Welcome to IJPT

ABSTRACT 

Quinolines, aryl thiosemicarbazides and their synthetic analogs have been found to exhibit a broad-spectrum antimicrobial activity.  In continuation of our work we have made an attempt to synthesize some new novel compounds. Comprising 3-formyl-2-hydroxy quinoline nucleus with aryl thiosemicarbazides in alcoholic medium offered series of N-aryl(2-hydroxyquinoline-3-carbaldehyde) thiosemicarbazones. For the proposed work 3-formyl-2-hydroxy quinoline nucleus was selected as a synthon. The present work is an attempt to the synthesized series of N-aryl(2-hydroxyquinoline-3-carbaldehyde) thiosemicarbazones and have been characterized by analytical and spectral (IR, ¹HNMR and Mass) properties. Significant anti-microbial activities were observed for members of series.

Keywords: 3-Formyl-2-Hydroxy-Quinoline, thiosemicarbzide, thiosemicarbazone, antibacterial and anti-fungal.

ABSTRACT
The present study was aimed to preparing a floating drug delivery system to design a controlled release oral dosage form of Verapamil Hydrochloride to overcome the demerit of the limited residence time of the controlled release dosage form in the gastrointestinal track and hence to increase the duration of release, The intragastric hydro dynamically balanced or floating system was convenient, Hence hydrophilic polymer was choosed as the matrix material, which swell and float in the medium. This swelling retardant was used to control the release of drug. To formulate and prepare the single layered
intragastric floating delivery system of verapamil hydrochloride by direct compression method with hydroxyl propyl methyl cellulose (HPMC k4m and k15m) each alone or in combination with different drug: polymer ratios. Thus the study aims to improve the oral bioavailability of the drug and to achieve extended retention in the stomach which may result in prolonged absorption. Tablets were evaluated by different parameters such as weight uniformity, thickness, hardness test, friability test, swelling index, Buoyancy studies and In vitro release studies. Conclusion of this study was the % drug release was found to be 95.13 %, The Marketed product gave 92.25 % of drug release in 8 hours of dissolution study. The formulation F1 with 95.13 % of drug release has better control over release of drug was compared with marketed product.

Keywords: Verapamil Hydrochloride, Hydroxy Propyl Methyl Cellulose K4m and K15m, Direct compression method, Floating Matrix Tablet, Evaluation and Invitro Studies.

ABSTRACT
The present study was to scientifically evaluate anti-diarrhoeal effects of ethanolic (90%) extract of bark of Alocassia macrorhiza (L.) (EEAM) was studied against castor oil-induced-diarrhoea model in rats. The weight and volume of intestinal content induced by castor oil were studied by enteropooling method. Standard drug atropine (3mg/kg, i.p) showed significant reductions in fecal output and frequency of droppings whereas EEAM at the doses of 100 and 200 mg/kg i.p significantly retarded the castor-oil induced enteropooling and intestinal transit. The gastrointestinal transit rate was expressed as the percentage of the longest distance travelled by the charcoal divided by the total length of the small intestine. EEAM at the doses of 100 and 200 mg/kg significantly inhibited (P<0.001) weight and volume of intestinal content. The results obtained establish the efficacy and substantiate the folklore claim as an anti- diarrheal agent.
Keywords: Anti-diarrhoeal activity, Alocassia macrorhiza (L.), Traditional medicine, Castor oil- induced diarrhoea, Enteropooling method.

ABSTRACT
An isocratic RP-HPLC method was developed and validated for the quantitation of Simvastatin and Amlodipine besylate in combined tablet dosage forms. Quantitation was achieved using a reversed-phase Hypersil silica BDS (250x4.6mm with 5μ particle size) column at ambient temperature with mobile phase consisting of 0.05M ammonium acetate buffer (pH-4) and acetonitrile in the ratio (40 + 60, v/v). The flow rate was 1.0 mL/min. Measurements were made at a wavelength of 240nm. The proposed method was validated for selectivity, precision, linearity and accuracy. The assay method was found to be linear from 30.0-70.0 μg/mL for Amlodipine besylate and 60.0-140.0 μg/mL for Simvastatin. All validation parameters were within the acceptable range. The developed method was successfully applied to estimate the amount of Simvastatin and Amlodipine besylate in combined dosage forms.

Keywords: Simvastatin, Amlodipine besylate, RP-HPLC.

ABSTRACT
Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of hydrophobic drugs. Solid dispersions of a poorly water-soluble drug Meloxicam in Polyvinylpyrrolidone (PVP) were prepared by solvent evaporation method. The physicochemical properties of the Products and drug-polymer interactions were characterized by Fourier Transform Infrared spectroscopy, Determination of drug content, XRay Diffraction studies. Meloxicam was found to be amorphously dispersed in solid dispersion systems with the drug to polymer weight ratio of 1:9. The solid dispersion of the Meloxicam (Ratio-1:9) has shown better release of drug and good dissolution rate. The drug release in the solid dispersions Drug: PVP K-15 (1:9), Drug: PVP K-30 (1:9) and Drug: PVP K-90 (1:9) are 98.85%, 97.14% and 84% respectively. PVP processing could provide an effective pharmaceutical formulation technology to improve the bioavailability of poorly water-soluble drug.

Keywords: Solid dispersion, Meloxicam, In-vitro dissolution study, Solvent evaporation method.

ABSTRACT
A series of novel 4-(2H- chromen-3-y1)-6- phenyl pyrimidin-2-amine IIIa-h and (2Z)-2- {(4-(2H-chromen-3-y1)-6- phenyl pyrimidin-2-y1)imino}-,3-thiazolidin-4-one Va-h analogs is described. Reaction of 3[(E)-3-Aryl-propen-2-enoyl]-2Hchromen-2-ones II with guanidine hydrochloride in presence of potassium hydroxide and ethanol yielded 4-(2H-chromen-3-y1)-6-phenyl pyrimidin-2-amineIII. Subsequent reaction of III with chloro acetyl chloride in tri ethyl amine gave 2-chloro-N-(4-(2H- chromen-3-y1)-6-phenyl pyrimidin-2-y1) acetamide IVa-h which upon treatment with ammonium isothiocyanate in ethanol furnished (2Z)-2- {(4-(2H-chromen-3-yl)-6-phenyl pyrimidin-2-yl) imino }-1,3 –thiazolidin-4-ones.All the title compounds III(a-h) and V(a-h) were screened for Invitro Cytotoxic activity using A-549 lung cancer cell lines and HT-29 colon cancer cell lines by MTT method. The structures of newly synthesized compounds were established on the basis of elemental analysis,IR and 1H NMR spectral data.

Keywordst:-Cytotoxic activity,Thiazolidinones,Pyrimidines,cisplatin.

ABSRACT

Peptic ulcer disease is a serious gastro intestinal disorder that requires well-targeted strategy. A number of drugs including proton pump inhibitors & histamine H2 receptor antagonists are available for treatment of peptic ulcer. Clinical evaluations of their drugs has shown incidence of side effect. Thus the development of new antiulcer drugs and the search for novel molecules has been extended to herbal drugs that offer better protection and decreased relapse. Medicinal plants provide an effective and safer way in disease management. Many medicinal plants exhibit antiulcer activity and found useful in the treatment of peptic ulcer. The present paper reviews the data reported on pharmacologically active phytoconstituents obtained from the different plants involved in anti-ulcer activity along with pharmacological status which have been experimentally studied for anti-ulcer activity during January-December 2011. This work stimulates the researchers for further research on the potential use of medicinal plants having anti-diabetic potential.

Key words: Annual review, Phytoconstituents, Medicinal plants, Anti-ulcer activity.

ABSTRACT

Acupuncture has traditionally been successfully employed in China to treat most illnesses and there is little doubt that acupuncture is an excellent therapy for people suffering with many eye conditions. There are several studies suggesting that acupuncture can be very helpful in the treatment of many eye problems such as glaucoma and cataract. The objective of this study is to measure the prevalence of acupuncture treatment among eye related problems people and the relationship between age, gender, race and possible adverse effect in three different states (Kedah, Perak and Kuala Lumpur) in Malaysia. A cross sectional study was chosen as an appropriate method to achieve the aims. Interview with the patients and also questionnaire form has been distributed to them in order to collect statistical data from the period of January to October 2011. A sample of 250 patients (n=250) has been interviewed. The research has been conducted in private acupuncture clinic in particular state. All the data collected is analyzed using SPSS version 17.0.

KEYWORDS: Cross sectional study, Acupuncture, Eye related problems, Prevalence.

ABSTRACT

                A series of oxazolones (3) were prepared by cyclization reaction of hippuric acid (1) with different aromatic aldehydes (2) using sodium acetate and acetic anhydride as solvent. Two series of imidazolones (4&5) were synthesized from oxazolones (3) by condensation reaction. The 4-(substituted benzylidene)-2-phenyloxazol-5-ones (3) were refluxed with equimolecular quantity of aniline in dioxan in water bath for 6 hrs and urea in pyridine in an oil bath at 150⁰c for 6 hrs to yield the  4-(substituted benzylidene)-1,2-diphenyl-1H-imidazol-5-ones (4)  and  4-substituted benzylidene)-5-oxo-2-phenyl-4,5-dihydroimidazole-1-carboxamides (5) respectively. The yield of the synthesized imidazolones ranged from 60-72%. The structures of the synthesized compounds were characterized and confirmed by IR, ¹H-NMR,¹³C-NMR, mass spectral data and physical analysis. The synthesized compounds were screened for their in vitro antimicrobial activity against standard pathological bacterial strains and fungal strains using disc diffusion and broth micro-dilution assays. All the compounds, exhibited a MIC values ranging between 1.6 to 204.8 μg and the MBC/MFC values ranging between 6.4 to >204.8μg for tested bacterial and fungal species. The compounds have better activity against the tested fungal species than bacteria species.

KEYWORDS:-Imidazolones, oxazolones, antibacterial & antifungal activities.

ABSTRACT

A simple, specific, accurate and precise RP HPLC method has been developed for the determination of Rivastigmine from Bulk dosage form by reverse phase HPLC.C₁₈ column (Inertsil, C₁₈, 250 x 4.6mm. 5m). The sample was analyzed using Potassium phosphate mono basic buffer (pH 2.5± 0.05): Acetonitrile (70:30) as a mobile phase at a flow rate of 1.0ml/min and detection at 217nm. The retention time for Rivastigmine was found to be 3.66 min. The stability assay was performed and was validated for accuracy, precision, linearity, specificity and sensitivity in accordance with ICH guidelines. Validation revealed the method is specific, rapid, accurate, precise, reliable, and reproducible. Calibration plots were linear over the 10-100mg/ml of concentration ranges for drug. The method can be used for estimation of Rivastigmine drug in bulk dosage form.

Keywords: Method Development, Validation of Rivastigmine, Bulk Dosage Form.

ABSTRACT

Some new Synthesis of (N-carbamimidoyl 1-4-(2-oxo-1-(piperidine-1-ylmethyl) indolin-3-ylidineamino) benzene sulphonamide) has been synthesized from isatin & different p-substitute aniline. In the next step, I (a-h) on treatment with isatin, sulfanilamide and reflux with glacial acetic acid Synthesis of carbamimidoyl - 3 – (2-oxo-indalin-3 – yl- indene amino) benzene sulphonamide (a-h) In the last step, which on mannich reaction with piperidine and formaldehyde  gave(N-carbamimidoyl 1-4-(2-oxo-1-(piperidine-1-ylmethyl) indolin-3-ylidineamino) benzene sulphonamide) (a-h) under microwave irradiation at a power of 140 watts. MW irradiation led to higher yields in much less time than that by conventional method. The newly synthesized compounds were characterized on the basis of elimental analysis, IR, H NMR, and mass spectra. All the synthesized isatin derivatives have been investigated for their anthelmintic activity.

Key Words:  Microwave, conventional, Synthesis, Isatin, Anthelmintic activity.