1. | FORMULATION DEVELOPMENT OF AQUEOUS INJECTION OF A POORLY WATER-SOLUBLE DRUG (HYDROCHLOROTHIAZIDE) USING MIXED SOLVENCY CONCEPT AND ITS EVALUATION |
| Himanshi Gupta* and R.K. Maheshwari |
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In this current era of pharmaceutical research, maximum newly invented drugs are found to be very poorly soluble in water. It poses difficulties in various developmental, manufacturing and administrating processes, which lead to the high failure of clinical trials of the drug due to poor pharmacokinetics. Parenteral dosage form could be expected to be an effective tool for avoiding the oral side effects and also achieving maximum bioavailability. Poor solubility of drugs in water is currently the biggest challenge and limitation in injectable formulation developments. The prime purpose of any research work should be highly efficient and most effective in the pharmaceutics field to serve the society’s needs by developing a formulation after literature survey and market review. The ultimate objective of this present research was to promote the use of mixed solvency concept by formulating the aqueous injection of the poorly water soluble drug and to decrease the concentration of individual solubilizers required to produce a substantial increase in solubility and thereby resulting in expected synergistic enhancement of solubility of the drug in water. In the present work, poorly water-soluble drug, hydrochlorothiazide was selected and its aqueous injection was formulated. Hydrochlorothiazide is a thiazide diuretic often considered a prototype member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This leads to increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several diseases including edema, hypertension, diabetes insipidus, and hypoparathyroidism. (BCS class II: highly permeable and low soluble). Due to the poor water solubility of hydrochlorothiazide, the products are available in the market in tablet form. In order to get expected synergistic enhancement on solubility, various blends of solubilizers can be tried thereby reducing the amount of individual solubilizer employed to achieve the desired solubility enhancement ratio. Thus, the successful completion of the research work will enable the preparation of stable aqueous injection of hydrochlorothiazide. Keywords: Mixed solvency concept, Hydrochlorothiazide, Solubility Enhancement, injection.
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2. | CURCUMIN DRUG DELIVERY SYSTEM |
| Sonali P. Mahaparale, Apoorva P. Bauskar |
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Curcumin (diferuloylmethane) is the natural polyphenolic compound. It is bioactive and major phenolic component of turmeric. It is derived from the rhizomes of the plant ‘Curcuma longa’ Linn of family Zingiberaceae. It is water-insoluble and has potent anticancer, anti-inflammatory, and antioxidant activities. Besides this it also plays significant and pleiotropic role in cardiovascular diseases, Alzheimer’s disease, and other neuromuscular diseases. It controls inflammation, oxidative stress, cell secretion, cell survival, homeostasis, and proliferation. The clinical implication of curcumin is hindered as due to low solubility, physicochemical instability, and poor bioavailability, rapid metabolism, and poor pharmacokinetics. These issues can be overcome by utilizing efficient delivery systems. A number of formulations exist that can be translated toward medicinal use upon successful completion of pre-clinical and human clinical trials. Nano-systems can deliver the active constituents at sufficient concentration directing it to desired site of action. In this article a brief overview of different drug delivery systems of curcumin and their recent advances have been discussed.
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3. | YNTHESIS AND ANTI- BACTERIAL ACTIVITY OF NOVEL ISONIAZIDYL SCHIFF BASE DERIVATIVES |
| Kencha Swathi*, Nivedhitha N, Dilraj E |
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Synthesis of novel derivatives of N -Benzylidene benzohydrazide Schiff bases (Isoniazidyl Schiff bases) has been done
by using hydrolysis reaction which involves one step synthesis. Schiff bases are Synthesized by using Isoniazid and different
aldehydes like vanillin, anisaldehyde, benzaldehyde. The aqueous solution of isoniazid is added to a warm solution of
aldehydes in water, after 15 min, by hydrolysis reaction the Schiff bases will form in the mixture. The yield is good for the
products. Recrystallization was done to obtain pure crystals. The newly synthesized compounds were characterized by melting
point, TLC, and IR spectra. The synthesized compounds were evaluated for antibacterial activity by agar diffusion method. All
the compounds were screened for their antibacterial activity against Staphylococcus aureus (Gram positive bacteria) and E.coli
(Gram-negative bacteria).Compounds showed significant anti-bacterial activity against both gram +ve and gram-ve, but less
effective than the standard, amoxicillin.
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4. | IN SILICO DESIGN, BASE CATALYSED SYNTHESIS OF 2-CHLORO- 5-FLUORO (4, 5-DIPYRIMIDINE) 2-AMINE |
| M. T. Mohite1, K. V. Chandgude, N. Krishna and V.V. Dudhabale |
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Tuberculosis remains the second leading cause of death from an infectious disease globally, despite the incessant efforts
to control it. Research and development into new TB medicine is imperative for effective TB control, however new strategies
for the rational use of existing drug such as finding the binding affinity between drug and target by molecular docking could
also significantly enhance this process. The base catalyzed study of synthesis of 2-chloro-5-flouro-(4,5-Bipyrimidine )2’-amine
to improve the yields and economically viable industrialization process from its biological active pyrimidine derivative of 5-
fluorouracil.In this study, the designed compounds were docked with receptors such as protease, Reverse Transcriptase and
Vascular Endothelial Growth Factor by using Mcule Docking. Among these Reverse Transcriptase shows good binding affinity
with compound on the basis of docking score.
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5. | LIQUID CHROMATOGRAPHY TANDEM MASS SPECTROMETRYMETHOD FOR ESTIMATION OF ROFLUMILAST IN HUMAN PLASMA |
| I. Ahmed, l. Thomas, S. Kumar, S. Reddy, A. Mukhopadhyay and S. Thangam |
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Roflumilast was estimated by LCMS/MS in presence roflumilast N-oxide. LLE method was used for sample
preparation. A gradient (solution A: 2 mM ammonium acetate and solution B:acetonitrile) was used to elute the sample from a
C8 column. Flow rate was maintained as 1.0 – 1.5 mL/min. Roflumilast D4 was used as an internal standard. The analysis was
performed on LCMS/MS API 4000 using positive atmospheric pressure ionization mode. MRM transitions were monitored for
roflumilast as m/z 402.9? 187.0 (fragment 1) and m/z 402.9? 241.1 (fragment 2). A linear response was observed over the
concentration ranges 75.70pg/mL to 16149.46pg/mL. The intra-day and inter-day precisions were within 14.0%. The assay
accuracy was 81.0 –105.0%. Mean recovery was 62.80% (3.30%). The limit of detection was 18.94pg/mL. This LC–MS/MS
method for determination of roflumilast in human plasma is relatively simple, fast, sensitive and specific. This method is also
cost effective and can be successfully used in a bioequivalence study
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