Natural products formulation

Cott J. (1995). NCDEU update. Natural product formulations available in europe for psychotropic indications. Psychopharmacol Bull. 31(4) 745-51. 

Liquid-liquid extractions with two immiscible liquids is useful for sample clean-up of complex samples such as creams, suppositories, fermentation broths or natural product formulations. It takes advantage... 

Soap as used in personal cleansing products has a long safe history of use. Modem soaps have been specifically formulated to be compatible with skin and to be used on a daily basis with minimal side effects. Excessive use of soap for skin cleansing can dismpt the natural barrier function of skin through the removal of skin oils and dismption of the Hpid bdayer in skin. This can result in imperfect desquamation or a dry appearance to skin and cause an irritation response or erythema, ie, reddening of the skin. Neither of these is a permanent response and the eHcitation of this type of skin reaction depends on the individual s skin type, the product formulation, and the frequency of use. 

Avemiectin is the most effective of the averniectia family of natural products against agriculturally important insects and mites (14). It has been commercialized for agricultural use under the nonproprietary name abamectin. This mixture of avermectins contains at least 80% of avermectin (C4gH 20 and not more than 20% of avermectin B Abamectin for use in foHar spray appHcations is formulated as an emulsiftable... 

Adhesives. Clays, especially kaolin and attapulgite, are widely used in various adhesive formulations. Adhesives (qv) containing clays can be derived from natural products such as starch or protein, or be whoUy synthetic, eg, latex, hot melt, emulsion, etc. 

Other natural product-based resins also became widely used, such as the light colored Lewis acid oligomerized products of terpenes such as a-pinene, p-pinene, and limonene. These natural product resins are relatively expensive, however, and formulators now often use the newer, less expensive synthetic resins in present day natural rubber PSAs. These are termed the aliphatic or C-5 resins and are Lewis acid oligomerized streams of predominately C-5 unsaturated monomers like cis- and /rawi-piperylene and 2-methyl-2-butenc [37]. These resins are generally low color products with compatibility and softening points similar to the natural product resins. Representative products in the marketplace would be Escorez 1304 and Wingtack 95. In most natural rubber PSA formulations, rubber constitutes about 100 parts and the tackifier about 75-150 parts. 

Microbial insecticides are very complex materials in their final formulation, because they are produced by fermentation of a variety of natural products. For growth, the bacteria must be provided with a source of carbon, nitrogen, and mineral salts. Sufficient nutrient is provided to take the strain of choice through its life cycle to complete sporulation with concomitant parasporal body formation. Certain crystalliferous bacilli require sources of preformed vitamins and/or amino acids for growth. Media for growing these bacilli may vary from completely soluble, defined formulations, usable for bench scale work, to rich media containing insoluble constituents for production situations (10,27). Complex natural materials such as cottonseed, soybean, and fish meal are commonly used. In fact, one such commercial production method (25) is based on use of a semisolid medium, a bran, which becomes part of the final product. 

The first commercial trialkyl phosphate esters (TAP) were tricresyl phosphate (TCP) and trixylenyl phosphate (TXP), referred to as "natural" phosphate esters because the cresols and xylenols used as raw materials are derived from petroleum oil or coal tar (Marino and Placek 1994). These products are not commercially significant at present however, at waste disposal sites, contaminants from older product formulations may be encountered, particularly those containing the neurotoxic tri-o/T/io-cresyl phosphate isomer. "Synthetic" phosphate esters are derived from synthetic feedstocks. Specific synthetic reactions have been developed to produce triaryl, trialkyl, and alkyl Aryl esters. The triaryl phosphates are currently... 

In API manufacture, whether via chemical synthesis, rDNA technology, or extraction from natural products, there are significant changes (physical and chemical) from the starting materials to the API. In the formulation process, however, the quality and specifications of the API are retained. The addition of excipients to produce the drug product in a finished dosage form does not present physical or chemical changes to the API. 

Fine particle powders can be produced by various methods, such as micronization or spray drying. The physicochemical nature of these fine particles largely defines the stability of the bnlk powder, which in turn is critical to the long-term effective performance of the dry powder product. The section Fine Particles and the Solid State in this article is an introduction to understanding better the fundamental properties that underlie the behavior of bulk powders. Commentary on the various means of producing fine powders follows in the section Powder Production Formulation and Processing. ... 

The classic cholinesterase inhibitor is the alkaloid physostigmine (6)/ eserine (7). It was first isolated from the calabar bean, the seeds of Physostigma venenosum. Many novel natural products with AchE-inhibifing properties have shown promise as therapeutics for AD. Some examples of such products (pure compounds/plant extracts or formulations) are briefly reviewed here. 

Formidable chemical obstacles stood in the way of clinical development of these agents derived from natural products, notably in formulation of very poorly soluble compounds for intravenous infusion and in manufacture of bulk drug. For a time, production of Taxol from the bark of the Pacific Yew tree aroused public controversy, which became a story of nature and politics in pursuit of an anti-cancer drug [22]. 

In 1979, Bohlmann and Zdero reported the isolation and an unusual sesquiterpene hydrocarbon from Senecio oxyodontus This substance was formulated as 766 on the basis of its spectral characteristics and called senoxydene. However, Galemmo and Paquette have recently prepared this particular compound and determined that it is not identical to the natural product. Their pathway, which is summarized in Scheme LXXXVII, begins by transforming 4,4-dimethylcyclopentenone into bicyclic... 

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