DESIGN AND STATISTICAL OPTIMIZATION OF A BILAYERED TABLET OF METOPROLOL SUCCINATE SUSTAINED RELEASE AND ATORVASTATIN CALCIUM IMMEDIATE RELEASE: ONCE A DAY FORMULATION IN THE MANAGEMENT OF HYPERTENSION

 Objective: The current study involves the fabrication of oral bilayer matrix designs of a combination of two drugs, metoprolol succinate and atorvastatin calcium, the optimization of their in vitro release and characterization using the design expert software. Metoprolol succinate, a β1- selective adrenergic receptor blocking agent, is used in the management of hypertension has a half-life of approximately 4–5 h; thus, there is the need to use extended-release formulation for prolonged action. Atorvastatin is a hydroxymethylglutaryl-coenzyme A reductase inhibitor, an antilipidemic, used to lower blood cholesterol. The rationale for this fixed-dose combination is to coadminister two drugs acting by different mechanisms of action together, reduce dosing frequency, and increase patient compliance.Methods: A 32 factorial design was selected to analyze the effect of critical factors, polymer concentration of Kollidon sustained release (SR), and Eudragit RS and their interaction on the in vitro release of the SR part containing metoprolol succinate. The drug release at 2 h (Q2), 8 h (Q8), and 20 h (Q20) was taken as responses. The blends of both layers were prepared, evaluated for precompression characteristics, and compressed by direct compression. The compressed bilayer tablets were evaluated for their hardness, weight variation, friability, content uniformity, diameter, and in vitro release.Result and Conclusion: The release profile indicates Higuchi's kinetics. Contour and surface response plots show significant interaction among the formulation variables. Formulation MS06 containing 70 mg Kollidon SR and 10 mg Eurdragit RS was found to be the optimized formulation, controlling the drug release for a 24 h period

FORMULATION DEVELOPMENT AND STATISTICAL OPTIMIZATION OF A BILAYER TABLET OF BOSENTAN MONOHYDRATE AND SILDENAFIL CITRATE IN MANAGEMENT OF PULMONARY ARTERIAL HYPERTENSION

Objective: The current study aims at fabrication of an oral bilayer matrix tablet of bosentan monohydrate and sildenafil citrate; the optimisation of their in vitro release and characterization, thereby reducing the side effects associated with bosentan, reducing dosing frequency and increasing patient compliance in the management of pulmonary arterial hypertension. Methods: Methocel K4M Premium DC2, a directly compressible HPMC grade was used as the sustained release polymer. Pregelatinised starch is used as a diluent and release modifier and sodium lauryl sulphate (SLS) as a solubiliser. The blends of both layers were prepared, evaluated for precompression characteristics and compressed by direct compression. The compressed bilayer tablets were evaluated for their hardness, weight variation, friability, content uniformity and swelling index. The principle objective was to assess the influence of the above variables on in vitro drug release of Bosentan using a 23 factorial design. Responses are measured as drug release at 2h (Q2), 6h (Q6) and 10h (Q10). Results: HPMC and pregelatinized starch form a synergistic gel thereby controlling drug release of bosentan for a 12 hour period. Batch BS09 consisting of 40 mg HPMC, 30 mg Pregeletinized starch and 5 mg SLS showed adequate controlled release for a 12 h period. Immediate release layer of sildenafil citrate showed optimum drug release of 102.96% within 30 min. Conclusion: Bilayer tablet of bosentan and sildenafil is an ideal combination for patients failing monotherapy in pulmonary arterial hypertension

SYNTHESIS OF 4-HYDROXY-3-(1-HYDROXY-2-(SUBSTITUTEDAMINO)ETHYL)-1-PHENYL/ METHYL QUINOLIN-2(1H)-ONE AS ANTICANCER AGENTS

  Objective: The current work is concerned with the synthesis of a series of 4-hydroxy-3-(1-hydroxy-2-(substituted amino)ethyl)-1-phenyl/ methylquinolin-2(1H)-one[III-a(1-5)/III-b(1-5)] and evaluation of its in vitro anticancer activity.Methods: The starting material for linomide analogs was synthesized by following literature procedures. The carbonyl group was reduced to hydroxyl group using sodium borohydride, and the methyl group was brominated using bromine in acetic acid. Further bromine was nucleophilically substituted by primary amines. All the synthesized compounds were satisfactorily characterized by infrared, nuclear magnetic resonance, and mass spectral data. The synthesized compounds were tested for in vitro anticancer activity against MDA-MB cell line using the MTT assay method.Results: Among all the synthesized compounds, compound [III-a1;R=C6H5,R1=n-propylamine], [III-b1;R=CH3,R1=n-propylamine], and [III-b2;R=CH3,R1=methylamine] were found to be most cytotoxic with IC50 value=25 μg against the MDA-MB cell line.Conclusion: The results of screening studies concluded that compounds with (C6H5 at C1) and (long chain aliphatic and cyclic amines at C3) position of quinolin-2-one ring showed moderate activity

Design and Optimization of a Polyethylene Oxide-Based Matrix Tablet of Metoprolol Succinate Using Design Expert Software

Hypertension is a common lifestyle disorder, the prevalence of which advances with age. In the case of antihypertensive therapy, patient compliance is hampered, especially in geriatric patients, if the dose is b.i.d or more, as it is difficult for the patient to remember and take medicine at a scheduled time. The present study involves the fabrication of a sustained-release matrixdesigned tablet using a combination of polyethylene oxide (PEO) polymers and metoprolol succinate as the model drug. The tablet is optimized and evaluated for its in-vitro release using the Design expert software. Polyethylene oxide is a non-ionic hydrophilic polymer which is directly compressible. Polyox WSR 301 and 303 grades have been used in the study to get the desired sustained release of 12 h. The formulations were analysed for various pre-compression and post-compression characteristics. The polymers Polyox WSR 301 and 303 influence drug release are measured using a 32 factorial design where the concentration of drug released at various time points has been analysed statistically as a response. Response surface plots demonstrate and depict the effect of the variables, thus aiding in optimization. All the formulated batches exhibited acceptable pre and post-compression characteristics. The optimized formulation M05 showed a sustained drug release up to a 12 h period. Thus polyethylene oxide can be used as an excellent sustained-release matrix polymer due to its ability to gel and prolong drug release from a matrix. Due to their molecular weight, a combination of two grades of polyethylene oxide helps reinforce the drug release. </jats:p

DESIGN AND STATISTICAL OPTIMIZATION OF A BILAYERED TABLET OF METOPROLOL SUCCINATE SUSTAINED RELEASE AND ATORVASTATIN CALCIUM IMMEDIATE RELEASE: ONCE A DAY FORMULATION IN THE MANAGEMENT OF HYPERTENSION

 Objective: The current study involves the fabrication of oral bilayer matrix designs of a combination of two drugs, metoprolol succinate and atorvastatin calcium, the optimization of their in vitro release and characterization using the design expert software. Metoprolol succinate, a β1- selective adrenergic receptor blocking agent, is used in the management of hypertension has a half-life of approximately 4–5 h; thus, there is the need to use extended-release formulation for prolonged action. Atorvastatin is a hydroxymethylglutaryl-coenzyme A reductase inhibitor, an antilipidemic, used to lower blood cholesterol. The rationale for this fixed-dose combination is to coadminister two drugs acting by different mechanisms of action together, reduce dosing frequency, and increase patient compliance.Methods: A 32 factorial design was selected to analyze the effect of critical factors, polymer concentration of Kollidon sustained release (SR), and Eudragit RS and their interaction on the in vitro release of the SR part containing metoprolol succinate. The drug release at 2 h (Q2), 8 h (Q8), and 20 h (Q20) was taken as responses. The blends of both layers were prepared, evaluated for precompression characteristics, and compressed by direct compression. The compressed bilayer tablets were evaluated for their hardness, weight variation, friability, content uniformity, diameter, and in vitro release.Result and Conclusion: The release profile indicates Higuchi's kinetics. Contour and surface response plots show significant interaction among the formulation variables. Formulation MS06 containing 70 mg Kollidon SR and 10 mg Eurdragit RS was found to be the optimized formulation, controlling the drug release for a 24 h period

A Review of Antiulcer Activity of Some Medicinal Plants: A Review of Antiulcer Activity of Some Medicinal Plants.

Peptic ulcer is a gastrointestinal disorder and with increased prevalence. Peptic ulcer is breaking of endothelial lining of stomach and exposing underlying tissues. Peptic ulcer occurs due to high secretion of acid and reduced defensive factors in stomach and duodenum. It is imbalance between aggressive and defensive factors. Non-steroidal anti-inflammatory drugs and Helicobacter pylori infection also increases the risk of peptic ulcer. Indiscriminate use of synthetic drugs leads to adverse effects and concomitant use of antibiotics potentiates drug-drug interaction thus search of drugs from natural sources especially herbs is need of hour. several herbal medicines have been evaluated for its antiulcer efficacy using several ulcer inducing models in laboratory animals. Present study aims at review of gastroprotective and ulcer healing potential medicinal herbs and compilation of data. This article is only restricted to antiulcer efficacy of the medicinal plants. This review presents information about the anti-ulcer efficacy of medicinal plants and various antiulcer models used to screen them. Keywords: Peptic ulcer, Gastric ulcer, Gastroprotective activity, Phyllanthus urinaria, Adiantum lunulatum, Ulcer healing activit

FORMULATION DEVELOPMENT AND STATISTICAL OPTIMIZATION OF A BILAYER TABLET OF BOSENTAN MONOHYDRATE AND SILDENAFIL CITRATE IN MANAGEMENT OF PULMONARY ARTERIAL HYPERTENSION

Objective: The current study aims at fabrication of an oral bilayer matrix tablet of bosentan monohydrate and sildenafil citrate; the optimisation of their in vitro release and characterization, thereby reducing the side effects associated with bosentan, reducing dosing frequency and increasing patient compliance in the management of pulmonary arterial hypertension.&#x0D; Methods: Methocel K4M Premium DC2, a directly compressible HPMC grade was used as the sustained release polymer. Pregelatinised starch is used as a diluent and release modifier and sodium lauryl sulphate (SLS) as a solubiliser. The blends of both layers were prepared, evaluated for precompression characteristics and compressed by direct compression. The compressed bilayer tablets were evaluated for their hardness, weight variation, friability, content uniformity and swelling index. The principle objective was to assess the influence of the above variables on in vitro drug release of Bosentan using a 23 factorial design. Responses are measured as drug release at 2h (Q2), 6h (Q6) and 10h (Q10).&#x0D; Results: HPMC and pregelatinized starch form a synergistic gel thereby controlling drug release of bosentan for a 12 hour period. Batch BS09 consisting of 40 mg HPMC, 30 mg Pregeletinized starch and 5 mg SLS showed adequate controlled release for a 12 h period. Immediate release layer of sildenafil citrate showed optimum drug release of 102.96% within 30 min.&#x0D; Conclusion: Bilayer tablet of bosentan and sildenafil is an ideal combination for patients failing monotherapy in pulmonary arterial hypertension.</jats:p

A Pharmacognostic, phytochemical and pharmacological review of Pterocarpus marsupium: Comprehensive Review

Research in herbal drug is need of the hour to find definite lead for discovery of medicine from plant source. Many traditional medicinal plants are under screening to scientifically reinforce their traditional claims. Pterocarpus marsupium is time tested important source of herbal medicine which has been used extensively for treatment of diabetes mellitus. It has also exhibited antimicrobial activity, analgesic activity, anticataract activity. Acute toxicity test determines safe dose of the Pterocarpus marsupium. Various extraction methods such as Infusion, Decoction, Maceration, Percolation and Hot Water Extraction s employed for efficient extraction of phytoconstituents. Primary phytoconstituents present in the bark comprises of liquiritigenin, isoliquiritigenin, pterosupin, epicatechin, and pterostilbene. Current review is carried out to study pharmacognstic, phytochemical and pharmacological activity of the drug, which can be useful for researcher to provide synoptic overview about Pterocarpus marsupium &nbsp; Keywords: Pterocarpus marsupium, Review, Fabaceae, Indian kino, Asa

SYNTHESIS OF 4-HYDROXY-3-(1-HYDROXY-2-(SUBSTITUTEDAMINO)ETHYL)-1-PHENYL/ METHYL QUINOLIN-2(1H)-ONE AS ANTICANCER AGENTS

  Objective: The current work is concerned with the synthesis of a series of 4-hydroxy-3-(1-hydroxy-2-(substituted amino)ethyl)-1-phenyl/ methylquinolin-2(1H)-one[III-a(1-5)/III-b(1-5)] and evaluation of its in vitro anticancer activity.Methods: The starting material for linomide analogs was synthesized by following literature procedures. The carbonyl group was reduced to hydroxyl group using sodium borohydride, and the methyl group was brominated using bromine in acetic acid. Further bromine was nucleophilically substituted by primary amines. All the synthesized compounds were satisfactorily characterized by infrared, nuclear magnetic resonance, and mass spectral data. The synthesized compounds were tested for in vitro anticancer activity against MDA-MB cell line using the MTT assay method.Results: Among all the synthesized compounds, compound [III-a1;R=C6H5,R1=n-propylamine], [III-b1;R=CH3,R1=n-propylamine], and [III-b2;R=CH3,R1=methylamine] were found to be most cytotoxic with IC50 value=25 μg against the MDA-MB cell line.Conclusion: The results of screening studies concluded that compounds with (C6H5 at C1) and (long chain aliphatic and cyclic amines at C3) position of quinolin-2-one ring showed moderate activity.</jats:p