Oxytetracycline HCl is an antibacterial drug used in the treatment of acne vulgaris and dermatitis. Its oral bioavailability is intermediate i.e., 60% and it is rapidly excreted through renal route. This drug has many side effects such as epigastric pain, nausea, vomiting, diarrhea, hypersensitivity, and tooth discoloration when taken orally. To overcome the side effects and to increase the bioavailability of Oxytetracycline HCl, topical formulations were prepared. Organogels were prepared using sorbitan monostearate as gelling agent and isopropyl myristate as vehicle with different permeation enhancers. The prepared formulations were evaluated for drug content, viscosity, extrudability, homogeneity, skin irritation test, in vitro drug release, and antimicrobial activity. A formulation containing eucalyptus oil with isopropyl myristate, showed better in vitro permeation and higher antimicrobial activity as compared to other formulations with different penetration enhancers.

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Objectives: Human microdosing studies or phase 0 studies have been proposed to supplement pharmacokinetic (PK) studies in animals. In phase 0 studies, extremely low, nonpharmacologically active doses of a drug are given to a few subjects before phase 1, to define the agent's PK profile in humans. This study has been conducted to compare the values of different PK parameters, as determined by microdosing and conventional therapeutic dose studies in healthy volunteers, and target patient population. Methods: In the first phase of study, 30 healthy adult male volunteers were divided into three groups of 10 each; receiving 14C-labelled atenolol, enalapril and losartan orally, in single microdose. After a wash-out period of 10 days, the same individual received the same drug in single therapeutic dose. In second phase of study, 30 hypertensive patients were divided into three groups and given same drugs. Parameters studied were t½, AUC, Cmax and tmax. Blood samples collected at intervals were subjected to accelerator mass spectrometry (AMS) and high performance liquid chromatography (HPLC), for microdosing and therapeutic dose studies respectively. Results: Microdosing results were comparable with therapeutic dose values for all the drugs studied and showed linearity over therapeutic dose. Conclusions: Microdosing PK parameters are comparable to the ones determined by therapeutic dose studies up to a permissible limit. So the idea of phase 0 PK studies supplementing phase 1 PK studies can be furthered.

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The aim of this study is to enhance the dissolution rate of raloxifene hydrochloride and to prepare tablets by PEGylation. The high-molecular-weight polyethylene glycols, PEG 15 000 and PEG 35 000, were used for PEGylation of raloxifene hydrochloride, a water-insoluble BCS Class II drug. The PEG conjugates were prepared with PEGs in the weight ratios of (1:1), (1:2), and (1:3.5) by using the solvent evaporation technique and the kneading technique. The conjugates were analyzed by FTIR, XRD, and DSC and subjected to dissolution studies. FTIR analysis revealed the interaction of raloxifene HCl with PEG indicating the formation of a conjugate. RLX: PEG 35 000 (1:3.5)(KM) conjugate exhibited the highest dissolution rate of 99.12% at in vitro level among all the RLX: PEG 15 000 and RLX: PEG 35 000 conjugates. The tablets of raloxifene hydrochloride were prepared by using RLX: PEG 35 000 (1:3.5) by the direct compression technique and evaluated. The prepared tablets exhibited optimum drug release characteristics of 99.12% in 60 min and the physical characteristics such as hardness (4.5 kg/cm ² ), friability (less than 1%) and percent drug content (99.79 ± 0.62). The ideal drug release pattern from prepared tablets was indicated by T50 and T90 values as 29.5 and 42 min, respectively, from the dissolution data. Hence, the present studies indicated that the PEGylation of raloxifene HCl was a successful technique to enhance the dissolution rate of raloxifene HCl and to prepare its tablets.

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Sustained-release polymeric beads containing diclofenac sodium were fabricated with hydrophilic polymers, sodium carboxymethyl cellulose (Na CMC), and sodium alginate (Na alginate). Particulate beads of Na CMC and Na alginate were prepared by the ionotropic gelation method using calcium chloride as a cross-linking agent. Beads of diclofenac sodium were prepared with different concentrations of polymers. Prepared beads were evaluated for their yield, particle size, drug entrapment efficiency, release behavior and tested for the presence of incompatibility using FTIR measurement. The drug entrapment efficiency varied between 73 and 92% in different formulations. For the same concentration of polymer, the release of diclofenac sodium from the beads was observed to be 82.69% and 91.33% for Na CMC and Na alginate, respectively, at the end of 10 h . The drug in beads maintained its identity after bead formation as observed by the FTIR study. From the study it could be concluded that multiparticulate beads of diclofenac sodium could be successfully prepared by the ionotropic gelation technique with high entrapment efficiency and sustained-release characteristics.

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Gastro retentive drug delivery systems are the systems which are retained in the stomach for a longer period of time and thereby improve the bioavailability of drugs. Different approaches for gastro retentive dosage forms include floating, raft, expanding/swelling, bioadhesive/ mucoadhesive and high/low density systems.Famotidine, an anti-ulcer drug, suffers from poor bioavailability (50% as famotidine is less soluble in alkaline pH. Famotidine used in combination with antacids promotes local delivery of these drugs to the receptor of the parietal cell wall. Local delivery also increases bioavailability at the stomach wall receptor site and increases the efficacy of drugs to reduce acid secretion. This study aim to formulate floating tablets of famotidine using an effervescent approach for gastroretentive drug delivery system. Floating tablets were prepared using direct compression techniques using polymers like HPMC K4M and HPMCK100M for their gel-forming properties. The HPMC polymer alone is unable to control release rate. It releases drug >90% in four to six hours. In combination with Xanthan gum it release >90% in eight hours. The results indicate that gas generated gastroretentive floating tablets of famotidine containing HPMCK100M and Xanthan gum provide better options for controlled release action and improved bioavailability.

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Hydro distillation of rhizomes and leaves of Curcuma longa resulted in the isolation of 0.36% and 0.53% of oils (w/v) respectively on a fresh weight basis. GC and GC-MS analysis resulted in the identification of 73 constituents in rhizomes comprising 95.2% of the oil, of which the major ones were ar-turmerone (31.7%), α-turmerone (12.9%), β-turmerone (12.0%) and (Z) β-ocimene (5.5%). In the oils, 75 constituents comprising 77.5% of the oils were identified, the major ones were α-phellantrene (9.1%), terpinolene (8.8%), 1,8-cinceole (7.3%), undecanol (7.1) and p-cymene (5.5%).

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Herbal medicines have been used since prehistoric times by different cultures worldwide for treatment of diabetes. In the present investigation, the effect of untreated and heat-treated aqueous extracts from Eugenia jambolana Lam (Myrtaceae) seeds on carbohydrate hydrolyzing enzymes, namely, porcine pancreatic á-amylase, rat intestinal α-glucosidase, and sucrase, have been studied using in vitro model systems. Untreated E. jambolana extract (EJU) significantly inhibited (p ≤ 0.01) α-amylase, α-glucosidase, and sucrase activities in a dose-dependent manner, with the exception of sucrase, where the increased sample concentration did not increase the sucrase inhibitory activity. Heat treatment of the sample resulted in a significant increase (p ≤ 0.01) in the α-amylase inhibitory activity of the sample, while a marginal increase in the α-glucosidase and sucrase inhibitory activities were observed, however, they did not reach statistical significance. EJU showed IC50 values of 3.4%, and 68 and 56 ìg mL-1 for α-amylase, á-glucosidase, and sucrase, respectively, while the IC50 values for heat-treated E. jambolana extract (EJH) were 2.4%, and 66 and 54 ìg mL-1, respectively. Further, a significant correlation (p ≤ 0.01; r = 0.833) was observed between α-amylase, α-glucosidase, and sucrase inhibitory activities of both EJU and EJH. These findings emphasize that inhibition of carbohydrate hydrolyzing enzymes is one of the mechanisms through which E. jambolana exerts its hypoglycemic effect in vivo.

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Punica granatum Linn. (Punicaceae) flower buds are used in the treatment of asthma traditionally, so the present work was undertaken to prove it scientifically using suitable animal models. Antihistaminic principles are useful in the treatment of asthma,;hence, in present work antihistaminic activity of various extracts of P. granatum flower buds was checked using clonidine-induced catalepsy and haloperidol-induced catalepsy in Swiss albino mice at the dose of 50 and 100 mg/kg, p.o. The results showed that ethanol extracts (100 mg/kg, p.o.) are having significant antihistaminic activity amongst other extracts. Thus, it can be concluded that tannins from the flower buds of P. granatum may be responsible for antihistaminic activity and may have potential role in the treatment of asthma.

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Leucas lavandulaefolia Willd. is mainly used in Indian folk medicine for the treatment of diabetes mellitus. The oral administration of 0.15, 0.20 and 0.25 g/kg of chloroform extract of the Leucas lavandulaefolia flowers (LLFEt) for 30 days resulted in a significant reduction in blood glucose, glycosylated hemoglobin and an increase in total hemoglobin, and the effect was highly significant in the case of 0.25 g/kg. It also prevents decrease in body weight. Oral glucose tolerance test was also performed in experimental diabetic rats in which there was a significant improvement in glucose tolerance in animals treated with LLFEt and the effect was compared with glibenclamide. Thus, the study shows that LLFEt has hypoglycemic action.

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This research aims to investigate the antidiabetic activity of Nerium indicum (Family: Apocynaceae) leaf extract in alloxan induced diabetic albino rats. A comparison was made between the action of Nerium indicum extracts and a known antidiabetic drug glibenclamide (600 µg/kg body wt.). An oral glucose tolerance test (OGTT) was also performed in experimental diabetic rats. The petroleum ether, chloroform, alcohol and aqueous extracts of Nerium indicum were obtained by simple maceration method and subjected to standardization by following pharmacognostical and phytochemical screening methods. Dose selection was made on the basis of acute oral toxicity study (50mg to 5000 mg/kg body weight) as per OECD guidelines. Nerium indicum chloroform extract (NICE) and ethanolic extract (NIEE) showed significant (P<0.001) antidiabetic activity. In alloxan induced model, blood glucose level of these extracts on the seventh day of study were NICE (113.33±6.662) and NIEE (169.33±9.735) in comparison of diabetic control (413.50 ±4.752) and petroleum ether extract (337.83±25.515). In OGGT model (glucose loaded rats), NICE exhibited glucose level after 30 min. (164.33±5.661) and 90 min. (121.00±2.966) whereas NIEE after 30 min. (174.16±3.380) and 90 min. (128.00±5.266). These extracts also prevented body weight loss in diabetic rats. The antihyperglycemic action of the extracts may be due to improving the glycemic control mechanisms. The drug has the potential to act as antidiabetic drug.

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The objective of the present study has been to evaluate the hepatoprotective activity of methanolic extract of Hordeum vulgare Linn. (MEHV) seeds against acetaminophen-induced liver damage in rats. Acetaminophen-induced liver damage was produced by the treatment of acetaminophen (3g/kg/d, p.o.) for three days. Other groups of rats were pretreated with two doses of MEHV seeds (300 and 500 mg/kg/d, p.o) and silymarin (200 mg/kg/d, p.o) 30 min prior to acetaminophen ingestion. Liver damage was evidenced by elevated levels of biochemical parameters such as serum glutamate oxaloacetic transaminase and glutamate pyruvic transaminase (SGOT and SGPT), alkaline phosphatase (ALP), total and direct bilirubin (TBL and DBL), lactate dehydrogenase (LDH), gamma glutamyl transferase (GGT), malondialdehyde (MDA), decreased level of total protein (TP) and reduced glutathione (GSH) along with increased histopathological scores in the APAP control. Pretreatments with MEHV seeds produced significant reversal in the above biochemical parameters and reduced histopathological scores of fatty degeneration, necrosis with significant evidence of regeneration. The results of this study indicate that pretreatment with MEHV seeds possessed the significant hepatoprotective activity. In conclusion, the possible mechanism of hepatoprotective action of methanolic extracts of Hordeum vulgare seeds may be due to its antioxidant activity as indicated by protection against increased lipid peroxidation and maintained glutathione contents.

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A deficit of cholinergic neurotransmission is considered to be one of the major causes of disturbance in learning and memory. Among the various therapeutic approaches investigated to enhance cholinergic transmission, acetylcholinesterase (AChE) inhibition is presently the most successful method to ameliorate cholinergic deficit. Keeping in view the activity of numerous quinoline derivatives reported as potential cognitive enhancers attempts were made to design and synthesize some 6-aminoquinoline derivatives. The title compounds were synthesized via an intermediate 6-nitroquinoline which was prepared by Skraup synthesis from 4-nitroaniline prepared from acetanilide by its nitration and subsequent hydrolysis. 6-Nitroquinoline after reduction was treated with various aldehydes (veratraldehyde, anisaldehyde, 3-hydroxybenzaldehyde, indole-3-carboxaldehyde etc.) to give the target compounds. Some of the compounds showed a significant memory enhancing activity using elevated plus maze at 5 mg/kg and 10 mg/kg doses. Biochemical studies have shown the compounds to possess unexpectedly good acetylcholinesterase inhibitory activity (max %inhibition 65.27).

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A simple new spectrophotometric method has been developed for estimation of Tenofovir disoproxil fumarate in bulk and tablet dosage form. Tenofovir disoproxil fumarate is estimated to be 261 nm in triple distilled water. The Beer's law is obeyed in the concentration range of 5 - 90 µg/mL of the drug. The slope and intercept values are 0.0109 and 0.1075, respectively. Results of analysis of this method have been validated statically and by recovery studies. The method is applied to the marketed tablet formulation. A result of the analysis of tablet formulation, given as a percentage of label claim ± standard deviation is 98.15 ± 0.76. The precision and accuracy has been examined by performing recovery studies and found to be 100.06 ± 1.24. The developed method is simple, sensitive, and reproducible, and can be used for the routine analysis of Tenofovir disoproxil fumarate in bulk and tablet dosage form.

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This study describes the development and validation for the simultaneous estimation of rupatadine and montelukast by the first-order derivative UV spectroscopy method. The quantification was achieved by the first-order derivative spectroscopy method at 273.46 nm and 297.27 nm over the concentration range of 5-25 µg/ml for estimation of rupatadine and montelukast in a combined tablet formulation. Procedure does not require prior separation of components from the sample. Rupatadine and montelukast were determined at 15 µg/ml with a mean recovery of 99.59 + 0.225 and 99.21 + 0.76, respectively. Calibration curves were linear with a correlation coefficient of 0.9994 and 0.9992 for rupatadine and montelukast, respectively. The relative standard deviation was found to be <2.0%. The present result shows that the proposed method can be successfully used for simultaneous determination of the drug content in marketed formulations.

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A simple, accurate, and precise HPTLC method has been developed and validated for the estimation of efavirenz from bulk drug and capsule formulations. The separation was achieved on TLC plates using an appropriate solvent system. The spots so developed were densometrically scanned at 247 nm. The linearity of the method was found to be within the concentration range of 1-40 µg/ml. The validation parameters, tested in accordance with the requirements of ICH guidelines, prove the suitability of this method. The method was successfully applied for determination of drug in capsules, wherein no interference from capsule excipients was observed, indicating the specificity of the developed method. Thus, the proposed method can be used successfully for routine analysis of efavirenz from capsule and bulk formulations.

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A simple, accurate, precise, economic, and specific stability indicating the RP-HPLC method has been developed for the estimation of Miglitol in tablet dosage form and spiked rabbit plasma. Chromatographic separation was achieved using Lachrom HPLC with Lichrospher, ODS, (250õ 4.6) mm, ô 5 column at ambient temperature with 0.05 M ammonium acetate as a mobile phase at a flow rate of 0.5 ml/min and 216 nm was selected as a wave length for detection of a method. The retention time was 6.45 min. The standard curve was found to be linear (r ² = 0.996) in the concentration range 800-1200 µg/ml using 1000 µg/ml as the test concentration. Apparent recovery was 98.338-101.704 % with RSD 0.942-0.964 for two brands. The method was repeatable with RSD 0.736. The intraday and interday precisions were RSD 0.957 and 1.019, respectively. LOD and LOQ of the method were 20 and 70 µg/ml, respectively. The presented study separates degradents and peaks appeared after spiking drug with plasma with a resolution of more than 1.5.

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The rapid, simple, and accurate chromatographic (high-performance liquid chromatography) and spectrophotometric method for the determination of progesterone in capsule was elaborated. Methanol was found to be a suitable extraction solvent. The samples were chromatographed on Linchrocart C18 column and UV detection at 254 nm. The elution was achieved isocratically with a mobile phase of methanol - water (80:20, v/v). The method was validated for precision, linearity, accuracy, and limit of detection.

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More than 850 patients' medication history forms were evaluated, retrospectively, for possible irrationalities in the prescribing pattern of antibiotics for management of hospitalized diabetic foot cases. Primary anti-diabetic therapy included insulin, oral anti-diabetic, or combination of both. Supportive therapy included antibiotics for diabetic foot cases and other physical measures like routine wound dressings and washing. Antibiotic therapy was analyzed based on the reported medical literature. It was deduced that in addition to other supportive measures advised for the management of diabetic foot, the antibiotic therapy for management of diabetic foot (n=410) was in the order of ceftriaxone (83.3%) > co-amoxiclav (36.66%) > clindamycin and ciprofloxacin (26.66%) > cefuroxime and levofloxacin (10.0%) > clarithromycin and cefoperazone / sulbactam, cephradine and fusidic acid (6.6%) > cefotaxime sodium and oxytetracyclin (3.33%). Placing ceftriaxone as a first choice (83.3%) in the antibiotic therapy carries no logic as ceftriaxone has low activity against reported higher incidence (85 %) of gram-positive organisms such as Staphylococcus aureus and streptococcus species. Prescribing irrationality of antibiotics is a global phenomenon that shall be addressed right from the medical/pharmacy schools levels.

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Business method patent grants to its holder exclusive rights to a particular way of doing business. Business method patents are a relatively new species of patent and there have been several reviews investigating the appropriateness of patenting business methods. The U.S. Patent and Trademark Office (USPTO) reports that, in 1998, 1300 patent applications pertained to business methods and 420 such patents were issued. In 2000, 7500 applications for business method patents were filed, and 1000 such patents were issued. In India The Patents (Amendment) Act, 2002, with effect from May 20, 2003 declared a mathematical or business method or a computer program per se or algorithms, as not being an invention within the meaning of the patent statute.

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