IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
FEBRUARY 2018
1

SCREENING OF PHYTOCHEMICALS AND DETERMINATION OF TOTAL PHENOLIC CONTENT, ANTI-OXIDANT AND ANTIMICROBIAL ACTIVITY OF METHANOLIC EXTRACT OF PIPER NIGRUM LEAVES

Redina Sapam, Partha Pratim Kalita, Manash Pratim Sarma, Nayan Talukdar, Harajyoti Das
Assam Down Town University, Panikhaiti,Guwahati- 26, Assam, India.

The study involves two methods of methanolic extraction of the powdered leaves, which ensure all the plant components of the extracted for better results. Phytochemical analysis from the extracts was performed by using standard protocols. Total phenolic content was determined by Folin–Ciocalteau’s (FC) method. The antimicrobial susceptibility of the extracts was tested against E coli, Pseudomonas and Klebsilla sp. using agar disc diffusion method. Antioxidant property of the plant was evaluated using DPPH Method. The plant extracts were used at varying concentrations to ensure which plant extract and concentration causes the most inhibition. Phytochemical analysis of the extract indicated the present of phenol, tannin, terpenoid(except in heat extraction method of methanol extract) and carbohydrates while protein, flavonoid, steroidwere absent. The phenolic content in cold extraction of methanol extract is 360?g/ml of GAE or 0.36mg of phenolic compound and in heat extraction of methanol extract is 340?g/ml of GAE or 0.34mg of phenol compound were present. The cold extraction of methanol extract demonstrated the maximum zone of inhibition against Pseudomonas followed by E. coli and Klebsiella sp. In case of heat extraction of methanol extract the maximum zone of inhibition against Pseudomonas followed by E.coli and Klebsiella sp. were seen respectively. The plant showed a significant activity with both methods. Out of the two extracts cold extraction showed the maximum antioxidant activity (78.81% inhibition in 200?g/ml) with increase in concentration. The heat extraction method showed the maximum of 77.62% inhibition in 200?g/ml concentration which reveals the dose dependent increase in percentage of inhibitory activity.

2

FORMULATION AND EVALUATION OF TOPICAL MICROSPONGE BASED GEL OF TURMERIC

Suniti Shinde, Shamika Shirke, Mrs. Manisha Karpe,Dr. Vilasrao Kadam
Bharati Vidyapeeth’s College of Pharmacy, Sector-8, C.B.D. Belapur, Navi Mumbai – 400614, India.

A drug delivery system enables the introduction of a therapeutic substance in the body and improves its efficacy and safety by controlling the rate, time and place of release of drug in the body .One of these includes topical preparations. These are used for localized effect at the site of their application [3, 4] A new method approached in TDDS is microsponge. Microsponge drug delivery system is a patented, higher cross linked porous, polymeric microsponge that can entrap wide range of activities and release them with desired rate [3, 4] . With lots of synthetic and inorganic drugs used in the market for treatment of various diseases; natural drugs have also gained appreciation and still has high market demand even today. Natural drug helps by reducing toxicity and any adverse drug effects and thus adding for better pharmacological effect. Curcumin which is active ingredient obtained from the powdered dry rhizomes of the plant Curcuma longa (which is commonly called turmeric). It is widely used as a colouring agent, medicinal agent and as a spice in many food items. It also can be used for treatment for conditions ranging from flatulence, jaundice, hepatitis, pains and haemorrhage [5]. An approach is being made in combining the old tradition with the new technology to gain more appreciation in the market. This leads to the formulation of “Gel Loaded Turmeric Microsponge” as a Novel Drug Delivery.

3

“INFLUENCE OF NSAIDS ON BLOOD PRESSURE IN HYPERTENSIVE PATIENTS UNDER TREATMENT: A CROSS SECTIONAL STUDY”

Cherian Anish1, Mathew Cherry1, Geevarughese Merlin1, T.Chaitanya Kumar2*
1Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka, India.
2Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka, India.

Raised blood pressure is one of the leading risk factors for global mortality and is estimated to have caused 9.4 million deaths. There are chances of using anti-hypertensives and NSAIDs together with increasing age for a long time to treat many diseases.The objective of this study was to determine the change in blood pressure in hypertensive patients on Anti-hypertensives after consumption of NSAIDs. The cross-sectional analytical study was conducted for a period of 6 months.In our study out of 70 NSAID users, 55.71% were males and 44.29% were females and from 140 NSAID non users, 61.43% were males and 38.57% were females.26.67% of patients were having Diabetes mellitus as a comorbid condition along with hypertension.From all the covariates studied, light physical activity was 1.44 and moderate physical activity was 1.06 times more likely to have this influence than vigorous physical activity. A difference of 3.67mmHg in systolic blood pressure was noted between NSAID users and non-users.When comparing Amlodipine, Enalapril and Telmisartan, Telmisartan was the only drug that showed a significant difference in blood pressure after consumption of NSAIDs i.e, 8.35mmHg .Mostly prescribed NSAIDs were Diclofenac followed by Etoricoxib and Aspirin . We found that NSAIDs may increase blood pressure and may blunt the effects of many anti-hypertensives. The small increase in systolic blood pressure associated with NSAIDs seen in this study may not affect a physician’s decision to change the therapy, however in long term, such an increase would be associated with significant comorbidity consequences.

4

FAST DISSOLVING SYSTEMS: FDT VS FDF

R. Santosh Kumar, Sahithi Mudili
GITAM Institute of Pharmacy, GITAM University, Rushikonda, Visakhapatnam-45.

Fast dissolving drug delivery systems are ideal for all types of people, including for people who have swallowing difficulties, pediatric, geriatric, and bedridden patients. It is also for active patients who are busy, travelling and may not have access to water. Fast dissolving drug delivery systems includes both fast dissolving tablets and fast dissolving films. This type of drug delivery system disintegrates quickly once introduced into the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The active ingredients can be absorbed directly through oral mucosa into the systemic circulation bypassing the first pass metabolism. Hence, quicker onset of action, reduction in dosage and frequency, avoidance of gut wall and hepatic metabolism, and increase in bioavailability are eminent. This review article presents the common and differentiating features between the fast dissolving tablets (FDT) and fast dissolving films (FDF) and the list of common drugs which are manufacturing as both fast dissolving tablets and fast dissolving films.

5

DESIGN, OPTIMISATION AND EVALUATION OF ATENOLOL FAST DISSOLVING TABLETS EMPLOYING STARCH GLUTAMATE-A NEW SUPERDISINTEGRANT

R. Santosh Kumar*, A. Suresh
GITAM Institute of Pharmacy, GITAM University, Rushikonda, Visakhapatnam, A.P 530045, INDIA.

The purpose of the present study is to evaluate starch glutamate as a superdisintegrant in the formulation of fast dissolving tablets of poorly soluble drugs. Starch glutamate was synthesized by gelatinization process. The synthesized starch glutamate was subjected to physical and micromeritic evaluation. To establish as starch glutamate as a superdisintegrant, fast dissolving tablet of atenolol was prepared employing starch glutamate in different proportions in each case by direct compression method employing 23 factorial design. All fast dissolving tablets prepared were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), Dissolution efficiency in 5 minutes (DE5) and first order rate constant (K1).The starch glutamate prepared was found to be fine, free flowing slightly crystalline powder. Starch glutamate exhibited good swelling in water. The swelling index was 50% all micrometric properties indicated good flow and compressibility needed for solid dosage from manufacturing. All the fast dissolving tablets formulated employing starch glutamate were of good quality with regard to drug content, hardness and friability and fulfilled the official (IP/USP) requirements of compressed tablets with regard to the above mentioned physical properties. Starch glutamate was found to be a superdisintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, crosscarmellose sodium, with the atenolol and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5minutes.

6

“A STUDY ON PRESCRIBING PATTERN AND RATIONALITY OF ANTIBIOTICS IN THE POST OPERATIVE PATIENTS IN A TERTIARY CARE HOSPITAL”

Prasad Honey, Kurup.B.Shruthy, Thomas Soumya, N.Upendra, T.Chaithanyakumar*
Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka, India.

Surgical site infections are confined to the incisions and wounds that were exposed during operation. Surgical antibiotic prophylaxis is the use of antibiotics to prevent infections at the surgical site. Prescription pattern analysis issued to determine the prescribing frequency of commonly used antibiotics. Rational drug prescribing is defined as the use of the least number of drugs to obtain the best possible effect in the shortest period and at a reasonable cost. The objective of this study is to assess the prescribing pattern and rationality of antibiotics in the post operative patients. A prospective observational review of the antibiotic prescription was carried out in the post-operative department of a tertiary care teaching hospital, Davangere.150 case records of the patients were identified, assessed, evaluated and analyzed for the rational use of antibiotics for a period of 6 months. Among 150 prescriptions,64% surgery were done in general surgery department,26% were done in OBG department,10.67% were done in orthopeadics department. In 150 prescriptions, more no. of patients had received 2 antibiotics, followed by 3 antibiotics and most of them were given for five days of duration of treatment. Among 312 antibiotics, Cephalosporins 122(39.1%) class of antibiotics were frequently prescribed followed by metronidazole 76(24.35%). Most of the antibiotics were prescribed parenterally (96.47%). Our study provides insights into the patterns of antibiotic use, appropriateness of prescriptions and rationality of antibiotics in post operative patients based on ASHP guidelines and major, minor and moderate drug interactions, medication errors were found.

7

METHOD DEVELOPMENT AND VALIDATION FOR ESTIMATION OF ATOMOXETINE HCl BY USING RP-HPLC IN BULK AND TABLET DOSAGE FORM

Priyanka .T, Prof. M. Sumakanth, Bhavya Vani. Tuppa
RBVRR Women’s College of Pharmacy, Osmania university, Hyderabad, India.
Osmania University.

A simple, rapid and sensitive RP-HPLC method was developed by trail and error and validated for estimation of Atomoxetine HCl in bulk and tablet dosage form. Chromatography was carried out by using pre packed Luna C18,?(250 x 4.6mm) phenomenex column as a stationary phase with mobile phase containing a mixture of 0.1% Triethylamine (pH-3.5)adjusted with OPA:acetonitrile in the ratio of 50:50v/v. The flow rate was 1ml/min.The effluent was monitered at 271nm and retention time of drug is 3.0mins.calibraton curve was plotted with the range of 2-12?g/ml for atomoxetine HCl and the correlation coefficient was found to be 0.999. The percentage values for all the parameters was found to be not more than 2 for RP-HPLC . Validation studies revealed that method is specific, rapid, reliable and reproducible. The high recovery and low relative standard deviation and relative standard deviation confirm the suitability of the method for routine determination of Atomoxetine HCl in bulk and tablet dosage form. The developed method used for routine analysis of Atomoxetine HCl in pharmaceutical dosage form and method is developed and validated as per ICH guidelines.

8

TRANSDERMAL DRUG DELIVERY: A REVIEW

Bandi Ramesh*, Parre Rajeswari, Kamma Ramya, Boppana Sravya, Parchuru Arshad, Kappuravuri L Govardhani, Velpula Prameela.
Dept. of Pharmaceutics, Hindu College of Pharmacy, Amaravathi Road, Guntur-522002, A.P., India.

Transdermal drug delivery systems (TDDS), also known as “patches,” are dosage forms designed to deliver a therapeutically effective amount of drug across a patient’s skin. It’s a desirable form of drug delivery because of the obvious advantages e.g.convenient and pain-free self-administration for patients, avoidance of hepatic first. The first commercially available prescription patch was approved by the U.S. Food and drug administration in December 1979,which administered scopolamine for motion sickness. This review article covers brief outline advantages, skin pathways for transdermal drug delivery systems (TDDS), various components of transdermal patch, and approaches for preparation of transdermal patches, evaluation of transdermal system, general clinical considerations in the use of transdermal drug delivery systems and limitation of transdermal drug delivery systems.

9

STABILITY INDICATING METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF SOFOSBUVIR, VELPATASAVIR AND VOXILAPREVIR IN A PHARMACEUTICAL FORMULATION BY UHPLC

K. Kranthi Kiran1*, Dr. A. Srinivasa Rao1, Prof. D. Gowri Sankar2
1Pharmaceutical Analysis and Quality Assurance Division, Sri Vishnu College Of Pharmacy, Bhimavaram-534261.
2Department of Pharmaceutical Analysis and Quality Assurance, University College of Pharmaceutical Sciences, Andhra University, Visakhapatnm-530003, India.

A Precise, accurate, Robust, Rugged, Specific, Stability indicating RP-UHPLC method has been developed and validated for the estimation of anti viral drugs Sofosbuvir, Velpatasavir and Voxilaprevir in pharmaceutical dosage form(Tablets) was carried out on Agilent UHPLC with Acquity BEH C18 (50 x 3.0mm. 1.7?m) column with mobile phase contains 0.05% Orthophoshoric acid: Acetonitrile: Methanol (40:40:20) at a flow rate of 1.0mL/min, detection was carried out at 270nm. The retention time of the Sofosbuvir, Velpatasavir and Voxilaprevir 2.04, 3.50&5.37mins respectively. The method produces linear responses in the range of 200?g/mL to 600?g/mL for Sofosbuvir, 50?g/mL to 150?g/mL for Velpatasavir, 50?g/mL to 150?g/mL for Voxilaprevir with correlation coefficients(r2 1.00), The % Recoveries between 100.5 to 101.7 for Sofosbuvir , 99.0 to 99.9 for Velpatasavir and 100.3 to 101.1 Voxilaprevir. Peak purity was more than 0.999 of main peaks in all forced degraded samples.

10

“MEDICATED CIGARETTES: A PROMISING UNUSUAL DOSAGE FORM”

Shivprasad H. Majumdar, Tatyaba V. Madane
Satara College of Pharmacy, Satara.

Several route of administration of drug have not only been described but also practiced for numerous times. Depending upon the physical property of drug it can be injected, swallowed, applied, instilled etc by selecting suitable dosage form for the administration. Similarly the medicines can be administered through smoke by the use of medicated cigarettes. Convenience of administration and patient compliance are gaining significant importance in the design of dosage forms. Recently, more emphasis is laid down on the development of an organoleptically elegant and patient-friendly drug delivery system for patients. Novelty in terms of dosage form designing is needed for several reasons like taste masking, better therapeutic efficacy etc but the primary objective is better patient compliance. Unusual dosage form compared to routine / conventional dosage forms are better in terms of its user friendly nature. So, better patient compliance can be achieved. We hesitate to talk about “Cigarette”, but this technique could be used for delivery of medicine; it could be interesting to study and apply for research.! The concept of medicated cigarette is discussed in detail with emphasis on history, development and future scope in this field.

11

CASE REPORT ON THROMBOLYTIC THERAPY ASSOCIATED PONTINE HAEMORRHAGE AND ITS RISK FACTORS.

Dr. Soniya Davis1*, Dr. Anju Paul1, Dr Chinnu Reeba George1, Dr. Priya Thomas1, Dr. Arun Kumar2, Dr. Jessy Thomas3
1Department of Clinical Pharmacy, Lisie Hospital.
2Department of Neurology, Lisie Hospital.
3Department of Paediatric, Lisie Hospital

Thrombolytic therapy is of proven and substantial benefit for patients with Acute Ischemic Stroke. But the intracranial haemorrhage associated with thrombolysis said to be the most dreaded complication. This is a case report of thrombolysis induced intracranial haemorrhage that lead to the death of a 65year old male patient with the history of Acute Ischemic Stroke. Factors that influence risk of thrombolytic therapy associated intracranial haemorrhage are low body weight, age greater than 65years, history of Hypertension, Diabetes Mellitus, use of anticoagulant drugs before admission, heparin therapy during admission, smoking and alcoholism. Therefore patients who are at increased risk should be recognised earlier. One suggestion would be to lower the dose of thrombolytic agents, recombinant tissue Plasminogen Activator (rtPA) in patients who are at greatest risk. If these risks can be minimised through better recognition of risk factors and appropriate dosing, then the thrombolytic therapy can be effectively used.

12

DEVELOPMENT AND APPLICATION OF LIQUID CHROMATOGRAPHIC METHOD FOR SIMULTANEOUS DETERMINATION OF OMBITASVIR, PARITAPREVIR AND RITONAVIR IN FIXED TABLET DOSAGE FORM

Mrs. Parbati Kirtania1, Dr. Nemala Appala Raju
Sultan-ul-Uloom College of Pharmacy, Road No.3, Banjara Hills, Hyderabad 500034.

Technivie® is a fixed-dose combination of ombitasvir, a hepatitis C virus NS5A inhibitor, paritaprevir, a hepatitis C virus NS3/4A protease inhibitor, and ritonavir, a CYP3A inhibitor and is indicated in combination with ribavirin for the treatment of patients with genotype-4 chronic hepatitis C virus (HCV) infection without cirrhosis. Developing a single analytical method for the estimation of individual drugs in a quad pill is very challenging, due to the formation of drug-drug and drug-excipient interactions. The present study demonstrates the applicability of chromatographic method to develop a new, sensitive, single HPLC method for the simultaneous quantitative determination of four antiviral agents in fixed pharmaceutical dosage form. Chromatographic separation of the four antiviral drugs was achieved by using a gradient elution at a flow rate of 1.5 mL/min on Inertsil ODS 3V C18 column (250m×4.6mm, 5?m particle size, 100Å pore size) at ambient temperature. Mobile phase A of the gradient solvent system was KH2PO4 (0.03M) in 1000 ml of water and by adjusting the pH to 3.2 with dilute ortho-phosphoric acid and mobile phase B was Methanol and water in the ratio of 85:15 v/v. UV detection at 265 nm was employed to monitor the analytes. A linear response was observed for Paritaprevir over the concentration range 30–180 ?g/ mL for Paritaprevir, 5-30?g/ mL of Ombitasvir and 20-120 ?g/ mL Ritonavir. Limit of detection (LOD) for Paritaprevir, Ombitasvir and Ritonavir were 0.075?g/mL, 0.125?g/mL, 0.00575?g/mL and 3?g/mL respectively. Limit of quantification (LOQ) for Paritaprevir, Ombitasvir and Ritonavir were 0.225?g/mL, 0.375?g/mL, and 0.015?g/mL respectively.