Current Research in Pharmaceutical Sciences

99-109

Authors: Pranjal Jain, Shriya Jain, Ashwani Mishra and Anupam Pathak

Systemic effect producing medicinal and other curative agents can be taken by several route of administration but oral route is considered to be more effective route and possess high degree of patient compliance. Orodispersible tablet is the solid unit dosage form containing super disintegrates which impart the quality of quick disintegration in the presence of saliva and without producing any difficulty in swallowing of tablet. ODTs have very porous structure and highly soluble composition which get dispersed even in small presence of water such as saliva because this dosage form has been developed mainly for geriatric, pediatric and bedridden or disabled patients. For Rapid drug delivery ODTs are considered to be preferred dosage form.

116-119

Authors: Bushra Malik and Manoj Goyal

Exposure of Titanium trichloride to pregnant rats during the period of organogenesis is known to induce sever embryotoxicity, however, the overall mechanism is not know. Disturbances in the carbohydrate metabolism in the exposed mother may induced physiological alteration which are transported to the fetuses through Placenta. Glycogen contents, the activity of adenosine triphoshatase and glucose-6-phosphatase play an important role in inducing embryotoxicity and therefore these parameters has been studied in placenta, fetal liver and kidney of rats exposed to titanium trichloride. Doses of titanium trichloride 0.72 ml/kg of the body weight (1/5th of LD50) were administered orally once on 9th and 15th day of gestation p.c. and 0.36 ml/kg of the body weight (1/10 of LD50) were also administered orally daily from 6th to 14th day and 15th to 20th day of gestation. It has been observed that at doese of 0.72 and 0.36 ml/kg of body weight during organogeneises (from 6th to 14th and 9th day of gestation) and fetal development (from 15th to 20th and 15th day of gestation) significant depletion in glycogen contents in fetal livker and placenta was observed, however, no changes were recorede in kidney. The activity of ATPase during organogenesis and fetal development causes significant increase in kidney and liver. However, the activity of Glucose-6-phosphatase during organogenesis was significantly decreased in liver, kidney and placenta. Disturbances in carbohydrate metabolism in treated animals may become the cause of embryotoxicity.

77-83

Authors: Priyanka Gupta and Vikas Jharia

Moringa oleifera Lam [Moringaceae] is a highly valued plant, distributed in many countries of the tropics and subtropics. It has an impressive range of medicinal uses with high nutritional value. It is known by such regional names as drumstick tree, Sajiwan, kelor, Murungai kaai, marango, mulangay, saijhan, and sajna. Different parts of this plant such as the leaves, roots, seed, bark, fruit, flowers and immature pods contain a profile of important minerals, and are a good source of protein, vitamins, β -carotene, aminoacids and various phenolics which act as cardiac and circulatory stimulants, possess anitumor, antipyretic, antiepileptic, antiinflammatory, antiulcer, antispasmodic, diuretic, antihypertensive, cholesterol lowering, antioxidant, antidiabetic, hepatoprotective, antibacterial and antifungal activities, and are being employed for the treatment of different ailments in the indigenous system of medicine. This plant have broad spectrum activities so, further studies on other models and extensive clinical trials are needed to confirm these findings. The present study was undertaken to screen various phytochemicals like flavonoids and terpenoids present in the stem bark and evaluate the potentials for use of this plant, which will help to formulate effective herbal preparation that will be used to combat various disorders.

87-91

Authors: Rajendra Chauhan, Priyanka Arjariya, Gurdeep Singh, Naveen Sharma, Ashish Mangal

The main objective of the present study is to develop a single unit gastric floating drug delivery system (GFDDS) of Cefpodoxime Proxet.Tablets were prepared using various proportions of polymers such as HPMCK4M and Eudragit RS 100. Direct compression method was used for the preparation of tablets. Five different formulations were developed. Tablets were evaluated for physical characterization viz. weight variation, thickness, hardness, friability, drug content, swelling index, buoyancy determination, and in vitro drug release study. All parameters complied with IP limits. Formulation with both the polymers (F5) showed sustained release. Formulations with hydrophilic polymer (F1, F2) showed high release of drug when compared to formulations with hydrophobic polymers (F3, F4). Polymer HPMCK4M and the combination of Eudragit RS100 were found to have optimum floating characters for a longer period. It may be concluded from whole study that the combinations of hydrophilic polymers with hydrophobic polymers are suitable to optimize sustained release formulation of Cefpodoxime Proxetil.

44-47

Authors: Pramila Ghumare, D B Jirekar, Mazahar Farooqui and S D Naikwade

Nature has been a good source of medicinal agent for thousands of years and an impressive number of modern drugs have been isolated from natural sources, many based on their use in traditional medicine. Pongamia pinnata commonly known as karanj and has been recognized in different traditional system of medicine for the treatment various diseases of human beings. Different parts of this plant are traditionally used for treatment of various ailment including bronchitis, whooping cough, rheumatism, diarrhoea, gonorrhoea and leprosy. Therefore present study reveals that comprehensive information of Pongamia pinnata with various scientifically documented pharmacologically activities, traditional uses along with its role in industry.

57-63

Authors: Nidhi Patearia Mishra and Archana Verma

Medicinal plants have played an essential role in the development of human culture. Plant products have been part of phytomedicines since time immemorial. The phytochemical research based on ethno pharmacological information is generally considered an effective approach in the discovery of new anti-infective agents from higher plants. These can be derived from any part of the plant like bark, leaves, flowers, seeds, etc i.e., any part of the plant may contain active components. In the present work, qualitative phytochemical analysis was carried out of Bauhinia variegata of Caesalpiniaceae in three different solvents viz. ethanol, methanol and water. During the antimicrobial study it was observed that the ethanolic and methanolic extracts of leaves and stem of Bauhinia variegata showed best results against S.aureus (19mm) and P.aeruginosa (19mm) respectively among the bacterial strains and in fungal strains it gave good results in C.albicans (17.25mm) and C.albicans (16mm). The preliminary phytochemical screening of leaves and stem of Bauhinia variegata showed the presence of alkaloids, carbohydrates, glycosides, flavonoids, phenols, tannins, lignin, saponins, terpenoids and amino acids in all the three solvents used. The present investigation reported the crucial fact that phytochemicals present in different extracts of selected plant parts are highly responsible for their ethnomedicinal and antimicrobial potency.

8-14

Authors: Ankita Jain, A K Parashar, R K Nema, T Narsinghani

HPTLC is a most versatile technique and is known for uniformity, purity profile, assay values and precision and accuracy of results. It can handle several samples of even divergent nature and composition. HPTLC is a modern analytical separation method with extensive versatility, although already much utilized, is still with great potential for future development in research and development. It is accepted as a time-saving and most economical machine practically with minimum trouble shootings. It speeds up analysis work which is usually not possible with other parallel chromatographic techniques available. The scope of hyphenation of HPTLC with other analytical techniques appears to hold considerable promise for the analysts who previously have had reservation towards the use of planar chromatography. Its hyphenation with mass/infra red/laser spectroscopy, etc. opens a new dimension which makes it the most prestigious among the analytical chemists in the present perspective. In this article, we present a practical view of the concepts of various parameters in the validation fields of quantitative high-performance thin layer chromatography analytical methods in pharmaceutical analysis, as well as several recent methods to serve as an introduction to applications of analytical validation, whether they are for an academic or an industrial researcher.

21-28

Authors: Asheesh Singh,Vinayaditya Singh, Jagrati Singh, Naveen Sharma

Trovafloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class and is used to treat severe or life-threatening bacterial infections or bacterial infections that have failed to respond to other antibiotic classes. It is sold under various brand names, such as Trovan and Tavanic, the most common. Trovafloxacin is considered to be same as Ofloxacin by the U.S. Food and Drug Administration (FDA), with the exception of the potency shown in vitro against mycobacteria. In vitro, it is, in general, twice as potent as ofloxacin, whereas d-ofloxacin is less active against mycobacteria. The advantage of administering a single dose of a drug that is released over an extended period of time instead of numerous doses is now a day’s area of interest for formulation scientists in Pharmaceutical industry. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance due to less frequent drug administration, maximum utilization of the drug, increased safety margin of potent drug, reduction of fluctuation in steady-state drug levels, reduction in healthcare costs through improved therapy and shorter treatment period. Wide varieties of polymers like Hydroxy Propyl Methyl Cellulose (HPMC), Carboxy Methyl Cellulose (CMC), Ethyl Cellulose (EC), Cellulose Acetate Phthalate, HPMC K100M, Xanthan gum, Carrageenan gum, Karaya gum, HPMC K15, Carbopol 971P and Carbopol 974P etc. are available for retarding the release rate of drugs hence sustains the action of drugs.

108-113

Authors: Neha Sahu, Jagdish K Sahu and Atul Kaushik

Triazole is an entity which is being synthesized in many of its derivative form from past few years; the entity is major source of interest for many of medicinal chemist to explore its various pharmacological potentials. Various methods for synthesizing triazoles are discussed with their chemistry. Studying this chemistry different substituted and fused compounds of triazole are analyzed here for varying pharmacological activities. In present article we review the chemistry of triazole and its pharmacological actions as antihelmintics, anticancer, antifungal and anti-inflammatory agent by studying its various synthesized derivatives.

122-131

Authors: H K Sharma and V Alagarsamy

In this study we aimed to fix Rungia repens (L) Nees botanical identity, macroscopical, microscopical diagnostic characters and to isolate the bio-active principle responsible for biological actions shown by ethyl acetate and methanol extracts. Bioactive compounds were isolated by running column chromatography, characterized and percentage of activity of bioactive principle was calculated. Microscopical study reveals the characteristic nature of stomata, trichome, leaf mid rib and stem. The extracts were found to be non toxic upto the dose of 3000 mg/kg of Rungia repens ethyl acetate extract (RREAE) and methanolic extract (RRME) respectively. RREAE and RRME produced a significant and dose dependent inhibition of analgesic, anti inflammatory and antipyretic activity. Bioactive principle isolated was a flavonoid luteolin shows maximum activity equal to that of standard drug. We believe that the antipyretic, analgesic, and anti-inflammatory activity of the RREAE and RRME were due to its bioactive principle flavonoid luteolin present in the extract.

138-143

Authors: Asheesh Singh, Amit Jain and Bhawna Mishra

A QSAR study on 4-benzylideneamino-benzenesulfonamide & 4-phenyliminomethyl-benzenesulfonamides derivatives as selective cyclooxygenase-2 (COX-2) & COX-1 inhibitors was performed with 21 (16 training + 5 test) compounds. Molecular modeling studies were performed using Chemoffice 6.0 supplied by cambridgesoft. The sketched structures were subjected to energy minimization and the lowest energy structure was used to calculate the physiochemical properties. The regression analysis was carried out using a computer program called VALSTAT. The best models were selected from the various statistically significant equations. The substitution Different monosubstituents preferably at the 3- or 4-position of the phenyl ring had the greatest influence on selectivity (COX-1 & COX-2). Replacement of the 4-hydroxy moiety with an electron withdrawing group such as 4-fluoro, 4-methoxycarbonyl, or 4-nitro substituents increased inhibitory potency and selectivity. However, 3-nitro substituent resulted in loss of inhibitory potency. On the other hand, the 4-N, N-dimethylamino substituent exhibited potent and selective inhibition of cyclooxygenase. Among these compounds with monosubstituted at the para-position, cyclooxygenase the inhibitory selectivity order was 4-F > 4-CO2Me > 4-NMe2 > 4-NO2 > 4-OH > unselective 3-NO2. The analysis resulted in QSAR equation, which suggests that, n=16, r=0.880, r2=0.774, adjusted squared multiple R=0.713, Standard error of estimate(s) = 0.106 & validated r2 (q2) =0.671. This study can help in rational drug design of new cyclooxygenase-2 inhibitor with predetermined affinity.

148-153

Authors: Veerendra Sharma, Pooja Sinoriya and S C Mehta

To investigate the anticonvulsant and CNS depressant activity of methanolic extracts of whole plant of Sida acuta and Sida rhombifolia in mice. The methanolic extract of whole plant of Sida acuta (MESA) and Sida rhombifolia (MESR) (100, 200 and 400 mg/kg, p.o.) was studied for its anticonvulsant effect on maximal electroshock (MES) induced seizures and Pentylenetetrazole (PTZ) induced seizures and CNS depressant activity at the same dose level using traction test, rota rod and locomoter activity in mice. MESA and MESR at dose 100, 200 and 400 mg/kg significantly reduced the duration of the seizures as compared to control group. In CNS depressant activity and the mean time duration on rotating rod was significantly decreased (P<0.0001) and decline in motor co-ordination.