In situ forming formulation: development, evaluation, and optimization using 3(3) factorial design. 2009

Ramesh C Nagarwal, and A Srinatha, and Jayanta K Pandit
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi 221005, India.

The present investigation concerns with the development and optimization of an in situ forming formulation using 3(3) full factorial design experimentation. Metformin, an antidiabetic drug with upper part of gastrointestinal tract as absorption window was used as a model drug. The formulations were designed with an objective to retain in stomach for an extended time period. The effect of three independent factors--concentrations of sodium alginate (X(1)), gellan gum (X(2)), and metformin (X(3)) on in vitro drug release were used to characterize and optimize the formulation. Five dependent variables-release exponent (Y(1)), dissolution efficiency (Y(2)), drug release at 30 min (Y(3)), 210 min (Y(4)), and 480 min (Y(5)) were considered as optimization factors. The data were statistically analyzed using ANOVA, and a p < 0.05 was considered statistically significant. Three dimensional surface response plots were drawn to evaluate the interaction of independent variables on the chosen dependent variables. Of the prepared 27 formulations, the responses exhibited by batch F17 containing medium level sodium alginate (X(1)), low level gellan (X(2)), and medium level metformin (X(3)) were similar to the predicted responses.

UI MeSH Term Description Entries
D007004 Hypoglycemic Agents Substances which lower blood glucose levels. Antidiabetic,Antidiabetic Agent,Antidiabetic Drug,Antidiabetics,Antihyperglycemic,Antihyperglycemic Agent,Hypoglycemic,Hypoglycemic Agent,Hypoglycemic Drug,Antidiabetic Agents,Antidiabetic Drugs,Antihyperglycemic Agents,Antihyperglycemics,Hypoglycemic Drugs,Hypoglycemic Effect,Hypoglycemic Effects,Hypoglycemics,Agent, Antidiabetic,Agent, Antihyperglycemic,Agent, Hypoglycemic,Agents, Antidiabetic,Agents, Antihyperglycemic,Agents, Hypoglycemic,Drug, Antidiabetic,Drug, Hypoglycemic,Drugs, Antidiabetic,Drugs, Hypoglycemic,Effect, Hypoglycemic,Effects, Hypoglycemic
D008687 Metformin A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289) Dimethylguanylguanidine,Dimethylbiguanidine,Glucophage,Metformin HCl,Metformin Hydrochloride,HCl, Metformin,Hydrochloride, Metformin
D011135 Polysaccharides, Bacterial Polysaccharides found in bacteria and in capsules thereof. Bacterial Polysaccharides
D002119 Calcium Carbonate Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement. Aragonite,Calcite,Chalk,Limestone,Marble,Milk of Calcium,Vaterite,Calcium Milk,Carbonate, Calcium
D002626 Chemistry, Pharmaceutical Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use. Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D005079 Excipients Usually inert substances added to a prescription in order to provide suitable consistency to the dosage form. These include binders, matrix, base or diluent in pills, tablets, creams, salves, etc. Excipient,Stabilizing Agent,Stabilizing Agents,Suspending Agent,Suspending Agents,Agent, Stabilizing,Agent, Suspending,Agents, Stabilizing,Agents, Suspending
D000464 Alginates Salts and esters of ALGINIC ACID that are used as HYDROGELS; DENTAL IMPRESSION MATERIALS, and as absorbent materials for surgical dressings (BANDAGES, HYDROCOLLOID). They are also used to manufacture MICROSPHERES and NANOPARTICLES for DIAGNOSTIC REAGENT KITS and DRUG DELIVERY SYSTEMS. Alginate,Alginic Acid, Barium Salt,Alginic Acid, Calcium Salt,Alginic Acid, Copper Salt,Alginic Acid, Potassium Salt,Alginic Acid, Sodium Salt,Alloid G,Barium Alginate,Calcium Alginate,Calginat,Copper Alginate,Kalrostat,Kalrostat 2,Kaltostat,Potassium Alginate,Sodium Alginate,Sodium Calcium Alginate,Vocoloid,Xantalgin,poly(Mannuronic Acid), Sodium Salt,Alginate, Barium,Alginate, Calcium,Alginate, Copper,Alginate, Potassium,Alginate, Sodium,Alginate, Sodium Calcium,Calcium Alginate, Sodium
D000465 Algorithms A procedure consisting of a sequence of algebraic formulas and/or logical steps to calculate or determine a given task. Algorithm
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D015233 Models, Statistical Statistical formulations or analyses which, when applied to data and found to fit the data, are then used to verify the assumptions and parameters used in the analysis. Examples of statistical models are the linear model, binomial model, polynomial model, two-parameter model, etc. Probabilistic Models,Statistical Models,Two-Parameter Models,Model, Statistical,Models, Binomial,Models, Polynomial,Statistical Model,Binomial Model,Binomial Models,Model, Binomial,Model, Polynomial,Model, Probabilistic,Model, Two-Parameter,Models, Probabilistic,Models, Two-Parameter,Polynomial Model,Polynomial Models,Probabilistic Model,Two Parameter Models,Two-Parameter Model

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