ABSTRACT

3-methylbenzthiazolinone-2(3H)-hydrazone is a chromogenic reagent used in spectrophotometric determination of pharmaceuticals. This review explains the work done by different researchers so far for estimation of the drugs by spectrometric analysis. Therefore, this review gives compiled data on utilisation of MBTH reagent in spectrometric analysis

Key Words: Spectrophotometry, MBTH, Chromogen.

ABSTRACT

Recent development in drug delivery system are going on aims to enhance safety and efficacy of drug molecules by formulating a convenient dosage form for ease of administration and to achieve better patient compliance. Novel technologies with improved performance, patient compliance, and enhanced quality have emerged in the recent past. Oral fast-dispersing dosage forms, three-dimensional Printing (3DP) and electrostatic coating are a few examples of a few existing technologies with the potential to accommodate various physico-chemical, pharmacokinetic and pharmacodynamic characteristics of drugs. This article provides a comprehensive review on various formulation aspects, technologies and evaluation methodologies, suitability of drug candidates, and future prospects of oral fast-dispersing dosage forms.

Key words: Improved patient compliances, oral fast–dispersing dosage form, quick-disintegrating tablets

ABSTRACT

The main aim of this study was to determine the sensitivity and resistance pattern of Urinary tract pathogens. Knowledge of sensitivity and resistance pattern of uropathogens in geographical locations is an important factor for choosing suitable antibacterial treatment. Patient information was obtained from medical record files. A total of 146 samples were analyzed. The organisms were isolated as the causative factors. E.coli (57.46%) Klebsiella (23.13%) and Staphylococcus (20.89%). Analysis of the samples showed that UTI was more common in females of younger age group as compared to males. The most common organism to cause UTI was found to be E.coli followed by Klebsiella. E.coli was found to be sensitive to Furazolidone (52%) and Nitrofurantoin (52%). Similarly Klebsiella to Furazolidone and Nitrofurantoin and Staphylococcus to Nitrofurantoin and Amikacin.

Key words: Urinary tract, Pathogens, Ueopathogen, E.coli

ABSTRACT

The Pulmonary route has been conventionally used to treat diseases of the respiratory tract and also non-respiratory tract. The significant research work from the last two decades have exposed that in addition to treating local diseases, a wide range of systemic diseases can be treated by delivering drugs to the lungs. In general inhalable formulations of various drugs have been developed to treat the systemic diseases via the lungs. But the problem with those inhalable formulations is they need repeated doses of drug to control the disease condition, since the inhaled drug cleared rapidly. Therefore new technologies have been investigated, where inhaled particles are capable of controlled release of drug from the lungs. In those nanotechnology based drug delivery systems are being developed as a tremendous field. Nano refers to particles size range of 1-1000nm. An important feature of these technologies is the large geometric size of the particles than normal aerosol solutions, which makes it difficult for the lung macrophages to clear these particles. Therefore it results in longer residence times for the particles in the lungs after delivering the drug to the lungs. The present review discusses about the anatomy and structure of lungs, various conventional formulations for pulmonary delivery, and the various colloidal carriers like liposomes, dendrimers, nanoparticles, which involves the delivering of drugs to lungs.

Key words: targeted drug delivery, pulmonary drug delivery, nanotechnology, colloidal particles.

ABSTRACT

Chikungunya virus (CHIKV) is a mosquito-borne alpha virus that induces in humans a disease characterized by fever, rash, and pain in muscles and joints. The virus causing Chikungunya disease was identified over 50 years ago; however, because the disease appeared only in developing countries, little research on it has been done. CHIKV infection in these animals recapitulated the viral, clinical, and pathological features observed in human disease. In the macaques, long-term CHIKV infection was observed in joints, muscles, lymphoid organs, and liver, which could explain the long-lasting CHIKV disease symptoms observed in humans. In addition, the study identified macrophages as the main cellular reservoirs during the late stages of CHIKV infection in vivo.

Keywords: Chikungunya, CHIKV, Aedes mosquitoes, Alpha virus, arbovirus.

ABSTRACT

Eye is the most exclusive organ of the body and various drug delivery systems are used to deliver drug into eye but there are various limitations like rapid precorneal drug loss of conventional systems. Ocular disposition and elimination of a therapeutic agent is dependent upon physicochemical, microbiological, pharmaceutical properties and ophthalmic irritancy properties of ocular dosage forms as well as the relevant ocular anatomy and physiology. To improve ocular drug contact time, bioavailability and residence time, and to reduce the  patient discomfort, frequency of dose, as well as to slow down the elimination of the drug  there are significant efforts concentrating towards newer drug delivery systems for ophthalmic administration. This review focuses on the various new drug delivery systems applied in eye like inserts, in-situ gel, the newly developed particulate and vesicular systems like liposomes, pharmacosomes and discomes, niosomes, nanoparticles, iontophorosis, corneal shields, drug embedded contact lenses, ocular wafers etc and the most recent advanced approaches of the ocular delivery systems like  the delivery of the genes and proteins to the internal structures which were used in treating the diseases  caused due to genetic mutation, along with safety evaluation of ocular drug delivery formulations with some case studies.

Key words: Ophthalmic disorders, advanced ocular therapy, control drug delivery systems, vesicular systems, safety evaluation.

ABSTRACT

From ancient time Allium sativum has been used as food, spice and household medicine for several common problems such as dog bites, insect stings, earaches, burns, wounds, baldness, headaches, chest colds etc. The therapeutic effect of Allium sativum is due to Allin, Allicin, protein, fixed oil, thiamine, ascorbic acid and minerals. This review covers the study of Pharmacognosy, pharmachemistry, pharmacology and pharmaceutical aspects of this herb. Moreover, its valuable medicinal effects along with its economical value are being discussed. 

Keywords: Garlic, pharmaceuticals, economics, medicinal uses, herbs

ABSTRACT

In ancient Greek ‘Nano’ means dwar. Nanotechnology is the creation and utilization of materials, devices, and systems through the control of matter on the nanometer-length scale, i.e. at the level of atoms, molecules, and supramolecular structures. These technologies have been applied to improve drug delivery and to overcome some of the problems of drug delivery for cancer treatment. The magic of nanoparticles mesmerize everyone because of their multifunctional character and they have given us hope for the recovery from this disease. Nanoparticles can be used to deliver hydrophilic drugs, hydrophobic drugs, proteins, vaccines, biological macromolecules, etc. They can be formulated by aptamer conjugation for targeted delivery to the lymphatic system, brain, arterial walls, lungs, liver, spleen, or made for long-term systemic circulation. Therefore, numerous protocols exist for synthesizing nanoparticles based on the type of drug used and the desired delivery route. In modern medicine technologies the oral administration of solid forms is the preferred route for drug delivery. Thus, in pharmaceutical applications, size, shape and morphology of the solid particles are important because they can affect the solubility as well as bioavailability of the drug particles.

Keywords: Nanoparticles, Bioavailability, Aptamer, Targeted drug delivery system

ABSTRACT

Controlled release of drug from micrometrics is of the particular therapeutic importance for oral medication in patients. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. One such approach is using microparticles as carriers for drugs. The idea behind a controlled drug delivery system is to incorporate the drug within a polymeric carrier that controls the release rate of the drug. Various processes, such as diffusion, erosion, and/or swelling can be involved in the control of the overall drug release rate, resulting in a broad spectrum of possible release profiles. Solvent evaporation and extraction based processes are required for the preparation of microparticles. The microparticles show lower percentage compressibility but good flowability, hence a capsule dosage form was thought to be suitable. The microparticle formulation was optimized with respect to size distribution and increased drug loading. The microparticles was physically evaluated with respect to bulk density, angle of repose, and percent compressibility, drug content, swelling study and in-vitro release study. Polyvinyl alcohol is proposed as a polymer to be used for the present controlled release formulation development. The intent of the paper is to highlight the potential of microparticles as a vital dosage form in novel drug delivery.

Key words: Microparticles, Sustain release, Solvent evaporation, Release profile, Therapeutic range, Compressibility

ABSTRACT

Now a days as very few drugs are coming out of research and development and already existing drugs are suffering the problem of resistance due to their irrational use specifically in case of drugs like antibiotics. Hence, change in the operation is a suitable and optimized way to make the some drug more effective by slight alteration in the drug delivery. An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target sites. The development of oral controlled release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. Matrix type drug delivery systems are an interesting and promising option when developing an oral controlled release system. This review focuses on the progress made in the design of controlled release dosage forms employing various types of matrices as carriers for the active ingredients.

Key Words: Controlled drug delivery, Matrices, Oral controlled release system, Matrix tablets.

ABSTRACT

Beta-blockers are the first line drugs in lowering the elevated and normal intraocular pressure associated with neuropathy of glaucoma, but for many reasons the use of this group of drugs requires supportive medications. The systemic side effects due to overdose of these drugs leads to pathetic complications in patients suffering with cardiac and pulmonary diseases. This article provides necessary information for the safe use of beta-blockers with detailed information about the disease glaucoma. Recent advances in the glaucoma therapy with beta-blockers and novel drug delivery systems developed are reviewed in this study.

Key words: Glaucoma, beta-blockers, intraocular pressure, Timolol, Levobunolol

ABSTRACT

Coatings are an essential part in the formulation of pharmaceutical dosage form to achieve superior aesthetic quality (e.g., color, texture, mouth feel, and taste masking), physical and chemical protection for the drugs in the dosage forms, and modification of drug release characteristics. Most film coatings are applied as aqueous- or organic-based polymer solutions. Solventless coatings are the alternative coating technologies for solid pharmaceutical dosage forms in which coating materials are directly coated onto solid dosage forms without using any solvent and then cured by various methods to form a coat. As a result, these technologies can overcome the disadvantages which are caused by solvents in conventional liquid coating. This review discusses and compares six solventless coating methods - Compression coating, Powder / dry coating, Hot-melt coating, Supercritical fluid spray coating, Magnetically Assisted Impaction Coating’ (MAIC), Solventless photo curable coating that can be used to coat the pharmaceutical dosage forms. Powder coating also called as dry coating which include plasticizer-dry coating, electrostatic-dry-coating, heat-dry-coating and plasticizer-electrostatic-heat-dry-coating. This review summarizes the fundamental principles and coating processes of various solventless coating technologies.

Keywords: Solventless, Photo curable, Impaction, Supercritical

ABSTRACT

Triazine is the chemical species of six-membered heterocyclic ring compound with three nitrogens replacing carbon-hydrogen units in the benzene ring structure. The names of the three isomers indicate which of the carbon-hydrogen units on the benzene ring position of the molecule have been replaced by nitrogens, called 1,2,3-triazine, 1,2,4-triazine, and 1,3,5-triazine respectively. Symmetrical 1, 3, 5-triazine is the common.  Triazines are prepared from cyanic acid amide by trimerization (1, 3, 5-triazine). Pyridine is the aromatic nitrogen heterocyclic compound having only one nitrogen, and diazines are with 2 nitrogen atoms, triazine having three nitrogen and tetrazines are with 4 nitrogen atoms on the benzene ring system. Triazines are weak base. Triazines have much weaker resonance energy than benzene, so nucleophilic substitution is preferred than electrophilic substitution. Heterocyclic bearing a symmetrical s-triazines or 1, 3, 5-triazines moieties, represent an interesting class of compounds possessing a wide spectrum of biological activities such as anti-cancer, antiviral, fungicidal, insecticidal, bactericidal, herbicidal and antimicrobial, antimalarial agents. They also find applications as dyes, lubricants and analytical reagents.

Key words: Triazine, Nucleophilic substitution, Cyanuric chloride, 1, 3, 5-triazine, s- Triazine

ABSTRACT

The whole-plant, Pergularia daemia (Family: Asclepediaceae), extract (50% alcohol) was investigated for phytochemical, physico-chemical parameters and its anti-inflammatory activity. Preliminary organic analysis revealed the presence of alkaloids, flavonoid, steroid, triterpenoid and phenolic compounds in the extract. Physiochemical studies revealed that total ash is 13.62%, acid insoluble ash is 1%, alcohol soluble extractive value is 17.6%, water soluble extractive value is 30.4% and loss on drying at 105°C is 10.6%.  The anti-inflammatory activity was evaluated using carrageenan-induced paw edema (acute inflammation) and chronic models like; cotton pellet granuloma and carrageenan air pouch granuloma. Oral administration of the extract (50 and 100 mg/kg) exhibited significant anti-inflammatory activity in acute and chronic models (p < 0.01) of inflammation. In conclusion, present investigation established specific identities that will be useful in identification and authentication of the raw drug and pharmacological evidences to support the folklore claim that P. daemia is used as anti-inflammatory agent.

Key words: Pergularia daemia, physicochemical, carrageenan, cotton-pallet

ABSTRACT

The aim of this study was to evaluate the bioequivalence of test and reference losartan potassium 50 mg formulations in healthy volunteers. This open label, balanced, single-dose, randomized, 2-period, crossover oral bioequivalence study was conducted in 54 healthy human adult subjects under fasting condition. Subjects received losartan 50 mg of either test or reference formulation with a washout period of 7 days. After study drug administration, serial blood samples were collected over a period of 48 hours. The plasma concentrations of losartan and its active metabolite were determined by a validated method using LC/MS/MS. Pharmacokinetic parameters C_max, T_max, t_1/2, AUC_0-t, AUC _0-∞, and k_el, were determined for both the  formulations. The formulations were to be considered bioequivalent if the log-transformed ratios of C_max, AUC_0-t, and AUC_0-∞ were within the predetermined bioequivalence range of 80% to 125%. A total of 54 subjects were enrolled. No significant differences were found based on analysis of variance.  The mean values and 90% confidence intervals (CI) of test/reference ratios for these parameters of losartan as follows: C_max 274.90 Vs 286.93 ng/mL (83.95 -113.69); AUC_0-t 434.67 Vs 438.68 ng.hr/mL (93.30 -104.03); and AUC_0-∞ 463.23 Vs 464.71 ng.hr/mL (94.65 -104.80) and for its active metabolite (losartan carboxylic acid) the mean values and 90% CI of test/reference ratios for these parameters  as follows: C_max 572.63 Vs 543.82 ng/mL (96.87-109.37); AUC_0-t 3987.89 Vs 4051.07 ng.hr/mL (93.48-104.22); and AUC_0-∞ 4215.58 Vs 4271.67 ng.hr/mL (94.84-105.26). This study shows that the test formulation is bioequivalent to the reference formulation for losartan and its main active metabolite.

Key Words: Bioequivalence, Losartan, losartan carboxylic acid, Pharmacokinetics.

ABSTRACT

The task of developing immediate release tablet is accomplished by using a suitable diluents and super-disintegrants. Faster disintegration of the tablet administrated orally minimizes absorption time and improves its bioavailability in less time. Immediate Release tablet of Antibiotic drug is formulated using dry granulation using super disintegrant croscarmellose sodium. Azithromycin is Antibiotic drug is used to treat STDs due to Chlamydia and gonorrhea, community-acquired pneumonia, pelvic inflammatory disease, pediatric otitis media and pharyngitis, and Mycobacterium avium complex (MAC) in patients with advanced HIV disease. One of the important studies included in the present investigation is of study on process parameter effect on performance of the Immediate Release tablets. The effect of selected process parameters on critical properties of immediate release (IR) tablets were studied, like effect of disintegration time, friability, dissolution profile.

Key words: Immediate release, Azithromycin, Croscarmellose sodium

ABSTRACT

The current study was undertaken to investigate the effect of the avipattikar churna against experimental gastric ulcers. Pretreatment of aqueous extract of churna at the dose of 540 mg/kg, for seven days was studied against ethanol-induced gastric mucosal damage. The aqueous extract showed significant reduction in gastric ulceration against ethanol-induced gastric mucosal damage. The results were comparable with omeprazole (reference standard). In the ethanol-induced gastric ulcer model, treatment with both the aqueous extract and omeprazole showed significant antioxidant activity as evident from the reduction in the extent of lipid peroxidation that was measured in terms of malondialdehyde (MDA), when compared with the control group. Pretreatment of aqueous extract of churna for 7 days in 6-h pylorus-ligated animals, showed significant reduction in the ulcer index. Furthermore, in the pylorus  ligation model, significant reduction (p<0.05) was observed in total acidity, total acid output, pepsin activity, and pepsin output, along with a significant rise in the total carbohydrate to protein ratio (reflecting mucin activity) when compared with the control group. The mechanism of its antiulcer activity could be attributed to a decrease in gastric acid secretory and antioxidant activities leading to gastric cytoprotection. The ulceroprotective activity of aqueous extract of Avipattikar churna could be mediated through its antioxidant activity, vasodilatation, and gastric cytoprotection.

Keywords: Cytoprotective, Antioxidant activity, stress ulcer, gastric ulcer, avipattikar churna

ABSTRACT

Any agent, which increases DNA damage or cell proliferation, can cause increased rate of mutation also increase the probability of cancer. A mutagen is considered an agent capable of destroying the integrity of hereditary mechanism of the cell or organism. Majority of known cancer causing agents are mutagens. The rate of tumor evolution and progression is accelerated by mutagenic agents. Mutation is now a day’s increase in human being. Here screening of in vitro anti-mutagenic activity of selected plants Spheranthus indicus, Asteracantha longifolia, Jateorhiza palmata, Mucuna Pruriens, Tecomella undulate, Picrorhiza kurroa, Grewia tiliifolia, Myristica fragrans, Oroxylum indicum, Gymnosporia montana were investigated. The activity was assayed by Ames Salmonella mutagenicity test using histidine mutants of Salmonella typhimurium tester strains, MTCC 98, MTCC 1251 and MTCC 1252. The hydroalcoholic extract of the plants significantly inhibited (P < 0.001) the in vitro by direct mutagens sodium azide (NaN3), 4-nitro-o-phenylenediamine (NPD), and indirect mutagens benzo[a]pyrene (B[a]P) 2-aminoflourene(2-AF) induced his  revertants in adose dependent manner. The results indicated that the hydroalcoholic extract of Spheranthus indicus occurring in India possessed significant antimutagenic activity.

Keywords: In-vitro, Anti-mutagenic, Salmonella typhimurium, mutagens

ABSTRACT

Present research work was focused to enhance bioavailability and reduce the short half life problem of Furosemide by preparation of sustained release microcapsule. Cellulose acetate microcapsules were prepared by co-acervation phase separation technique and phase separation was induced using distilled water. Prepared microcapsules were evaluated for Particle Size Analysis, Flow properties i.e. Angle of Repose Carr’s Index and Hauser’s Ratio, Scanning Electron Microscopy, Coating Wall Thickness, Drug Content and Microencapsulation efficiency, Dissolution studies. All the studies were performed in triplicate and standard deviation was calculated.

Key Words: Furosemide, Microcapsules, co-acervation phase separation technique.

ABSTRACT

In the present research a simple, accurate, precise and cost effective UV-Vis spectrophotometric method for the estimation of Clobazam, in bulk and pharmaceutical dosage form was illustrated. The absorption maxima of the drug was found to be 230 nm in methanol: water (1:1). A linear response was observed in the range of 6- 16 µg/ml with a regression coefficient of 0.999. Validation parameters were carried out as per the guidelines of International Conference for Harmonization. This method can be used in the industries for determination of Clobazam to analyze the quality of formulation without interference of the excipients.

Key words: Clobazam, Anti-epileptic, λmax, ICH, UV-Vis spectroscopy.

ABSTRACT

A simple, sensitive and accurate spectrophotometric method was developed in ultraviolet region for the estimation of Clopidogrel bisulfate in pure drug, pharmaceutical formulation. Linear response obtained was in the concentration range of 25-50 µg/ml with correlation coefficient of 0.999 in 0.1 N HCl. Excellent recovery proved that the method was sufficiently accurate. There is no interference from any common pharmaceutical additives and diluents. Results of the analysis were validated by recovery studies according to ICH Q2B guidelines.

Keywords: Clopidogrel bisulfate, UV- Spectrophotometry, recovery, accuracy.

ABSTRACT

Two simple and sensitive visible spectrophotometric methods (A and B) have been developed for the quantitative estimation of Pioglitazone, in bulk drug and pharmaceutical dosage forms. Methods were based on the formation of Pale yellow coloured and green coloured chromo gens, which were measured 267 nm and 297 nm, respectively. The results obtained with the proposed methods are in good agreement with the labeled amounts when tablet dosage forms were analyzed.  For the first method, UV-spectrophotometry, standard solutions were measured at 267 nm. The first method was linear from 2.5-20 mg/mL. The second method was based on the formation of an ion association complex with Methyl orange (MO) and Bromocresol Green (BCG).The assay was found to be linear over the concentration range of 2.5-20 µg/mL. The wavelengths were selected dependent on the maximum obtained values. The formation of ion- pairs are formed between secondary amino group of PIO and MO, BCG reagents via the protonated nitrogen atom. The proposed methods were validated according to the ICH guidelines (1996) with respect to specificity, linearity, accuracy, precise and robustness. The results demonstrated that the procedure is accurate, precise, specific and reproducible (percent relative standard deviation <2%), while being simple and less time consuming. The two methods have been successfully applied to the assay of Pioglitazone.

Key words: Antidiabetic, PIO, BCG, MO, UV-spectroscopy, Validation, Ion pair

ABSTRACT

The present research has been undertaken with the aim to formulate and evaluate the herbal gel containing Calophyllum inophyllum extract. The gel formulation was designed by using methanol extract of Calophyllum inophyllum stem barks in concentration (5%) and evaluated using physiological measurements. The gel was prepared by using accurately weighted amount of drug along with other additives were poured into the fixed amount of hydrated Carbopol-934 dispersion with constant stirring. Finally the required amount of 0.5M sodium hydroxide solution was added to induce gelation. All the prepared gel formulations were subjected for preliminary evaluation such as pH, Viscosity and Rheological studies, Spreadability, Drug content uniformity, Skin irritation test, In vitro diffusion study, In vitro permeation studies, Drug Polymer Compatibility Studies. The optimized herbal gel formulation of the drug was subjected to accelerated stability studies at both 4⁰C and 37⁰C for about 3 months. A suitable UV method was developed for herbal gel formulation by using Phosphate buffer 6.8 as solvent and l_max found to be 284 nm. The pH of all the formulations was in the range of 6.63 to 7.35, which lies in the normal pH range of the skin. The drug content was in the range of 96.6 to 99.5 %. The formulations did not produce any skin irritation, i.e., erythema and edema for about a week, when applied over the skin. The drug interaction FT-IR studies indicated that there was no chemical interaction between the drug and the polymers used in gel formulations.

Key Words: Calophyllum inophyllum, Methanolic extract, Herbal gel formulations, Carbopol 934, pH, Phosphate buffer.

ABSTRACT

Solid dispersion is a widely accepted technique for enhancing the dissolution rate of poorly soluble BCS class II drugs. In the present study starch phosphate- a new modified starch, PVP and PEG 4000 were evaluated as a carriers in solid dispersions for enhancing the dissolution rate and efficiency of nimesulide, a BCS class II drug. Their individual and combined (interaction) effects in enhancing the dissolution rate and dissolution efficiency of nimesulide were evaluated in a 2³- factorial study. Among the individual effects PEG 4000 gave highest enhancement in the dissolution rate of nimesulide (14.23 fold), followed by starch phosphate (11.34 fold). Addition of PVP and PEG 4000 to the solid dispersions in starch phosphate has further enhanced the dissolution rate upto 75.70 fold and dissolution efficiency upto 26.67 fold.

Key words: Solid dispersions, Nimesulide, Starch Phosphate, PVP, PEG 4000, Factorial Study.

ABSTRACT

A novel, simple, selective and rugged quantitative method for the determination of Fenofibric acid the active metabolite of fenofibrate  in human plasma (Na₂EDTA) using liquid chromatography-tandem mass spectrometric (LC-MS/MS) method has been developed and validated with 200µL human plasma. Fenofibric acid-d₆ was used as an internal standard. Analyte and the internal standards were extracted from human plasma by liquid-liquid extraction using Methyl tertiary butyl ether as extraction solvent and ammonium acetate (5mM, pH 2.5) as extraction buffer. The reconstituted samples were chromatographed on a C18 column by using isocratic mobile phase. The method was validated over the concentration range of 79.89–20021.87 ng/mL. The Quattro Premier XE mass spectrometer was operated under the multiple reaction-monitoring mode (MRM) using the electro spray ionization technique for quantification of ion transitions at m/z 317.06/231.00 and 323.24/231.04 for the drug and the internal standard respectively. The method was validated for precision and accuracy, stability, matrix effect, dilution integrity, ruggedness, selectivity and extraction efficiency, and method has been proved to be simple, sensitive, selective, rugged and reproducible. A run time of 2.00 min for each sample made it possible to analyze more than 400 plasma samples per day. The proposed method can be applied for the estimation of the Fenofibric acid in real time plasma samples for pharmacokinetic, drug-drug interaction and toxicological studies.

Key words: Fenofibric acid, Validation, Human Plasma, LC-MS/MS, Electrospray ionization.

ABSTRACT

First and second order derivative UV-Spectrophotometric methods have been developed and validated for the estimation of Iloperidone in bulk and its tablet formulations. The solutions of standard and sample were prepared in methanol. The Iloperidone solution was showed the maximum absorbance at 262nm and 248nm for the first and second order UV-Spectrophotometric methods respectively. Beer’s law was obeyed in the concentration range of 4- 12 μg / ml with r² value 0.999 for both the methods. These methods were tested and validated for various parameters according to ICH guidelines. The precision expressed as relative standard deviation and was found within the range of 0.13 % to 1.7 % for the both methods. Limit of detection was 0.0133 μg/ml (first order), 0.0216 μg/ml (second order) and  limit of quantification was found to be 0.0403 μg/ml (first order), 0.0657 μg/ml (second order). Recovery of Iloperidone was found to be within the range of 99.51 – 100.16 % for the two methods. The proposed methods were successfully applied for the determination of Iloperidone in tablet formulations. In addition, the proposed methods are simple, easy to apply, low cost, and requires relatively inexpensive instruments.

Keywords: Iloperidone, Method Validation, Derivative UV-Spectrophotometric methods.

ABSTRACT

Hemin degradation by various thiols including cysteine, homocysteine, N-acetylcysteine, glutamyl-cysteinyl-alanine, mercaptoethanol and dithiothreitol, and also the effect of transition metal ions like cobalt(II), copper(II), manganese(II), zinc(II), chromium(III), iron(II) and iron(III) on this degradation have been investigated. Glutathione (GSH) and other thiols have successfully degraded hemin.  Metals like Cobalt(II), Copper(II), Chromium(III) and iron(II) inhibited GSH mediated hemin degradation. However this inhibition was marginally reversed by the addition of metal chelators and diethylenetriaminepentaacetic acid (DTPA). Manganese(II) and zinc(II) were increased the degradation but the DTPA abolished this increase. Iron(III) had no effect on GSH mediated degradation but co-incubation with DTPA resulted a remarkable inhibition. The effect of cobalt(II), manganese(II), Fe(II) and Fe(III) on hemin degradation by homocysteine, dithiothreitol and glutamyl-cysteinyl-alanine showed differences vis-à-vis GSH. In conclusion the results indicate that thiols other than GSH should also be explored for their protective effect on hemin-mediated membrane destabilization by virtue of their hemin degrading ability.

Key Words : Hemin, glutathione, thiols, transition metal ions, RBC membranes.

ABSTRACT

Mucoadhesive delivery systems were proven to be suitable for the purpose of reduction of transit time of the dosage form through the gastro-intestinal tract, and increasing bioavailability of drug. Buccal tablets of Carvedilol were prepared by direct compression method for using various compositions of combination of Starch: C934 and Starch: HPMCK15M in various ratios. The tablets were evaluated for their characteristics properties, mucoadhesion and in vitro-in-vivo study. All the physicochemical properties were acceptable within the limit. Formulation containing starch and Carbopol 934(E4) showed better bioavailability as compared to tablet containing  Starch and HPMCK15 (F5) and The bioadhesive strength of the formulations containing polymers were in the order of E4> F5. Stability studies were carried out as per ICH guidelines and formulations were found to be Stable.

Keywords: Bioadhesive, Buccal tablets, Bioavailability, Bioadhesion, Polymers

ABSTRACT

The aim of the present study was to prepare and characterize twice-daily sustained-release matrix tablets of Timolol maleate (TM) using different concentrations of hydrophilic Hydroxypropylmethylcellulose (HPMC K100M CR) alone and its combination with hydrophobic ethyl cellulose (EC). Formulations prepared by the wet granulation technique and were evaluated for the release of TM over a period of 12 hours using United States Pharmacopoeia (USP) type-II dissolution apparatus. Along with physical properties, the dynamics of water uptake and erosion degree of tablets were also studied. The in-vitro drug release study revealed that formulation F3 (40% wt/wt HPMC K100M) could extend the drug release up to 8 hours. The most successful formulation of the study, F5 (HPMC to EC, 1:1), extended the drug release up to 12 hours, exhibited satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile. The drug release from optimized formulation (F5) followed first-order kinetics via Non-Fickian (anomalous) diffusion. FTIR studies revealed that there was no interaction between the drug and excipients. In conclusion, the results indicated that the prepared sustained-release tablets of TM could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance.

Key words: Timolol maleate; Matrix tablets; Sustained-release; Ethyl cellulose; Hydroxypropylmethylcellulose; In-vitro drug release.

ABSTRACT

A simple, specific, accurate and precise reverse phase high performance liquid chromatographic method was developed for simultaneous estimation of diazepam and propranolol hydrochloride in pharmaceutical tablet formulation. The separation was achieved on Phenomenex C₁₈ column (250 mm i.d., 4.6 mm, 5 µm particle size) using methanol: acetonitrile: water (50 : 25 : 25, v/v/v, pH adjusted to 2.8 ± 0.05 with ortho- phosphoric acid) as the mobile phase at a flow rate of 1.0 ml min^-1. The quantification was achieved with PDA detector at 235 nm. The injection volume was 20 µl. The retention times of diazepam and propranolol hydrochloride were 5.38 ± 0.29 min and 3.80 ± 0.15 min, respectively. The method was validated for linearity, precision, specificity, robustness and recovery according to the ICH guidelines. The linearity was obtained in the concentration range of 0.1-5.0 µg/ml for both drugs with mean recovery of 100.3 ± 0.47 and 100.2 ± 0.78 % for diazepam and propranolol hydrochloride, respectively. The limit of detection and quantification for diazepam were 0.015 and 0.050 µg/ml, respectively and for propranolol hydrochloride were 0.014 and 0.045 µg/ml, respectively. The method was found to be simple and highly sensitive and can be useful in the routine quality control of diazepam and propranolol hydrochloride in bulk manufacturing and pharmaceutical dosage forms.

Key words: Diazepam, propranolol hydrochloride, RP-HPLC, validation, simultaneous, tablet

ABSTRACT

The present research work aimed at development and optimization of niosome based gel (NBG) for the vaginal delivery of Tenofovir disoproxil fumarate (TDF). The TDF was   incorporated into niosomes using span 60 and cholesterol. Box-Behnken statistical screening design with 3 factors, 3 levels, and 15 runs was selected to statistically optimize the formulation parameters. The independent variables selected were parts of cholesterol (X₁), surfactant loading (X₂), amount of stabilizer (X₃). Fifteen batches were prepared by thin film hydration method and evaluated for percentage drug entrapment (PDE) and vesicle size. The transformed values of the independent variables and the PDE (dependent variable) were subjected to multiple regressions to establish a full-model second-order polynomial equation. F value was calculated to confirm the omission of insignificant terms from the full-model equation to derive a reduced-model polynomial equation to predict the PDE of niosome. A model was validated for accurate prediction of the PDE by performing checkpoint analysis. The niosomal dispersion was incorporated in to Carbopol 940NF gel. The NGB was evaluated for drug content, pH, spreadability, consistency and texture analysis. The in-vitro drug release study shows sustained release gel effect whereas the in-vivo study shows no signs of irritation on the applied vaginal site in rat. The gel was kept for 6 weeks accelerated stability studies. The niosomes and niosomal gel showed maximum stability at 2 to 8 °C.

Key-words: Niosome, vaginal drug delivery, Tenofovir disoproxil fumarate, span 60, Box Behnken design

ABSTRACT

Itraconazole, a poorly water soluble antimycotic agent, is promising agent for various diseases. To improve the solubility of itraconazole, the inclusion compound of Itraconazole with β-cyclodextrin was prepared by spray drying, solvent evaporation, kneading, lyophilization, physical mixture method and characterized by solubility, scanning electron microscopy, differential scanning calorimetry, FTIR and dissolution study. DSC and FTIR confirmed the formation of complex. The solubility of the prepared complex was found to be improved. Itraconazole complex by spray drying method and Itraconazole showed 95.65 % and 80.55% of drug release at the end of 48 h in dissolution study. It was concluded that the complex of itraconazole may be of potential use for improving the solubility of itraconazole and hence its bioavaibility.

Keywords: Itraconazole, β cyclodextrin, inclusion compound, Antimycotic.

ABSTRACT

Matrix tablets of Indomethacin were prepared by wet granulation method. Guar gum as a carrier, 10% starch paste, HPMC, citric acid and the mixture of talc and magnesium stearate at 2:1 ratio were used. Coating was carried out by using 10% Eudragit L 100. All the prepared formulations were evaluated for hardness, drug content uniformity, stability study and were subjected to in vitro drug release studies in rat caecal contents. The highest in vitro dissolution profile at the end of 24 h was shown by IF6 followed by IF7, IF8. The other formulation IF4, IF3, IF2 and IF1 were failed to target in colon and these formulation releases the majority of drug within 10 h of study. It may be due to the less proportion of guar gum to retard the drug release.  The colon targeted matrix tablet of Indomethacin showed no change either in physical appearance, drug content or in dissolution pattern after storage at 30˚ C/ 65±5 % RH for 2 months.

Key words: Colon targeted, Eudragit L-100, Guar gum, Indomethacin, Matrix tablets, Rat caecal content.

ABSTRACT

A novel mucoadhesive, thermoresponsive vaginal gel for microbicide was developed with gelation temperature 24-35 °C. Poloxamer 407 (P407) or: and poloxamer 188 (P188) were used to confer the temperature-sensitive gelation property. The mixtures of P407 (15%) and P188 (15–20%) existed as a liquid at room temperature, but gelled at 30–36°C. To modulate the gel strength and the bioadhesive force of Ciclopirox olamine gel, mucoadhesive polymer such as polyox WSR N-60K was used. Among bioadhesive polymers, polyox polymer enhanced gel strength most efficiently. These polymers reinforced the bioadhesive forces 4-7 fold compared to P407/P188 (15:15) alone and 3-6 fold compared to P407/P188 (15:20) alone. Differential scanning calorimetry (DSC) was employed to investigate the effect of poloxamer gel on the conformational changes of rat vaginal membrane. The in-situ gelling liquid with polyox polymer inserted into the vagina of women without difficulty and leakage and retained in the vagina at least 6-8 h. These results suggest that in situ-gelling and mucoadhesive vaginal microbicide gel for women can be further developed as a more convenient and effective vaginal dosage form for treating sexually transmitted disease.

Key-words: Mucoadhesion, Vaginal drug delivery, Polyox polymers, Microbicide, Sexually transmitted disease, Conformational change

ABSTRACT

The present manuscript describe simple, sensitive, rapid, accurate, precise and economical first derivative spectrophotometric method for the simultaneous determination of nebivolol and hydrochlorothiazide in combined tablet dosage form. The derivative spectrophotometric method was based on the determination of both the drugs at their respective zero crossing point (ZCP). The first order derivative spectra were obtained in methanol and the determinations were made at 270.5 nm (ZCP of hydrochlorothiazide) for nebivolol and 282.5 nm (ZCP of nebivolol) for hydrochlorothiazide. The linearity was obtained in the concentration range of 5-100 μg/ml for nebivolol and 2-14 μg/ml for hydrochlorothiazide. The mean recovery was 100.04 + 0.93 and 99.87 + 1.16 for nebivolol and hydrochlorothiazide, respectively. The method was found to be simple, sensitive, accurate and precise and was applicable for the simultaneous determination of nebivolol and hydrochlorothiazide in pharmaceutical tablet dosage form. The results of analysis have been validated statistically and by recovery studies.  

Key words: Nebivolol, hydrochlorothiazide, recovery, first order derivative spectrophotometric method, tablet, validation.

ABSTRACT

Formulation and characterization of an ophthalmic delivery system of an antibacterial agent, ofloxacin, based on the concept of pH triggered in situ gelation. Polyacrylic acid (Carbopol 974P) was used as the gelling agent in combination with Noveon^® AA-1 USP Polycarbophil as a viscosity enhancer. Formulation optimization was carried out using a 3² full factorial design. The effect of independent variables was evaluated using dependent variables such as gel strength, bioadhesive force, viscosity and in vitro drug release of the formulation. The multiple regression analysis of the results led to equations that adequately describe the influence of the independent variables on the selected responses. Polynomial regression equations and surface plots were used to relate the dependent and independent variables. Furthermore, the desirability function was employed in order to determine the best batch which was then evaluated for in vivo antimicrobial efficacy study, effect of sterilization, ocular irritation study and accelerated stability study. It was found that the optimum values of the responses for pH triggered in situ ophthalmic gel formulation could be obtained at medium levels of Carbopol 974P and Noveon^® AA-1 USP Polycarbophil (0.5/0.5%w/w respectively). The formulation retained antimicrobial efficacy, showed insignificant effect over sterilization and found non irritant to the corneal surface confirmed by microscopy of the corneal mucosal membrane compared with reference marketed formulation. The optimized formulation was found to be stable, therapeutically efficacious and providing sustained release of the drug over an 8 h period even after accelerated stability study over three months. The developed system is thus a viable alternative to conventional ophthalmic formulations.

Key words: In situ gelation; Factorial design; Desirability function; Carbopol 974P;Noveon^® AA-1 USP Polycarbophil; Ofloxacin