Indian Journal of Pharmaceutical Sciences : 2011 - 73(3)

Boswellia serrata , a potential antiinflammatory agent: An overview

MZ Siddiqui — Sat,3 Mar 2012

MZ Siddiqui

Indian Journal of Pharmaceutical Sciences 2011 73(3):255-261

The resin of Boswellia species has been used as incense in religious and cultural ceremonies and in medicines since time immemorial. Boswellia serrata (Salai/Salai guggul), is a moderate to large sized branching tree of family Burseraceae (Genus Boswellia), grows in dry mountainous regions of India, Northern Africa and Middle East. Oleo gum-resin is tapped from the incision made on the trunk of the tree and is then stored in specially made bamboo basket for removal of oil content and getting the resin solidified. After processing, the gum-resin is then graded according to its flavour, colour, shape and size. In India, the States of Andhra Pradesh, Gujarat, Madhya Pradesh, Jharkhand and Chhattisgarh are the main source of Boswellia serrata. Regionally, it is also known by different names. The oleo gum-resins contain 30-60% resin, 5-10% essential oils, which are soluble in the organic solvents, and the rest is made up of polysaccharides. Gum-resin extracts of Boswellia serrata have been traditionally used in folk medicine for centuries to treat various chronic inflammatory diseases. The resinous part of Boswellia serrata possesses monoterpenes, diterpenes, triterpenes, tetracyclic triterpenic acids and four major pentacyclic triterpenic acids i.e. β-boswellic acid, acetyl-β-boswellic acid, 11-keto-β-boswellic acid and acetyl-11-keto-β-boswellic acid, responsible for inhibition of pro-inflammatory enzymes. Out of these four boswellic acids, acetyl-11-keto-β-boswellic acid is the most potent inhibitor of 5-lipoxygenase, an enzyme responsible for inflammation.

Revisiting curcumin chemistry part I: A new strategy for the synthesis of curcuminoids

E Venkata Rao — Sat,3 Mar 2012

E Venkata Rao, P Sudheer

Indian Journal of Pharmaceutical Sciences 2011 73(3):262-270

A new strategy for the synthesis of curcuminoids is described involving the reaction of acetylacetone difluroboronite with an aromatic aldehyde in the presence of n-butylamine as catalyst. The new intermediate products, curcuminoid difluroboronites, of symmetrically substituted curcuminoids like curcumin and bisdemethoxycurcumin are stable, can be isolated and hydrolysed with aq. methanol at pH 5.8 to get the curcuminoids of high purity. The method is applicable for unsymmetrical curcuminoids like demethoxycurcumin also with some modification involving column chromatography. The intermediate curcuminoid difluroboronites, as also the natural β-diketone pongamol difluroboronite, prepared for the first time were characterized on the basis of physical and chemical properties and spectroscopic data. The advantage of using borontrifluoride to protect the enol group in acetylacetone over the generally used boric oxide is brought out. The importance of conducting biological activity studies using pure curcuminoids is explained.

Enhancing hepatoprotective bioactives of Phyllanthus amarus through immobilization by growth promoters and media changes

JS Thakur — Sat,3 Mar 2012

JS Thakur, RK Agarwal, MD Kharya

Indian Journal of Pharmaceutical Sciences 2011 73(3):271-275

The present paper describes enhancement of lignans, phyllanthin and hypophyllanthin present in Phyllanthus amarus plant. Supplementation was done to enhance secondary metabolites by modifying the media and treatment with different growth promoters and abiotic elicitors to increase the content of hepatoprotective bioactives in immobilized cell cultures, after incubation for 21 days. MS medium was supplemented with gibberellic acid and to make whole process commercially viable, when coconut water, sugarcane juice and water-melon extract were treated, it was revealed that watermelon extract, enhances maximum phyllanthin and hypophyllanthin yield followed by sugarcane juice, coconut water and gibberellic acid after estimation by HPTLC. The present method was found to be accurate, economical and viable to enhance the content of phyllanthin and hypophyllanthin in P. amarus for large-scale commercial production.

Preparation of evodiamine solid dispersions and its pharmacokinetics

H Xu — Sat,3 Mar 2012

H Xu, T Zhang, H Yang, X Xiao, Y Bian, D Si, C Liu

Indian Journal of Pharmaceutical Sciences 2011 73(3):276-281

In order to increase the dissolution rate and bioavailability, solid dispersions of evodiamine in PVP K 30 with different enriched samples of evodiamine to PVP K 30 ratios were prepared by solvent method. Our studies showed that the dissolution rate of evodiamine was significantly higher in the solid dispersion system in comparison with that in enriched samples of evodiamine or physical mixtures. The increase of the dissolution rate was evidently related to the ratio of evodiamine to PVP K 30 . The solid dispersion system (enriched samples of evodiamine/PVP K 30 = 1/6, w/w) gave the highest dissolution rate: about 27.7-fold higher than that of enriched samples of evodiamine in hard capsules. Powder X-ray diffraction studies showed that enriched samples of evodiamine presented a total chemical stability after its preparation as solid dispersions. In vivo administration studies indicated that solid dispersions of evodiamine in hard capsules had a higher Cmax and a shorter Tmax than those of physical mixture in hard capsules, and the differences of Cmax and Tmax between them were significant. These results suggest that solid dispersions of evodiamine in hard capsules has a notably faster and greater absorption rate than enriched samples of evodiamine in physical mixture hard capsule and corresponds with the in vitro dissolution.

Comparison of aerosol formulations of formoterol fumarate and budesonide

NM Nirale — Sat,3 Mar 2012

NM Nirale, MS Nagarsenker, SB Mendon, R Chanagare, A Katkurwar, V Lugade

Indian Journal of Pharmaceutical Sciences 2011 73(3):282-286

The aerodynamic diameter of pharmaceutical aerosols is the main factor governing their deposition in the human respiratory tract. Particle size of the pharmaceutical aerosols is characterized by liquid impingers and Andersen Cascade Impactors. The present study was aimed at comparing two metered dose inhaler formulation containing formoterol fumarate (6 μg) and budesonide (200 μg). These two formulations were evaluated by using Twin Stage Impinger and Andersen Cascade Impactor. Study revealed that developed metered dose inhaler I formulation of the formoterol fumarate and budesonide had lower mass median aerodynamic diameter and higher fine particle fraction than marketed formulation.

Identification of forced degradation products of itopride by LC-PDA and LC-MS

Payal Joshi — Sat,3 Mar 2012

Payal Joshi, Suvarna Bhoir, AM Bhagwat, K Vishwanath, RK Jadhav

Indian Journal of Pharmaceutical Sciences 2011 73(3):287-291

Degradation products of itopride formed under different forced conditions have been identified using LC-PDA and LC-MS techniques. Itopride was subjected to forced degradation under the conditions of hydrolysis, photolysis, oxidation, dry and wet heat, in accordance with the International Conference on Harmonization. The stress solutions were chromatographed on reversed phase C18 (250×4.6 mm, 5 μm) column with a mobile phase methanol:water (55:45, v/v) at a detection wavelength of 215 nm. Itopride degraded in acid, alkali and oxidative stress conditions. The stability indicating method was developed and validated. The degradation pathway of the drug to products II-VIII is proposed.

Synthesis, antimicrobial and antioxidant activity of some oxindoles

SS Rindhe — Sat,3 Mar 2012

SS Rindhe, BK Karale, RC Gupta, MA Rode

Indian Journal of Pharmaceutical Sciences 2011 73(3):292-296

The present work describes the synthesis and spectral analysis of some new 3(Z)-{4-[4-(arylsulfonyl)piperazin-1-ylbenzylidene)-1,3-dihydro-2H-indol-2-one (5a-j). Ten of the synthesized compounds were screened in vitro against six species of microorganisms, Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Asperigellus niger and Asperigellus clavatus. Most of the compounds exhibited significant antimicrobial activity. All of these compounds were also screened in vitro for the antioxidant activity using DPPH assay. Most of them have shown very significant antioxidant activity.

Development and validation of simultaneous spectrophotometric methods for drotaverine hydrochloride and aceclofenac from tablet dosage form

SA Shah — Sat,3 Mar 2012

SA Shah, DR Shah, RS Chauhan, JR Jain

Indian Journal of Pharmaceutical Sciences 2011 73(3):296-300

Two simple spectrophotometric methods have been developed for simultaneous estimation of drotaverine hydrochloride and aceclofenac from tablet dosage form. Method I is a simultaneous equation method (Vierodt's method), wavelengths selected are 306.5 and 276 nm. Method II is the absorbance ratio method (Q-Analysis), which employs 298.5 nm as λ1 and 276 nm as λ2 (λmax of AF) for formation of equations. Both the methods were found to be linear between the range of 8-32 μg/ml for drotaverine and 10-40 μg/ml for aceclofenac. The accuracy and precision were determined and found to comply with ICH guidelines. Both the methods showed good reproducibility and recovery with % RSD in the desired range. The methods were found to be rapid, specific, precise and accurate and can be successfully applied for the routine analysis of drotaverine and aceclofenac in their combined tablet dosage form.

Role of Butea frondosa in ameliorating gastric markers in induced gastric lesions of rats

D Banji — Sat,3 Mar 2012

D Banji, Otilia J. F. Banji, Meenu Singh, AR Annamalai

Indian Journal of Pharmaceutical Sciences 2011 73(3):300-302

The study evaluated the ability of the alcohol extract of Butea frondosa to protect the gastro-duodenal lining from injury inflicted by acetic acid and pyloric ligation in rats. The induced gastric lesions lead to the generation of alkaline phosphatase and pepsin, which serve as important markers of gastric damage. Alcohol extract of Butea frondosa was administered in doses of 10, 100, 300 and 500 mg/kg as a single schedule and for the time dependent studies in a dose of 100 mg/kg for 7, 14, 21 and 28 days, respectively. Our studies reveal a decline in the formation of alkaline phosphatase and pepsin with 300 and 500 mg/kg of the extract and following treatment for 21 and 28 days, respectively. Extract of Butea frondosa produces significant diminution in the formation of gastric markers implying possible gastro-protective action.

Evaluation of wound healing potential of topical formulation of leaf juice of Tridax procumbens L. in mice

B Yaduvanshi — Sat,3 Mar 2012

B Yaduvanshi, Rajani Mathur, SR Mathur, T Velpandian

Indian Journal of Pharmaceutical Sciences 2011 73(3):303-306

Tridax procumbens L. (Compositae) is a common weed that grows in the rice fields of India. Traditionally the juice from leaves of Tridax procumbens has been used for healing dermal wound. However, in experimental studies, equivocal pro and anti-healing action of T. procumbens has been demonstrated. The present study evaluates the effect of topical ointment formulation of the leaf juice of T. procumbens using excision wound model in mice. Excision wounds (4 mm, i.d.) were inflicted on depilated back of mice. Ointment formulation of TP (50 mg of either 1 or 4 mg/g) was applied twice daily for 4 days on the dermal wound. Similarly, control group was treated with VEGF ointment (50 mg of 1 μg/g). The parameters observed were re-epithelization, vascularity, fibroblast number, collagen content. The healing exerted by TP (1 mg/g) was comparable to VEGF (1 μg/g). On the other hand, TP (4 mg/g) induced inflammation, edematous tissue and decreased vascularity. Taken together, the results imply that TP possesses dose dependent pro-healing potential, and its high dose exerts inflammatory reaction.

Diuretic effects of young fruit extracts of Bombax ceiba L. in rats

SS Jalalpure — Sat,3 Mar 2012

SS Jalalpure, NB Gadge

Indian Journal of Pharmaceutical Sciences 2011 73(3):306-311

The present study was aimed to investigate the diuretic effects of aqueous and crude ethanol extracts of Bombax ceiba L. fruits (family, Bombacaceae) using acute model in rats. A single individual dose of aqueous and ethanol extract of B. ceiba fruit (200 mg/kg and 400 mg/kg, p.o., each), frusemide and hydrochlorothiazide, (25 mg/kg, p.o., each) as reference diuretic drugs, were administered orally to dehydrated rats. Control group rats were fed with normal saline (25 ml/kg, p.o.). All rats were caged in metabolic cages in pairs and their urine output was monitored at 5 and 24 h intervals. Both extracts significantly increased the urine output in higher doses. Although, the onset of this diuretic action was gradual (within 5 h), it lasted throughout the studied period (up to 24 h). Further, the intensity of diuresis induced by aqueous extract (400 mg/kg) in 5 h was almost similar to that of frusemide and hydrochlothiazide. Aqueous extract of B. ceiba fruit also caused marked increase in urinary Na + and K + levels. However, the routine urinalysis showed non-significant alterations in pH and specific gravity by either dose of crude extracts of B. ceiba fruits. These effects demonstrate possible diuretic actions of B. ceiba fruit extracts and support its folklore use in various urinary ailments. Further studies need to be done to characterize the active phytoconstituents from fruits.

Microencapsulation of eugenol by gelatin-sodium alginate complex coacervation

Ujwala Shinde — Sat,3 Mar 2012

Ujwala Shinde, Mangal Nagarsenker

Indian Journal of Pharmaceutical Sciences 2011 73(3):311-315

Present study describes microencapsulation of eugenol using gelatin-sodium alginate complex coacervation. The effects of core to coat ratio and drying method on properties of the eugenol microcapsules were investigated. The eugenol microcapsules were evaluated for surface characteristics, micromeritic properties, oil loading and encapsulation efficiency. Eugenol microcapsules possessed good flow properties, thus improved handling. The scanning electron photomicrographs showed globular surface of microcapsules prepared with core: coat ratio1:1.The treatment with dehydrating agent isopropanol lead to shrinking of microcapsule wall with cracks on it. The percent oil loading and encapsulation efficiency increased with increase in core: coat ratio whereas treatment with dehydrating agent resulted in reduction in loading and percent encapsulation efficiency of eugenol microcapsules.

Extended Hildebrand solubility approach: Satranidazole in mixtures of dioxane and water

PB Rathi — Sat,3 Mar 2012

PB Rathi, VK Mourya

Indian Journal of Pharmaceutical Sciences 2011 73(3):315-319

The extended Hildebrand solubility parameter approach is used to estimate the solubility of satranidazole in binary solvent systems. The solubility of satranidazole in various dioxane-water mixtures was analyzed in terms of solute-solvent interactions using a modified version of Hildebrand-Scatchard treatment for regular solutions. The solubility of satranidazole in the binary solvent, dioxane-water shows a bell-shaped profile with a solubility maximum well above the ideal solubility of the drug. This is attributed to solvation of the drug with the dioxane-water mixture, and indicates that the solute-solvent interaction energy is larger than the geometric mean (δ1δ2 ) of regular solution theory. The new approach provides an accurate prediction of solubility once the interaction energy is obtained. In this case, the energy term is regressed against a polynomial in δ1 of the binary mixture. A quartic expression of W in terms of solvent solubility parameter was found for predicting the solubility of satranidazole in dioxane-water mixtures. The method has potential usefulness in preformulation and formulation studies during which solubility prediction is important for drug design.

A sensitive RP-HPLC method for simultaneous estimation of diethylcarbamazine and levocetirizine in tablet formulation

J Mahesh Reddy — Sat,3 Mar 2012

J Mahesh Reddy, MR Jeyaprakash, K Madhuri, SN Meyyanathan, K Elango

Indian Journal of Pharmaceutical Sciences 2011 73(3):320-323

A simple, sensitive and reproducible method was developed and validated for the simultaneous estimation of diethylcarbamazine and levocetirizine in its tablet formulation by reverse phase high performance liquid chromatography using Waters1515 HPLC with UV detector at the λmax of 224 nm, using Princeton Sphere-100 C 18 (250×4.6 mm. 5 μ) column. The mobile phase used was 20mM potassium dihydrogen orthophosphate buffer (pH: 3.2):acetonitrile (50:50 v/v) with isocratic flow (flow rate 1 ml/min) and the pH was adjusted with orthophosphoric acid. Losartan potassium was used as an internal standard. The compounds diethylcarbamazine, levocetirizine and losartan potassium were eluted at 2.12, 4.27 and 5.96 min, respectively. The peaks were eluted with better resolution. The method was accurate with assay values of 96.32 and 93.04% w/w, precise (%RSD) with intra-day 1.72 and 1.89 and inter-day 1.85 and 1.92, recoveries 102.86 and 101.1% w/w, which are very sensitive with limit of detections (LOD)'s 75, 50 ng/ml and limit of quantification (LOQ)'s 100, 75 ng/ml and linear with R 2 values 0.994 in the range of 5 to 30 μg/ml 0.1 to 1 μg/ml for diethylcarbamazine and levocetirizine, respectively. Hence this method can be applied for quantification of different formulations containing diethylcarbamazine and levocetirizine simultaneously.

Formulation and evaluation of niosomes

VC Okore — Sat,3 Mar 2012

VC Okore, AA Attama, KC Ofokansi, CO Esimone, EB Onuigbo

Indian Journal of Pharmaceutical Sciences 2011 73(3):323-328

Span 20-based niosome was prepared by lipid film hydration technique and loaded with Newcastle disease vaccine. Three batches with Span 20, cholesterol and dicetyl phosphate in micro molar ratios of 10:10:1; 15:15:1 and 20:20:1 were prepared and evaluated for encapsulation efficiency using haemagglutination test. The morphology of the vesicles was studied by means of transmission electron microscopy. Particle size, zeta potential and polydispersity index were determined by photon correlation spectroscopy using a nanosizer. Adjuvanticity was assessed using haemagglutination inhibition test. The vesicles of Span 20-based niosomes were distinct, near spherical large unilamellar vesicles. The vesicles were of varied sizes (<1000 nm) with the entrapped Newcastle disease vaccine in the core of the vaccine. The zeta potential had a peak at -50 mV. The polydispersity index was 0.68. Haemagglutination inhibition test showed a 71% increment in immune response over that of the marketed La Sota® vaccine which had a 60% increment in immune response. The niosomal vaccine did not alter but rather enhanced the immunogenicity of the Newcastle disease vaccine.

Evaluation of the Antibacterial and Antidiarrhoeal activities of Heeria Insignis O. Ktze

A Agunu — Sat,3 Mar 2012

A Agunu, AA Ahmadu, SO Afolabi, AU Yaro, JO Ehinmidu, Z Mohammed

Indian Journal of Pharmaceutical Sciences 2011 73(3):328-332

Heeria insignis O. Ktze (Anacardiaceae) is an indigenous African shrub used in treatment of diarrhea, venereal diseases, tapeworm, hookworm, schistosomiasis, kidney trouble and for increasing lactation in women after childbirth. The methanol and dichloromethane extracts of the leaves were evaluated for antibacterial activity (using agar-diffusion method) and antidairrheal activity (using isolated rabbit jejunum and castor-oil induced diarrhea in mice). The methanol extract gave higher antibacterial activity than dichloromethane. The order of susceptibility of test microorganisms to methanol extract were Salmonella typhi>Pseudomous aeruginosa> Staphylococcus aureus>Bacillus subtilis>Escherichia coli which were comparable to standard. The minimum inhibitory concentration of the methanol extract for these microorganisms was also determined. The minimum inhibitory concentration (mg/ml) of methanol extract against microorganisms is; B. subtilis (3.9), S. aureus (1.95), E. coli (62.5), Ps. aeruginosa (3.9) and S. typhi (1.95). On the isolated rabbit jejunum evaluation, both extracts produced concentration-dependent relation of isolated rabbit jejunum that was not blocked by phentolamine, suggesting that extracts act via mechanisms other than alpha-adrenergic receptor. In the castor oil-induced diarrheoeal test, each extract gave 80% protection at 200 mg/kg, which is comparable to loperamide 2 mg/kg with 80% protection. This finding may explain the use of the plant in diarrhea and bacterial diseases.

New 6-bromo-2-methyl-3-(Substituted Phenyl)-(3H)-quinazolin-4-Ones with Antimicrobial and Antiinflammatory activities

Y Murti — Sat,3 Mar 2012

Y Murti, AK Singh, D Pathak

Indian Journal of Pharmaceutical Sciences 2011 73(3):333-337

New quinazolin-4-one derivatives, 6-bromo-2-methyl-3-(substituted phenyl)-(3H)-quinazolin-4-one, were synthesized and evaluated for antimicrobial and antiinflammatory activities. The structures attributed to synthesized compounds 1-8 were supported by the results of elemental analysis as well as by the UV, IR and 1 H NMR spectral data. Investigation of antimicrobial activity was performed using cup-plate agar diffusion method against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa and Candida albicans, Aspergillus niger and Curvularia lunata. Antiinflammatory activity was evaluated using the carrageenan-induced paw oedema test in rats. The results showed that compounds 2b, 2c, 2d, 2g and 2h exhibited significant antibacterial and antifungal activity comparable to standard drugs and compounds 2b and 2c showed good antiinflammatory activity comparable to ibuprofen.

FIP/AAPS joint workshop report: Dissolution/In vitro release testing of novel/special dosage forms

Cynthia K Brown — Sat,3 Mar 2012

Cynthia K Brown, Horst Dieter Friedel, Amy R Barker, Lucinda F Buhse, Susanne Keitel, Todd L Cecil, Johannes Kraemer, J Michael Morris, Christos Reppas, Mary P Stickelmeyer, Chikako Yomota, Vinod P Shah

Indian Journal of Pharmaceutical Sciences 2011 73(3):338-353