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The objective of the present study was to identify critical formulation parameters affecting the drug release from controlled porosity osmotic tablet of milnacipran hydrochloride. Most of the highly water-soluble drugs, if not formulated properly, may readily release the drug at a faster rate and are likely to produce undesirable side effects on oral administration. Controlled porosity osmotic tablets were developed in which the pores are formed by the incorporation of a leachable component in the coating. Once the tablet come in contact with the aqueous environment, the water-soluble component will dissolve and pores are generated. Subsequently, water diffuses into the core through the micro porous membrane, setting up an osmotic gradient and thereby controlling the release of drug. Ethocel was used as a release retarding agent in core tablet. The objective of using Ethocel was to explore the possibility of use of this type of release retardants for the development of the novel formulation of milnacipran HCl. Mannitol was used as osmogent in present study because mannitol is directly compressible and it exhibits good osmogenic property. Cellulose acetate is used as semi permeable membrane as a film former. Sorbitol was selected as pore former, because it is hydrophilic material. It is best suited with cellulose acetate as pore former. The presence of insoluble excipients such as Ethocel is desirable in the core for modulation of drug release. The amount of mannitol played a dominant role in controlling the drug release in the initial phase. Sorbitol created pores in the coat for smooth passage of drug solution. These can be considered as critical formulation parameters while going for optimization study. [ABSTRACT FROM AUTHOR]

Objective: In current exploration, systematic attempts have been made to improve the entrapment efficiency of a model hydrophilic drug substance, i.e. acyclovir, in poly (d, l) lactide (PLA) nanoparticles (NPs) using a modified nanoprecipitation technique. Methods: Formulation parameters such as drug to polymer ratio, antisolvent selection, electrolyte (NaCl) addition, pH alteration and temperature were screened to improve the entrapment efficiency of acyclovir in PLA NPs. The temperature of the system (0-5 °C), phase volume ratio (1:2), stirring speed (2000 rpm), sonication time (5 min), etc. were kept constant during the preparation of NPs. Drug to polymer ratio and electrolyte addition emerged as critical formulation parameters affecting particle size as well as entrapment efficiency. Hence, in the present investigation a 32 full factorial design was used to investigate the combined influence of two factors, i.e. drug to polymer ratio ( X1) and the amount of electrolyte, i.e. NaCl ( X2) on particle size ( Y1) and entrapment efficiency ( Y2). The NPs were also evaluated for drug-excipient compatibility study by employing DSC and FT-IR analysis, whereas in vitro drug release studies were performed using dialysis bag technique in phosphate buffer pH 7.4. Results: Statistically significant models were evolved to predict entrapment efficiency and particle size. The effect of factors X1, X2 and was found to be statistically significant in nature. Response variables, i.e. entrapment efficiency and particle size, were simultaneously optimized using desirability function using Design Expert software. This process allowed the selection of most suitable level of factors to achieve desired level of particle size and entrapment efficiency. The results of multiple linear regression analysis revealed that for obtaining desirable particle size (less than 250 nm) and entrapment efficiency (more than 17%), the NPs should be prepared using 1:3 drug to polymer ratio and 0.04 M NaCl. Acyclovir was found to be compatible with PLA as indicated by DSC and FT-IR studies. The experimental values obtained from the optimized formulation highly agreed with the predicted values. The drug release from the optimized formulation exhibited biphasic pattern and the drug release kinetics was best explained by Weibull model. Conclusion: In conclusion, results of the present study demonstrated that PLA NPs with expected particle size and entrapment efficiency can be obtained by adopting the concept of quality by design. [ABSTRACT FROM AUTHOR]

The aim of present work was to prepare pulsatile drug delivery system of metoprolol succinate. In the presnt work pulsatile drug delivery system was prepared by using swellable and rupturable polymer. The polymers like Ac-di-sol and crospovideone was selected as swellable polymer while ethyl cellulose was selected as rupturable polymer. In present work, core tablet (150 mg) containing 100 mg metoprolol succinate was prepared by wet granulation technique. This prepared core tablet was coat by using 2.5% ethyl cellulose containing triethyl citrate as plasticizer. This coating solution was sprayed to core tablet to achieve different percentage of weight gain into the core tablet. The prepared film coated tablet was evaluated for in vitro drug dissolution study to get desirable immediate release of drug after lag time of 6 hour. Initially, compatibility study was carried out by differential scanning calorimetric study showing that all the excipients were compatible with the drug substance. The stability study was carried out for desired optimized batch for period of one year. The result of stability study indicates insignificant difference between before and after storage of pulsatile formulation. [ABSTRACT FROM AUTHOR]

The objective of the present study was to obtain programmed drug delivery from hard gelatin capsules containing a hydrophilic plug (HPMC or guar gum). The significance of factors such as type of plug (powder or tablet), plug thickness and the formulation of fill material on the release pattern of diltiazem HCl, a model drug, was investigated. The body portion of the hard gelatin capsules was cross-linked by the combined effect of formaldehyde and heat treatment. A linear relationship was observed between weight of HPMC K15M and log % drug released at 4 h from the capsules containing the plug in powder form. In order to accelerate the drug release after a lag time of 4 h, addition of an effervescent blend, NaHCO3 and citric acid, in the capsules was found to be essential. The plugs of HPMC in tablet form, with or without a water soluble adjuvant (NaCl or lactose) were used for obtaining immediate drug release after the lag time. Sodium chloride did not cause significant influence on drug release whereas lactose favourably affected the drug release. The capsules containing HPMC K15M tablet plug (200 mg) and 35 mg effervescent blend in body portion of the capsule met the selection criteria of less than 10% drug release in 4 h and immediate drug release thereafter. It is further shown that the drug release was also dependant on the type of swellable hydrophilic agent (HPMC or guar gum) and molecular weight of HPMC (K15M or 20 cPs). The results reveal that programmed drug delivery can be obtained from hard gelatin capsules by systemic formulation approach. [Copyright &y& Elsevier]

Long acting parenteral formulations are preferred over conventional formulations for the treatment of chronic diseases. Prevalence of such diseases provoked the interest of researchers and pharmaceutical industries in the development of long acting parenteral formulations. The regulatory guidelines and pharmacopoeia have remained silent on dissolution methods for long acting parenteral formulations due to their diverse nature. The lack of compendial method for dissolution testing increases the duration of approval process for long acting parenteral formulations. This article reviews various dissolution methods used to study in vitro drug release profile of long acting parenteral formulations. Compendial as well as noncompendial methods, such as- rotating dialysis cell, dialysis tube, rotating bottle, shaking flask, single drop, inverted cup and incubation, are used by researchers for drug release profile of long acting parenteral formulations. This review article also highlights the advantages and disadvantages of reported dissolution methods along with the suitability of these methods for particular type of long acting formulation. The compiled work will help the researchers in designing the biorelevant dissolution method and expedite the development of long acting parenteral formulations.

Metformin hydrochloride exhibits poor compressibility during compaction, often resulting in weak and unacceptable tablets with a high tendency to cap. The purpose of this study was to develop directly compressible metformin hydrochloride by the spray-drying technique in the presence of polymer. Metformin hydrochloride was dissolved in solutions containing a polymer, namely polyvinylpyrrolidone (PVP K30), in various concentrations ranging from 0-3% (m/V). These solutions were employed for spray-drying. Spray-dried drug was evaluated for yield, flow property and compressibility profile. Metformin hydrochloride spray-dried in the presence of 2% PVP K30 showed an excellent flow property and compressibility profile. From the calculated Heckel's parameter (Py = 2.086), it was demonstrated that the treated drug showed better particle arrangement in the initial compression stage. Kawakita analysis revealed better packability of the treated drug compared to the untreated drug. Differential scanning calorimetry and Fourier transform infrared spectroscopy experiments showed that the spray-dried drug did not undergo any chemical modifications. Tablets made from the spray-dried drug (90%, m/m) were evaluated for crushing strength, friability and disintegration time and the results were found satisfactory.

Aims and Objectives: Obesity and overweight have become a worldwide epidemic, and there is an urgent need to examine childhood obesity and overweight across countries using a standardized international standard. In the present study we have investigated the prevalence of obesity and overweight and their association with socioeconomic status (SES) and the risk factors like diet, physical activity like exercise, sports, sleeping habit in afternoon, eating habits like junk food, chocolate, eating outside at weekend, family history of diabetes and obesity., Material and Methods: The study was carried out in 5664 school children of 12-18 years of age and having different SES. The obesity and overweight were considered using an updated body mass index reference. SES and life style factors were determined using pre-tested questionnaire., Results: Age-adjusted prevalence of overweight was found to be 14.3% among boys and 9.2% among girls where as the prevalence of obesity was 2.9% in boys and 1.5% in girls. The prevalence of overweight among children was higher in middle SES as compared to high SES group in both boys and girls whereas the prevalence of obesity was higher in high SES group as compared to middle SES group. The prevalence of obesity as well as overweight in low SES group was the lowest as compared to other group. Eating habit like junk food, chocolate, eating outside at weekend and physical activity like exercise, sports, sleeping habit in afternoon having remarkable effect on prevalence on overweight and obesity among middle to high SES group. Family history of diabetes and obesity were also found to be positively associated., Conclusion: Our data suggest that the prevalence of overweight and obesity varies remarkably with different socioeconomic development levels.