk powder and combined dosage form without prior separation. The first method is RP-HPLC which depended on isocratic elution using an agilent C18 column and mobile phase consisting of ammonium acetate buffer (pH 7) – methanol – acetonitrile--triethylamine (50:30:20:0.1, v/v) pumped at flow rate of 1 ml/min with UV detection at 258 nm. The second method is based on TLC separation of the three drugs followed by densitometric measurements of their spots at 248, 380 and 275 nm for PAR, THIO and ACE, respectively. The separation was carried out on silica gel 60 F254 using ethyl acetate-toluene-methanol –glacial acetic acid (2:2:1:20.25 v/v/v/v) as a developing system. The suggested methods were tested using laboratory-prepared mixtures and were successfully applied for the analysis of pharmaceutical preparations. The methods retained their accuracy and precision when the standard addition technique was applied. HPLC method was applied over the concentration range (1-120 ?g/ml) for Paracetamol, (0.8-60 ?g/ml) for Thiocolchicoside and (10-80 ?g/ml) for Aceclofenac while densitometric method was linear over the concentration range (200-10000ng/spot) Paracetamol, (10-1000ng/spot) for Thiocolchicoside and (100-10000ng/spot) for Aceclofenac, respectively. The developed RP-HPLC and TLC densitometric methods are rapid, sensitive and accurate and can be applied in quality control laboratories for routine determination of Paracetamol, Thiocolchicoside and Aceclofenac simultaneously in their ternary mixture without prior separation. 


 


7

AN OVERVIEW ON NEWER ANTIDIABETIC AGENTS

Maliha Nishath, Amber Azeem, Sai Veena, Kadarla Rohith Kumar*
Department of Pharmacy Practice, Sree Chaitanya Institute of Pharmaceutical Sciences, Thimmapur, Karimnagar, Telangana, India-505527.

Diabetes mellitus is a group of metabolic diseases characterized by chronic hyperglycemia resulting from defects in insulin secretion, insulin action. Different classes of diabetes mellitus type1, type2 ,gestational is summarized. It is predicted that the prevalence of DM in adults of which type2 is becoming prominent mostly in developing countries. The treatment strategies are listed and many new drugs are currently in development for treatment of diabetes including more products with new mechanisms .Drugs with application submitted for US food and Drug administration (FDA) approval and drugs currently in phase3 clinical trials are summarized.Diabetes mellitus is a group of metabolic diseases characterized by chronic hyperglycemia resulting from defects in insulin secretion, insulin action. Different classes of diabetes mellitus type1, type2 ,gestational is summarized. It is predicted that the prevalence of DM in adults of which type2 is becoming prominent mostly in developing countries. The treatment strategies are listed and many new drugs are currently in development for treatment of diabetes including more products with new mechanisms .Drugs with application submitted for US food and Drug administration (FDA) approval and drugs currently in phase3 clinical trials are summarized. 


 


8

BILATERAL PEDAL EDEMA, HEPATOTOXICITY AND CUTANEOUS REACTIONS DUE TO OFLOXACIN-A CASE REPORT

Talha Jabeen1*, Mohd. Abdul Khader1, Kothakoti Greeshma1, Ramanachary Namoju2
1Bhaskar Pharmacy College, Moinabad, Hyderabad, Telengana, India.
2GITAM University, Department of Pharmacology, Bhaskar Pharmacy College, Moinabad, Hyderabad, Telengana, India
.

Bilateral pedal edema is a common adr associated with many medications. If left untreated, it can pose various complications and interfere with the normal activities of daily living. To the best of our knowledge, there is no data yet published on bilateral pedal edema due to Ofloxacin. Hepatotoxicity and cutaneous reactions to drug therapy are the major health problems and identifying and omitting the offending drug at the earliest holds the keystone in management and prevention from a more severe form. We report a case of Ofloxacin induced bilateral pedal edema, hepatotoxicity and cutaneous reactions in a 72 year old Indian male that got resolved after withdrawal of the drug. The adverse reaction assessment was done using "Naranjo's causality assessment scale" which showed a 'probable' type of reaction with Ofloxacin in edema, cutaneous reactions and hepatotoxicity.Drug induced reactions are major threat for patient's quality of life and often go unnoticed.This case emphasizes that all clinicians should be aware of Ofloxacin induced adr's and it should be added to the list of drugs associated with the development of bilateral pedal edema. 


 


9

A REVIEW: REGULATORY REQUIREMENTS OF DRUG MASTER FILE IN CONTEXT TO GHANA

Rushikesh B. Katkar1*, Sunil T. Galatage2, Sandip M. Honmane3, Supriya Darandale4
1Jr. Executive Quality Assurance Department Shri Anand Life Science Belgaum, Karnataka.
2Sant Gajanan Maharaj College of Pharmacy Mahagaon, Kolhapur, Maharashtra.
3Annasaheb Dange College of B. Pharmacy, Ashta. Sangli, Maharashtra.
4LSDP College of Pharmacy Pune, Maharashtra.

Drug Master Files are required in most African countries as supporting documents for the registration of drug products. Africa is world’s second fastest growing pharmaceutical market. The CGAR of African Pharmaceutical market is 11.6%. African people suffer from numerous diseases. The local pharmaceutical market is weak and insufficient to meet the demand of such diseased condition and so Africa relies heavily on externally developed and procured drugs. This combination of economic strength and prevalence of diseases is already driving a demand for medicines across Africa. DMFs generally contain information pertaining to the chemistry, manufacturing and controls (CMC) sections of the drug submission and reflect the drug’s identity, strength, purity and quality. Ghana and Australia which are consider as highly regulated markets (HRMs). In GHANA, DMF filing was done through New Drug Submission (NDS) for both drugs and biologic products. They use MF terminology for DMF which contain four types of MASTER FILE- ASMFs, CCS MFs, Excipient MFs, Drug product MFs. In AUSTRALIA different application processes and regulatory requirements apply depending on the type of therapeutic goods that is applied. They consist of eight phase for DMF registration. Where EU guidelines adopted in Australia include references to EU legislation. Now from 2018 onwards most of the regulated countries will use eCTD or their electronic format for their DMF submission. 


 


10

SINGLE VERSUS DUAL ANTI-PLATELET DRUG THERAPY IN THE MANAGEMENT OF CORONARY ARTERY DISEASE, ADDING ASPIRIN TO CLOPIDOGREL VERSUS CLOPIDOGREL ALONE

Uzma Farheen*
Department of Pharmacology, Sultan-Ul-Uloom College of Pharmacy, Hyderabad, Telangana State, India.

Introduction- Coronary artery disease is one of the most common amongst the heart diseases. It occurs when the blood supplying arteries to the heart becomes very narrow and hard due to the plaque buildup. Therefore, the single or dual antiplatelet drug therapy (clopidrogrel + Aspirin or clopidogrel alone) is widely accepted and challenging strategy in the patients with Coronary artery disease to reduce myocardial infarction and stent thrombosis. The outcomes and prescribing patterns associated with these therapies are observed in this study. Method- The retrospective study was conducted for a period of 8 months in which 150 case reports/ prescriptions with single anti-platelet therapy (clopidrogrel) or Dual anti-platelet therapy (clopidogrel + Aspirin) were collected and noted in a data form. The data obtained is used to observe the prescribing patterns and their outcomes. Results- The data was collected from 150 patients in Medical intensive care unit (MICU), Critical intensive care unit (CICU), Intensive care unit (ICU), and general ward. The male to female ratio was found to be 103 (68.66%): 47 (31.33%). The usage of Single Anti-Platelet Therapy was found to be quite lesser than Dual Anti-Platelet Therapy. The patients with Dual anti-platelet therapy were at the higher risk of life threatening bleeding and ischemic complications but the use of dual anti-platelet therapy has found to be beneficent in reducing the myocardial infarction and stent thrombosis. The choice of dual anti-platelet therapy or single anti-platelet therapy depends upon the duration of patients, their profile, risk, benefits and management therapy. Conclusion- The main focus of our study was the prescription of Aspirin and Clopidogrel both as single drug and in combination, the medication given while admission of patient in the hospital were 20, (13.33%) of Aspirin, 7, (4.66%) of Clopidogrel and 25, (16.66%) Aspirin + Clopidogrel and medication given while discharging of patient in the hospital were 46, (37.70%) of Aspirin, 25, (20.49%) of Clopidogrel and 51, (41.80%) Aspirin + Clopidogrel 65.33% were Other Miscellaneous drugs. 


 


11

POLLENS-A TOOL FOR PHARMACOGNOSY

Shivamanjunatha M P, Mahesh C D, Naveen V
Department of Dravyaguna, Sri Sri College of Ayurvedic Science and Research, Bangalore, Karnataka, India-560082.

Medicinal plants are the natural sources of drugs to cure various ailments. There are number of ancient literatures about the natural drugs, these literatures are usually found in Sanskrit and in vernacular language. Names of these botanicals are based on the morphology of officinal part. Now a day most of the phyto-pharmaceutical companies are depends on wanders for raw material supply in bulk. The wanders were collecting herbs in the wild without knowing the difference among the herbs, sometimes intentionally. In case of closely related species, it is very difficult to identify and differentiates the species. Our approach is to investigating the pollens of medicinal plants. Pollens play a very important role to identify the species due to their uniqueness in the shape, apertures, polarity, ornamentations and symmetry. Present investigation was conducted on pollens of 25 medicinal plants of varied habits belonging to 12 families of angiosperms. Medicinal plants Cardiospermum canescens. Wall and Cardiospermum halicacabum. L., belongs to Sapindaceae have triangular shaped pollens but they have difference in the apex of their angular structure. Whereas in Malvastrum coromandelianum. (L) Garcke, Hibiscus sabdariffa. L and Abelmoschus moschatus. Medik, belonging to Malvaceae, all three medicinal plants have almost spheroidal pollen grains and there is difference in spine’s shape, arrangement and density. Investigated pollens of 25 medicinal plant species are unique in any one or more features of pollen parameters. Pollens of botanicals belonging to the same genus or different genus of the same family may have a similar shape and structure but there is a minor difference in the shape, aperture, polarity and other parameters of the pollens. Each botanical has its own unique pollen as a finger print. So pollen can be used as a one of the parameter in pharmacognostic studies of natural drugs in addition to organoleptic, microscopic, physico-chemical and other parameters. It can be include to The Ayurvedic Pharmacopeia of India. 


 


12

FORMULATION DEVELOPMENT OF ANTIMICROBIAL ZINC OXIDE NANOPARTICLE LOADED TRANS DERMAL PATCH BY USING 23 FACTORIAL DESIGN.

Sagar Kothawade1*, Udhhav Bagul1, Chandrakant Kokare1, Shubhangee Giikwad1, Rutuja Wakure1, Shubham Biyani2, Chetan Harne1
1STES, Sinhgad Institute of Pharmacy, Narhe, Pune (MH), 411041, India.
2School of Pharmacy S.R.T.M University, Nanded (MH), 431606, India.

Inorganic metal oxide nanoparticles are well known for significant antimicrobial activity. The zinc oxide nanoparticles have potential to act as antimicrobial agent in microbial infections due to its unique properties. Zinc oxide nanoparticles prefer as an alternative for antibiotics. It having shorter half-life and poor bioavailability. In the present work, the Trans dermal patch of zinc oxide nanoparticles were prepared to extended the release as well as improve bioavailability. The Trans dermal patch was prepared by solvent evaporation method. The preliminary trial batches were formulated with different polymer viz. HPMC E15, HPMC E5, HPMC E3, sodium alginate, along with plasticizer used as PEG. The prepared batches were evaluated for weight variation, thickness, Folding endurance, tensile strength, Moisture content, and in-vitro drug release. Amongst all five formulation batches, batch no A4 containing HPMC E5 and PEG 20% of formulation has shown thickness 0.312, folding endurance 340-fold along with 100% drug release within 12 hrs. The compatibility study of drug and excipients was carried out by FT-IR spectroscopy. Based on the results, the batch No A4 was selected for optimization by 23 factorial designs. Optimised batch was evaluated for various parameter thickness weight variations, folding endurance, tensile strength, In-vitro % drug release. Optimised batch was subjected for stability studies were found to be stable. To avoid first pass metabolism and improve the bioavailability ZnO NPs is having promising antimicrobial agent and it can be formulated in transdermal patches for treatment of microbial infection.