IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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JULY 2015
1

PHYSIOLOGICALLY BASED PHARMACOKINETIC MODELLING: REVOLUTIONISING DRUG DISCOVERY AND PHARMACOKINETIC STUDIES

R. S. Nikam, V. N. Garge, Dr. V. J. Kadam

BharatiVidyapeeth’s College of Pharmacy, C.B.D. Belapur, Navi Mumbai.

Abstract

Physiologically based pharmacokinetic (PBPK) models are the mathematical expressions that predict the drug disposition based upon its physicochemical, physiological and biochemical properties. This review article discusses the principles and applications of the PBPK model.Designing the model for a particular drug and tissue/ organ/ full body is a systematic process which takes into consideration the physicochemical and biochemical properties of the drug, the species involved in the study, route of drug administration and parameters that need to be included in the model is decided. Steps involved in modelling are designing model according to its application, setting mathematical equations and validation of model. Accuracy of PBPK model depends upon extent of detailing incorporated in model designing and hence upon its closeness to real physiology. Considering involvement of tremendous amount of data and complexity of models, software such as Gastroplus, PK-Sim, MATLAB, PKQuest etc. are used. PBPK models have great scope for use in the area of Drug Discovery. They can precisely predict the pharmacokinetics of a particular drug for a particular model. Hence they are useful in the drug discovery process, for making the personalised medicines, for prediction of the possible toxicity and carcinogenicity of a particular environmental xenobiotics. But use is limited because of large amount of data is needed to be processed and expert personal are required to design such complex models.

2

AN EPIDEMIOLOGICAL STUDY OF HEMODIALYSIS PATIENTS IN A TERTIARY CARE TEACHING HOSPITAL

Dr. S. Chandra Babu1, K. Purushothama Reddy2, Rubeena Begum Hakeem3, Dakshiraju Naresh & Mallesh Mandha3

1Associate Professor, MBBS, MD, Rajiv Gandhi Institute of Medical Sciences, Kadapa, A.P – 516003.

2Assistant Professor, Department of Pharmacy Practice, P. Rami Reddy Memorial College of Pharmacy, Kadapa, A.P – 516003. 

3Pharm.D Intern, Department of Pharmacy Practice, P. Rami Reddy Memorial College of Pharmacy, Kadapa, A.P – 516003.

Abstract

Chronic kidney disease is a progressive loss of function occurring over several months to years, and characterized by the gradual replacement of normal kidney architecture with interstitial fibrosis. Chronic kidney disease globally resulting in 735,000 deaths in 2010 up from 400,000 deaths in 1990,to develop the comprehensive description of the epidemiology of hemodialysis treated patients a prospective observational study was carried out between March 2013 and September 2013 at Rajiv Gandhi Institute of Medical sciencesan 800 bedded tertiary care teaching hospital, Kadapa. A total of 180 patients were studied during this period out of which 141 (78.3%) patients were male and 39 (21.7%) patients were female, majority of the patients 74 (41.1%) were found to be in the age group of 41-50 years, least 2 (1.1%) patients were found in the age group of 70-80 years, 58 (32.2%) patients were smokers and 39 (21.7%) patients were alcoholics,124 (68.9%) patients (Male patients-99 & Female patients-25) had HTN, 27 (15%) patients (Male patients-20 & Female patients-7) had both HTN & DM, 19 (10.6%) patients (Male patients-14 & Female patients-5) had DM alone, This study concludes that there is a high prevalence and incidence of Hemodialysis in the Kadapa region. Hypertension and Diabetes mellitus are the leading causes for the kidney diseases.Awareness of hemodialysis patients on the disease, medication, diet along with the life style modifications through the patient education will be helpful for the patients to control their risk factors and to improve the compliance to the dosage regimen.

3

IN-USE TESTS FOR DETECTION OF MICROBIAL CONTAMINATION IN HOSPITAL DISINFECTANTS AND ANTISEPTICS

Kamaljeet1*, Devinder Kaur2, Mohit Thalquotra3, Dr Varsha A. Singh4, Dr K. N. Dubey1

1Jan Nayak Ch. Devi Lal Dental College, Sirsa, Haryana, India.

2Shri Guru Gobind Singh College of Pharmacy, Sector 26 Chandigarh, India.

3Government Medical College, Jammu, J&K, India. 4Maharishi Markandeshwar Institute of Medical Science and Research (MMIMSR), Mullana, Ambala, Haryana, India.

Abstract

Disinfectants and antiseptics play a vital role in the infection control. In-use tests study was aimed to determine the contamination level in the commonly used disinfectants. A total of 160 samples were collected from the various departments. Ten milliliters (10 ml) sample of each disinfectant / antiseptic being used in the hospital was collected and processed by the method of Kelsey and Maurer (1974). Neutralization was done with the help of nutrient broth or nutrient broth with 3% v/v Tween 80. One milliliter of the disinfectant / antiseptic fluid was transferred to 9.0 ml of the diluents. A volume of 0.02 ml of this mixture was inoculated on to ten different areas of each of two well-dried nutrient agar plates. One plate was incubated at 37°C for 3 days and the other for 7 days at room temperature. Disinfectant and antiseptics was contaminated if they were growing five or more drops any plates. The organism thus grown was identified on the basis of colony morphology and biochemical reaction. In these 16 samples were failed in the test, out of 160 samples revealed the growth of Pseudomonas aeruginosa Staphylococcus sp.; Candidosis. In conclusion, all the disinfectants and antiseptics should be used in proper concentration and monitoring of disinfectants / antiseptics should be under taken on regular basis while they are being used.

4

NOVEL SPECTROPHOTOMETRIC METHODS FOR SIMULTANEOUS DETERMINATION OF CIPROFLOXACIN HYDROCHLORIDE AND DEXAMETHASONE SODIUM PHOSPHATE IN THEIR BINARY MIXTURE

Manal Mohamed Fouad

Analytical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

October University for Modern Sciences and Arts, 6 October City, Egypt.

Abstract

Smart spectrophotometric methods have been applied and validated for the simultaneous determination of a binary mixture of ciprofloxacin hydrochloride and dexamethasone sodium phosphate without preliminary separation. The first method is the well established dual wavelength method. The second and third methods are utilizing the isoabsorptive point; absorbance subtraction and absorbance ratio. The other two methods are manipulating ratio spectra namely; ratio subtraction and ratio difference. Linear correlation was obtained in the range of 5–30 μg/mL for ciprofloxacin hydrochloride and 5–50 μg/mL for dexamethasone sodium phosphate by the five proposed methods. The suggested methods were validated according to ICH guidelines and successfully applied to the determination of the studied drugs in various laboratory prepared mixtures. Moreover, the methods were successfully applied to the assay of drugs in their pharmaceutical formulation; Peopo-otic® ear drops with mean recoveries ranging from 99.96 to 101.52 % ± 0.238–0.919. The results obtained were statistically compared to that of a reported spectrophotometric method showing no significant difference regarding both accuracy and precision. The developed methods were economical in terms of time taken, with minimum manipulation steps and don’t need any sophisticated apparatus, making them suitable for the simultaneous determination of the studied drugs in routine analysis and in quality control laboratories.

5

CASE REPORT ON NEVIRAPINE INDUCED DRESS SYNDROME

Greeshma Hanna Varghese, Hanna Alexander, Swethalekshmi. V, Neethu Ros Tom, T. R. Ashok Kumar, Dr. T. Sivakumar,

Nandha College of Pharmacy and Research Institute, Erode-52.

Abstract

Nevirapine-induced drug reaction with eosinophilia and systemic symptom (DRESS) is uncommon but a potentially life-threatening condition, with significant morbidity and mortality rates due to multiple-organ involvement. DRESS syndrome has also been reported with a number of other drugs including allopurinol, minocycline, terbinafine, sulfonamides, azathioprine and dapsone. It was earlier referred to by various names such as Dilantin hypersensitivity syndrome and anticonvulsant hypersensitivity. It is a severe adverse drug reaction characterised by skin rash, fever, lymph node enlargement, hepatic dysfunction and internal organ involvement. Here we are going to describe a rare case of nevirapine-induced dress syndrome that was successfully treated with systemic steroid.

6

SYNTHESIS OF 8 - AZABICYCLO [3.2.1] OCTANES DERIVATIVES AND ITS DOCKING STUDY ON 2A79, 3G90 AND 1FF4.

Kumari Vandana, Verma S.M

Birla Institute of Technology, MesraRanchi-4, Jharkhand, Pin-835215.

Abstract

Tropane Alkaloids have received much attention because of their various biological activity. Due to their influence on neurotransmitter, tropinone structured compounds or 8-azabicyclo[3.2.1] octane analogues received considerable attention in medicinal chemistry field. Due to their unique structural feature, it was a challenge to synthesize tropinone analogues but here we have attempted to synthesize few 8-azabicyclo[3.2.1] octanes derivatives using hydrazines and studied on receptors with pdb id’s- 2A79,3G90 and 1FF4. Docking study on Acetylcholine receptor binding protein (1FF4) inferred that the synthesized product possessed some anticholinergic activity. Similarly voltage-gated potassium channel beta-2 subunit (2A79) and mitogen - activated protein kinase 10(3G90) docking studies were done for anticonvulsant activity. Thus by the help of these docking studies further these synthesized product can be tested on animal objects for anticholinergic and anticonvulsant activity.

7

ANALYTICAL METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS ESTIMATION OF ESCITALOPRAM OXALATE AND FENOFIBRATE USING RP- HPLC METHOD

Nikam Rahul, Garge Vaibhavi, Dr. Kadam Vilasrao

BharatiVidyapeeth’s College of Pharmacy, C.B.D. Belapur, Navi Mumbai.

Abstract

Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) methods for simultaneous estimation of drugs are developed for analysis and accurately quantification of two or more drugs. It was found from literature that significant number of patients concomitantly consume Escitlaopram oxalate and Fenofibrate. As there there was not any analytical method for the estimation of these two drugs, this method was developed. Analysis was carried out using Agilent C18, 250 × 4.6 mm, 5μ particle size column. Optimised method was Methanol: Phosphate buffer (pH 6.0) :: 80:20, Flow rate: 1ml/min, Detection wavelength: 239 nm, Run time: 10 minutes. Retention times for Escitlopram oxalate and Fenofibrtae were 2.7 minutes and 8.3 minutes respectively. The method was validated using ICH guidelines. Hence, this method can be used for accurate, simultaneous estimation of Escitalopram oxalate and Fenofibrate combination formulation. Further this method can be used for development of bioanalytical method for simultaneous estimation of the two drugs.

8

A SIMPLE KINETIC SPECTROPHOTOMETRIC METHOD FOR DETERMINATION OF STRONTIUM RANELATE IN BULK AND PHARMACEUTICAL DOSAGE FORM

MohamedRizk, Maha M. AbouEl-Alamin, MervatI. Moawad*

Analytical Chemistry Department, Faculty of Pharmacy, Helwan University, 11795, Cairo, Egypt.

Abstract

A Simple and highly sensitive kinetic spectrophotometric method was introduced for the determination of Strontium Ranelate (SRN) in bulk and pharmaceutical dosage form using potassium permanganate in alkaline medium as an oxidizing agent. The method involved determination of SRN by kinetic study of its oxidation at 35oC for a fixed time of 30 minutes. The absorbance of the produced manganate ion was measured at 610 nm. The absorbance-concentration graph was found to belinear over the concentration range of 5.0-55.0 μg/mL (R2=0.9997) with limit of detection (LOD) of 1.2 μg/mL and limit of quantitation (LOQ) of 3.7 μg/mL. Various experimental parameters influencing the development and stability of the colored product have been thoroughly examined and optimized. Determination of SRN by the rate-constant and fixed-absorbance methods was applicable using the appropriate calibration equations; however the fixed-time method was verified to be the most advantageous. The proposed method was successfully applied for the determination of SRN in its sachets. The anticipated method provides the advantages of selectivity, simplicity and accuracy. The obtained results were validated and shown to be reproducible and in great agreement with those obtained from the comparison reference method of the investigated drug. A proposed mechanistic pathway was also presented.

9

MONONUCLEAR MIXED LIGAND TRANSITION METAL COMPLEXES: SYNTHESIS, CHARACTERIZATION, ANTIOXIDANT AND ANTIMICROBIAL ACTIVITY ALONG WITH DNA CLEAVAGE STUDIES

Sulochana P Melinmath1, Venkatesh K B3, Rekha N D2, AshaIyengar T1*

1Yuvaraja's College (Autonomous), University of Mysore, Mysore-570005, Karnataka, India.

2JSS College of Arts,Commerce and Science, Ooty road, Mysore, Karnataka, India.

3Aalto University, School of Chemical Technology, Espoo, Finland.

Abstract

The mixed ligand transition metal complexes of Ni+2, Co+2, Zn+2, and Cu+2 have been prepared with second-generation quinolone antibacterial agent enrofloxacin (L1) and 8-hydroxyquinoline (L2). The metal complexes were characterized by elemental analysis, Infrared, ESI-mass, and conductivity measurements. All the metal complexes are mononuclear and have octahedral geometry. Synthesized metal complexes were screened for antimicrobial, antioxidant activity and DNA cleavage study by gel electrophoresis.

10

ACNE-CAUSES AND AMAZING REMEDIAL MEASURES FOR ACNE

P. Ravisankar*1, O. Sai Koushik1, V. Himaja1, J. Ramesh1, P. Pragna2

1Department of Pharmaceutical Analysis and Quality Assurance, Vignan Pharmacy College, Vadlamudi, Guntur (Dist.) - 522213, Andhra Pradesh State, India. 2Malla Reddy Medical College for Women, Jeedimetla, Hyderabad-500055, Telangana State, India.

Abstract

The word acne comes from the word acme meaning "the highest point," which comes from the Greek akme meaning “point or spot”. In the entire world 650 million people with acne have been suffering, which is about 9.4 % of the world population out of which females are 9.8 % men amounting to 9.0 % which indicates females are more prone to this acne disease .It attracts nearly 40 to 50 million population in the United States (16 %) and more or less 3 to 5 million people in Australia (23 %). Acne is most common skin disease. Acne effects all races and ages and became the most common skin disease, especially in teenagers and young adults. It is estimated approximately 90 % out of age group between 11 and 30 are being attacked by acne outbreaks and during puberty in both sexes, acne can born owing to an increase in androgens such as testosterone and 90 % are suffering from acne at puberty stage all over the globe. Nearly 80 % out of age group of 11 to 30 year-olds are the sufferers with acne at any time of this stage basing on their physiological condition of their body and some people in their age at 40s and 50s still get acne disease. Acne is one of the greatest skin problems faced by adults. As many as 25 percent of all adult men and 50 percent of adult women suffer from acne disease at some point in their life. But adult acne can be particularly frustrating. Research shows 35 % of women in their 30s, 26 % in their 40s, and 15 % age 50 + are the sufferers from acne disease. Women over the age of 33 are more likely to get premenstrual pimples than younger women. The chief ground for this disease is the bad environment, eating an inflammatory diet or living a sedentary lifestyle or both can contribute to the underlying cause of acne. The information on this article can help to understand acne, types of acne, causes for development of acne treatment and home remedies and treatment.

11

FORMULATION AND EVALUATION OF VALSARTAN AND HYDROCHLOROTHIAZIDE (160/25MG) FILM COATED TABLETS

Shailesh Sharma, Tanusha Kapoor

Department of Pharmaceutical Research Divison ASBASJSM College of Pharmacy, BELA (Ropar), Punjab 140111 India.

Abstract

Present study is aim to formulate and evaluate the Valsartan-Hydrochlorothiazide (160/25mg) film coated tablets. The oral route is most important and preferable for the delivery of drugs to the systemic circulation due to the ease of administration, patient compliance and flexibility etc. These tablets produce reduction in the multiple dosing and more effective in management of the hypertension. The combination tablets of two hypertensive drugs are formulated accordingly that one drug released early and second drug give sustained release. The film coating was used form the sustainability of drug release. All the official and non-officialparameters were evaluated for the coated tablets. The tablet passes all the evaluation parameters. On the stability stress of three months the prepared formulations were fond stable. The prepared tablet found compatible and convienent to the patient in the management of hypertension.

12

PHYSICO-CHEMICAL AND PHYTOCHEMICAL STUDY OF HYDROETHANOLIC PETAL EXTRACT OF PINK NELUMBO NUCIFERA GAERTN

Saraswathi RV, Gricilda Shoba F*

P.G. & Research Department of Zoology, Voorhees College, Vellore - 632009, Tamilnadu, India.

 Abstract

Nature has given rise to medicinal agents for thousands of years. Various medicinal plants have been used for years in daily life to treat the disease all over the world. The therapeutic use of herbs is as old as human civilization and has evolved along with it. Medicinal plant drug discovery continues to provide new and important leads against various effects like cancer, malaria, cardiovascular diseases and neurological disorders. Interest in herbal drugs and natural medicine is undergoing a renaissance now. The curative properties of plants are due to the presence of active principles such as alkaloids, phenolics, tannins and flavonoids that constitute of many pharmacologically active compounds. The aim of the present study was to know about the physico-chemical evaluation of the extract, phytochemical screening and quantification of primary and secondary metabolites in the Nelumbo nucifera petal extract. The results obtained in the present study reveal the following: physico-chemical parameters show a good result in Nelumbo nucifera petal extract and can be used for the formulation of the drug. phytochemical screening and quantification of primary and secondary metabolites in the Nelumbo nucifera petal extract shows the presence of primary metabolites viz., carbohydrates, proteins and lipids and the secondary metabolites such as tannins, phenols flavonoids and alkaloids on phytochemical screening. Quantification of primary metabolites of the extract shows its nutritive value and the secondary metabolites were responsible for its medicinal properties of the petals of the Nelumbo nucifera Gaertn that was used by the traditional herbalists. Finally, the present finding of the study concludes, that the hydro ethanolic Nelumbo nucifera petal extract possess abundant phytochemicals, which act as a source of natural antioxidants having a great importance in preventing various diseases and further study was needed to find out the active principle present in the Nelumbo nucifera petals.

13

“A STUDY OF INTRAVENOUS DROTAVERINE Hcl Vs VALETHAMATE BROMIDE ON DURATION OF LABOR”

Dr. U. Agnes Vijaya1*, Purushothama Reddy. K2, A. Nagaraju3, Mallesh. M3

1Associate Professor, MD, D.G.O, Department of Obstetrics & Gynaecology, RIMS, Kadapa, India.

2Assistant Professor, Department of Pharmacy Practice, P. Rami Reddy Memorial College of Pharmacy, Kadapa, India.

3Pharm.D Interns, Department of Pharmacy Practice, P. Rami Reddy Memorial College of Pharmacy, Kadapa, India.

Abstract

Background: The phenomenon of labor is dynamic from the onset till the delivery of the new born. The myometrial contractions of Labor are painful which is why the term “Labor- pains” is used to describe this process. Any measure that would shorten the duration of labor without jeopardising the maternal or fetal interest is most welcome both by the patient and the obstetrician so that close monitoring will be feasible. So, for induction of labor with method like oxytocin, prostaglandins, insertion of bougies have been used. It has been proved that cervical dilatation is one of the important factors that determine the duration of labor.The drugs drotaverine/valethamate can be used to cause cervical dilatation and thereby increasing the coordination of contractions which improves the uterine activity.Aim of the study: To evaluate the efficacy of intravenous Drotaverine Hcl and Valethamate bromide on duration of 1st stage of labor, rate of cervical dilatation and its effects on mother and fetus. Material & methods: Study was conducted at Rajiv Gandhi Institute of Medical Sciences (RIMS), Kadapa. A total of 300 cases were selected and divided into 3- groups as control group, Drotaverine Hcl group and Valethamate bromide group.Results: 62% of the cases were booked in Group I. 62% of the cases in Group II and 66% in Group III. Mean duration of reduction is almost 3 hours in Primi gravidae and 1.5 hrs in multi gravidae, when compared to valethamate it is 2.5 hrs in primi gravidae 1 hr. 15 min. in multi gravidae. Drotaverine co - ordinated the uterine activity by hastening the cervical dilatation. The side effects on mother are much less when compared to valethamate, except for mild headache and nausea.Conclusion: The present study found that drotaverine is superior to valethamate as it reduces the duration of labor more effectively.

14

EVALUATION OF ANTI-CANCER ACTIVITY DOLICHANDRONE ATROVIRENS IN EXPERIMENTAL INDUCED ANIMAL MODEL

P. Natarajan*1, R. Arunpandian2

1Sankaralingm Bhuvaneswari College of Pharmacy, 3/77-c Anaikuttam Road, Anaikuttam, Sivakasi, Tamil Nadu, India.

2Micro Therapeutics, Coimbatore, Tamil Nadu.

Abstract

The anticancer activity of the extract of Dolichandrone atrovirens (DA) has been evaluated against Dalton’s ascitic Lymphoma (DAL) in Swiss albino mice. It has a significant enhancement of mean survival time of treated groups tumor bearing mice was found with respect to DAL control group. Drug treatment was found to be an increase non-viable cell counts. After the treatment of extracts with DAL bearing mice shows that the tumor cell growth was found to be inhibited. After 14 days of inoculation, extracts is able to reverse the changes in the hematological parameters, liver function test and PCV consequent to tumor inoculation that near to the normal control group. The DA were decreased the ascitic fluid volume, viable cell count, and increased the percentage of life span of animals. It may be concluded that DA by decreasing the nutritional fluid volume and arresting the tumor growth, this could be the reason for the increase life span of DAL-bearing mice.

15

PRESCRIBING PATTERNS OF ANALGESICS IN THE POST-OPERATIVE PERIOD OF SURGICAL INTERVENTIONS

Allam Roshini, A. Siva Abhishek, K. Ashwini, J. Manasa , Mohd.Tahir Siddiqui

Department of Pharmacy Practice, Malla Reddy College of Pharmacy, Maisammaguda, Secundrabad, Telangana.

 Abstract

Objectives:-To evaluate the variety of analgesics prescribed after surgery along with the doses administered and routes of administration. Study Design, Study Period And Study Site: A prospective observational study conducted for 4 months in the inpatient surgery departments of Malla Reddy hospital, a 373Bedded tertiary care teaching hospital. Methodology:-All patients who have under gone surgery were included in the study. Post-operative analgesics prescribed along with the route of administration and doses were noted in a specially designed proforma. Results And Discussion:-218 patients were included in the study who were prescribed with 465 analgesics. Post-operative analgesics are prescribed in all the patients who undergone surgery. For 80.73% (176) patients injectable analgesics were prescribed immediately after surgery and in 19.26% (42) patients oral analgesics were prescribed immediately after surgery. Diclofenac was the most commonly prescribed among the injectable analgesics (35.74%). Tramadol+ Acetaminophen was most commonly use oral analgesic (38.37%). The use of analgesics depends upon the severity of pain. In case of mild pain, single analgesics are commonly used where as for moderate and severe pain two or more analgesics are used. The study summarizes that, cost of therapy can be reduced by changing of prescription drugs from brand name to Generic name, also this plays an important role in Rational use of Drug (Proper dispensing of drugs, Cost, safety and efficacy). By using pain intensity scales, pain assessment should be practiced so that right choice of analgesics can be prescribed according to the intensity of pain.

16

QUALITY OF SLEEP AMONG TUBERCULOSIS PATIENTS’- A PILOT STUDY

Ahamada Safna Mariyam. M*1, Sudhakar. R2, Yasaswini Bandlamudi2, Suhas Reddy .C3

1Assistant Professor, Department of Pharmacy Practice, Acharya & B.M Reddy College of Pharmacy, Bangalore, India.

2Pharm.D Interns, Nandha College of Pharmacy, Erode, India.

3Lecturer, Department of Pharmacy Practice, Acharya & B.M Reddy College of Pharmacy, Bangalore, India.

Abstract

Sleep is a normal and vital physiological phenomenon to lead a normal and quality livelihood. Approximately 7-8 hours of sleep is essential for maintaining a healthy life. Chronic sleep deprivation affects the physical function, cognitive function of humans and also jeopardizes the quality of life. Several factors like chronic disease conditions, anxiety, depression leads to sleep deprivation. Tuberculosis is a chronic disease condition, where the patients’ suffer from co morbid depression and anxiety and ultimately may lead to sleep deprivation. Several studies have postulated the prevalence of co morbid depression and anxiety among tuberculosis patients’ but there exist a paucity of literature about the quality of sleep among tuberculosis patients’. This prospective observational study aims to assess the quality of sleep among tuberculosis patients’ in relation to their co morbid depression and anxiety using Beck Depression, Beck Anxiety and Pittsburg Sleep Quality Index scales. The average value of PSQI in our study cohorts was found to be 6.92 ± 1.5. Also there exists a strong positive correlation (r= 0.277) between anxiety and depression level, as well as between quality of sleep and depression (r= 0.684, (p<0.001)) and anxiety level (r= 0.340, (p<0.001)) of the patient. Patients’ with chronic disease conditions are highly susceptible to emotional disturbances like depression, and anxiety, which impairs the quality of sleep. Our study which aims in assessing the quality of sleep among tuberculosis patients’ demonstrated that the quality of sleep reduces significantly with associated depression and anxiety level of the patients’.

17

FORMULATION AND EVALUATION OF FAST DISSOLVING METRONIDAZOLE TABLET

Subahan Ali1, Berpal Sing1, K K Jha2 and Arkendu Chatterjee*1

1Department of Pharmaceutics, Teerthankar Mahaveer University,Moradabad, Uttarpradesh, India.

2Department, of Pharmaceutical Chemistry, Teerthankar Mahaveer University, Moradabad, Uttarpradesh, India.

Abstract

The oral estimation structures are the most common system for taking medication despite having a couple weights like moderate maintenance and along these lines onset of movement is drag out. This can be overcome by administrating the prescription in liquid from in the mean time, various APIs have compelled level of dauntlessness in liquid structure. In this way, Effervescent Tablets goes about as a choice estimations structure. The present work is taking into record the arrangement of gurgling granules of metronidazole ie F1 to F4. Four arrangements were prepared using particular, diluents and superdisintegrants by the wet granulation procedure. The prepared tablets of all the formulations were evaluated for precompression parameters like angle of repose, bulk density, tapped density and compressibility index and physical characters like tablet hardness, friability, weight variation, buoyancy lag time. The formulations showed good flow property and Carr’s index. Angle of repose ranged from 30±1.020 to 34±2.390, Carr’s index ranged from 4.0±0.62 to 6.25±1.12 and the Hausner ratio ranged from 1.0±1.14 to 1.06±2.29. The state of tablets of all definitions stayed white, smooth, curved confronted round with no unmistakable splits. The thickness of tablets was extended between 2.44±2.11mm to 3.56±1.56mm separately. The hardness of the tablets found in between 5.2±1.29to 6.4±1.34kg/cm2. The friability was discovered to be 4.34±1.07 % to 6.38±1.91%, which is a sign of palatable mechanical resistance of the tablets. The medication content estimations demonstrated values in the scope of 95.8% to 99.2% which reflects great consistency in medication content among distinctive definitions. Every one of the tablets breezed through weight variety test as the % weight variety was 8.11±0.76 to 9.86±1.54mg and effervescent time shown 6±2.13 to 10±1.45 second. Out of that we wear optimized formulation was F2.

18

ANTIOXIDANTS: MIRACLE FOR AGE AND AGE RELATED DISORDERS

Palak Landge*, Stuti Dave, Abhishek Jagani, Ruchit Patel

Department of Pharmaceutical Chemistry, Babaria Institute of Pharmacy, Varnama, Vadodara, Gujarat, India.

Abstract

In the past few years there is a rapid growth in the augmentation of antioxidants. Age is a matter of concern among all the individuals. Age related disorders like Parkinson‟s, Alzheimer‟s, and dementia are now common terms which we hear. The requirement of drugs to bring these disorders under control is the current research area worldwide among the scientists. Antioxidants both natural and synthesized once play a significant protective role in many age-related disorders. They act as free-radical scavengers. Free radicals produced in the body are the major cause of these disorders. Antioxidants prevent the neurodegenerative processes and may also improve the standard of living of the geriatrics. Major discovery can be achieved by involving both the natural and synthetic sources to serve as antioxidants.

19

ANTIBACTERIAL AND ANTIOXIDANT POTENTIAL OF METHANOLIC LEAF EXTRACT OF PUTRANJIVA ROXBURGHII WALL

Dr.Narendra Kumar

Senior Lecturer, Amity Institute of Biotechnology, Amity University Haryana, Manaser-122413, Gurgaon, Haryana, India.

Abstract

For antibacterial activity the methanolic extracts of 12 plants leaves were extracted. The antibacterial testing in vitro was done following disc diffusion method against Bacillus subtilis, Erwinia herbicola, Escherichia coli, Salmonella typhi, Pseudomonas putida Staphylococcus aureus Klebsiella pnemoniae ,Vibrio cholera.Amongst the leaf methanolic extracts tested, the extracts of Aegle marmelos (L.) Corre, Anethum graveolens L and Eupatorium capillifolium (Lam.) Small showed significant antibacterial activity against the bacterial pathogen. Putranjiva roxburghii Wall showed highest antibacterial activity followed by Artabotrys hexapetalus (L.f.) Bhandari. The 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay was used to determine the antioxidant activity of potent extract. Putranjiva roxburghii Wall showed the appreciable antioxidant activity. This showed highest antioxidant activity at 40 mg/ml concentration with a percent inhibition of 65.54 and IC50 value 7.29 mg/ml. The reducing power of the extracts was found to increase with increasing concentration of the extract .The results provide evidence that the methanolic leaf extract extract of Putranjiva roxburghii can be further recommended in the treatment of the infections caused by the bacterial pathogens .The result indicates that Putranjiva roxburghii is a potential source of antibacterial and natural antioxidants.

20

EVALUATION OF BETA BLOCKERS USE AT A TERTIARY CARE HOSPITAL

Sukesh Krishna Chaitanya Loka*, Vinuthna Yashki, Alekhya Vissampally, Divya Jose

Malla Reddy Institute of Pharmaceutical Sciences, Hyderabad.

Abstract

Drug Utilization Evaluation (DUE) is an ongoing, authorized and systematic quality improvement process designed to review drug use and promote appropriate drug use through interventions. Beta blockers, one of the prescribed classes of cardio vascular medications reduce morbidity and mortality in patients with cardiac disease. The present study aimed to evaluate the prescribing pattern of beta blockers use. A prospective, observational study was carried out in inpatients of general medicine, and surgical departments of tertiary care hospital. Structurally designed proforma was used to collect patient data such as demographics, medical history, and treatment. The data was then analyzed using Microsoft Excel and evaluated. A total of 135 patients have been identified who were prescribed with beta blockers among which females accounted for 51.1% while males for 48.8%. Average length of hospital stay was 6 days. The most common diagnoses were Hypertension (62.2%), and Diabetes mellitus (34.8%). Beta blockers were mostly prescribed among the age group 50-69 years (50.3%) and the widely prescribed was metoprolol (39.2%). The other anti hypertensive drugs concurrently prescribed with beta blockers included diuretics (51.1%). Major drug interactions were found in 9.83% only. Beta blockers most commonly prescribed include Metoprolol followed by atenolol. It is highly necessary for the clinical pharmacist to review and clinically check all prescriptions presented at the wards (check for appropriate dose, frequency, drug interactions etc.).

21

EFFECTS OF PARACETAMOL-INDUCED LIVER DAMAGE ON SOME HEMATOLOGICAL PARAMETERS: RED BLOOD CELL (RBC) COUNT, WHITE BLOOD CELL (WBC) COUNT, AND PACKED CELL VOLUME (PCV) IN WISTAR RATS OF EITHER SEX

*Seriki A. Samuel, Adebayo O. Francis, Oshagbemi Ayomide, Uche-Orji Onyinyechi 

Department of Physiology, Faculty of Medical Sciences Bingham University, Karu, Nigeria.

Abstract

Paracetamol is a widely used analgesic and antipyretic. It is classified as a mild analgesic commonly used for the relief of headaches and other minor aches and pains. While it is generally safe for use at recommended doses (1000mg per single dose and up to 3000mg per day for adults human), acute overdoses of paracetamol can cause potentially fatal kidney, brain and liver damage, and in rare individuals, a normal dose can do same. The current study investigates the effect of paracetamol-induced liver damage on some haematological parameters in wistar rats. Twenty wistar rats were randomly allocated in two groups of 10 each, and were well fed for the duration of the research work. Rats in group 1(control) were fed with just normal rat feeds. But the rats in group 2 were, in addition, given over dose (300mg) of paracetamol for two days. On the third day, they were sacrificed using chloroform. The results showed that there was a significant decrease in Red Blood Cell (RBC) count between the control group and the treated (p<0.05). There was also a significant increase in white Blood Cell (WBC) count between the control group and treated group (P< 0.05). There was also a significant decrease in the Packed Cell Volume (PCV) values between the control group and the treated group (P<0.05). Paracetamol 300mg/kg administered for two days significantly reduced RBC count and PCV, and increased WBC count of the wistar rats. Serum transaminase, an important indication of severe liver damage also increased.

22

INCIDENCES OF LOOSE SHELL SYNDROME (LSS) IN CULTURED LITOPENAEUS VANNAMEI, ANDHRA PRADESH

S.A. Mastan

P V S Laboratories Limited, Aqua Division, Kohinoor Apartments, Kalanagar, Benz Circle, Vijayawada-520 010, Andhra Pradesh, India.

Abstract

The present work was undertaken to study the loose shell syndrome (LSS) in farmed Litopenaeus vannamei during the period of 2014 - 2015. The affected shrimps were collected from cultured ponds of West Godavari, East Godavari and Prakasam districts of Andhra Pradesh, India and were subjected to microbiological studies. Four species of bacteria were isolated from the diseased shrimps and were identified as V. harveyi, V. alginolyticus, V. fluvialis and V. parahaemolyticus based on their morphological characteristics and biochemical tests. In the present study, it has also been observed that mineral deficiency, poor water quality, bad management practices and association of Vibrio bacteria may be the causes of loose shell syndrome in L. vannamei.

23

AN ASSAY METHOD FOR THE SIMULTANEOUS ESTIMATION OF ACETAMINOPHEN AND TRAMADOL USING RP-HPLC TECHNOLOGY

Fayeza Batool*, Osman Ahmed, Anas Rasheed

Department of Pharmaceutical Analysis & Quality Assurance, Deccan School of Pharmacy, Hyderabad, T.S.

Abstract

A simple and selective RP-HPLC method is described for the determination of Acetaminophen and Tramadol dosage forms. Chromatographic separation was achieved on a C18 column using mobile phase consisting of a mixture of mixed Phosphate buffer pH: 3.4 Acetonitrile (30:70v/v/v), with detection of 236nm and flow rate at 1.2mL/min. Linearity was observed in the range 100-300 μg /ml for Acetaminophen (r2 =0.99) & 10-30μg /ml for Tramadol (r2 =0.99) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim. The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods, sensitivity, precision and reproducibility. It can be used for routine analysis of pharmaceutical dosage form.

24

ETHNIC KNOWLEDGE OF DYE YIELDING PLANTS USED BY THE KANI TRIBES OF PONMUDI HILL: A CASE STUDY

Bosco Lawarence, S Mahesh, Aswathy J M, Greeshma Murugan, K. Murugan

Plant Biochemistry and Molecular Biology Laboratory, Department of Botany, University College, Trivandrum 695 034, India.

Abstract

Dyes are the natural or artificial chemicals used to add colour to materials. Most of the natural dyes are made from plant parts such as leaves, flowers, roots, berries, bark, rhizomes, tubers, shoots, sap and wood. Textile dyeing dates back to the Neolithic period. The present work is the first comprehensive account of the dye yielding plant diversity of Ponmudi hills, a part of Western Ghats being utilised by the Kani tribes including local inhabitants. A survey has been done on the ethnic use of dye yielding plants with its utility values. Pterocarpus marsupium Roxburgh (Fabaceae), Woodfordia furticosa Kurz (Lythraceae), Terminalia paniculata (Roxb.) Wight & Arn. (Combretaceae), Morinda citrifolia Linn. (Rubiaceae), Clitoria ternatea Linn. (Fabaceae), Butea monosperma Taub. (Fabaceae), Butea superba Roxb. Ex Willd. (Fabaceae), Pandanus odorifer (Forssk.) Kuntze (Pandanaceae), Carthamus tinctorius L. (Asteraceae), Diospyros paniculata Dalz. (Ebenaceae), Cordia dichotoma Forst. (Boraginaceae), Nyctanthes arbor-tristis Linn (Oleaceae), Curcuma aromatica Salisb. (Zingiberaceae), Tectona grandis Linn.f (Verbenaceae) and many Osbeckia species such as O. aspera, O. reticulata, O. wynadensis and O. parviflora are the most common dye plants used by the people for multi purposes. The dyeing parts of the plants are used by the ethnic communities for various religious purposes. Further, they are confident regarding the non toxic and eco-friendly nature of the natural dye. However, the indigenous information, practice of extraction and processing of natural dyes has now declined due to readily available cheaper synthetic dyes. It is high time that proper documentation and conservation of this knowledge to conserve these natural dye plants. Osbeckia species being promising in this line, further studies are designed to analyze the major phytochemicals like anthocyanin and its biological characterization.

25

SPECTRAL AND ANTIBACTERIAL STUDIES ON SOME ETHNOBOTANICALLY IMPORTANT MEDICINAL PLANTS USED BY THOTTIANAICKANS OF SEMMALAI

Thiravia Doss Dons, Sebastian Soosai Raj*

Department of Botany, St. Joseph’s College, Tiruchirappalli – 620002, Tamilnadu, India.

Abstract

Ethanolic extract from four medicinal plants, Justicia tranquebariensis, Tribullus terrestris, Aloe vera and Curcuma longa were tested for their antibacterial activity against four wound associated infectious microorganisms such as Staphylococcus aureus, Bacillus subtilis, E. coli and Klebsiella pneumonia by disc diffusion method. The Ethanolic stem extracts of Justicia tranquebariensis showed significant antibacterial activity against all test organisms. The spectrum of activity observed in the present study may be indicative of possible source of new and effective drugs from these herbals. The Ethanolic extracts of these four species were analyzed to identify electron transition and the functional group by FT–IR and UV Spectroscopy. The presence of the secondary alcohol, phenol, amines, alkanes and halogen has been revealed by FT-IR analysis. UV –VIS analysis of Justicia tranquebariensis, Tribullus terrestris and Curcuma longa confirm the presence of Aniline.

26

DEVELOPMENT AND IMPLEMENTATION OF A DRUG FORMULARY FOR THE MEDICINE DEPARTMENT OF TERTIARY CARE TEACHING HOSPITAL

Sushilkumar P L 2*,3, Dr. Baishnab S2, Johnson G1, John J A1, Philip L A1, Philip M S1, Chaitanya Kumar T2, Dr. Sam G K2

1 Intern, Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka.

2 Lecturer, Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka.

3 Research Scholar, R K University, Rajkot, Gujarat.

Abstract

The purpose of the study was to prepare an open drug formulary for the medicine department of tertiary care teaching hospital and publish it in a convenient size and format. The study was conducted in a tertiary care teaching hospital for a period of six months. The final master list of drugs was prepared in accordance with the opinion of the physicians. Then monograph for the drugs were prepared by referring Micromedex, NFI, and other authentic resources. After the completion of the monographs, they were given to five physicians and five lecturers for validation. The fixed dose combinations, vitamins and minerals were enlisted. Finally the formulary was published in a more convenient size and format for a quick reference. There were about 533 generic drugs are used in the medicine department of SSIMS & RC. The drug list was prepared with 533 drugs. From those, drugs were categorized according to pharmacotherapeutic classification and finally classified according to the organ systems. Monographs of 350 drugs were completed and given for validation. After the validation, appropriate changes were made and formulary was prepared. Micromedex was the main resource used for monograph preparation. Out of 350 monographs, the half-life of 34 drugs, volume of distribution of 139 drugs and clearance of 252 drugs were not found and not documented. Drug interactions for 23 drugs were not found and documented. The more number of drugs are under pregnancy risk category C compared to category A, B, D, X and N.

27

A STUDY TO ASSESS MEDICATION ADHERENCE TOWARDS ANTI – DIABETIC THERAPY IN PATIENTS DIAGNOSED WITH TYPE 2 DIABETES MELLITUS OF DAVANGERE, KARNATAKA

Dr. Baishnab S3*, Dr. Basavarajappa A P2, Sushilkumar P L3,4, Morla S1, Patel Y A1, Kukadiya A G1, Chaitanya Kumar T3, Muneerudeen J3

1 Intern, Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka.

2 Principal, Bapuji Pharmacy College, Davangere, Karnataka.

3 Lecturer, Department of Pharmacy Practice, Bapuji Pharmacy College, Davangere, Karnataka.

4 Research Scholar, R K University, Rajkot, Gujarat.

Abstract

The purpose of the study was to assess and report Medication Adherence in selected Type II Diabetes Mellitus patients by using Morisky’s Adherence Predictor Scale (4-item) questionnaire, to develop data collection form and informed consent form, and to identify factors linked to poor adherence in selected patients of Davangere, Karnataka. A prospective observational questionnaire based study was conducted for a period of 6 months by using Morisky’s Adherence Predictor Scale (4-Item) Questionnaire. Among 151 cases, which were collected 70 were males and 81 were females. The adherence levels were 64.90% (high adherence), 29.80% (medium adherence) and 5.29% (poor adherence). The correlation between the patient’s socio demographic details and adherence rate indicated that higher adherence was among middle age group (69.83%) and those with primary education (96.30%). The most common reasons for non adherence was when the patient felt better (75.47%), cost of medications being expensive (92.45%) and high quantity of medications i.e. too much medications (66.04%). It is concluded that the participants in the area of study were highly adherent to their anti-diabetic medications. Various factors of medication non-adherence were identified and evaluated. Therefore, we recommend interventions that will still address these factors of non-adherence in order to improve adherence the more. Some of such interventions include the physicians and pharmacists improving on the areas of patient education and medication counselling, communication between them and patients, encouraging patients to monitor their blood glucose level regularly, simplifying drug regimen with decreasing the number of drug taken, medication selection bearing in mind cost and intolerable side effects of the medications.

28

SPECTROPHOTOMETRIC SIMULTANEOUS DETERMINATION OF LAMIVUDINE, TENOFOVIR AND NEVIRAPINE IN COMBINED TABLET DOSAGE FORM BY RATIO DERIVATIVE AND FIRST ORDER DERIVATIVE METHOD

G. D. Biradar, S. N. Deshpande, *V. P. Choudhari

Department of Pharmaceutical Analysis and Quality Assurance, MAEER’S Maharashtra Institute of Pharmacy, Kothrud, Pune-411038.

Abstract

Two simple, precise, rapid and accurate methods for simultaneous determination of lamivudine (LAM), tenofovir (TEN) and nevirapine (NEV) in combined tablet dosage form are developed. Method A is based on ratio spectra derivative and method B is based on derivative spectra, methanol is used as solvent for both these method. Quantitation by ratio derivative amplitude was achieved at 352.9 nm, 359.9 nm and 348.9 nm for lamivudine, nevirapine and tenofovir, respectively for method A. Similarly the amplitudes at 324.01nm, 298.9 nm, 311.9 nm were measured for lamivudine, tenofovir and nevirapine for receptive drugs in method B. Beer’s law is obeyed in the range of 9-27 μg/ml by lamivudine, tenofovir and 6-18 μg/ml by nevirapine. The percentage assay in laboratory formulation was found to be in the range 99.39%100.23% by the proposed methods. The methods were validated with respect to precision, accuracy, specificity and robustness. The recovery was found in the range of 99.21-101.13 %. The methods developed are simple, economical, precise and accurate and can be used for routine quality control of analytes in combined tablets.

29

FORMULATION & EVALUATION OF GASTRIC FLOATING DRUG DELIVERY SYSTEM OF METOPROLOL SUCCINATE

Monica.G*, V.Vasu Naik, A. Anka Rao, A. Rajesh

Hindu College of Pharmacy, Amaravathi Road,Guntur, Andhra Pradesh, India.

Abstract

The present research work discusses the formulation and evaluation of controlled release floating matrix tablets of metoprolol by using natural polymers by direct compression method. Floating drug delivery system mainly aims at increase in drug gastric retention time. Metoprolol succinate is ß2 selective blocking agent which is used in management of hypertension. Metoprolol succinate floating drug delivery system was prepared using natural polymers like xanthan gum, Karaya gum and gas forming agent Sodium bicarbonate. Tablets were prepared using directly compression and were evaluated for buoyancy test, swelling study, drug content and In Vitro release profile. The prepared tablets showed acceptable physicochemical characteristics. All the prepared batches showed fine In Vitro buoyancy. The release data were subjected to different models zero order, first order Higuchi and Pappas in order to evaluate their release kinetics and mechanisms. Floating matrix tablets of Metoprolol succinate can be prepared well with combination of Xanthan gum and Karaya gum that shows controlled drug release up to 12 hours.

30

SIDE EFFECTS OF AYURVEDIC MEDICINES

Ms. Shruti B. Patil, Ms. Vaibhavi N. Garge, Dr. Vilasrao J. Kadam

Department of Pharmacology and Toxicology, Bharati Vidyapeeth’s College of Pharmacy, C. B. D. Belapur, Navi Mumbai-400614, Maharashtra, India.

Abstract

Ayurveda is considered one of the effective complementary medicines. Large number of people consume ayurvedic medicines on long term basis to treat the ailments. But it should be known that though herbs empower ayurvedic medicines, it is no exception to the side effects. There are side effects to ayurvedic medicines. In the following article, various ayurvedic herbs which are normally consumed are presented with side effects, followed by the case studies that are reported due to the medicines consumed. It should be noted that though Ayurveda is effective in treating most of the diseases, it also has few side effects and on long term consumption of those medicines they may be life threatening.

31

DISSOLUTION RATE ENHANCEMENT OF PIOGLITAZONE BY SOLID DISPERSION TECHNIQUE

Prabhjot Kour1, Mahesh Kumar Kataria2, Ajay Bilandi3

1Student, M. Pharmacy 4th Semester (Pharmaceutics), Seth G.L. Bihani S.D. College of Technical Education, Sri Ganganagar.

2Professor and Head of Department (Pharmaceutics), Seth G.L. Bihani S.D. College of Technical Education, Sri Ganganagar.

3Assistant Professor, Seth G.L. Bihani S.D. College of Technical education, Sri Ganganagar.

Abstract

Pioglitazone an oral hypoglycaemic second generation agent is characterized by low solubility in gastric fluid, low dissolution rate and inter-individual variability in bioavaibility. The objective of study was therefore to design optimized solid dispersion of Pioglitazone with polymer like Croscarmellose sodium and sodium starch glycolate. The binary systems i.e. both physical mixtures as well as solid dispersions were prepared with drug and polymers. The solid dispersions were prepared by solvent evaporation method. Infrared spectroscopy was performed to identify any physicochemical interaction between the drug and the carrier. Tablets containing best solid dispersion formulation, optimized, having Croscarmellose sodium (1:5 ratio of Pioglitazone & Croscarmellose sodium) were formulated and compared with the commercial conventional release product. The tablets formulation under investigation was then characterized for their various physicochemical properties such as weight variation, percentage friability, disintegration and in vitro dissolution profiles. A significant improvement in the dissolution of Pioglitazone in solid dispersion products has been observed (>91% within 60 minutes). Tablets containing solid dispersion exhibited better dissolution profile than commercial tablets with same release kinetics i.e. higuchi model. Thus, it may be concluded that solid dispersion technique can be successfully used for the improvement of dissolution of Pioglitazone.

32

IN SILICO ADME AND BIOACTIVITY PREDICTION OF PHYTOCONSTITUENTS OF MORINGA OLEIFERA AGAINST ALZHEIMER’S DISEASE

Lalit Rajan Samant, Vikrant Chandakant Sangar, Anuya Rege, Shahid Chowdhary, Sandip Pawar, Abhay Chowdhary Haffkine

Institute for Training Research and Testing.

Abstract

Alzheimer’s disease (AD) is a progressive neurological disease of the brain. It’s is the most common form of dementia which demolishes the vital brain cells causing trouble with memory, thinking and behaviour, brutal enough to affect work. The plant considered for the study was Moringa oleifera, had several phytochemicals in extracts out of which few were selected and studied for in silico adsorbtion, distribution, metabolism, excretion and bioactivity and druglikness property. 1 heptano, 2-Pyrrolidinone, Trans-linaloloxide, linalool oxide were following the rules which required for better drug like leads which can be further considered for in-vivo study.

33

AN IMPROVED PROCESS FOR PREPARATION OF PALIPERIDONE PALMITATE, AN ANTI-PSYCHOTIC AGENT

N. V. D. Harikiran Maddi, 1,2 Suribabu Madasu,1,2 N.A.Vekariya,1 Koteswaramma Ch,1 T. Chandiran,1 Aminul Islam,1 Paul S Douglas,2 Korupolu Raghubabu2
1Chemical Research and Development, Aurobindo Pharma Ltd.,Survey No.71&72,Indrakaran (V), Sangareddy (M), Medak Dist 502329. Telangana State, India.
2Engineering Chemistry Department, AU College of Engineering, Andhra University, Visakhapatnam-530003, Andhra Pradesh, India.

Abstract

An improved process for the preparation of Paliperidone palmitate, an anti-psychotic drug substance, with an overall yield of >87.0% (including purification) and >99.9% purity. Process optimization was done based on design of experiments (DOE) concept. Isolated product meets all regulatory requirements and quality target product profile (QTPP). Formation and control of all possible impurities are also addressed.

34

DEVELOPMENT, CHARACTERISATION AND EVALUATION OF SILDENAFIL ASPIRIN CO-CRYSTALS

Avani P. Khristi, Dr.Tejal Soni, Dr. B.N.Suhagia

Faculty of Pharmacy/ Dharmsinh Desai University, Nadiad- Gujarat.

Abstract

Sildenafil citrate is a selective inhibitor of phosphodiesterase type 5 enzyme (PDE5) extensively used for the treatment of erectile dysfunction (ED). Sildenafil citrate is BCS class II drug, practically insoluble in water. It’s absolute bioavailability is 41% and half life is 4 hours. Aspirin is a Cyclooxygenase Inhibitors (COX-1 & COX-2) having a mechanism by dilating blood vessels in vivo, probably through direct effect on vascular smooth muscle. Therefore, the vasodilator action of aspirin which dilates the blood vessels gives synergistic effect to Sildenafil Citrate. The active pharmaceutical ingredients (APIs) in crystalline forms are more promising towards the stability, reproducibility and purification of the same in comparison to other types of solid forms, hence having the most priority in comparison to other forms. The properties like dissolution rate and intrinsic solubility of several crystalline forms are different and thus are playing an important role in enhancing the bioavailability. The stability with respect to temperature and humidity are more significantly depending on packaging of crystals. Sildenafil Aspirin Pharmaceutical co-crystals were successfully engineered with succinic acid as coformer under reflux condition. A new solid phase (cocrystals) was characterized by Fourier transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD). Physical characterization showed that Sildenafil Aspirin cocrystalline phase had unique thermal, powder X-ray diffraction property. The physicochemical properties of pure Sildenafil and corresponding co-crystals were accessed in terms of melting point, drug content uniformity, dissolution studies. The rapid rate of dissolution of cocrystals was observed in initial 10 min. The extent of dissolution was also enhanced on account of cocrysatllization.

35

DIPEPTIDYL PEPTIDASE-4 INHIBITORS: THEIR ROLE IN THE MANAGEMENT OF TYPE 2 DIABETES

P. Sujatha*, S. Vijaya

Rajiv Gandhi Institute of Medical Sciences, Srikakulam.

Abstract

A primary objective in the management of type 2 diabetes, optimal glycaemic control is difficult to achieve and usually not maintained over time. Type 2 diabetes is a complex pathology, comprising altered insulin sensitivity and impaired insulin secretion. Recent advances in the understanding of the physiological functions of incretins and their degrading enzyme dipeptidyl-peptidase (DPP)-4 have led to the ‘discovery’ of a new class of oral anti-diabetic drugs. Several DPP-4 inhibitors (or gliptins) with different chemical structures are now available. These agents inhibit the degradation of the incretins. glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) and hence potentiate glucose-dependent insulin secretion. DPP-4 inhibitors inhibit DPP-4 activity by almost 100% in vitro, maintaining a >80% inhibition throughout the treatment period in vivo, thus prolonging GLP-1 half-life, and significantly reducing HbA1c generally by -0.7 – 0.8% as well as fasting and postprandial glycaemia. They are well-tolerated with no weight gain and few adverse effects, and, of particular interest, no increase in hypoglycaemic episodes. Although different by their chemical structure and pharmacokinetic properties, the DPP4 inhibitors currently available have proven similar glucose lowering efficacy. The production of glucagon-like peptide 1 (GLP-1), an incretin hormone, has been shown to be abnormally low in patients with type 2 diabetes, suggesting that GLP-1 may be a contributor in the pathogenesis of the disease. New type 2 diabetic medications target incretin hormones in their mechanism of action. The incretin effect is based on the understanding that oral glucose has a greater stimulatory effect on insulin secretion than that of intravenous glucose. Over the past few years, a number of therapeutic agents, acting either as incretin mimetics, e.g. GLP-1 agonists, or inhibitors of the breakdown of GLP- 1, e.g. dipeptidyl peptidase-4 inhibitors, have become available as treatment options for the management of type 2 diabetes.