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A controlled release matrix formulation for mesalamine was designed and developed to achieve a 24 h release profile. Using compritol 888 ATO (glyceryl behenate) as an inert matrix-forming agent to control the release of mesalamine, formulation granules containing the solid dispersions were investigated. Pectin, a polysaccharide, was used as bacterial dependent polymer for colon targeting. The matrix tablets for these formulations were prepared by direct compression and their in vitro release tests were carried out. A 3(2) full factorial design was used for optimization by taking the amounts of glyceryl behenate (X(1)) and pectin (X(2)) as independent variables and percentage drug released at 2 (Q(2)), 16 (Q(16)) and 24 (Q(24)) h as dependent variables. Drug release from the matrix tablets formulations lasted for over 24 h. Images of the tablet surface and cross-section were characterized by scanning electron microscopy to show the formed pores and channels in the matrices. These may provide the release pathway for the inner embedded drugs. The co-mixing of polysaccharide pectin, into the waxy matrices played a meaningful role in targeting the tablets to colon. The drug release from the novel formulation may be attributed to the diffusion-controlled mechanism. The results of the full factorial design indicated that an optimum amount of compritol ATO 888 and a high amount of pectin favors the colon targeting and controlled release of mesalamine from dosage form.

Phytochemical and synthetic chemistry based pharmaceutical industry severed the historical connection between food, plants and medicines. Discovering new chemical entity (NCEs) based drugs through high throughput screening methods may reconnect plants and human health at a high level of technological sophistication. Botanical therapeutics with multi-component that comprise functional foods, nutraceuticals, dietary supplements and botanical drugs hold several advantages over conventional drugs that may earn them a more prominent place in the medicine of the next generation. Botanical therapeutics and deliver mixtures of multi functional molecules with synergistic and potentiating effects and pleiotropic targeting at a reasonable cost and with some regulatory constraints. They are well suited for long-term disease prevention in an era of genetic testing and increased life expectancy. They also provide additional vehicles for delivering health and wellness. Technologies that address the needs of discovery, development and manufacturing of multi-components botanical therapeutics are emerging, include computational and bioinformatics approaches, cell based gene expression and high-content screening systems. Phytochemical elicitation and unique plant cultivation / extraction methods designed to optimize the production of bioactive, standardized overall extract compositions and assure batch to batch product consistency are needed. Nevertheless, multi-components botanical therapeutics carry risks associated with potential interactions with conventional drugs and adverse reactions, which are difficult to detect and diagnose. Acceptance by medical community and pharmaceutical industry, safety, poor standardization and quality control, and difficulties in identification of active ingredients and determination of their complex mode of action are some of the problems. Solving these problems will accelerate the merger of grocery stores with pharmacies and agriculture with chemical manufacturing and provide physicians and patients with broader and more individualized choices of disease prevention and treatment. Multi-components botanical therapeutics will be useful for next generation.

The drug release profiles were optimized using different grades of polyethylene glycols (PEGs). Phase diagrams of ternary mixtures of ethylcellulose, PEG and TEC were obtained and used for optimization of drug release. The phase diagrams showed that addition of higher molecular weight of PEGs increased the phase separation and caused precipitation of ethylcellulose from the ternary mixtures. The effect of different grades and concentrations of PEGs in novel oral intragastric controlled release gel formulations were also investigated. In conclusion, the in situ forming oral controlled release formulations were successfully developed and the formulations were able to control the release of hydrochlorothiazide up to 24 hours., Los perfiles de liberación farmacológica se optimizaron mediante diferentes grados de glicoles de polietileno (PEGs). Se obtuvieron diagramas de fase de mezclas ternarias de etilcelulosa, PEG y TEC, que se usaron para optimizar la liberación farmacológica. Los diagramas de fase mostraron que la adicción de PEGs de mayor peso molecular incrementaba la separación de fases y causaba precipitación de etilcelulosa de las mezclas ternarias. Se investigó también el efecto de distintos grados y concentraciones de PEGs en nuevas formulaciones de geles orales de liberación controlada intragástrica. En conclusión, las formulaciones orales de liberación controlada in situ se desarrollaron con éxito y fueron capaces de controlar la liberación de hidroclorotiazida hasta 24 horas.

OBJECTIVE: To investigate the effects of a newer antipsychotic drug, risperidone (a potent serotonin 5-HT2A/2C and dopamine D2-receptor blocker), on the quantity and quality of sleep in patients with schizophrenia. DESIGN: Prospective pilot study. SETTING: Outpatient treatment at a mental health hospital. PATIENTS: Two groups of age- and sex-matched patients with schizophrenia receiving either risperidone (n = 8) or a typical antipsychotic drug (n = 8), and a group of age- and sex-matched controls (n = 8). OUTCOME MEASURES: Sleep quality, measured by a visual analogue scale, and sleep continuity, measured using a movement index calculated from actigraph data. RESULTS: Patients with schizophrenia had more disturbed sleep than controls. Compared with patients treated with typical antipsychotic drugs, patients treated with risperidone reported significantly better sleep quantity and quality as well as general functioning. CONCLUSION: Improvement by risperidone may be related to 5-HT2A/2C receptor blockade; however, further controlled studies are required to confirm these results.