Compression and evaluation of extended release matrix pellets prepared by the extrusion/spheronization process into disintegrating tablets

Nesse trabalho, estudou-se nova abordagem para a compressão de matrizes de péletes em comprimidos desintegrantes, com o intuito de resolver os problemas relativos à ruptura do polímero de revestimento durante a compressão dos péletes do tipo reservatório. Matrizes de péletes de liberação estendida foram preparadas pela técnica de extrusão/esferonização, utilizando dispersões aquosas comercialmente disponíveis de etil celulose, polímeros acrílicos e alginato de sódio a 10%, 20% e 30% p/p. O cloridrato de sertralina foi utilizado como fármaco modelo e focalizou-se no perfil de liberação in vitro de 12 horas. Os comprimidos contendo matrizes de péletes foram preparados pelo processo de compressão direta. O valor de aceitação, teste farmacopéico, foi aplicado para estudar a uniformidade de distribuição do fármaco. O efeito da força de compressão (2-6 kN), o tamanho da abertura de extrusão, a composição da mistura diluente, a porcentagem de pélete na liberação de fármaco e o valor de aceitação foram estudados. Como o polímero é uniformemente distribuído dentro de cada pélete, o padrão de liberação do fármaco dos péletes não-comprimidos foi comparável àquele dos comprimidos. As mudanças morfológicas da superfície devidas ao tratamento com cloreto de cálcio foram observadas utilizando-se a microscopia eletrônica de varredura. O pélete segregado da superfície do comprimido mostrou-se plano em direção à força de compressão aplicada com menores deformidades. Em conclusão, os péletes matriz podem se constituir em abordagem alternativa para péletes do tipo reservatório na obtenção de comprimidos desintegrantes para fármacos de liberação estendida.In this study, a novel approach for compression of matrix pellets into disintegrating tablets has been studied in an attempt to overcome the issues pertaining to rupture of polymer coat during compression of reservoir-type pellets. Extended release matrix pellets were prepared by the extrusion/spheronization technique using commercially available aqueous dispersions of ethyl cellulose, acrylic polymers and sodium alginate at 10%, 20% and 30%w/w levels. Sertraline hydrochloride was used as the model drug and an in vitro release profile of 12 h was targeted. Tablets containing matrix pellets were prepared by the direct compression process. Acceptance Value, a pharmacopeial test, was applied to study the uniformity of drug distribution. Effect of compression force (2-6 kN), extrusion screen aperture size, diluent blend composition and pellet percentage on drug release and acceptance value were studied. As polymer is uniformly distributed within each pellet, the drug release pattern from uncompressed pellets was comparable to compressed tablets. Surface morphological changes due to calcium chloride treatment were observed using Scanning electron microscopy. The pellet segregated from the surface of the tablet was found to be flattened in the direction of applied compression force with minor deformities. In conclusion, matrix pellets can constitute an alternative approach to reservoir-type pellets in obtaining disintegrating tablets for extended delivery of drugs

AZETIDIN-2-ONE FUSED QUINOLINE ANALOGUES: SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME NOVEL 2-CHLORO-3-FORMYL QUINOLINE DERIVATIVES

Objective: The aim of the present invention is to synthesize and find out the biological significance of the series of the designed azetidin-2-one fused 2-chloro-3-formyl quinoline derivatives. Methods: A new series of 2-chloro-3-formyl quinolines derivatives 3-chloro-4-(2-chloro-8/7/6-methoxyquinolin-3-yl)-1-phenyl amino)azetidin-2-one, 3-chloro-4-(2-chloro-8/7/6-chloroquinolin-3-yl)-1-(phenylamino) azetidin-2-one, 3-chloro-4-(2-chloro-8/7/6-methylquinolin-3-yl)-1-(phenyl -amino)azetidin-2-one were synthesized by four steps. The cyclization is facilitated by N-aryl acetamides bearing electron donating groups at ortho-position. However yields of quinolines having electron donating groups in all cases. The structures of the synthesized compounds have been established on the basis of physical and spectral data and are screened for diuretic, some of the exhibited significant activity. Results: The moderate yield of the proposed compounds was obtained. Spectral analysis and physical characteristic showed that the structural confirmation of the quinoline derivatives of the synthesized compounds. Some of the compounds showed lower to moderate level of significant activities. Conclusion: From the result of spectral data and diuretic activity it has concluded that the compounds were found to exhibited significance activity

Preliminary Investigation of Antipyretic Activity of Trinpanchmool Extracts

Current research work is to evaluate the antipyretic activity of hydro-alcoholic extract of trinpanchmool on the wistar rats. Brewer’s yeast induced pyrexia method was used to evaluate febrifuge effect of trinpanchmool extract along with its comparison with its individual constituents on the wistar rats. Darbh, Ikshu and SAR was having better antipyretic activity than the standard drug paracetamol. Combination of the drugs was having better antipyretic that paracetamol but lesser than the individual drugs. Trinpanchmool and its individual drugs are having febrifugatic effect better than our standard paracetamol

COMPARATIVE IN VITRO ANTIOXIDANT ACTIVITY OF ETHYL ACETATE AND ETHANOL EXTRACTS OF CALLICARPA MACROPHYLLA

Objective: The objective of the study was to evaluate and compare the antioxidant activity of (EA and E) ethyl acetate and ethanol extracts of (CM) Callicarpa macrophylla. Methods: The physiochemical parameters were assessed according to guidelines given by the world health organization. The total content of phenols and flavonoids was assessed by Folin–Ciocalteu and aluminum chloride methods. In vitro, antioxidant activity was screened by (DPPH) 1, 1-diphenyl-2- picrylhydrazyl and(H2O2) hydrogen peroxide scavenging and reducing power assay. Results: The physicochemical parameters fulfilled the standards of WHO guidelines. Total phenol and flavonoid content were more in ethanol extract as compared to ethyl acetate extract of CM. The antioxidant activity of ethanol extract was further high as compared to ethyl acetate extract of Callicarpa macrophylla. The IC50 of Callicarpa macrophylla ethanol extract was less than the ethyl acetate extract. So, more antioxidant activity of ethanol extract compared to ethyl acetate extract of CM. Conclusion: Overall, both the extracts showed antioxidant activity and can be used further for diseases that can be managed using antioxidants. Ethanol extract possessed significant antioxidant effects than the ethyl acetate extract

Preliminary Investigation of Antipyretic Activity of Trinpanchmool Extracts

Current research work is to evaluate the antipyretic activity of hydro-alcoholic extract of trinpanchmool on the wistar rats. Brewer’s yeast induced pyrexia method was used to evaluate febrifuge effect of trinpanchmool extract along with its comparison with its individual constituents on the wistar rats. Darbh, Ikshu and SAR was having better antipyretic activity than the standard drug paracetamol. Combination of the drugs was having better antipyretic that paracetamol but lesser than the individual drugs. Trinpanchmool and its individual drugs are having febrifugatic effect better than our standard paracetamol

Synthesis, Characterization And Antimicrobial Activity Of Novel Substituted Aryl- 1,3,4-Oxadiazolo-[3,2-A]-1,3,5-Triazine Derivatives

Bioactive heterocyclic rings 1,3,4-oxadiazole and 1,3,5-triazine are fused with expectation of enhanced biological activity of the newly synthesized compounds. Hence Synthesized fused heterocyclic compounds as a substituted aryl- 1,3,4-oxadiazolo-[3,2-a]-1,3,5-triazine derivatives The structures of all the compounds were confirmed by physical and spectral analysis. The newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains and fungal strains. Some of these compounds have shown significant antibacterial and antifungal activity

OPTIMIZATION AND PREPARATION OF SOLID LIPID NANOPARTICLE INCORPORATED TRANSDERMAL PATCH OF TIMOLOL MALEATE USING FACTORIAL DESIGN

Objective: Transdermal patch of timolol maleate was prepared in order to increase the permeability of the drug topically. Methods: The timolol maleate (TM) loaded solid lipid nanoparticles (SLN) were prepared by the solvent evaporation method. For the optimization process full factorial (three-factor and three-level), hydroxypropyl methylcellulose (HPMC) range from 100 to 300 mg, ethylcellulose 100 to 200 gm and almond oil 3 to 4 ml. The response noted in form of tensile strength and percent drug release. These transdermal patches were evaluated for physical characterization like weight variation, thickness, percentage moisture absorption, percentage moisture loss, water vapor transmission rate, folding endurance, tensile strength, and content uniformity. Results: Solid lipid nanoparticles of TM were optimized and prepared, the data presented that drug release percent ranged from 66.12 to 91.75. 2FI model was observed to fit for response % drug permeation with a p and F value of 0.0271 and 4.50. The tensile strength varies from 0.358 to 0.508. The linear model was observed to fit for the tensile strength response with a p-value and F-value of<0.0001 and 52.41. Conclusion: The controlled release formulation of Timolol Maleate was successfully optimized and prepared, a study conducted to investigate the effect of different polymers and type of permeation time profiles from Timolol Maleate patches

A REVIEW FROM HISTORICAL TO CURRENT-CELASTRUS PANICULATUS

Celastrus paniculatus is commonly known as “Malkangani”, widely distributed in the Maldives, Australia, China, Cambodia, Malaysia, Taiwan, Nepal, Thailand as well as in the Pacific Islands and all over India mainly Maharashtra, Orissa and Andaman and Nicobar group of Islands on an altitude of 1800m. It climbs up to over 10m. The leaves are ovate or elliptic in shape with dentate margin. Seeds are ellipsoid or ovoid, yellowish-brown in color and grow inside the capsules. Celastrus paniculatus (Malkangni) is used in Ayurveda as a nervine tonic, tranquilizer and diuretic and in rheumatism, gout, leprosy and asthma. Different Parts of Celastrus paniculatus after extraction and fractionation give different active constituents such as sesquiterpene esters-malkanguinol, malkangunin, sesquiterpene alkaloids-celapanin, celapanigin, alkaloids-celastrine, paniculatine, fatty acids-oleic acid, palmittic acid, linoleic acid and stearic acid, crystalline substance tetracasanol and sterol. Different pharmacological activities are anti-rheumatic, anti-fungal, nootropic activity, antimalarial activity, anti spermatogenic effect, anti-anxiety and anti-atherosclerotic effect. In the present review, our target is to search, bring together and compile the data of Celastrus paniculatus, which have less side effects and very valuable for the treatment of rheumatism. Related information is procured from various scientific publications using online, seek out engines such as Google scholar, Pubmed and Science Direct. A total of 200 articles was reviewed out of which 55 articles are selected to review for the description of the plant, parts used, chemical constituents, traditional uses and for reported activities

GC-MS Analysis of Methanol and Ethyl Acetate Extract of fruits of Sphaeranthus indicus

Introduction: To identify the various phytoconstituents present in the plant Sphaeranthus indicus by using gas chromatography and mass spectrometry. Meth­ods: The fruits of Sphaeranthus indicus were extracted with Different solvents of increasing polarity. The methanol and ethylacetate extract were subjected to GCMS analysis to detect the phytoconstituents. Results: Totally 26 compounds were identified. Among these 13 constituents in methanol extract and 13 constituents in ethylacetate extract were identified during the GC-MS analysis. Stigmasterol and lupeol which were identified in the plant is considered to have antiarthritic properties. Keywords: Sphaeranthus indicus, Gas chromatography, Mass spectrometry

OPTIMIZATION AND CHARACTERIZATION OF CHITOSAN-BASED NANOPARTICLES CONTAINING METHYLPREDNISOLONE USING BOX-BEHNKEN DESIGN FOR THE TREATMENT OF CROHN’S DISEASE

Objective: The present research was designed to produce methylprednisolone containing chitosan-based nanoparticles using Box-Behnken Design (BBD) and Response Surface Methodology (RSM) for optimization. Methods: Nanostructures were prepared using the ionic gelation method with screened process parameters. According to the design, methylprednisolone chitosan-based nanoparticles (MCSNPs) were optimized using factors like methylprednisolone concentration, stirring speed and temperature whereas particle size, zeta potential and % encapsulation efficiency as responses. From the observed values of responses with confirmation location and desirability, the predicted values were very close to the observed values. Results: Observed values for the optimized formulation have a particle size of 243±2.33 nm with an encapsulation efficiency of 79.3±7.2%. Morphology of the particles using scanning electron microscopy reveals nearly spherical shaped particles. Methylprednisolone was released in vitro in a sustained manner for about 24 h in simulated colonic fluid pH 7, pH 7.8 (Fasted state) and phosphate buffer pH 7.4, when compared to simulated colonic fluid at pH 6 (Fed state). Optimized MCSNPs followed Korsmeyer peppas kinetics with drug release mechanism as anomalous transport. Conclusion: Application of Box-Behnken design and Response Surface Methodology using Design Expert software was successfully used in the optimization of methylprednisolone loaded chitosan-based nanoparticles with high encapsulation efficiency