Metformin Hydrochloride (MF) is glucose lowering agent that is widely used for management for type II diabetes. MF is reported to be absorbed mainly in upper part of GIT. It is having narrow absorption window and high water solubility, and it would be more beneficial to retain the drug in stomach for prolonged duration so as to achieve maximum absorption and better bioavailability. A conventional oral CR formulation releases most of the drug content at the colon, which requires that the drug will be absorbed from the colon. The present investigation is aimed to develop novel gastroretentive (GR) drug delivery system, which not only release the drug in the absorption window but also provides controlled release drug profile that may result patient compliance and therapeutic success. Floating tablets of MF was prepared using sodium alginate, and sodium carboxymethylcellulose was used as a gelling agent, and release modifiers, respectively. Eudragit NE 30 D was used as sustained release polymer to control the initial burst release. Drug and excipients compatibility studies were monitored by thermal analysis by using differential scanning calorimeter. 32 full factorial design was applied to optimize the formulation. The DSC thermogram of drug, polymer and physical mixtures revealed that there was no known interaction between drug and polymers. The prepared tablets were evaluated for in vitro dissolution, in vitro buoyancy, percentage swelling, percentage erosion and similarity factors with marketed tablets. The optimization study using a 32 full factorial design revealed that the amount of sodium alginate and sodium carboxymethylcellulose had a significant effect on t50, t90, Flag and f2. Thus, by selecting a suitable composition of release rate modifier and gel forming agent, Gastro retentive system can be developed with the desired dissolution profile. This study indicated that the MF GR tablets prepared using sodium alginate and sodium carboxymethylcellulose can successfully be employed as a once-a-day oral controlled release drug delivery system.

Drug development plays an important role in patient safety and effectiveness. The therapeutic suitability of a new drug depends on the solubility. The solubility of the sparingly soluble drug remains a problem in identifying new active compounds. Solubility plays an important role in achieving optimal drug concentration. Low solubility is not only a concern for the production of formulations, but also an obstacle from the outset when identifying active chemicals for therapeutic purposes. Due to its simplicity in terms of ease of administration and economy, the oral route is the preferred route of drug administration over other routes. Effective aqueous solubility is the first prerequisite for oral medication, since low solubility has poor absorption and bioavailability and unpredictable toxicity of the gastrointestinal mucosa. To avoid these crises, different methodologies are used to improve the solubility and bioavailability of poorly soluble drugs, and hydrotropic solubilization is one of them. Hydrotropic agents have the potential to improve the solubility of water-insoluble drugs. In this review, we try to address hydrotropic solubilization methodologies. Keywords: Hydrotropy, Micelles, Solubility, Formulation.

Gastric retention will provide advantages such as delivery of drugs with narrow absorption windows in the small intestinal region, namely proximal parts of the gastrointestinal tract (stomach and/or duodenum). Pharmaceutical dosage forms which remain in stomach for a prolonged period of time after oral administration and release the active ingredient in a controlled manner are important for the delivery of a wide variety of drugs (1-5).Metoprolol succinate (MS) is a b1-selective adrenergic blocking agent (6). Since the half-life of MS is~3 to 4 h (7), multiple doses are needed to maintain a constant plasma concentration for a good therapeutic response and improved patient compliance. It has also been reported that MS absorption mainly takes place in the duodenum and jejunum and is directly proportional to the dose available (8). A gastroretentive is particularly useful for drugs that are primarily absorbed in the duodenum and upper jejunum seg- Metoprolol succinate (MS) gastroretentive (GR) controlled release system was formulated to increase gastric residence time leading to improved drug bioavailability. Box-Behnken model was followed using novel combinations of sodium alginate (SA), sodium carboxymethylcellulose (NaCMC), magnesium alumino metasilicate (MAS) as independent variables. Floating lag time (Flag), t 25 , t 50 , t 75 , diffusion exponent as dependent variables revealed that the amount of SA, NaCMC and MAS have a significant effect (p < 0.05) on t 25 , t 50 , t 75 and Flag. MSGR tablets were prepared and evaluated for mass, thickness, hardness, friability, drug content and floating property. Tablets were studied for dissolution for 24 h and exhibited controlled release of MS with floating for 16 h. The release profile of the optimized batch MS01 fitted first--order kinetics (R 2 = 0.9868, n = 0.543), indicating non--Fickian diffusion or anomalous transport by diffusion and swelling.

The hypothesis of the present investigation was to develop adapalene (ADP), a high lipophilic, and low solubility anti-acne drug-loaded niosomal topical gel formulation in order to improve its therapeutic efficacy....