The use of natural excipients to deliver the bioactive agents has been hampered by the synthetic materials. However advantages offered by these natural excipients are their being non-toxic, less expensive and freely available. The performance of the excipients partly determines the quality of the medicines. The traditional concept of the excipients as any component other than the active substance has undergone a substantial evolution from an inert and cheap vehicle to an essential constituent of the formulation. Excipients are any component other than the active substance(s) intentionally added to formulation of a dosage form. This article gives an overview of herbal excipients which are used in conventional dosage forms as well as novel drug delivery systems.

In the 1990s, drug resistance has become an important problem in a variety of infectious diseases including human immunodeficiency virus infection, tuberculosis, and other bacterial infections which have profound effects on human health. At the same time, there have been dramatic increase in the incidence of fungal infections, which are probably the result of alterations in immune status associated with the acquired immuno deficiency syndrome epidemic, cancer chemotherapy, and organ and bone marrow transplantation. The rise in the incidence of fungal infections has exacerbated the need for the next generation of antifungal agents, since many of the currently available drugs have undesirable side effects, are ineffective against new or reemerging fungi, or lead to the rapid development of the resistance. This review will focus on the pathogenic yeast Candida albicans , since a large body of work on the factors and mechanism associated with antifungal drug resistance in this organism is reported sufficiently. It will certainly elaborate the probable molecular targets for drug design, discovered to date.

Transdermal route is an evolving panorama in novel drug deliverance and with oral route they proffer immense potential. Most recently there is hastening in approaches for delivering bioactives via these routes, amongst them revolution has been made by dendrimers. Encapsulation and conjugation of bioactives with these virus sized robots have shown immense employment for delivery of hydrophobic and labile remedies. Transport of these nano-cruises from corner to corner of skin and through epithelial hurdle of gastrointestinal tract depends upon dendrimer characteristics. An improved thoughtful of these characteristics is an obligation for their use in these rambling fields. These characteristics embrace generation size, molecular weight, surface charge, incubation time and concentration. This context demarcates the imperative role of dendrimers in transdermal and oral drug delivery. This review also highlights concerning mechanism of convey of nanoarrays via epithelial hurdle of GIT.

The ethanol extract of Curculigo orchioides was evaluated for antiasthmatic activity by using various in vitro and in vivo animal models. In vitro models like isolated goat tracheal chain preparation and isolated guinea pig ileum preparation were studied to know basic mechanism by which extract shows relaxant activity. The study showed that extract is effective against histamine-induced contraction. In isolated goat tracheal chain preparation and isolated guinea pig ileum preparation extract exhibits maximum relaxant effect (p<0.01) against histamine at concentrations 100mg/ml and 25mg/ml respectively. Animal studies involved use of histamine induced bronchoconstriction in guinea pigs, egg albumin induced passive paw anaphylaxis in rats and haloperidol-induced catalepsy in mice. These studies showed significant (p<0.01) protection at lower doses while further increase in the dose level showed reduced activity. Biochemical estimations in milk-induced total leukocytes count and milk-induced differential leukocyte count were also studied. In this study there was maximum increase in leucocytes and lymphocytes (99%) and maximum decrease in eosinophils up to 0% at dose 375mg/kg p.o. body weight was observed. The results of these studies indicated usefulness of ethanol extract of Curculigo orchioides in asthma.

Curcumin, the bioactive component of turmeric, Curcuma longa has an exceptionally wide spectrum of activities including antioxidant, anti-inflammatory and anti-cancer properties, and is currently under different phases of clinical trials for various types of soft tissue cancers. However, although in vitro and animal studies have shown anticancer activities of curcumin for virtually all types of human cancers, its poor bioavailability in the human body has severely limited its application to these diseases. Methods to increase its oral bioavailability are a subject of intense current research. Reconstituting curcumin with the non-curcuminoid components of turmeric has been found to increase the bioavailability substantially. In the present clinical study to determine the bioavailability of curcuminoids, a patented formulation, BCM-95^® CG was tested on human volunteer group. Normal curcumin was used in the control group. Curcumin content in blood was estimated at periodical intervals. After a washout period of two weeks the control group and drug group were crossed over BCM-95^® CG and curcumin, respectively. It was also compared with a combination of curcumin-lecithin-piperine which was earlier shown to provide enhanced bioavailability. The results of the study indicate that the relative bioavailability of BCM-95^® CG (Biocurcumax ^TM ) was about 6.93-fold compared to normal curcumin and about 6.3-fold compared to curcumin-lecithin-piperine formula. BCM-95^® CG thus, has potential for widespread application for various chronic diseases.

Two chemometric methods, inverse least square and classical least square, were applied to simultaneous assay of clopidogrel bisulphate and aspirin in their combined dosage tablet formulation. Twelve mixed solutions were prepared for the chemometric calibration as training set and 10 mixed solutions were prepared as validation set. The absorbance data matrix was obtained by measuring the absorbance at 16 wavelength points, from 220 to 250 nm with the interval of 2 nm (Dl= 2 nm). The developed calibrations were successfully tested for laboratory mixtures as well as commercial tablet formulation for their clopidogrel bisulphate and aspirin concentration. Mean recoveries for clopidogrel bisulphate and aspirin were found to be in good agreement with the label claim.

In the present investigation chitosan has been chemically modified by treating with two different aldehydes like acetaldehyde and propionaldehyde to form Schiff's bases. Schiff's bases of chitosan with acetaldehyde and propionaldehyde were named as polymer A and polymer B, respectively. Fourier Transform Infra Red (FTIR) spectral data have confirmed the reaction carried out on chitosan. Drug free polymeric films of chitosan, chemically modified chitosan and chitosan/hydroxypropylmethylcellulose blend were prepared and evaluated for various physicochemical characters. Further, the films were incorporated with anti-inflammatory drug, etoricoxib using glycerol as plasticizer. The drug loaded films were cross-linked with sodium citrate and studied for permeation characteristics across dialysis membrane and rat skin. All the films were evaluated for bursting strength, swelling index, moisture uptake, thickness uniformity, drug content uniformity, tensile strength, percent elongation at break, percent flatness, water vapour transmission rate and in vitro drug permeation study.

The aim of the present study was to prepare and characterize controlled-release matrix tablets of zidovudine using hydrophilic HPMC K4 M or Carbopol 934 alone or in combination with hydrophobic ethyl cellulose. Release kinetics was evaluated by using USP XXIV dissolution apparatus No.2 (paddle) type. Scanning electron microscopy was used to visualize the effect of dissolution medium on matrix tablet surface. The in vitro results of controlled -release zidovudine tablets were compared with conventional marketed tablet Zidovir. The in vitro drug release study revealed that HPMC K4 M or Carbopol 934 preparation was able to sustain the drug release near to 6 hours. Combining HPMC K4 M or Carbopol 934 with ethyl cellulose sustained the drug release for nearly 12 h. The in vitro evaluation showed that the drug release may be by diffusion along with erosion. Results suggest that the developed controlled-release tablets of zidovudine could perform therapeutically better than marketed dosage forms, leading to improve efficacy, controlling the release and better patient compliance.

Rofecoxib, a practically insoluble cox-2 selective nonsteroidal antiinflammatory agent was subjected to improvement in solubility by preparing its binary mixtures with β cyclodextrin using various methods such as physical mixing, co-grinding, kneading with aqueous methanol and co-evaporation from methanol-water mixture. Characterization of the resulting binary mixtures by differential scanning calorimetry and X-ray diffraction studies indicated partial amorphization of the drug in its binary mixtures. In vitro dissolution studies exhibited remarkable increase in rate and extent of dissolution of the drug from its complexes with β -cyclodextrin. Pure rofecoxib as well as its co-ground binary mixture were formulated as aqueous gels for topical application. In vitro skin permeation of rofecoxib from formulation containing rofecoxib-cyclodextrin complex was significantly higher (p<0.05) at 1, 2, 12, 18 and 24 hr as compared to formulation containing pure rofecoxib. This could be attributed to better solubility of binary mixture in the aqueous gel vehicle leading to greater concentration gradient between the vehicle and skin and hence higher flux of the drug.

The purpose of this research was to prepare a sustained release drug delivery system of venlafaxine hydrochloride by using a wax matrix system. The effects of bees wax and carnauba wax on drug release profile was investigated. A 3 ² full factorial design was applied to systemically optimize the drug release profile. Amounts of carnauba wax (X ₁ ) and bees wax (X ₂ ) were selected as independent variables and release after 12 h and time required for 50% (t ₅₀ ) drug release were selected as dependent variables. A mathematical model was generated for each response parameter. Both waxes retarded release after 12 h and increases the t ₅₀ but bees wax showed significant influence. The drug release pattern for all the formulation combinations was found to be approaching Peppas kinetic model. Suitable combination of two waxes provided fairly good regulated release profile. The response surfaces and contour plots for each response parameter are presented for further interpretation of the results. The optimum formulations were chosen and their predicted results found to be in close agreement with experimental findings.

The multiparticulate formulation of sodium para aminosalicylate for oral administration was developed by extrusion spheronization technique. Microcrystalline cellulose was used as filler in concentration of 14.4% w/w. Pellets were coated with Eudragit L 30 D-55 using fluidized bed processor. Different weight gains of acrylic polymer were applied onto the pellets and evaluated for in vitro dissolution behavior in 0.1 N HCl for two hours and then media was changed to phosphate buffer pH 6.8. A 60% w/w coating level of Eudragit L30 D 55 has produced the most acceptable results against the gastric attack. 3% Seal coat of HPMC E5 was also applied in order to protect the drug from migration into the Eudragit coat and film coat was applied in order to prevent aggregation of pellets in the dissolution media. Morphological characteristics of developed pellets were also investigated by scanning electron microscopy and found to be smooth and spherical. Developed system was found to be suitable for the delivery of Sod PAS in to intestinal region.

Proper characterization is an important aspect of any dosage form design. The objective of this work was to characterize tannate salt and hydrochloride salt of diphenhydramine. As a part of characterization studies, Differential scanning calorimetry was used to investigate thermal effects and nature of salts, supported by X-ray powder diffraction. Scanning electron microphotographs was used to surface topography of salts of diphenhydramine. Fourier-transform infrared spectroscopy, solubility study and flowability studies were carried out as part of characterization. Differential scanning calorimetry and X-ray powder diffraction studies indicated amorphous nature of the tannate while hydrochloride salt has crystalline properties. Scanning electron microphotographs indicated the differences in surface topography between both the salts. Solubility studies at different pH showed pH dependant solubility of both the salts and less solubility of tannate. Stability of bulk drug at accelerated conditions of 40 ^o /75% RH was determined for both salts. Good stability of both salts was observed.

The present study was aimed to replace the alum type adjuvant for hepatitis B vaccine. The hepatitis B vaccine was encapsulated in poly (DL-lactide-co-glycolide) microspheres by solvent evaporation technique. The formulated microspheres were characterized in terms of morphology, particle size analysis, in vitro release study and in vivo immune response in male Wistar rats. The FT IR spectrum illustrates the characteristics bands of poly (DL-lactide-co-glycolide) microspheres and hepatitis B vaccine at 1750 cm ^-1 and 1650 cm ^-1 , respectively. The hepatitis B vaccine loaded poly (DL-lactide-co-glycolide) microspheres were able to release antigens till day 42. Significant enhancement of specific antibodies to HBsAg was produced till day 90 after a single administration of HBsAg encapsulated poly (DL-lactide-co-glycolide) microspheres. However, the conventional alum adsorbed hepatitis B vaccine was not found to produce any significant specific antibody levels till day 90 after a single dose. The results showed that poly (DL-lactide-co-glycolide) microspheres show potential as an adjuvant for hepatitis B vaccine.

A simple, precise, accurate, rapid and reproducible reverse phase high performance liquid chromatographic procedure was developed for simultaneous determination of nitazoxanide and ofloxacin in tablet dosage form at a single wavelength. The mobile phase used was a combination of acetonitrile:0.25M potassium dihydrogen phosphate buffer (80:20) with 0.5%v/v of triethylamine and the pH was adjusted to 2.5 by adding orthophosphoric acid. The detection of the combined dosage form was carried out at 320 nm and flow rate was set to 1ml/min. Linearity was obtained in the concentration range of 5 to 25 mg/ml of nitazoxanide and ofloxacin with correlation coefficients of 0.9987 and 0.9995, respectively. The results of the analysis were validated statistically and recovery studies confirmed the accuracy of the proposed method.

A simple, specific, accurate, and precise reverse phase liquid chromatographic method was developed and validated for the estimation of risperidone in tablet dosage forms. A Phenomenex Gemini C-18, 5 µm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase containing methanol: acetonitrile: 50 mM potassium dihydrogen orthophosphate (80:10:10 v/v) was used. The flow rate was 1.3 ml/min and effluents were monitored at 234 nm. Clozapine was used as an internal standard. The retention time of risperidone and clozapine were 2.5 min and 3.3 min, respectively. The method was validated for linearity, accuracy, precision, specificity, limit of quantification, limit of detection, robustness and stability. The limit of detection and limit of quantification for estimation of risperidone was found to be 500 ng/ml and 990 ng/ml, respectively. Recovery of risperidone was found to be in the range of 99.02-101.68%. Proposed method was successfully applied for the quantitative determination of risperidone in tablet formulations.

Indomethacin suppositories were prepared by using water-soluble and oil soluble suppository bases, and evaluated for in vitro release by USP I and modified continuous flow through bead bed apparatus. Effect of the Tween 80 (1% and 5%) was further studied on in vitro release of the medicament. Release rate was good in water-soluble suppositories bases in comparison to oil soluble suppositories bases. Release was found to be greater in modified continuous flow through bead bed apparatus. When surfactant was used in low concentration then release rate was much greater, as compared to high concentration. When stability studies were performed on the prepared indomethacin suppositories it was found that suppositories made by water-soluble base had no significant changes while suppositories prepared by oil soluble bases, had some signs of instability.

A simple accurate, sensitive and reproducible spectrofluorimetric method was developed for the analysis of duloxetine hydrochloride in pure and pharmaceutical dosage form. Duloxetine hydrochloride showed strong native fluorescence in 0.05 M acetic acid having excitation at 225 nm and emission at 340 nm. Effect of different solvents were thoroughly investigated. The calibration graph was linear in the range from 0.020 to 0.400 µg/ml. The proposed method was statistically validated and successfully applied for analysis of capsule dosage forms. The limit of detection and limit of quantification were found to be 0.003 µg/ml and 0.010 µg/ml, respectively. The percentage recovery was found to be in the range of 98.71% to 99.17%.

Hypercholesterolemia is the major cause of cardiovascular diseases leading to myocardial infarctions leading to considerable morbidity and mortality. During the past decade a group of molecules referred to as statins such as simvastatin, atrovastatin have been tried with great success in reducing total cholesterol. These molecules act by inhibiting the HMG CoA reductase enzyme thereby interfering with the synthesis of cholesterol. But statins reduce all the cholesterol including HDL cholesterol. Long term drug vigilance activity has revealed serious side effects of tendinopathy and related musculoskeletal disorders in some of the subjects. In an effort to manage hypercholesterolemia without serious side effects in a natural way we had tried the use of Amlamax ^TM a reconstituted, purified, standardized dried extract of amla ( Emblica officinalis ) containing 30% ellagitannins with other hydrolysable tannins on humans. We report the hitherto unobserved significant elevation of HDL cholesterol by the administration of Amlamax ^TM

Spectrophotometric method for the determination of certain proton pump inhibitors belonging to the benzimidazole class of compounds has been developed. The method is based on the reaction of omeprazole, lansoprazole, pantoprazole, rabeprazole and esomeprazole with iron (III) and subsequent reaction with ferricyanide under neutral condition which yields Prussian blue product with maximum absorption at 720-730 nm. The commonly encountered excipients and additives that often accompany pharmaceutical preparations did not interfere with the determination. The method was applied for the determination of omeprazole, lansoprazole, pantoprazole, rabeprazole and esomeprazole in pharmaceutical preparations and no difference was found statistically. Thus, the spectrophotometric method can be applied as inexpensive, rapid, easy, accurate and precise method for the routine analysis of the five proton pump inhibitors in pharmaceutical preparations.

The present work describes a two-wavelength method for simultaneous determination of metoprolol and hydrochlorthiazide in fixed dose combination tablet. The wavelengths selected for method were 257.8 nm, 282.9 nm and 315.0 nm. The absorbance difference at first two wavelengths was used for determination of metoprolol and the latter was used for determination of hydrochlorthiazide. The recovery value for the drugs from the tablet matrix was found to be 100.55% (metoprolol) and 99.97% (comparison with standard) and 98.09% (E1%, 1cm) for hydrochlorthiazide. The method has an advantage that hydrochlorthiazide can be estimated in combination, as there is no interference of metoprolol at 315.0 nm. The method was evaluated statistically for its accuracy and precision.

Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot's method) were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 µg/ml, 1-40 µg/ml and 1-30 µg/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

Phytochemical examination of the peel of grapefruit resulted in the isolation of five compounds namely friedelin, β -sitosterol, 7(3',7',11',14'-tetramethy)pentadec-2',6',10'-trienyloxycoumarin, limonin and cordialin B. These compounds have been characterized on the basis of spectral data, and 7(3',7',11',14'-tetramethy)pentadec-2',6',10'-trienyloxycoumarin is a hitherto unreported compound.

A simple, rapid and selective method was developed. The method was validated and found to be linear in the range of 100-4000 ng/ml. Chromatographic peaks were separated by means of a 5 µm, C18 silica column using acetonitrile and phosphate buffer (0.05 M) in proportion of 40:60 (pH 4.0) as a mobile phase. The retention time of torsemide was 5.00±0.20 min. The chromatograms showed good resolution and no interference from plasma. The mean recovery from human plasma was found to be above 82%. Both inter-day and intra-day accuracy and precision data showed good reproducibility. This method was applied to a single dose bioequivalence study. Log transformed values were compared by ANOVA followed by classical 90% confidence interval. Confidence limits for C _max , AUC _0-t and AUC _0-inf ranged from 98.6 to 102.8, 101.8 to 105.3 and 102.4 to 105.5 respectively. These results suggested that the analytical method was linear, precise and accurate. Test and reference product were found to be bioequivalent.

Essential oils from fresh leaves, flowers and dried fruits of Vitex negundo were obtained by hydrodistillation. Using Soxhlet extractor five successive extracts from dried and powdered leaves were also taken. The chemical constituents of essential oil of leaves, flowers and dried fruits were analyzed by GC-FID and GC/MS techniques. Main constituents identified in leaves oil were d-guaiene, carryophyllene epoxide and ethyl-hexadecenoate; in flowers oil - a-selinene, germacren-4-ol, carryophyllene epoxide and (E)-nerolidol while fruit oil showed β -selinene, a-cedrene, germacrene D and hexadecanoic acid as the main constituents. β -Caryophyllene was only the constituent identified as common to all three oils. a-Guaiene and guaia-3,7-diene were identified as common constituents in leaf and dried fruit oil while leaf and flower oils showed p -cymene, valencene, caryophyllene epoxide and (E)-nerolidol as common constituent. All the essential oils and successive extracts were evaluated for antibacterial potential against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa bacterial strains. Each of the essential oils and extracts were found to give promising results against B. subtilis and E. coli. Ethyl acetate and ethanol extracts showed prominent antibacterial activity against all the tested strains. Fruits and leaves oil were found to be most active against E. coli and S. aureus, respectively. Only flowers oil was found to be active against P. aeruginosa.

Mouth dissolving tablets constitute an innovative dosage form that overcomes the problems of swallowing and provides a quick onset of action. In view of enhancing bioavailability an attempt has been made to study two different methods direct compression and sublimation in formulation of mouth dissolving tablets of clozapine. Total four formulations using various superdisintegrants and subliming agents were prepared. All prepared formulations were evaluated for physico-chemical parameters. The formulations exhibited good disintegration properties with total disintegration time in the range of 25 to 35 s. Comparative evaluation of two methods showed direct compression method is a better alternative to sublimation method as its formulations rapidly disintegrate in oral cavity. In vitro cumulative percentage drug release for formulations prepared by direct compression with explotab superdisintegrants shows 99.79 while sublimation method using camphor 93.58 release in 12 min. Kinetic studies indicated that all the formulations followed first order release with diffusion mechanism.

Quinapril hydrochloride and hydrochlorothiazide were simultaneously determined by HPTLC in pharmaceutical formulations. The drugs were separated on silica gel 60 F ₂₅₄ plates using suitable combination of solvents as mobile phase. The validation parameters, tested in accordance with the requirements of ICH guidelines, prove the suitability of methods.

An oral controlled release suspension of chlorpheniramine maleate was prepared using ion-exchange resin technology. A strong cation exchange resin Indion 244 was utilized for the sorption of the drug and the drug resinates was evaluated for various physical and chemical parameters. The drug-resinate complex was microencapsulated with a polymer Eudragit RS 100 to further retard the release characteristics. Both the drug-resinate complex and microencapsulated drug resinate were suspended in a palatable aqueous suspension base and were evaluated for controlled release characteristic. Stability study indicated that elevated temperature did not alter the sustained release nature of the dosage form indicating that polymer membrane surrounding the core material remained intact throughout the storage period.

A series of 1,2,4-dithiazole were synthesized from 1,2,4-thiadiazoles in the presence of CS ₂ and evaluated for their antimicrobial, anticonvulsant, analgesic and neurotoxicity potential. The compounds provided significant protection against maximal electroshock-induced seizures and seizures induced by 300 mg/kg of subcutaneous pentylenetetrazole administration. The designed compounds (3a-g) were screened in vitro for antibacterial activity against Staphylococcus aureus Escherichia coli , Bacillus subtilis and Pseudomonas aeruginosa and antifungal activity in fungal strains of Candida albicans and Aspergillus niger. Synthesized compounds exhibited moderate antibacterial and antifungal activity. N,N -Di-naphthalen-1-yl- N -(thioxo-5 H -[1,2,4]dithiazol-3-yl)-guanidine and N,N -Bis-(4-fluoro-phenyl)- N -(5-thioxo-5 H -[1,2,4]dithiazol-3-yl)-guanidine showed analgesic activity by tail flick method.

Mango butter was explored as a functional, natural supplement and active skin ingredient in skin care formulations. A foot care cream was developed with mango butter to evaluate its medicinal value and protective function in skin repair. Qualitative comparison and clinical case studies of the product were carried out. Wound healing potential of foot care cream was investigated on the rat excision and incision wound models. Results of the clinical studies demonstrated complete repair of worn and cracked skin in all the human volunteers. Furthermore, foot care cream exhibited significant healing response in both the wound models. The project work could be concluded as establishment of high potential for mango butter to yield excellent emolliency for better skin protection. Improving the product features and medicinal functionality further validate mango butter as a specialty excipient in development of cosmeceuticals and has an immense value for its commercialization.

A fast, robust and stability indicating RP-HPLC method was developed for simultaneous determination of bisoprolol fumarate and amlodipine besylate in tablets. The mobile phase was mixture of 25 mM ammonium acetate adjusted to pH 5.0 and methanol (65: 35) at 0.8 ml/min. The stationary phase was Luna C18-2 column (3 m, 50×4.6 mm ID). UV detection was performed at 230 nm. Retention time was 1.45 min and 3.91 min for bisoprolol and amlodipine, respectively. Linearity was established in the range of 8-33 µg/ml. Mean recovery was 99.1% and 98.6% for bisoprolol fumarate and amlodipine besylate, respectively.