Contact spermicides represent a novel method of contraception. Many compounds with diverse pharmacological activity have been evaluated in vitro for their spermicidal activity. Drugs with membrane stabilizing action such as procainamide, quinidine, mexiletine, propranolol, certain ionophores, chelating agents such as EDTA, gramicidin, natural or synthetic surfactants such as saponins, nonoxynol, benzalkonium chloride, anti-liquefying agents have all been demonstrated to possess good spermicidal activity. However, there is a paucity of data regarding the safety profile of most of these agents. In case of propranolol, chlorhexidine, gossypol and nonoxynol where such data is available, the results are not worthy enough to recommend their widespread use. Nonoxynol is the only contact spermicide currently being employed clinically. Combination formulations of two or more contact spermicides are being evaluated in order to minimize their adverse effects. But there is still a need to develop more safe contact spermicides.

Taste is an important parameter governing compliance. Several of the oral pharmaceuticals, numerous food and beverage products and bulking agents, have unpleasant bitter-tasting components. In numerous cases, the bitter taste modality is an undesirable trait of the product or formulations and can considerably affect its acceptability by consumers. Bitter characteristics found in such systems have been eliminated or minimized by various known processes, but no universally applicable technology for bitterness inhibition has ever been recognized. The desire for improved palatability of these products has prompted the development of numerous formulations with improved performance and acceptability. This article discusses the recent approaches and methodologies for bitterness reduction for oral pharmaceuticals.

Liposomes were prepared by the versatile pH gradient method with an aim to modify drug disposition and increase the therapeutic efficacy of the drug, daunorubicin. The preparation were then characterized with respect to size and its distribution, entrapment efficiency, in vitro drug release profile and its stability under specified conditions of storage. Antitumor efficacy bearing solid tumor namely fibrosarcoma and organ toxicity studies in swiss albino mice were conducted with the liposomes administered by intravenous route at a dose of 5 and 10 mg kg-1 body weight. Liposomes were found to be spherical, multilamellar in nature with mean diameter being 5 pm. The entrapment efficiency of drug was found to be 82.5±1.28%, with the drug being incorporated into the aqueous layer of the vesicles. Prepared liposomes were stable under refrigeration (4) as evident by less drug leakage and released the loaded drug in a controlled fashion. Antitumor studies indicate an insignificant difference (P>0.05) in volume doubling time between the free drug and daunorubicin liposomes at both doses but the animals treated with drug formulation exhibited dramatic decrease in cardiac toxicity. The result revealed that encapsulation of daunorubicin in liposomes are a potential tool for the delivery of drug, as this formulation significantly decreases the inherent cardiac toxicity of daunorubicin.

Three simple Spectrophotometric methods for the determination of rifampicin (RIF) and isoniazid (INH) in pharmaceutical preparations have been developed. First method is based on the determination of graphical absorbance ratio at two selected wavelengths. In the second method, derivative spectroscopy is used to eliminate spectral interference and the third method is based on additivity of absorbances. All the three methods were found to be simple, rapid, accurate and can be adopted in routine analysis of drug in formulations.

The present investigation was taken up to prepare and evaluate Eudragit RS100 films as rate controlling membrane for transdermal use and to study the effect of different concentrations of various plasticizers on the permeability and mechanical properties. Drug free films of Eudragit RS100 were prepared by the casting method on mercury surface employing chloroform as a solvent and dibutyl phthalate (DBP) and polyethylene glycol-400 (PEG) as plasticizers. These films were evaluated for thickness uniformity, tensile strength, percentage of elongation and water vapor transmission. Permeability characters of these films were studied using verapamil hydrochloride (VPH) as a model drug. The thickness of the films was found to be uniform. Tensile strength of the films prepared using DBP as plasticizer was high compared to the films plasticized with PEG. Water vapor transmission and drug diffusion through films followed a pattern closed to zero order type and it was decreased with increase in the film thickness. Films plasticized with PEG showed higher permeability to verapamil hydrochloride. The permeability of the drug was decreased as the concentration of dibutyl phthalate was increased. Whereas increase in the concentration of PEG enhanced the permeability characteristics of the films.

Propranolol hydrochloride buccal films were prepared using three different polymers in various proportions and combinations. The physicochemical parameters like weight variation, thickness, folding endurance, drug content, percentage moisture absorption and percentage moisture loss were evaluated. An in vitro study was designed and it was carried out using commercial semipermeable membrane. In vitro release profile for the formulation F6 (drug reservoir with 6% ethyl cellulose (EC)+ 0.5% polyvinyl pyrolidone (PVP) and 8% EC as rate controlling membrane) showed sustained release upto 24 h. It also obeyed first order kinetics. The studies conducted in rabbits confirmed the sustained release.

A novel matrix system of flubiprofen as an oral controlled release formulation was prepared using gum karaya as release retardant. Lactose or dicalcium phosphate was incorporated to improve the drug release rate. Gum karaya matrices containing lactose showed satisfactory release characteristics. Flurbiprofen-gum karaya matrices showed first order release kinetics following super case Il transport, where as matrices with both of the co-excipient followed first order kinetics with anomalous diffusion release. The selected experimental formulation showed comparable in vitro dissolution profile and in vivo blood level pattern with those of the commercial sustained release formulation. The data support a Level A correlation between in vitro release rate profile and in vivo absorption for flurbiprofen from both the formulations.

A simple and rapid colorimetric method of assay of piperine is reported. It is an adaptation of Labat test for methylenedioxy group attached to an aromatic nucleus. The resultant blue green colour shows maximum absorbance at 656 nm and obeys Beer's law in a concentration range of 10-25 μg/ml. Results of analysis on different piperine samples are comparable with direct spectrophotometry and HPLC methods. The method is also suitable for assay of piperine in combination with rifampicin, isoniazid, and nimesulide.

Microspheres of chloroquine phosphate (CP) were prepared using cross-linked gelatin and were investigated for the in vitro release profile and in vivo drug release following subcutaneous injection. A series of batches of microspheres were prepared by cold congealing method to optimize parameters like the media of encapsulation (mixture of heavy and light mineral oil in the ratio of 1:3), stirring rate (250 rpm) and pH of the media (4.5) to obtain discrete microsphere in the size range of 50 to 100 mm. The study indicated the significance of the parameters like gelatin to drug ratio and the percentage of formaldehyde (crosslinking agent) to obtain microspheres with high drug entrapment and optimum drug release behaviour. Multiple regression analysis of the values of the cumulative percent drug released in 8 d for ten batches prepared by varying the above two parameters yielded a polynomial equation. This equation was used to calculate the optimum values of gelatin to drug ratio (2.0) and percentage of the formaldehyde (3.99%) for preparing microspheres with ideal drug release behaviour. Subcutaneous injection of microspheres as concentrated suspension in HPMC base in Wistar rats showed blood level concentration between 5.98 and 18.46 μg/ml for a period of 8 days in comparison to 34.8 μg/ml for 6 h following subcutaneous injection of CP solution. Mean residence time of the drug in the body calculated as the ratio of the area of the first moment curve to the area under the concentration vs time curve was 71.4 h for microspheres as against 2.4 h for the drug solution.

Lingha chendooram-1, a widely used Siddha drug was evaluated for acute, sub-acute and chronic toxicity in rats with reference to histopathological, haematolo'gical, parameters and detection of mercury from the tissues of liver and kidney, The drug showed acute toxicity from 100 mg onwards. But it produced sub-acute and chronic toxic effects from 50 mg onwards and elevation In blood urea level. Feed and water intake failed to reveal any marked changes in sub-acute and chronic toxicity studies. Mercury was detected from 75 mg with concurrent increase in dose in both sub-acute and chronic toxicity studies. The histopathological lesions were non-specific when compared to microscopic changes along with the drug dosages. In the present study the drug possessed no toxic effect below 20 mg.

Unsymmetrical 1,4-dihydropyridines having isoxazole and pyridine system been synthesized from 2,6-dimethyl-4[3"-nitrophenyl]-5-carbmethoxy-3-[3"-aryl propene-1"-one]-1,4 dihydropyridines of the type la-h. All compounds were tested for antitubercular activity against M.tuberculosis (H37Rv)strain by using Bactec 460 method. lsoxazole derivatives showed modest activity.

Niosomes containing salbutamol sulphate were prepared using different non-ionic surfactants like Tween 20, 40, 60, 80, Span 20, 40, 60, 80 and Brij 35 by transmembrane pH gradient method. The drug encapsulation efficiency varied from 28% to 79%. The vesicles have been characterized by infrared spectroscopy. In vitro drug release studies were carried out using dialysis bag and phosphate buffer, pH 7.4 as a dissolution medium for 24 h. The formulation exhibited retarded release for 24 h and Span 60 was found to be the most satisfactory surfactant which released 78.4% of drug in 24 h. Particle size distribution studies were carried out by optical microscopy technique. Most of the niosomes were found to be spherical in shape. Thermal stability studies were carried out at 4° 25° and 50° for one month. The product was lyophilized. Tissue distribution Studies were carried out on rabbits. The maximum concentration was seen in lungs.

In the present study, the antioxidant and antiinflammatory properties of methanolic extract of Citrus sinensis peel was investigated. Qualitative tests confirmed the presence of flavanoids and free phenolic compounds in the extract. The antioxidant property of the extract was tested qualitatively by thin layer chromatography using β-carotene-linoieate oxidation-The anti-inflammatory activity of the extract was performed on carrageenan- induced acute pedal paw edema model and Freund's complete adjuvant-induced chronic inflammatory model. In both acute and chronic anti- Inflammatory models, the extract exhibited significant antiinflammatory activity at two doses of 150 and 300 mg/kg.

Two simple, sensitive and accurate spectrophotometic methods are described for the determination of propranolol hydrochloride either in pure form or in pharmaceutical preparations. Each method involves nitration of the drug with uranyl nitrate or thorium nitrate in sulphuric acid medium. The yellow coloured nitro derivative has an absorption maximum at 377 nm. The nitro derivative obeys Beer's Law In the concentration range of 2-32 µg/ml and 1-30 µg/ml for uranyl nitrate and thorium nitrate respectively. The optium reaction conditions and other analytical parameters are evaluated. The influence of substrates commonly employed as excipients with propranolol drug has been studied. Results of analysis of pure drug and its dosage forms by the proposed methods are in good agreement with those of the official method.

The antitumour activity of the leaves of Elephantopus scaber has been evaluated against Dalton's ascitic lymphoma (DAL) in Swiss albino mice. A significant enhancement of mean survival time of Elephantopus scaber treated tumour bearing mice was found with respect to control group. Elephantopus scaber treatment was found to enhance peritoneal cell counts. When these Elephantopus scaber treated animals underwent I.p. inoculation with DAL cells, tumour cell growth was found to be inhibited. Fourteen days after transplantation, Elephantopus scabertreated group were able to reverse the changed in the haematological parameters, protein and PCV consequent to tumour inoculation.

Two simple spectrophotometric methods (A and B) have been developed for the determination of roxithromycin in pure and its pharmaceutical formulations. Method A is based on the formation of a blood red coloured complex with ferric chloride and 1,10-phenanthroline with absorption maximum at 520 nm. In method B, roxithromycin forms blue coloured complex with Folin-Ciocalteu (FC) reagent in the presence of sodium carbonate exhibiting maximum absorption 'at 760 nm. The chromogens obey Beer's law in the concentration ranges of 2.5 to 40 µg/ml and 2.5 to 12.5 µg/ml for method A and B, respectively.

The present communication deals with the development of a simple, specific, sensitive, rapid and economical procedure for simultaneous estimation of rifampicin and isoniazid in a combined dosage form. The method is based on the native ultraviolet absobance maxima of the two chemotherapeutic agents. As both compounds do not interact chemically in phosphate buffered saline, two wavelengths 263 nm and 333 nm (λmax of isoniazid and λmax of rifampicin, respectively) were used. In addition, rifampicin also shows absorbance at 263 nm in phosphate buffered saline. Both the drugs obey Beer's law in the concentration range that was employed in the method.

Since oral bioavailability of terbutaline sulphate is poor, pseudolatex transdermal patches incorporating terbutaline sulphate were prepared as an effective mode of therapy for nocturnal asthma in particular. The pseudolatex patches were formulated using combinations of Eudragit RS 100 and RL 100 and Eudraflex as plasticizer. The physicochemical characterization of the films were evaluated for suitability and drug release profile from the films as well as skin permeation aspects were evaluated for therapeutic efficacy. The resulted medicated patches were of average thickness (95-155 μm), and content uniformity of the drug varied from 94.5 to 99.1 percent. The formulation F3 showed least and F7 showed highest percentage of elongation. The percentage of moisture absorption varied from 2.91 to 3.65 at 63 percent relative humidity. The release profiles from the patches followed apparent zero order pattern up to a period 12 h, after which it levels off. The cumulative amount of drug permeated over a period of 24 h was found to be 4.8 mg/cm², which was about 50 percent of the loaded dose. The skin permeation took place at a steady rate over a period of 12 h after which the rate was reduced.

A novel method of synthesis of curcumin-I has been successfully developed using Claisen- Dieckmann condensation where dehydrozingerone is condensed with methyl ferulate in presence of sodium ethoxide In dimethyl sulphoxide. Various curcuminoids are prepared by changing the esters and α, β-unsaturated ketones. This reaction is utilized to prepare dehydrozingerone- ibuprofen condensation product (DZIBU), a potent antiinflammatory agent. The homogenecity of compounds synthesized was established and structures were confirmed by spectral data. DZIBU exhibited powerful antiinflammatory activity on carrageenan-induced paw edema model and formaldehyde-induced arthritis model in rats. Though the analgesic activity was less when compared to that of ibuprofen, the new compound did not induce gastrointestinal side effect In animal studies.

Three simple, rapid, accurate, economical and reproducible procedures for simultaneous estimation of gliclazide and metformin hydrochloride in two component tablet formulation have been developed. First method is based on an equation of area calculation of curve at two wavelength regions (228.6 to 224 nm and 235 to 231 nm). Second method employs simultaneous equation at two wavelengths corresponding to 226.3 and 233.2 nm. Third method employs derivative spectroscopy at zero crossing points (226 and 232.9 nm) in first order derivative spectra. Both the drugs obey Beer's law in the concentration ranges employed for these methods. The results of analysis have been validated statistically and by recovery studies.