Open Access Original Research Article

Drug Prescription Pattern in Pregnant Women Attending Antenatal Out Patient Department of a Tertiary Care Hospital

S. R. Gawde, S. S. Bhide, T. C. Patel, A. R. Chauhan, N. M. Mayadeo, S. B. Sawardekar

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2013/1943

Aims: Pregnant women requiring medication represent a challenge to healthcare providers to avoid any teratogenic risk to fetus. The purpose of this study was to provide information about the drug use among pregnant women in a tertiary care hospital, Mumbai, India.
Study Design: Cross-sectional study.
Place and Duration of Study: Department of Obstetrics and Gynecology and Department of Pharmacology, Seth GSMC & KEM Hospital, between July 2011 and December 2011.
Methodology: A cross sectional study was conducted by reviewing the antenatal care Outpatient department case papers of 760 random pregnant women. Demographic profile, detailed medical history and drug intake in current pregnancy was noted. The prescription pattern was assessed and the drugs were classified based on the US FDA Risk Classification.
Results: Out of 760 women, one third (33.18%) women were anemic. Majority drugs were prescribed for the treatment of upper respiratory tract infection, vaginal discharge, fever with chills, nausea and vomiting. The average number of drugs per prescription was 2.27. Only 4% drugs were prescribed by their brand name and 96 % by generic name. Iron, folic acid and calcium were prescribed to all pregnant women. Majority of the patients were prescribed Category A and B drugs. No patient was given Category X drugs.
Conclusion: Findings of our study showed that all pregnant women were provided with prophylactic iron and folic acid therapy. The occurrence of contraindicated medicines was desirably low, thereby minimizing overall risk to developing fetus. Thus prescribing pattern observed in our study sets a good example, as selection of drugs was rational in most of the cases.

Open Access Original Research Article

Phytochemical, Physicochemical and Chromatographic Profiling in Quality Control Systems for Select Herbal Medicines (Conavir and Niprd-AM1)

Sunday Ameh, Mujtaba Abubakar, Aminu Ambi, Patrick Ikokoh, Obiageri Obodozie, Magaji Garba, Herbert Cocker

Journal of Pharmaceutical Research International, Page 13-36
DOI: 10.9734/BJPR/2013/1887

Background: Conavir, an immunostimulant from aerial parts of Andrographis paniculata (AP) and Niprd-AM1, an antimalarial from roots of Nauclea latifolia (NL), are dry water extracts for capsulation. AP and NL have been in use in Asia and Africa for centuries.
Purpose: The study aimed to ascertain the criteria for quality assured production of Conavir and Niprd-AM1.
Experimental Details: Procedures of World Health Organization (WHO) were applied to evaluate quality parameters of AP/Conavir and NL/Niprd-AM1.
Results and Discussion: Conavir is granular, greenish brown, intensely bitter and practically odourless. Tests on AP and Conavir revealed alkaloids, saponins, tannins and terpenoids, but cardiac and cyanogenic glycosides (considered toxic) were not detected. Normal phase TLC of AP and Conavir yielded 5 principal spots each, while the reverse phase TLC yielded 6. HPLC fingerprints of AP, Conavir and a reference standard were reproducible but differed from each other. The GC-MS data of Conavir were consistent with the phytochemical profile of AP. Effect of storage suggested that both AP and Conavir were stable for up to 21 months or more. Niprd-AM1 is granular, yellowish brown and faintly aromatic, with an exciting bitter taste. Both NL and Niprd-AM1 contained alkaloids, saponins, flavonoids and terpenoids, but cardiac and cyanogenic glycosides were not detected. Normal phase TLC of NL yielded 9 principal spots, while Niprd-AM1 yielded 5, but the reverse phase TLC yielded 9 for each. HPLC fingerprints of NL, Niprd-AM1 and a reference standard were reproducible but differed from each other. The GC-MS data of Niprd-AM1 were consistent with the phytochemical profile of NL. Most of the quality variables of NL and Niprd-AM1 remained unchanged up to the 39th month of storage.
Conclusion: The results are consistent with NIPRD’s intention to file for the registration of Conavir and Niprd-AM1 for use in Nigeria.

Open Access Original Research Article

Drug Utilization Pattern and Cost Analysis in Rheumatoid Arthritis Patients – A Cross–Sectional Study in Tertiary Care Hospital, Mumbai

S. R. Gawde, Y. C. Shetty, S Merchant, U. J. Kulkarni, M. Y. Nadkar

Journal of Pharmaceutical Research International, Page 37-45
DOI: 10.9734/BJPR/2013/2229

Aims: To study the current prescription pattern and to analyze the cost of the treatment Prescribed to RA patients referred to rheumatology OPD in KEM hospital.
Study Design: Cross-sectional study.
Place and Duration of Study: Department of Medicine and Department of Pharmacology, Seth GSMC & KEM Hospital, between July 2011 and December 2011.
Methodology: The study protocol was approved by the institutional ethics committee. Patients attending Rheumatology OPD for existing RA disease were recruited as per inclusion criteria. Written informed consent was sought. It was a cross-sectional study. Total 100 consecutive rheumatoid arthritis patients (fulfilling the American College of Rheumatology Criteria 1987) were recruited from 1st July to 1st September 2011.
Results: Majority of patients (67%) in the study population were on combination of two DMARDs. Most frequently prescribed two DMARDs combination was methotrexate and hydroxychloroquine (64%). Average total cost per prescription was found to be 763.39 Indian rupees (US$ 14), while average hospital and out of pocket expense were 281.12 Indian rupees (US$ 5) and 482.88 Indian rupees (US$ 9) respectively.
Conclusion: The drug use pattern in RA was found to be DMARDs based and majority of the cost was borne by the patient. The total cost increased was due to administration of drugs to treat the adverse drug reaction. Prospective studies in a larger number of patients are needed to assess the utility of prescription audit and cost analysis of drugs used in RA.

Open Access Original Research Article

Rhoifolin; A Potent Antiproliferative Effect on Cancer Cell Lines

Omayma A. Eldahshan

Journal of Pharmaceutical Research International, Page 46-53
DOI: 10.9734/BJPR/2013/1864

Aims: To investigate the cytotoxic activity of rhoifolin against different cancer cell lines.
Study Design: Isolation, identification and cytotoxic activity evaluation.
Place and Duration of Study: Faculty of Pharmacy, Ain Shams University and Al-Azhar University, between October, 2010 and January, 2011.
Methodology: Rhoifolin, Apigenin 7-O-β neohesperidoside was isolated in a copious amount from the leaves of Chorisia crispiflora (Bombaceae). Its identity was unambiguously confirmed via different spectroscopic methods (UV, 1HNMR, 13CNMR and HMBC) and viability assay test was used to evaluate its cytotoxic activity.
Results: It exhibited potent anticancer activities, nearly similar to that of vinblastine, when evaluated against human epidermoid larynex (Hep 2) and human cervical (HeLa) carcinoma cell lines. Promising activities were also obtained against hepatocellular (Hep G2), colon (HCT-116) and fetal human lung fibroblast (MRC-5) carcinoma cell lines. A unique effect of rhoifolin was in having no cytotoxic activity against healthy normal cells (Vero cells) which indicates a high selectivity of this compound.
Conclusion: The findings of this study showed that rhoifolin could be used as an ideal anticancer agent. It discriminates between cancerous and non cancerous cell as it kills only the former one. So the side effects which may appear during chemotherapy could be overcome.

Open Access Original Research Article

Transmission Blocking of Year Round Resistant Malaria in Koraput (India) by OMARIA – A New Antimalarial Phytotherapy

Deepak Bhattacharya, B. M. Bhuyan, P. K. Pradhan, D. K. Nayak

Journal of Pharmaceutical Research International, Page 54-77
DOI: 10.9734/BJPR/2013/2207

Background: Globally, in resistant malaria endemic zones, even the latest lines of MDTs (multi drug therapes) are yielding chaotic results. These include unacceptable side effects/contraindications, with poor prognosis in juveniles/adolescents. Juvenile stage is intensely humoral and up-regulate infestation. MDTs are more unpredictable in the juveniles, and fail in the geriatric group. Pharmacies are also failing. Tropical-equatorial conditions necessitate frugal body cover cum bare foot life style. Typical geomorphology, orography, meteorology, flora and fauna provide year round conducive conditions for vector bionomics and for other types of infections. OMARIA (Orissa Malaria Research Indigenous Attempt) is a new anti-malaria phytotherapy that has been in mono station use (Koraput, India) since 1998 in drug resistant core endemic regions, also well known for tertian type. It transpired out of Koraput Model to Fight Malaria at Home with OMARIA.
Materials and Methods: OMARIA is composed of the dry rind of the Indo-year round fruiting Punica granatum (Dalimba). Principal drug moieties are: (i) ellagic acid; (ii) punicalagin (iii) punicalin and (iv) potassium (K+). Are physiologically compatible and has never been used before. All the moieties being non alkaloids offer a paradigm shift among anti-malarials.
Results: OMARIA kills and clears hemoprotozoas of all spp., at all stages (including gametocytes) in patients of all ages and chronicity. Is potently anti-inflammatory vis-a-vis WBCs; blocks transmission; prevents relapse and non- recrudescence; and is very useful in severe/acute/complicated/refractory malaria and in sickle cell patients. No development of resistance. Potassium (K+) probably acts as the drug’s efficacy upregulator.
Conclusion: OMARIA is prophylactic and therapeutic in target groups. Is useful in numerous forms of malaria, being active against key stages of the parasite (complicated or systemic status); and in patients having multiple infections. It has synergistic and possibly buffering roles. Koraput Model has been of much help to the afflicted communities and to the administrations.

Open Access Original Research Article

Phytochemical Investigation and Molecular Profiling by p21 and NF-κB of Chorisia crispiflora Hexane Extract in Human Breast Cancer Cells in Vitro

Samar S. Azab, Abeer M. Ashmawy, Omayma A. Eldahshan

Journal of Pharmaceutical Research International, Page 78-89
DOI: 10.9734/BJPR/2013/2001

Aims: The current study targets two main aims; 1st aim is the phytochemical investigation of the hexane extract of Chorisia crispiflora leaves. The 2nd aim is the evaluation of the in-vitro cytotoxic activity of the extract then examination of the molecular mechanisms underlying this cytotoxic effect.
Study Design: Isolation and identification of the compounds, cytotoxic activity investigation on breast cancer cell line and molecular mechanisms underlying the cytotoxic extract of Chorisia crispiflora which may interfere with several cell signaling pathways and insert anti-cancer effects through the suppression of NF-κB or activation of p21, on breast cancer cell lines MCF-7.
Place and Duration of Study: Faculty of Pharmacy, Ain Shams University and National Cancer Institute, Cairo University, Egypt. The study was completed within 10 months.
Methodology: n-hexane extract was tested against breast cancer cell line then investigated for its effect on NF-κB, p21 and DNA fragmentation. The compounds isolated were identified using different spectroscopic techniques.
Results: In this regard, three main compounds were isolated; β-sitosterol 1, β-sitosterol 3-glucoside 2 and stigmasterol 3-glucoside 3. The extract exhibited IC50 values of 7 and 4.2 μg/ml following 48 and 72 hrs of treatment; indicating its significant in-vitro cytotoxic activity. This cytotoxic activity was proven to be mediated through down regulation of NF-κB.
Conclusion: Our results suggest that n-hexane extract has potent cytotoxic effect on MCF7 cells in addition to down regulation of NF-κB. These findings consequently merit further exploration of the extract in subsequent in-vivo studies and later in controlled clinical trials.

Open Access Original Research Article

Formulation, in vitro and in vivo Characterisation of Diclofenac Potassium Sustained Release Tablets Based on Solidified Reverse Micellar Solution (SRMS)

S. A. Chime, A. A. Attama, F. C. Kenechukwu, E. C. Umeyor, G. C. Onunkwo

Journal of Pharmaceutical Research International, Page 90-107
DOI: 10.9734/BJPR/2013/1567

Aims: To formulate sustained release diclofenac potassium tablets based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties of the tablets.
Study Design: Formulation, in vitro and in vivo evaluation of sustained release diclofenac potassium.
Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka and Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria.
Methodology: SRMS, consisting of mixtures of phospholipid and triglyceride were prepared in the ratios of 1:1, 2:1 and 1:2 (Phospholipon® 90H: Softisan® 154) respectively. SRMS-based tablets containing 100 mg of diclofenac potassium each were prepared using validated plastic mould. The physicochemical properties of the tablet formulations were studied and compared with the market brands of the drug for sustained release properties. In vitro release was carried out in simulated intestinal fluid (SIF, pH 7.5) using the USP paddle method. Anti-inflammatory, analgesic/anti-nociceptive and ulcerogenic properties of the formulated tablets were studied using adult Wistar rats.
Results: The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix (LM) used (p < 0.05). The hardness of the tablets ranged from 4.55 ± 0.50 to 5.10 ± 0.39 kgf for tablets formulated with LM 1:2 and 1:1 (M3 and M1) respectively. Friability results indicated that all the SRMs tablets exhibited friability values less than 1 %. The erosion time ranged from 35.8 ± 1.10 to 120.3 ± 0.32 min. The release profile of the tablets showed maximum release between 8 – 11 h for all the batches. Diclofenac potassium tablets based on SRMS had good anti-inflammatory and analgesic properties and also inhibited the ulcerogenicity of the NSAID by up to 85 %.
Conclusion: Diclofenac potassium tablets based on SRMS could be used for once daily administration.

Open Access Original Research Article

Design, Formulation and Evaluation of Piroxicam Capsules Prepared by Solid Dispersion Technique

Shady A. Swidan, Hassan M. Ghonaim, Mamdouh M. Ghorab, Ahmed M. Samy

Journal of Pharmaceutical Research International, Page 108-134
DOI: 10.9734/BJPR/2013/2534

Objective: To improve the dissolution of poorly soluble Piroxicam (PRXM) by solid dispersion technique using water soluble carriers with or without the addition of sodium lauryl sulphate (SLS) as surfactant.
Methods and Materials: Solid dispersions of Piroxicam were prepared using different polymers such as polyethylene glycol (PEG 4000 and PEG 6000) polyvinylpyrrolidone (PVP K30 and PVP K90) without or with addition of 2% of (SLS). Solid dispersions were formulated in drug polymer ratios 1:1, 1:2, and 1:4, each ratio without or with 2% SLS using solvent evaporation method. The prepared formulae were assayed for drug content, production yield and stability properties. Dissolution profiles were done in phosphate buffer pH 7.4 and the in vitro release was evaluated according to the % released after 20, 30, 45 and 60 minutes. An accelerated stability study was done over 3 months at 40o and 60ºC and with relative humidity (RH) 75%.
Results and Discussion: All of the formulated solid dispersions displayed better dissolution profiles as compared to the pure drug. Formulae containing 2% SLS displayed better in vitro release results compared to formulae prepared without SLS. The degradation of PRXM was slow, indicating the chemical stability of PRXM in all prepared formulae.
Conclusion: A formula containing PRXM to PEG 4000 in the ratio 1:1 with 2% SLS was ranked first and gave the best results among prepared formulae.

Open Access Original Research Article

Antioxidant and Antibacterial Potential of Different Fractions from Roots of Eriosema chinense Vogel

Satyendra K. Prasad, Divya Jain, Manish Kumar, S. Hemalatha

Journal of Pharmaceutical Research International, Page 135-146
DOI: 10.9734/BJPR/2013/2661

Aim: The roots of the plant Eriosema chinense Vogel (Leguminosae-Papilionoideae) is taken in the form of vegetable and is traditionally used for the treatment of diarrhoea by the tribal people of Meghalaya, India. Therefore, the present study is an attempt to assess the antioxidant and antibacterial potential of different fractions from roots of Eriosema chinense along with quantitative estimations of phytoconstituents.
Study Design: Extraction, fractionation, analysis and antibacterial evaluation.
Place and Duration of Study: Department of Pharmaceutics, Indian Institute of Technology, Banaras Hindu University, India between April 2012 to October 2012.
Methods: Different fractions i.e. aqueous, ethyl acetate, chloroform and hexane fractions were obtained from ethanol extract of roots of Eriosema chinense and were subjected to preliminary phytochemical screening and quantification of total phenols, tannins, flavonoid and flavonol. All the fractions were then evaluated for in-vitro antioxidant activity by using different models, which includes total antioxidant capacity, assay of reducing power, free radical scavenging activity, nitric oxide scavenging assay, H2O2 scavenging activity and scavenging of hydroxyl radical. The study also included assessment of antibacterial activity of all fractions against bacterial strains including those implicated in diarrhoea.
Results: The chloroform fraction was found to be highly rich in flavonoids and phenols, which was followed by ethyl acetate fraction. In all the tested antioxidant models, chloroform and ethyl acetate fraction demonstrated the highest antioxidant potential as indicative through their IC50 values. All the fractions except aqueous fraction depicted a potent antibacterial activity at their respective higher concentration.
Conclusion: The antioxidant and antibacterial potential of Eriosema chinense may be attributed to the presence of phenols and flavonoids which plays a significant role in treatment of oxidative stress, cardiovascular arrests, inflammation, cancer and diarrhea.

Open Access Original Research Article

Oxidation of Bovine Albumin by Hypochlorous and Hypobromous Acids: Structural and Functional Alterations

Maicon S. Petrônio, João Roberto Fernandes, Manoel Lima de Menezes, Valdecir F. Ximenes

Journal of Pharmaceutical Research International, Page 147-160
DOI: 10.9734/BJPR/2013/3066

Aims: Hypochlorous (HOCl) and hypobromous (HOBr) acids are among the most powerful oxidants produced by the innate immune cells. Albumin is the predominant protein in most body fluids and is considered the most important antioxidant of blood plasma.
Study Design: Oxidation of bovine albumin (BSA) and study of its structural and functional alterations.
Place and Duration of Study: Faculty of Science and Faculty of Pharmaceutical Science, University of the State of Sao Paulo UNESP, between June and December 2012.
Methodology: BSA was oxidized with excess of HOCl or HOBr and its structural and functional alterations were analyzed by spectroscopic techniques as UV-Vis absorption, intrinsic and synchronous fluorescence, fluorescence quenching, Rayleigh scattering and circular dichroism.
Results: Both oxidants were able to deplete the intrinsic fluorescence of BSA, but HOBr was more effective than HOCl. The alterations in the synchronous fluorescence, UV-Vis absorption, and the appearance of a fluorescence band centered at 450 nm confirmed the difference between the oxidants. The oxidation did not induce aggregation of BSA as measured by Rayleigh scattering. The far-UV circular dichroism spectra showed a loss in the helical content and the near-UV-circular dichroism showed an alteration in the tertiary structure; HOBr was the more effective of the oxidants in this case. However, the oxidations did not induce significant alterations in the binding capacity of BSA, which was evaluated using hydrophobic (norfloxacin) and hydrophilic (ascorbic acid) drugs.
Conclusion: These results suggest that, although highly susceptible to oxidation, the alterations did not inhibit BSA’s physiological function as a transport protein.