Indian Journal of Pharmacy and Pharmacology

6-10

Authors: Research Article

Introduction: The cost of drug play important role in practice of medicine and disease outcome. In Indian market numerous brand available of generic drug. Tuberculosis is curable disease but if proper treatment not taken by patients then lead to development of drug resistance or pulmonary disability. AKT drugs used for the management of tuberculosis. Objective: To compare and analysed cost variation in AKT drugs with different brand name for same dosage form & same active compound. Materials and Methods: The price of the drug with same formulation and same strength (Dosage) was review from Indian drug review issue 3, 2017 (IDR) & CIMS (Apr- Jul 2017). Percentage of cost price variation and Cost ratio is analysed. Result: High percentage of cost variation among first line AKT drugs seen with Ethambutol (474.51%) followed by Isoniazid (432.60%). Least percentage of cost variation seen with streptomycin (1.01%) followed by rifampicin (1.33%). Maximum cost ratio of first line drugs seen with Ethambutol (5.74). Among 2nd line AKT drug Maximum and least percentage of cost variation are seen with levofloxacin 500 mg tablet formulations (1550.84%) and Ofloxacin 400 mg sustained Releases - tablet (1.57%) respectively. Higher percentage of cost variation seen with more manufacture company/ no. of brand. Conclusion: The wide percentage of cost variation is seen with AKT drugs available in Indian market. Regulation of drug price by concerned agencies and by government is needed. Rational drug prescription with low cost is important for treatment adherence and disease outcome

150-154

Authors: Hanumantha Rao K, Lakshmana Rao A, Chandra Sekhar KB

A simple, rapid, precise and accurate RP-HPLC method was developed and validated for the determination of Saroglitazar in tablet dosage form. Separation of the drug was achieved on a Kromasil C18 Column (150 mm x 4.6 mm I.D., 5 µm particle size). The method showed a linear response in the concentration range of 10-60 μg/ml using 0.1% orthophosphoric acid buffer: acetonitrile as the mobile phase in the ratio of 45:55 v/v with detection at 295 nm with a flow rate of 1 ml/min and retention time was 3.430 min. The method was validated as per the ICH guidelines. The method was successfully applied for routine quality control analysis of Saroglitazar in tablet dosage form.

160-168

Authors: Mohan Gandhi B, Lakshmana Rao A, Venkateswara Rao J

Objective: The main objective of this work is to develop simple, precise, accurate and reproducible UV-Spectrophotometric and Stability indicating RP-HPLC methods for simultaneous estimation of Gatifloxacin (GAT) and Flubiprofen sodium (FLU) in ophthalmic dosage form. Methods: Dual wavelength spectrophotometric method which involves solving of simultaneous equations based on the measurement of absorbances at 289 nm and 248 nm, which are the absorption maxima (λmax) of GAT and FLU respectively. The RP-HPLC analysis is carried out on Shiseido C18 column (250 mm × 4.6 mm I.D.), using 1% orthophosphoric acid in water and acetonitrile in the ratio of (40:60 % v/v) as the mobile phase with a flow rate of 0.9 ml/min. The detection was carried out at a wavelength of 236 nm. Results: The retention times were found to be 2.152±0.2 min and 7.881±0.2 min for GAT and FLU respectively. The linearity range was found to be 10-20 μg/ml and 1-2 μg/ml for Gatifloxacin and Flubiprofen sodium respectively by UV method and 10-30 μg/ml and 1-3 μg/ml for Gatifloxacin and Flubiprofen sodium respectively by HPLC method. The percentage recoveries of both the drugs GAT and FLU from the ophthalmic form were 99.51% and 99.58% respectively by UV method and 99.08% and 99.43% respectively by HPLC method. The correlation coefficients of both the drugs were found to be more than 0.99 by two methods. Other parameters like ruggedness, robustness etc. was well within the acceptance criteria. Conclusion: Both UV-spectrophotometric and stability indicating RP-HPLC methods were found to be accurate, rapid, precise and simple. These simple methods can be used for the simultaneous estimation of GAT and FLU in bulk and in ophthalmic dosage forms.

176-182

Authors: Aminabee SK, Lakshmana Rao A, Chinna Eswaraiah M

Objective: To evaluate the in-vivo antioxidant potential of ethanolic extract of whole plant of Michelia nilagirica against paracetamol induced toxicity in rats. Methods: Animals were treated with ethanolic plant extract for 7 days and the toxicity was induced with a single dose of paracetamol intraperitoneal injection. Pre-treatment with 70 mg/kg p.o of ethanolic extract of whole plant of Michelia nilagirica improved the SOD, catalase, peroxidase and glutathione levels significantly as compared to control group. Results: The present study revealed that Michelia nilagirica has significant in-vivo antioxidant activity and can be used to protect tissue from oxidative stress. The results showed that the activities of SOD, catalase, peroxidase and glutathione in group treated with paracetamol, declined significantly than that of normal group. Conclusion: Ethanolic extract of whole plant of Michelia nilagirica in the dose of 60 mg/kg, p.o. has improved the SOD, catalase, peroxidase and glutathione levels significantly. Based on this study we conclude that ethanolic extract of whole plant of Michelia nilagirica possesses in-vivo antioxidant activity and can be employed in protecting tissue from oxidative stress.

81-84

Authors: Bornali Dutta, Prasanta Kr. Bhattacharya, Mangala Lahkar

Aim: To explore the association of CYP2C9 genetic polymorphism in Type2 diabetic patient under the treatment of sulfonylurea (glimepiride) and undergoing adverse drug reactions (ADRs) Glimepiride, a sulfonylurea hypoglycemic agent, is metabolized by cytochrome P450 2C9 (CYP2C9) which is known to have genetic polymorphisms. The most frequent polymorphism is the single nucleotide polymorphism (SNP) which describes the occurrence of at least 2 different alleles for one gene differing only at one specific DNA position Studies shows that CYP2C91*,CYP2C9*2 and CYP2C9*3 are the most important known alleles of CYP2C9. The wild type allele CYP2C91* is with normal enzyme activity CYP2C92*allele has a nucleoside change from cytosine to thiamine at gene position 3608 and hence causes a substitution of arginine by cysteine at protein position144; it has only minor effect on substrate affinity. In CYP2C93* allele nucleoside change from adenine to cytosine at gene position 42614 , results in an amino acid substitution of isoleucine by leucine at protein position 359 this substitution results in a loss up to 70 % of the enzyme activity with CYP2C93* allele as compared with the wild type allele CYP2C91* Patient possessing a decreased enzyme activity because of its genetic disposition, will have a higher bioavailability and smaller clearance for drugs metabolized via this specific CYP. Impaired metabolism of sulfonylurea due to gene polymorphism in the metabolic enzyme CYP2C9 might lead to adverse drug reaction like hypoglycaemia, so genotyping of CYP2C9 may thus serve as a useful tool for predicting adverse effects caused by sulfonylurea and thus helps the clinicians for safer prescribing of oral hypoglycaemic agents. Material And Methods: Type2 diabetic patients of Guwahati Medical College Hospital, Assam under the treatment of sulfonylurea (glimepiride) was identified.70 patients with glimepiride treatment at a dose of 2mg once daily and undergoing therapy from day 1(one) to 2 years were possible to be identified in this 2 years of the study.32 patients had no complain for the drug but 38 patients suspected of having at least one adverse drug reaction(ADR) . Blood samples of patients experiencing ADRs as well as from patient without any complain for the drug were collected after written informed consent and prior ethical committee clearance ,reference no.MC/190/2007/Pt11/22 date:30/03/11.DNA was isolated , alleles CYP2C91*(wild type) and CYP2C92*, CYP2C93* variant form was detected by Polymerase chain reaction –Restriction fragment length polymorphism. Results: Variant form CYP2C92*and CYP2C93* allele on both groups with and without ADR experienced during the course of therapy was studied along with the wild type CYP2C91* from the variant form. Allele CYP2C9 1*(wild type, having 80% enzyme activity) predominates in the group experiencing no any adverse drug reaction. No variant form CYP2C92* allele was able to be identified in any of the two groups whereas variant form CYP2C93* allele was identified in few samples of the group with ADRs. A test for significance (chi square test) for occurrence of allele in parameter like adverse drug reaction was done. The p value (<0.05) obtained was found to be statistically significant.

90-99

Authors: G. Vidyasagar, Srinivasulu C

The stability of pharmaceutical products plays an important role from the economic point of view. There are not many studies that report about the stability of drugs past their expiration dates. The objective of the current study was to determine the tablet content of expired tablets of Frovatriptan where expiry date has not exceeded and to develop simple, accurate, sensitive and stability indicating RP-HPLC method for the determination of per cent drug remained of Frovatriptan in the presence of its degradation products in bulk drug, expired tablets and tablets whose expiry date has not been exceeded. Drug was subjected to all stress conditions such as hydrolysis (acidic and alkaline), oxidation, photolysis, thermal degradation and humidity study. Content determination was performed using RP-HPLC method; the percent of dissolved substance from tablets was also performed. All stressed samples were successfully analyzed on C18 column using mobile phase acetonitrile: methanol: 0.1% orthophosphoric acid 45:15:40 (v/v/v) mobile phase (pH5.6). A flow rate was maintained at 1 Ml/min and detection was made at 245 nm. The proposed method was validated with regard to linearity, sensitivity and accuracy and precision. No discrepancies between the results of determination and the declared values range for all the analyzed tablets were observed. The results of performed study might suggest that storage of analyzed batches of tablets over time period exceeding the expiry date given by the manufacturer did not influence their contents.

105-112

Authors: Aniket, A. Kumari, P. Kumari, S. Saurabh, L. Khurana, K. S. Rathore

The bioavailability and absorption of water soluble phyto constituents is erratic due to poor solubility of these constituents in gastrointestinal tract. This can be overcome by a novel delivery system known as phytosome technology in which water soluble phyto constituents are allowed to react with phospholipids. For better and improved bioavailability, natural phyto constituents must have a good balance between hydrophilicity (helps in dissolution in gastro-intestinal fluids) and hydrophobicity (helps to cross lipid rich cell membranes). This is achieved through phytosome technology. Phospholipids have a dual solubility and acts as an emulsifier. Phytosome technology acts as a bridge between novel and conventional delivery systems. Many products are available in the market based on this phytosome technology which includes popular herbal extracts such as Ginkgo biloba, Silybum marianum, grape seed, olive oil flavonoids etc.

119-133

Authors: Abhishek Soni, Raju L.

The aim of this study was to prepare Fast disintegrating tablet containing Hydrochlorothiazide by using Natural disintegrants. The tablets were prepared using micro crystalline cellulose as diluent and aspartame as sweetening agent along with Natural super disintegrant. The superdisintegrant used in this study was Isapghula mucilage and Banana powder. The tablets were evaluated for weight variation, hardness, friability, wetting time, water absorption ratio and disintegration time (DT) and dissolution study. Different concentration of superdisintegrant was used in this formulation as 2%, 4%, 6%, 8%. From the results obtained, it can be concluded that the tablet formulation prepared with 8% with Isapghula mucilage ie. 8 mg showed fast and higher drug release (97.68%) during in vitro dissolution study. Also the hardness, friability, dissolution rate and assay of prepared tablets (batch F8) were found to be acceptable according to standard limits.

139-142

Authors: Preeti Tyagi, Maloy B Mandal, A.N. Gangopadhyay

Atresia is the congenital obstruction with complete occlusion of intestinal lumen and responsible for 95% of congenital intestinal obstructions. Colonic atresia is a rare form of intestinal atresia. Because of its rarity, limited literature is available on management and outcome of this entity. Although new operative techniques and better perioperative managements have led to an improvement, but delay in intestinal motility recovery and long term decreased motility remained common problems in postoperative period. Most of the surgeons excise the atretic part and only few centimeter of just adjacent pre-atretic part. Most of the dilated pre-atretic part is not excised usually and considered as normal but study on its exact functional status is not available. This study was done on pre-atretic part of freshly excised specimen of a case of colonic atresia in vitro to know the functionality of this part which may be helpful to decide that it should be preserve or excise. After clearing of fecal matter, 2-3 millimeter wide and 15-20 millimeter long longitudinal strip was prepared and mounted in organ bath filled with Krebs Ringer solution continuously bubbled with 100% oxygen. Spontaneous contractions were observed with the frequency of approximately 3 peaks/ hour and amplitude of 27.23 gram per gram wet tissue. There was no response by lowest dose of histamine (0.1 μM) while dose dependent increase in the contractile force by different cumulative concentrations of histamine (1, 10 & 100 μM) was observed. It can be concluded that pre-atretic part is normal up to some extent especially in respect to the pacemaker activity and histaminergic pathway so it should be preserved. However, detailed functional and histopathological study on more number of cases as well as on control specimens by using different agonists and their blockers are needed.

1-5

Authors: Mallikarjun B Katte, Jagadishchandra S Ratnakar, Lopamudra Banerjee.

It was reported that some 3-amino 2-aryl-1-azolyl-2-butanol have antifungal effects. To understand the structural basis for antifungal activity and guide in the design of more potent agents, we performed quantitative structure activity. The Minimum Inhibitory Concentration (MIC) values of 3-amino-2-aryl-1-azolyl-2-butanol on yeast exhibited a strong correlation with the prediction made by the model developed in the present study. The statistical results of the Training Set, Regression coefficient r (0.841648) and r2 (0.708371) values gave reliability to the prediction of inhibitory activity of a series of Azole derivatives.

10-15

Authors: Anju Madhwar, Dharmender Gupta, Sujata Singh, N. A. Ansari

Objective: To determine the drug utilization pattern of antihypertensive agents in patients of hypertensive nephropathy in a tertiary care teaching hospital. Materials and Methods: This was a prospective observational study carried out in Shri Ram Murti Smarak Institute of Medical Sciences, Bareilly, over a period of three months. A total of 60 patients aged 40-79 years taking treatment for hypertension with associated nephropathy were enrolled in the study. All the relevant data were collected and drug utilization pattern of antihypertensive agents was determined. The study evaluated the percentage of use of multidrug therapy, drugs prescribed from Essential Drug List (EDL) and prescriptions with generic name. The cost of antihypertensive drugs used per day was calculated and linked with socioeconomic status of the patients. Results: Evaluation of the prescriptions demonstrates that a total of 63.3% males and 36.7% females with mean age of 58.9±11.9 years were enrolled out of which 70% patients were on multidrug therapy while only 30% were on monotherapy. The most common drug prescribed was amlodipine and around 60% drugs were from EDL 2011. Though only 16.67% patients were prescribed generic drugs but it did not affect the economic condition of the patient as most of enrolled patients belong to upper middle class. Conclusion: The prescriptions analysed were in accordance to guidelines of JNC-8 (Joint National Committee – 8) and most of the prescriptions were found to be rational and it also shows that management of hypertensive nephropathy needs combination therapy.

21-26

Authors: A. P. Dewani, D. S. Mohale, S. Hiware, R. L. Bakal, A. V. Chandewar

This work is concerned with application of simple, accurate, precise and highly selective reverse phase high performance liquid chromatographic (RP-HPLC) method for simultaneous estimation of Niacin (NA) and Simvastatin (SIM) in combined dosage form. Chromatographic separation was achieved by isocratic mode using a reverse phase C18 column (phenomenx, 150 х 4.6 mm i.d.). The mobile phase composed methanol:water in ratio 85:15 water consisting of Triethylamine (TEA) (0.05%v/v) v/v at flow rate of 1 ml/min pH was adjusted to 4 with orthophosporic acid. Detection was carried out using a UV-vis detector at 250 nm. The mean retention time of NA and SIM was found to be 1.8 min and 8.5 min. respectively. The method was found to be linear in the range of 80-120 μg/ml with mean recovery of 99.39% for NA and 99.18% for SIM. The correlation coefficients for both NA and SIM were close to 1. The developed method was validated according to ICH guidelines and values of accuracy, precision and other statistical analysis were found to be in good accordance with the prescribed values. Thus the proposed method was successfully applied for simultaneous determination of NA and SIM in routine analysis of formulation.

43-54

Authors: Hariprasad M .G, Rema Razdan, Yash T. C

Objectives: Anti-neoplastic drugs like Cisplatin, Taxols are associated with the development of peripheral neuropathy (PN). Severe neuropathy can occur in 3% to 7% of treated cases with single agents but can increase to 38% with combined regimens. The treatment options for PN currently include anti-depressants, anti-convulsants and opioid analgesics. These agents are modestly effective for symptomatic relief, but they do not affect the underlying pathology nor do they slow progression of the disease. Therefore, effective treatment for chemotherapy induced neuropathy would be a major advantage for cancer patients. It is well established thyroid hormones lays an important role in regulating the development and regeneration of the nervous system & local administration of triiodothyronine (T3) at the level of transected rat sciatic nerve increased the number and diameter of regenerated axons and SCG10 protein levels about two-fold in the different segments of transected nerve during the regeneration period.SCG10 protein is a regulator of microtubule dynamics in growth cones. The main objective of the study was to evaluate the neuroprotective activity of thyroxine in Cisplatin-induced PN in rats. Methods: PN was induced by Cisplatin - 2mg/kg,i.p. twice weekly for 8 weeks. The degree of protection was determined by measuring electrophysiological properties of sciatic nerve like nerve conduction velocity, motor in-coordination, thermal &cold hyperalgesia, grip strength and histopathological studies. Results: PN was evidenced in Cisplatin control rats and ameliorated with administration of T4 (0.1 mg/kg, s.c.) for 4weeks by augmenting all the above parameters. Conclusions: T4 exhibited neuroprotective activity, which would be attributed to its activity as neurotrophic effect.

62-69

Authors: Baweja Himanshu, Mishra Shyam, Mehta Yatin.

Indian Journal of Pharmacy and Pharmacology is a International, scholarly Peer-reviewed Journal which Published Four times per year by Innovative Publication. The journal publishes original and high-quality research papers in all areas of pharmacology and pharmacy. As an important academic exchange platform, scientists and researchers can know the most up-to-date academic trends and seek valuable primary sources for reference. The journal also publishes articles, reviews, etc., on any issues from the broadest range of Pharmacy and Pharmacology traditions and that cross disciplinary boundaries, through which it tries to provide the latest information on developments in Pharmacy and Pharmacology, and each issue is striving to bring you critical perspectives and cogent analyses.

74-82

Authors: Syed Ehtaishamul Haque, Ravindra Kumar Verma, Vasim Khan, Sumit Sharma

This review deals with homeopathic approach of treatment where focus is given to its principle, potency concept dosing pattern and symptomatic treatment. Special attention is given to a homeopathic drug Cactus grandiflorus. This review is a compilation of all therapeutic benefits of Cactus grandiflorus, giving more stress on cardioprotection.

1-17

Authors: PSRCHNP Varma D and A Lakshmana Rao

A simple, precise and rapid HPLC method has been developed for the simultaneous determination of Efavirenz, Tenofovir and Emtricitabine in pharmaceutical dosage form. The method was carried out using Zorbax C8 column (150 mm x 4.6 mm, 5 µm) and mobile phase comprised of mixture of dilute orthophosphoric acid solution pH 2.4±0.02 as buffer and acetonitrile in the ratio of 70:30 v/v and degassed under ultrasonication. The flow rate was 1.0 mL/min and the effluent was monitored at 252 nm. The retention times of Efavirenz, Tenofovir and Emtricitabine were 1.81 min, 2.80 min and 7.30 min respectively. The method was validated in terms of linearity, precision, accuracy, specificity, limit of detection, limit of quantitation and by performing recovery study. Linearity was in the range of 600.13 to 1800.39 µg/mL for Efavirenz, 300.54 to 900.44 µg/mL for Tenofovir and 200.46 to 601.38 µg/mL for Emtricitabine respectively. The percentage recoveries of all the three drugs were ranging from 98.2 to 101.9 for Efavirenz, 99.7 to 101.9 for Tenofovir and 98.7 to 101.6 for Emtricitabine respectively from the tablet formulation. The proposed method is suitable for the routine quality control analysis of simultaneous determination of Efavirenz, Tenofovir and Emtricitabine in bulk and pharmaceutical dosage form.

18-30

Authors: Raavi Kishna Swetha, K. S. G. Arul Kumaran, Jenila B, Ganesh P C, Sravan Kumar Y

Design, development and optimization of Aceclofenac SR matrix tablets by direct compression technique. It is composed of two different ratios of waxes. The optimization was carried out by using 32 factorial designs with Design Expert Software. IR studies reveled that drug and the waxes are compatible with each other. The tablets were subjected for various evaluations like pre and post compression parameters. All the parameters are within the limits. The release profile showed that as the concentration of bees wax increases the drug release decreases and it was not steady after definite concentration of bees wax. This may due to poor binding between the drug and waxes. The formulation (F7) with the ratios of 0.31:0.15 bees and lanette waxes respectively Show best sustained release and flow property. The dissolution profile showed 58.74% at 8th hr. It was observed that the bees and lanette waxes fulfilled the conditions for an optimum formulation for sustain release.

37-41

Authors: Priyadarshani S. Bansode, Mahendra Singh Ranawat, Ravindra Kamble, Chetan Singh Chauhan

Lercanidipine hydrochloride (LCD), a dihydropyridine calcium channel blocker is used in the treatment of hypertension. Atenolol (ATN), a cardio selective β-blocker is used as antihypertensive, antianginal and antiarrhythmic. The proposed method was development and validation of UV-Spectrophotometric and RP-HPLC for determination in bulk and tablet dosage form. In UV Spectroscopic method, LCD showed λmax at 237 nm in 50% v/v acetonitrile. The RP-HPLC analysis was performed by using a mobile phase of methanol: water (95:5 v/v), at a flow rate of 1.0 ml/min. By comparing validation results of both the methods, UV-spectrophotometric method is found to be simple, economical and rapid and RP-HPLC method were found to more precise, accurate, rugged and robust.

46-58

Authors: D.S. Mohale, A. S. Tripathi, J. B. Wahane, A.V. Chandewar

This review provides brief summary of structure, physiology and pharmacological role of Cyclooxygenase. Cyclooxygenase, an enzyme involved in the production of prostaglandins, exists in two isoforms, third isoform has been recently encountered. COX-1 is constitutively expressed and has a gastroprotective function. COX-2, induced at the site of injury, is responsible for the expression of pro-inflammatory prostaglandins. Despite overall similarities, COX-1 and COX-2 show subtle differences in amino acid composition at the active sites. COX-2 has valine at positions 89 and 523, while COX-1 has isoleucine, resulting in larger space availability in the former. Further, the presence of valine at position 434 in COX-2 as against isoleucine in COX-1 allows a gate mechanism to operate in favour of the former. The activity of cyclo-oxygenase-1 and 2 results in the production of a variety of potent biological mediators (the prostaglandins) that regulate homeostatic and disease processes.

64-106

Authors: Dr. P.D.Bharadia, Dr.Vikram M. Pandya

Indian Journal of Pharmacy and Pharmacology is a International, scholarly Peer-reviewed Journal which Published Four times per year by Innovative Publication. The journal publishes original and high-quality research papers in all areas of pharmacology and pharmacy. As an important academic exchange platform, scientists and researchers can know the most up-to-date academic trends and seek valuable primary sources for reference. The journal also publishes articles, reviews, etc., on any issues from the broadest range of Pharmacy and Pharmacology traditions and that cross disciplinary boundaries, through which it tries to provide the latest information on developments in Pharmacy and Pharmacology, and each issue is striving to bring you critical perspectives and cogent analyses.

110-112

Authors: Baweja Himanshu, Gupta Narmada Prasad

Indian Journal of Pharmacy and Pharmacology is a International, scholarly Peer-reviewed Journal which Published Four times per year by Innovative Publication. The journal publishes original and high-quality research papers in all areas of pharmacology and pharmacy. As an important academic exchange platform, scientists and researchers can know the most up-to-date academic trends and seek valuable primary sources for reference. The journal also publishes articles, reviews, etc., on any issues from the broadest range of Pharmacy and Pharmacology traditions and that cross disciplinary boundaries, through which it tries to provide the latest information on developments in Pharmacy and Pharmacology, and each issue is striving to bring you critical perspectives and cogent analyses.