DESIGN AND EVALUATION OF COLON SPECIFIC DRUG DELIVERY OF BUDENOSIDE

Objective: The objective of this research is to design and evaluate a colon specific drug delivery of budenoside using guar gum as enzyme dependent polymer.Methods: Matrix tablets of Budenoside were prepared by using wet granulation technique with different proportions of guar gum and evaluated for different evaluation tests and release profiles.Results: The formulations were studied for post compression parameters like hardness, friability, weight variation and drug content are in acceptable range of pharmacopoeial specifications. In vitro swelling and Invitro release studies was carried out at different pH ranges (1.2, 6.8 and 7.4). The release profile of budenoside from the matrix tablets is dependent upon the gelling property of guar gum and degradation of guar gum polysaccharide by colonic bacteria. High concentration of guar gum showed less drug release in the stomach as an enzyme dependent polymer. In vitro release data revealed that the presence of rat caecal content in dissolution medium showed the significant increase in drug release (97.12%), when compared to drug release study in absence of caecal content (76.86).Conclusion: The results were subjected to study the release kinetics. The values of correlation coefficient indicated that the drug release followed Zero order drug release kinetics with Peppas drug release mechanism. In vitro drug release studies shows that guar gum with high concentration (25%) has optimum release in a controlled manner for 24 hours.Â

A NEW STABILITY INDICATING UPLC METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF METOLAZONE AND SPIRONOLACTONE IN BULK AND IN ITS PHARMACEUTICAL FORMULATIONS

Objective: The objective of the work is to develop and validate a new, simple, highly sensitive RP-UPLC method for simultaneous estimation of Metolazone and Spironolactone in bulk and in its dosage forms. Methods: The method was developed on a reversed-phase Hypersil Gold C18 (2.1× 100 mm, 2.7 µm) column with isocratic elution. Detection was done by UV-Spectroscopy at a detection wavelength of 235 nm. The analytical procedure was validated by assessing the specificity, linearity, precision, accuracy, limit of detection, limit of quantification, robustness and ruggedness as per ICH guidelines. Results: The results were obtained as follows- the retention times were found to be around 2.888 min and 3.835 min, the percentage purity was observed to be 99 % w/v and 100 % w/v, the percentage recovery was found to be 99.90% and 99.9% respectively for Metolazone and Spironolactone. Calibration plots were linear (r2 > 0.999) over the concentration range of 12 to 28μg/ml for Metolazolone and 120 to 280μg/ml for Spironolactone. The LOD was 0.0002µg/ml for Metolazone and 0.01µg/ml for Spironolactone. The LOQ was found to be 0.0008µg/ml for Metolazone and 0.003µg/ml for Spironolactone. Conclusion: The developed analytical method for the simultaneous quantitation of Metolazone and Spironolactone was found to be specific, rapid, reliable, and reproducible. No interference from any component of pharmaceutical dosage form was observed. The method is amenable to the routine analysis of large numbers of samples with good precision and accuracy

3-(4-Methoxy­benz­yl)-1-benzothio­phene

In the title compound, C16H14OS, the dihedral angle between the benzothio­phene ring system and the benzene ring is 72.41 (12)°. A weak inter­molecular C—H⋯π inter­action from the benzene ring to the benzothio­phene ring system is observed in the crystal structure

4′-Ferrocenyl-1′-methylacenapthylene-1-spiro-2′-pyrrolidine-3′-spiro-2′′-indane-2,1′′,3′′(1H)-trione

In the title compound, [Fe(C5H5)(C29H20NO3)], the acenaphthyl­ene ring system makes a dihedral angle of 83.77 (3)° with the indane-1,3-dione ring system. The central pyrrolidine ring exhibits a twist conformation. In the crystal, mol­ecules are linked by a weak inter­molecular C—H⋯O inter­action into a chain along the b axis. Two weak intra­molecular C—H⋯O inter­actions are also present

Methyl 9-p-tolyl-8a,9,9a,10,11,12,13,14a-octa­hydro-8H-benzo[f]chromeno[3,4-b]indolizine-8a-carboxyl­ate

In the title compound, C28H29NO3, the fused pyrrolidine and piperidine rings of the octa­hydro­indolizine unit exhibit envelope and chair conformations, respectively. The dihedral angle between the naphthalene ring system and the benzene ring is 40.37 (5)°. The crystal packing is stabilized by weak inter­molecular C—H⋯O inter­actions

19-Ferrocenyl-18-oxa-8,16-diaza­penta­cyclo­[8.6.3.01,10.02,7.012,16]nona­deca-2(7),3,5-triene-9,17-dione

In the title compound, [Fe(C5H5)(C21H19N2O3)], both pyrrol­idine rings of the pyrrolizine substructure show an envelope conformation. In the ferrocenyl moiety, the unsubstituted cyclo­penta­dienyl ring is disordered over two orientations with site occupancies of 0.64 (2) and 0.36 (2). In the pyrrolizine ring, one C atom is disordered over two positions, with site occupancies of 0.71 (1) and 0.29 (1). Intra­molecular C—H⋯O inter­actions occur. The crystal packing is established through weak inter­molecular C—H⋯O and N—H⋯O inter­actions

Crystal structure of [4-(2-methoxyphenyl)-3-methyl-1-phenyl-6-trifluoromethyl-1H-pyrazolo[3,4-b]pyridin-5-yl](thiophen-2-yl)methanone

The title compound, C[subscript 26]H[subscript 18]F[subscript 3]N[subscript 3]O[subscript 2]S, a 2-meth­oxy-substituted derivative, is closely related to its 4-methyl- and 4-chloro-substituted analogues and yet displays no structural relationships with them. The thio­phene ring is disorder free and the -CF[subscript 3] group exhibits disorder, respectively, in contrast and similar to that observed in the 4-methyl- and 4-chloro-substituted derivatives. The torsion angle which defines the twist of the thio­phene ring is -69.6 (2)° (gauche) in the title compound, whereas it is anti­clinal in the 4-methyl- and 4-chloro-substituted derivatives, with respective values of 99.9 (2) and 99.3 (2)°. The absence of disorder in the thio­phene ring facilitates one of its ring C atoms to participate in the lone inter­molecular C-H...O hydrogen bond present in the crystal, leading to a characteristic C(5) chain graph-set motif linking mol­ecules related through glides along [010]. An intra­moleculr C-H...N hydrogen bond also occurs

Methyl 9-(4-bromo­phen­yl)-8a,9,9a,10,11,12,13,14a-octa­hydro-8H-benzo[f]chromeno[3,4-b]indolizine-8a-car­box­ylate

In the title compound, C27H26BrNO3, the mean plane of the naphthalene ring system makes a dihedral angle of 22.0 (1)° with the bromo-substituted benzene ring. The pyrrolidine and piperidine rings exhibit envelope and chair conformations, respectively. An inter­molecular C—H⋯Br inter­action is observed

Ethyl 2-acetoxy­methyl-1-phenyl­sulfonyl-1H-indole-3-carboxyl­ate

In the title compound, C20H19NO6S, the phenyl ring of the phenyl­sulfonyl group makes a dihedral angle of 83.35 (5)° with the indole ring system. The mol­ecular structure exhibits a number of short intramolecular C—H⋯O contacts