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S. P. Mahaparale ¹, I. D. Gonjari ², K. N. Jayaveera ³

Affiliations
1 Padm. Dr. D. Y. Patil College of Pharmacy, Sector No. 29, Pradhikaran, Near ZSI Building, Akurdi, Pune - 411 044, Maharashtra, IN
2 Government College of Pharmacy, Vidyanagar, Karad - 415 124, Maharashtra, IN
3 Jawaharlal Nehru Technological University, Anantapur - 515 002, Andhra Pradesh, IN

Abstract

The present paper describes simple, rapid, reproducible, accurate and precise stability indicating HPLC method developed for quantitative simultaneous estimation of metoprolol succinate and olmesartan medoxomil in bulk and combined pharmaceutical dosage form. A chromatographic separation of both drugs was achieved with Chromasil 250 × 4.6 mm, i.d 5 μm C-18 column using methanol:0.05% v/v Ophosphoric acid in water (50:50 v/v) at the flow rate of 1ml/min. The measurements were made at 228.0 nm as detector wavelength. The described method showed excellent linearity over a range of 5-80 μg/ml for metoprolol succinate and 5-70 μg/ml for olmesartan medoxomil. The coefficient of correlation for metoprolol succinate and olmesartan medoxomil was found to be 0.9990 and 0.9993 respectively. The retention time for metoprolol succinate and olmesartan medoxomil was found to be 3.485 min and 7.085 min, respectively. The tailing factor for metoprolol succinate and olmesartan medoxomil was found to be 1.02 and 1.13 respectively. Both drugs and their combination drug product were found to be stable in neutral, thermal, oxidative and photolytic stress conditions but mild degradation was observed in acidic and alkaline conditions.

Keywords

Metoprolol Succinate, Olmesartan Medoxomil, HPLC Method Validation, Stability-Indicating Method, ICH Guidelines.

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T. S. Vaseeha Banu ¹, K. V. Sandhya ², K. N. Jayaveera ³

Affiliations
1 Department of Pharmaceutics, M.M.U College of Pharmacy, K.K. Doddi, Ramanagara- 562159. Karnataka, IN
2 Department of Pharmaceutics, T. John College of Pharmacy, Bannerghatta Road, Bangalore- 560083. Karnataka, IN
3 Jawaharlal Nehru Technological University Anantapuramu, Anantapuramu- 515002, Andhra Pradesh, IN

Abstract

Lercanidipine Hydrochloride (LH) is a calcium channel blocker used to treat hypertension along with chronic stable angina related to myocardial ischemia characterised by chest discomfort rather than actual pain. The main goal of the treatment of stable angina pectoris is to control symptoms, slow progression of the disease and reduction of major cardiovascular events. In our present investigation an attempt has been made to formulate transdermal drug delivery system of LH to treat angina pectoris. Transdermal films of LH have been formulated by solvent casting technique using three different polymers hydroxy propyl methyl cellulose (HPMC), ethyl cellulose (EC) and polyvinyl pyrrolidine (PVP) (blend ratios viz; 0.5:1.5, 1:1 and 1.5:0.5% w/v), of varying degrees of hydrophilicity and hydrophobicity. Propylene glycol (PG 30% w/w) and dimethyl sulfoxide (DMSO 7% w/w) was incorporated as plasticizer and permeation enhancer respectively. The prepared films were evaluated for various physicochemical parameters and ex-vivo drug release through rat abdominal skin using Franz diffusion cell. The patch containing combination of HPMC:PVP shown maximum water vapour transmission rate, % moisture absorption and % moisture loss, which could be attributed to the hydrophilic nature of both the polymers. Ex-vivo data revealed that the released pattern from all the patches followed zero order; moreover it was sustained and extended over a period of 24 hours in all formulations. F7 emerged as the most satisfactory formulation by permeating drug upto 88.94%. Further the best formulation F7 was subjected to skin irritation studies, the results revealed that the F7 has no erythema and oedema.

Keywords

Antianginal Drug, DMSO, PVP, HPMC, EC.

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T. S. Vaseeha Banu ¹, K. V. Sandhya ², K. N. Jayaveera ³

Affiliations
1 Department of Pharmaceutics, M.M.U College of Pharmacy, K.K. Doddi, Ramanagara- 562159. Karnataka, IN
2 Department of Pharmaceutics, T. John College of Pharmacy, Bannerghatta Road, Bangalore- 560083. Karnataka, IN
3 Department of Chemistry, Jawaharlal Nehru Technological University Anantapur, Anantapur- 515002, Andhra Pradesh, IN

Abstract

The human skin is one of the most readily accessible organ/surface of the human body for drug delivery. Skin of an average adult body covers a surface of approximately 2 m2 and receives about one-third of the blood circulating through the body. Today about 74% of drugs taken orally are not effective as desired. Transdermal drug delivery system has emerged as an effective delivery system to improve such characters. Transdermal Drug Delivery System (TDDS) is the system in which the delivery of the drug occurs by the means of skin and deliver specific dose of the medicine (drug) into the bloodstream over a period of time. This includes high bioavailability, absence of first pass hepatic metabolism effect, steady drug plasma concentration, and the fact that therapy is non-invasive and also reduces dosing frequency.

This review article covers a brief outline of TDDS, its advantages over conventional dosage forms, drug delivery routes across human skin, penetration enhancers, the principles of transdermal permeation, various components of transdermal patch, types of Transdermal patches, approaches of transdermal patch, its application with its limitation with relevant examples, when these are used and when their use should be avoided.

Keywords

Transdermal Drug Delivery System, Skin Penetration, Transdermal Patches.

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V. Sreenivasulu ¹, K. N. Jayaveera ², P. Mallikarjuna Rao ³

Affiliations
1 Dept. of Biotechnology, KLR Pharmacy College, Paloncha-507115, Khammam- District, A.P, IN
2 Oil Technological Research Institute, JNT University, Anantapur–15001, A.P, IN
3 International Medical University, Kualalumpur, -57000, MY

Abstract

Production of L-asparaginase employing Aspergillus sp. VEM-9 under solid-state fermentation was optimized. Different substrates like rice bran, green gram bran, wheat rawa, wheat bran, Bombay rawa, black gram bran, barley, saw dust, jowar flour, rice flour, castor oil cake, ground nut oil cake, coconut oil cake, sesame oil cake were studied to optimize the best substrate. Groundnut oil cake showed the highest enzyme yield. Different physical fermentation factors were optimized. The maximum productivity of L-asparaginase (60 U/gds) was achieved by employing groundnut oil cake and optimized process parameters including incubation period of 5 days, initial moisture content of solid substrate 90%, 1: 10 (v/w) ratio of salt solution to weight of groundnut oil cake, inoculum level 20%(v/w), incubation temperature at 30°C and initial pH 6.5.

Keywords

L-Asparaginase, Aspergillus sp. VEM-9, Groundnut Oil Cake, Optimization, Solid-State Fermentation.

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V. Sreenivasulu ¹, K. N. Jayaveera ², P. Mallikarjuna Rao ³

Affiliations
1 Dept. of Biotechnology, KLR Pharmacy College, Paloncha-507115,Khammam- District, A.P, IN
2 Oil Technological Research Institute, JNT University, Anantapur–15001, A.P, IN
3 International Medical University, Kualalumpur, 57000, MY

Abstract

The extracellular L-asparaginase production by fungi isolated from soil samples by using pH and dye based method. Various physical and chemical parameters were optimized under submerged fermentation for Lasparaginase production. Maximum productivity of L-asparaginase (19.5 U/ml) was achieved by employing medium containing 2% (w/v) Lasparagine as substrate concentration, 1%(w/v) glucose as carbon source, 1% (w/v) ammonium sulphate as an additional nitrogen source with the incubation period of 96 h and incubation temperature at 30°C, initial pH 6.5 at an inoculum level 20% (v/v) with 48 h old inoculum was found to be optimum for maximum yield.

Keywords

L-Asparaginase, Optimization and Submerged Fermentation.

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G. Parthasarathy ¹, K. Bhaskar Reddy ², K. N. Jayaveera ³

Affiliations
1 Department of Pharmaceutics, R.R College of Pharmacy, Chikkabanavara, Bangalore-560 090, KA, IN
2 Sri Venkateswara College of Pharmacy, Chittoor- 517 127, AP, IN
3 Department of Chemistry, JNTUA, Anantapur- 515 001, AP, IN

Abstract

The delivery of drug through buccal mucosa provides potential advantages like prevention of enzymatic degradation in gastro intestinal tract and bypassing hepatic first-pass metabolism. However the significant aspect in transbuccal drug delivery is the very restrictive passage of drug through the buccal mucosa. In our earlier work we confirmed the ability of Carbamazepine (CBZ) to permeate through the porcine buccal mucosa. Our earlier study proved that CBZ crosses the membrane by passive diffusion. But the measured Flux (J_s) and permeation coefficient (K_p) of CBZ was s p insufficient to achieve plasma therapeutic concentration. In this study an approach was made to improve permeability of CBZ using some bile salts as chemical permeation enhancers like sodium taurocholate (STC) and sodium taurodeoxycholate (STDC) which are capable to lessening the barrier property of the mucosal tissue. These patches were subjected to ex vivo permeation studies. The six buccal patches of CBZ selected from our earlier reported formulations were subjected to this permeability improvement study. These patches were either based on HPMC K15M or Carbopol 934p or Chitosan in combination of PVA or PVP K30 or Sodium alginate. The significant change in J_s and K_p of formulations in presence and absence of chemical permeation enhancers STC or STDC (in two different p concentrations 0.1% and 0.5 % w/w) was evaluated by ex vivo permeation studies through porcine buccal mucosa under modified Franz diffusion cell. The calculated value of Flux (J_s) and Permeation coefficient (K_p) confirmed that s there was a significant increase in permeated amount of CBZ after the inclusion of permeation enhancers. The compatibility of bile salts with buccal mucosa was examined by histological studies and kinetic studies.

Keywords

Carbamazepine, Buccal Patch, Permeation Enhancer, Bile Salt.

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B. S. Ashok Kumar ¹, K. Lakshman ², K. N. Jayaveera ³, N. Vamshi Krishna ¹, M. Manjunath ⁴, M. V. Suresh ⁴, Shivatej ⁵, Hanumantha Reddy ⁵, Sudheer Naik ⁵

Affiliations
1 Department of Pharmacognosy, Sri K.V. College of Pharmacy, Chikkaballapur, Karnataka, IN
2 Department of Pharmacognosy, PES College of Pharmacy, Bengaluru, Karnataka, IN
3 Department of Chemistry, Jawaharlal Nehru Technological University, Anantapur, Andhra Pradesh, IN
4 Department of Pharmacognosy, Rural College of Pharmacy, Devanahalli, Karnataka, IN
5 Department of Pharmacognosy, Sri Krishna Chaithanya College of Pharmacy, Madanapalle, Andhra Pradesh, IN

Abstract

Tannins and Flavonoids present in the Terminalia chebula, Flavonoids like Rutin and quercetin possess many biochemical effects like inhibition of enzymes, regulatory role on different hormones and pharmacological activities like antimicrobial, antioxidant, anticancer, antihepatotoxic, protection of cardio vascular system. An HPLC method was developed for the estimation of rutin and quercetin from methanol methanolic extract of Terminalia chebula.

Keywords

Terminalia chebula, Rutin, Quercetin, HPTLC, Standardization.

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K. C. Panda ¹, A. V. Reddy ², N. Panda ², M. D. Shamim ², M. Habibuddin ³, K. N. Jayaveera ⁴

Affiliations
1 JNTUA, Ananthapuramu, Andhra Pradesh, IN
2 Anwarul Uloom College of Pharmacy, New Mallepally, Hyderabad, Telangana., IN
3 Adept Pharma and Bioscience Excellence, Balanagar, RR Dist., Telangana, IN
4 VEMU Institute of Technology, P. Kothakota, Chittoor, Andhra Pradesh, IN

Abstract

Vilazodone is approved for treatment of acute episodes of major depression (Major Depressive Disorder (MDD). It is a BCS Class - II drug, offer challenges in developing a drug product with adequate bioavailability. The aim of present investigation was to formulate and evaluate vilazodone sublingual tablets using poloxamer 407 as a carrier by lyophilized solid dispersion technique.The lyophilized solid dispersion of vilazodone prepared by poloxamer 407 (1:5) showed more than 85% drug release within 5 min, so it was used for the development of sublingual tablets by direct compression technique. The physicochemical, solid-state properties, dissolution behaviour of lyophilized solid dispersion as well as sublingual tablets were evaluated. Finally, the bioavailability studies of the prepared tablets were performed by sublingual administration to rabbits. The sublingual tablets showed a higher in vitrodis solution rate and bioavailability compared with the commercial tablets. It is evident from the results herein that the developed sublingual tablets provide a promising drug delivery system in drug development, owing to their excellent performance of a rapid onset of action and improved bioavailability.

Keywords

Vilazodone, Lyophilization, Sublingual, Dissolution.

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