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Journal of Pharmaceutical Negative Results
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   2010| October-December  | Volume 1 | Issue 2  
    Online since January 15, 2011

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How to select appropriate statistical test?
October-December 2010, 1(2):61-63
  54,509 5,213 3
Influence of solvents on the crystal habit and properties of rofecoxib and celecoxib: No evidence of polymorphism
MK Raval, PR Sathesh Babu, J Thimmasetty, RK Parikh, NR Sheth, C.V.S. Subrahmanyam
October-December 2010, 1(2):40-50
Background: In many cases, drugs can exist in more than one crystalline form; the phenomenon is known as "polymorphism." Though the polymorphs are chemically identical, they exhibit different physicochemical properties, viz., melting point, solubility, X-ray diffraction pattern, etc., which further affect the biological properties of drugs. The purpose of this work was to study the effect of solvents on crystallization, solubility and dissolution of rofecoxib and celecoxib. Materials and Methods: The crystals were prepared by using different solvents. The melting point, solubility, dissolution, Fourier-transformed infrared (FT-IR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) studies were carried out to confirm the polymorphism in drugs. Result: The results indicate that the crystals obtained from different solvents exhibited different physicochemical properties. Though FT-IR and XRD gave an indication of different crystal morphs, DSC proved absence of any polymorphic behavior in the crystals of rofecoxib and celecoxib. Conclusion: Crystals having the desired physicochemical properties may be obtained by selecting solvents of specific polarities.
  7,413 901 5
Influence of some hydrophilic polymers on dissolution characteristics of furosemide through solid dispersion: An unsatisfied attempt for immediate release formulation
MK Raval, DU Prajapati, SM Varma, MA Khodifad, JM Patel, NR Sheth
October-December 2010, 1(2):29-34
Background: The objective of the present investigation was to enhance dissolution characteristics of water insoluble drug, furosemide (FRMD), by solid dispersion in various hydrophilic carriers. Materials and Methods: The solid dispersions were prepared by solvent evaporation technique using urea and Hydroxy Propyl Methyl Cellulose (HPMC E50 LV). Physical mixtures of drug with above-mentioned polymers were also prepared. Phase solubility studies were performed for drug in the presence of excipients in different ratios. The formulations were evaluated for drug content, in vitro dissolution, Fourier transform infrared (FT-IR) and differential scanning calorimetry (DSC). Similarity factor (f2) was calculated for comparison between dissolution of pure drug and drug-polymer physical mixtures with solid dispersions. Results: Phase solubility studies indicated linear increase in the drug solubility with increase in carrier concentration. In vitro release studies revealed that dissolution characteristic of FRMD was improved by solid dispersion technique. All the preparations of FRMD exhibited significant improvement in its dissolution profiles. Solid dispersion of FRMD with HPMC E50 LV exhibited the highest rate and extent of dissolution. Optimized batches of solid dispersions of both the carriers were characterized by FT-IR and DSC analysis, which indicated absence of major interactions between FRMD and carriers. Conclusion: Solid dispersion technique is one of the finest techniques to improve dissolution of poorly soluble drugs.
  5,988 759 -
Beta vulgaris : A dearth of antidepressant activity in mice
Ashok Agrawal, Sunil Bavaskar, Pankaj Salunkhe, Nadeem Manyar, Dnyaneshwar Kale, Pravin Kawtikwar
October-December 2010, 1(2):55-57
The present study was undertaken to investigate antidepressant activity of ethanolic extract of Beta vulgaris [BV], by using forced swim test [FST] and tail suspension test [TST] in mice. Imipramine [10 mg/kg, i.p.] used as the standard drug significantly decreased immobility time in both TST and FST, while BV [50 and 100 mg/kg, i.p.] significantly increased immobility time in TST and FST. This suggests that BV has depressant activity and not antidepressant activity.
  5,536 451 -
Failure of calcium gluconate internal gelation for prolonging drug release from alginate-chitosan-based ocular insert of atenolol
Ritu Mehra Gilhotra, DN Mishra
October-December 2010, 1(2):35-39
Background: The aim of the investigation was to develop and evaluate ocular polymeric film of atenolol for the management of glaucoma. Materials and Methods: Fixed concentration blends of sodium alginate (NaAlg) and chitosan were combined with the varying concentration of calcium gluconate and the resulting hydrogels were casted as ocular films. Various physicochemical studies and in vitro release tests of the prepared films were carried out to study the effect of calcium gluconate addition to alginate-chitosan blend films. Results: Cumulative % drug released from the formulations ranged from 95 to 99% within 5- to 12-hour period. The drug release enhanced with incorporation of higher ratios of calcium gluconate. F1 (2% NaAlg and 1% chitosan without calcium gluconate) sustained the drug release for the longest period of time (12 hours). Addition of calcium gluconate to the formulation resulted in faster drug release rather than sustained drug release. Conclusion: The results showed that the addition of calcium gluconate leads to a change in the release capacities of the matrices. Despite the presence of calcium ions and thus the possibility of an ionic interaction, the internal gelation of the polymer matrix lead to enhanced drug release and poor sustaining of drug. The sustained release effect of NaAlg-chitosan matrices alone was the best among the formulations studied.
  3,958 533 -
Absence of central activity in Wrightia tinctoria bark ethanolic extract
P Bigoniya, AC Rana
October-December 2010, 1(2):51-54
Objective: The objective of the present study was to investigate the central activity profile of Wrightia tinctoria (Roxb) R.Br. Linn. (Family: Apocynaceae) in mice and rats using various models. Materials and Methods: The effects of ethanolic extract were observed in 3 different dose levels 300, 500, and 1000 mg/kg as the extract did not show any signs of toxicity up to 5000 mg/kg (p.o.) dose. Investigations were carried out for assessing the activity on pentobarbitone-induced hypnosis and maximum electro-shock (MES)- and leptazole-induced convulsions. Results: W. tinctoria ethanolic extract did not have any significant effect on pentobarbitone-induced hypnosis. The extract is devoid of any protective effect against leptazole- or MES-induced convulsions at any of the tested doses. Conclusion: W. tinctoria bark ethanolic extract had no central nervous system depressant or anticonvulsant activity.
  4,038 437 -
Insignificant antidiabetic activity of rhizome of Zingiber zerumbet
VK Lal, A Pandey, P Tripathi, RD Pandey
October-December 2010, 1(2):58-60
Objective: To investigate the antidiabetic activity of Z. zerumbet in streptozotocin (STZ)-induced diabetic rats. Materials and Methods: The diabetic rats were given aqueous extract of Z. zerumbet (200 mg/kg) and glibenclamide (10 mg/kg) for 21 days, and their hypoglycemic activity and effect on body weight were assessed. Result: The treatment with aqueous extract of Z. zerumbet and glibenclamide both showed hypoglycemic activity but efficacy of Z. zerumbet is not as significant as glibenclamide. Glibenclamide maintain the body weight of rats throughout the study period, whereas the body weight of Z. zerumbet-treated rats significantly falls. Conclusion: This study suggests that aqueous extract of Z. zerumbet shows no significant activity in STZ-induced diabetic rats.
  3,613 538 -
Some commonly observed statistical errors in clinical trials published in Indian Medical Journals
October-December 2010, 1(2):64-65
  2,708 429 -