Adinarayana Gorajana

Preparation and characterization of cefuroxime axetil solid dispersions using hydrophilic carriers

Aim: The objective of the current study is to increase the dissolution rate of cefuroxime axetil (CA) by formation of binary CA solid dispersion using water soluble carriers such as polyvinylpyrrolidone (PVP K30) and polyethylene glycol (PEG 4000). Methods: Solid dispersions (SDs) between CA and PVP K30/PEG 4000 were formed by dissolving both compounds in a common solvent, methanol, which were rotary evaporated at 40°C for 12 h. Physical mixtures between CA and PVP K30/PEG 4000 were also formulated as to compare the efficiency of SDs. The physicochemical properties of CA and all its formulations were then characterized using differential scanning calorimetric analysis (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR). Results: All SD formulations were found to have a higher dissolution rate comparatively to pure CA, while only physical mixtures of PVP K30 were found having a significantly higher dissolution rate. The enhancement of dissolution rate SD by PVP K30 may be caused by increase wettability, solubility, reduction in particle size or the formation of CA β crystalline. Increment of dissolution rate of CA SDs by PEG 4000 similarly may be caused by increase wettability, solubility, and reduction in particle size. This phenomenon may also be caused by amorphization as suggested by DSC and PXRD. Conclusions: The SD of CA with PVP K30 and PEG 4000, lends an ample credence for better therapeutic efficacy.

Preparation and in vitro characterization of non-effervescent floating drug delivery system of poorly soluble drug, carvedilol phosphate

Abstract The objective of the study was to enhance the solubility of carvedilol phosphate and to formulate it into non-effervescent floating tablets using swellable polymers. Solid dispersions (SD) of carvedilol were prepared with hydrophilic carriers such as polyvinylpyrrolidone and poloxamer to enhance solubility. Non-effervescent floating tablets were prepared with a combination of optimized solid dispersions and release retarding polymers/swellable polymers such as xanthan gum and polyethylene oxide. Tablets were evaluated for physicochemical properties such as hardness, thickness and buoyancy. SD prepared with the drug to poloxamer ratio of 1:4 by melt granulation showed a higher dissolution rate than all other dispersions. Formulations containing 40 mg of polyethylene oxide (C-P40) and 50 mg xanthan gum (C-X50) were found to be best, with the drug retardation up to 12 hours. Optimized formulations were characterized using FTIR and DSC and no drug and excipient interactions were detected.

Anti-Inflammatory, Antibacterial and Analgesic Potential of Cocos Nucifera Linn.: A Review

At present, approximately 25%of drugs in modern pharmacopoeia are derived from plant sources (phytomedicines) that can be developed for the treatment of diseases and disorders. Many other drugs are synthetic analogues built on the prototype compounds isolated from plants. Cocos nucifera Linn. (Arecaceae), which is commonly known as coconut, is a plant possessing a lot of potential as an ingredient in traditional medicines for the treatment of metabolic disorders and particularly as an anti-inflammatory, antimicrobial and analgesic agent. This review emphasizes on the recent literature and research findings that highlight the significant biological activities of C. nucifera Linn. such as its anti-inflammatory, antimicrobial and analgesic properties. This review can help researchers keen on exploiting the therapeutic potential of C. nucifera Linn. which may motivate them to further explore their commercial viability.

Preparation, Characterization, and In Vitro Evaluation of Nitrendipine Solid Dispersions

In order to enhance the absorption of dissolution rate of nitrendipine (NIT), solid dispersions were prepared using two water soluble carriers, polyvinylpyrrolidone K30 (PVP K30) and polyethylene glycol 4000 (PEG-4000), by solvent and fusion method. The dissolution profile of solid dispersions were compared to the pure drug in both pH 1.2 hydrochloric acid and pH 6.8 phosphate buffer and the results have shown profound improvement in drug release. The solubility of solid dispersion was increased by several folds when compared to pure NIT. The physicochemical properties of the solid dispersions were examined using analytical techniques. The results of microscopic studies, x-ray powder diffraction (XRPD), and differential scanning calorimetric (DSC) analysis confirmed the amorphous state of solid dispersion in comparison to the crystalline nature of pure drug, proposing that NIT was molecularly dispersed in the polymer matrices, which were accounted for by dissolution rate enhancement. Fourier transform infrared (FTIR) spectroscopic analysis indicated the presence of hydrogen bonding between NIT and the polymers, which also explained the improvement in solubility and dissolution rate. In conclusion, solid dispersion of NIT with PVP K30 and PEG-4000 improved the solubility and rate of dissolution, which may improve the absorption of the drug and subsequently the bioavailability of NIT.

Characterization and Solubility Study of Norfloxacin-Polyethylene Glycol, Polyvinylpyrrolidone and Carbopol 974p Solid Dispersions

OBJECTIVE Norfloxacin has a low aqueous solubility which leads to poor dissolution. Keeping this fact in mind the purpose of the present study is to formulate and evaluate norfloxacin solid dispersion. METHODS Solid dispersions were prepared using hydrophilic carriers like polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974pNF (CP) in various ratios using solvent evaporation technique. These formulations were evaluated using solubility studies, dissolution studies; Fourier transmitted infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetery (DSC). The influence of polymer type and drug to polymer ratio on the solubility and dissolution rate of norfloxacin was also evaluated. RESULTS FTIR analysis showed no interaction of all three polymers with norfloxacin. The results from XRD and DSC analyses of the solid dispersion preparations showed that norfloxacin existsin its amorphous form. Among the Norfloxacin: PEG solid dispersions, Norfloxacin: PEG 1:14 ratio showed the highest dissolution rate at pH 6.8. For norfloxacin: PVP solid dispersions, norfloxacin: PVP 1:10 ratio showed the highest dissolution rate at pH 6.8. For Norfloxacin: CP solid dispersions, norfloxacin: P 1:2 ratio showed the highest dissolution rate at pH 6.8. CONCLUSION The solid dispersion of norfloxacin with polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974p NF (CP), lends an ample credence for better therapeutic efficacy.

Preparation, Physicochemical Evaluation and Antimicrobial Potential of Topical Dosage Forms Containing Natural Anti-inflammatory Agent, Curcuma longa

In an attempt for better treatment of bacterial infections and burn wounds various topical formulations containing 1%w/w of Curcuma longa were prepared and evaluated for physical appearance, pH, rheological properties and stability studies. Antimicrobial activity of prepared formulations was found to be more effective against various strains of bacteria. Carbopol gel base is the most suitable dermatological base for Curcuma longa in comparison to various other dermatological bases. It also has aesthetic appeal, which other bases lack, an important aspect from patient compliance and consumer point of view. The therapeutic potential of such topical formulations may motivate researchers for its further exploitation so that it may be commercially viable. This innovative mode of formulation of Curcuma longa can be employed for enhancing the anti-microbial effect.

Cytotoxic compounds from a marine actinomycete, Streptomyces albovinaceus var. baredar AUBN 10 /2

Although the delayed-type hypersensitivity (DTH) skin reaction to tuberculin is used worldwide for tuberculosis (TB) detection, it has poor diagnostic specificity due to the presence of common antigens in tuberculin shared by many mycobacterial species. The problem is noticed, especially in countries where the Bacillus Calmette-Gue´rin (BCG) vaccination is widely practiced. Thus, a new skin test antigen specific for the diagnosis of Mycobacterium tuberculosis (MTB) infection is urgently needed. CFP-10, a mycobacterial secretary protein that is absent in Mycobacterium bovis BCG and most other mycobacterial species including Mycobacterium avium, Mycobacterium intracellulare, has been shown to elicit cellular immune responses in MTB infected individuals and can be a good candidate for MTB specific diagnosis. We prepared recombinant MTB CFP-10, rCFP-10, and its utility as specific antigen for TB diagnosis was evaluated by skin testing in guinea pigs sensitized with M . tuberculosis, M. bovis, and M. bovis BCG. Our results show that the purified MTB rCFP-10 antigen elicits a positive skin response only in the guinea pigs sensitized with M. tuberculosis and M. bovis , and not in the animals sensitized with M. bovis BCG vaccine. The data presented in this study supports further testing of the use rCFP-10 as the specific antigen in the skin test for the diagnosis of MTB infection in humans. Key words : Recombinant CFP-10 protein, skin test, delayed-type hypersensitivity, tuberculosis infection, Mycobacterium tuberculosis, Mycobacterium bovis, Bacillus Calmette-Gue´rin.

Development of a Validated HPLC Method for the Estimation of Metformin HCl and Propranolol HCl

The present investigation targets to develop a simple, specific, sensitive and accurate reverse phase high performance liquid chromatographic (RP-HPLC) method in human plasma for the estimation of metformin HCl and propranolol HCl from bulk drug and also from the marketed products. Human plasma samples were subjected to correct procedure for protein precipitation by methanol and protein free plasma samples were directly injected into HPLC C18 column. Chromatographic determination was performed on a reversed phase C18 column (3.9 mm X 300 mm, particle size 5 μm) using a mixture of acetonitrile and 0.1M pH 4.5 potassium dihydrogenortho phosphate buffer (mL) (40:60) at a flow rate of 0.8 mL/min and maintained at a pressure of 140 to 150 Kg/cm. The retention time for metformin HCl and propranolol HCl was found to be 9.084 min and 6.132 min respectively at 232 nm without any interference of endogenous compounds in Original Research Article British Journal of Pharmaceutical Research, 4(15): 1909-1922, 2014 1910 the plasma. The method was linear in the range between 50-2000 ng/mL. The peak areas were reproducible as indicated by low coefficient of variation. It was found that the excipients in the tablet dosage form do not interfere in the quantification of active drug by proposed method.

Evaluation of Topical Gels Containing Ketorolac Tromethamine on Inflammation and Hyperalgesia in Rats

Over recent years, non-steroidal anti-inflammatory drugs (NSAIDs) have been increasingly introduced as topical preparations as they are simple to apply and deliver high drug concentrations locally with limited side effects. Ketorolac trometamol (KT), a potent COX-2 inhibitor, produces typical side effects of NSAIDs when given orally and systemically. Hence the present investigation encompasses the development of topical formulations employing different dermatological bases and evaluated for its efficacy and safety. Standard procedures were followed to test the antiinflammatory and antihyperalgesic effects in male Wistar albino rats. Amongst the various semisolid formulations, the formulation containing hydroalcoholic carbopol gel base (KT1) was found to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation (79.69±1.51 after 5 h of carrageenan administration) as compared to formulation containing plain carbopol gel base (68.75±2.76) and PEG base 73.44±1.23. This demonstrates the suitability of carbopol gel base as an ideal dermatological base for ketorolac trometamol topical formulation and thus providing an ample credence for better therapeutic efficacy.