Formulations controlled-released

Tablet Formulations (Controlled Release). In this domain, the first studies were carried out in the early 1990s by Hussain and coworkers at the University...

Wong D, Larrabee S, Clifford K, et al. USP Dissolution Apparatus n (reciprocating cylinder) for screening of guar based colonic delivery formulations. / Control Release 1997 47 173-179. 

Common side effects of theophylline therapy include headache, dyspepsia, and nausea. More serious side effects such as lethal seizures or cardiac arrythmias can occur if blood levels are too high. Many derivatives of theophylline have been prepared in an effort to discover an analogue without these limitations (60,61). However, the most universal solution has resulted from the development of reliable sustained release formulations. This technology limits the peaks and valleys in serum blood levels that occur with frequent dosing of immediate release formulations. Controlled release addresses the problems inherent in a drug which is rapidly metabolized but which is toxic at levels (>20 7g/mL) that are only slighdy higher than the therapeutically efficacious ones (10—20 ag/mL). Furthermore, such once-a-day formulations taken just before bedtime have proven especially beneficial in the control of nocturnal asthma (27,50,62). 

It is difficult to formulate controlled release formulations for the drugs with short half-life (<1 h) due to the requirement of high maintenance dose. The development of these formulations is a time-consuming process and difficult to manufacture on a large scale, which makes them more expensive than the conventional dosage forms. These are posing new challenges to the researchers to develop controlled delivery formulations with minimal drawbacks. 

T. Coviello, P. Matricardi, C. Marianecci and E AUiaique, Polysaccharide hydrogels for modified release formulations,/. Control. Release, 119 5-24,2007. 

Paoh EE, Kruse DE, Seo J W, Zhang H, Kheirolomoom A, Watson KD et al. An optical and microPET assessment of thermally-sensitive hposome biodistribution in the Met-1 tumor model Importance of formulation. / Control Release 2010 143 13-22. 

Compressed Tablets. This popular type of dosage form offers convenience, stabiUty, accuracy and precision, and good bioavadabihty of active ingredients. After the best formulation has been estabflshed, compressed tablets can be manufactured at high rates of speed on advanced equipment. Tablets can be made to achieve rapid dmg release or to produce delayed, repeat, or prolonged therapeutic action (Controlled release technology, pharmaceutical). ... 

Improvements in asthma treatment include the development of more effective, safer formulations of known dmgs. The aerosol adrninistration of P2-agonists or corticosteroids results in a decrease in side effects. Also, the use of reUable sustained release formulations has revolutionized the use of oral xanthines which have a very narrow therapeutic index (see Controlled release technology). For many individuals, asthma symptoms tend to worsen at night and the inhaled bronchodilatots do not usually last through an entire night s sleep (26,27). 

Procardia XL. Procardia XL extended-release capsules, marketed by Pfizer Labs Division of Pfizer, Inc., contain nifedipine [21829-25-4] a calcium channel blocker of mol wt 346.3. The extended release tablet is formulated as a once-a-day controlled release capsule for oral adrninistration dehvering either 30, 60, or 90 mg nifedipine. Procardia XL is indicated for use in the management of vasospastic angina, chronic stable angina, and hypertension (see Cardiovascularagents). 

The main purpose of pesticide formulation is to manufacture a product that has optimum biological efficiency, is convenient to use, and minimizes environmental impacts. The active ingredients are mixed with solvents, adjuvants (boosters), and fillers as necessary to achieve the desired formulation. The types of formulations include wettable powders, soluble concentrates, emulsion concentrates, oil-in-water emulsions, suspension concentrates, suspoemulsions, water-dispersible granules, dry granules, and controlled release, in which the active ingredient is released into the environment from a polymeric carrier, binder, absorbent, or encapsulant at a slow and effective rate. The formulation steps may generate air emissions, liquid effluents, and solid wastes. 

Potential antidepressant activity of lusaperidone (14) and its derivatives were investigated on al, q 2A, q 2B and q 2C receptor binding tests (00BMCL71). Hydrophilic controlled release formulations of 14 were developed and patented (00MIP8). 

The acyl groups introduced included 4-phenylbenzoyl, phenylacetyl, 4-methoxybenzoyl, acetyl, 2,4-dichlorophenoxyacetyl, and 2,2-dichloropro-pionyl. Introduction of the last pair of acyl groups is important because they are bioactive (insecticides), i.e., the product can be employed in controlled-release formulations [159]. The structures of all these esters were determined by FTIR and NMR spectroscopy, whereas their solution properties, includ-... 

Cardarelli, N. F., "Controlled Release Pesticide Formulations. Chemical Rubber Co., Cleveland, Ohio, 1976. 

Anton, N., Benoit, J. P. Saulnier, P. (2008). Design and production of nanopartides formulated from nano-emulsion templates - A review. Journal of Controlled Release, Vol. 128, 3, (June 2008), pp. (185-199), ISSN 0168-3659... 

Occasionally in the synthesis of the copolymers, insoluble material is produced. This results from polymer containing blocks of polyglycolide rather than the desired random structure. Obviously, such compositions would have considerable effect on the performance of controlled release formulations utilizing those polymers. This problem is particularly evident when one is seeking to utilize the 50 50 glycolide/lactide copolymer as a biodegradable excipient. However, with carefully controlled polymerization conditions, useful 50 50 polymer is readily produced. 

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