Inactive list , pills .....

IngInzano · Fri Jun 03, 2005 12:55 pm

Featured Excipients Capsule Tablet Dilutens Excipients Emulsifiers Stabilizers ?
Any list, Data ?

Alguien tiene una lista de los excipientes mas usados, y deamas porquerias que traen los medicamentos ?

Smile

Grax. 10x

IngInzano · Sun Jun 05, 2005 1:00 am

Use this as a refrence guide and pay close attention to whether a given inactive is soluble in water, alcohol, or both. For those of you who run into problems sourcing Tetrachloroethylene/Perchloroethylene/TCE this is especially being posted with you in mind. You guys are going to need to familiarize yourself with the OTC-PSE inactives as by doing so will prove vital on down the line and perhaps sooner rather than later!!

Really all you need to focus on is the solubility/insolubility of a given inactive. And pay close attention to the emulsifiers as well!! they're down at the bottom of the list. If ever you've had a nightmare of a time trying to base the Post-Rxn these emulsifiers are almost certainly your culprit(s)!!

And anytime you're running into problems with a PSE Xtraction please be sure to post-up the list of inactives of the PSE tabs at hand. All of them if using multi-brands! But you just need to list the individual inactives only once of course.

At any rate here you go and make mental notes man. Because PSE's are going to prove your greatest hurdle/roadblock/reason for your Rxn failures. It all starts here with the PSE.

Featured Excipients-Capsule & Tablet-Dilutens/Excipients/Emulsifiers/& Stabilizers

Calcium Carbonate, USP
Properties: Calcium carbonate (CaCO3, MW 100.09, precipitated calcium carbonate, precipitated carbonate of lime, precipitated chalk) occurs as a fine, white, odorless, tasteless, microcrystalline powder that is stable in air. It is practically insoluble in water and insoluble in alcohol. It dissolves with effervescence in 1 N acetic acid, in 3 N hydrochloric acid and in 2 N nitric acid. When used in tablets containing aspirin, traces of iron may cause discoloration, which may be overcome by using a suitable chelating agent.

Dibasic Calcium Phosphate, USP
Properties: Dibasic calcium phosphate (CaHPO4, MW 136.06) is anhydrous or contains two molecules of water of hydration. It occurs as a white, odorless, tasteless powder that is stable in air. It is practically insoluble in water, insoluble in alcohol and soluble in 3 N hydrochloric acid and 2 N nitric acid. They are both used as excipients and as a source of calcium in nutritional supplements. It should not be used to formulate tetracycline antibiotics and has been reported to be incompatible with indomethacin, aspirin, aspartame, ampicillin, cephalexin and erythromycin. The coarse grade material has good flow properties, but is abrasive and requires a lubricant when used for tableting. The surface of the milled particles is alkaline and should not be used with drugs that are sensitive to alkaline pH. The surface of the unmilled particles may be acidic. It is widely used in oral pharmaceutical products, food products and toothpastes. It should be labeled to indicate whether it is anhydrous or the dihydrate.

Dibasic Calcium Phosphate Dihydrate, USP
Properties: Dibasic calcium phosphate dihydrate (CAHPO4.2H2O, MW 172.09) is nonhygroscopic but can lose its water of crystallization below 100 C.

Tribasic Calcium Phosphate, NF
Properties: Tribasic calcium phosphate [Ca5(OH)(PO4)3, MW 502.31, hydroxyapatite, precipitated calcium phosphate] is not a defined entity but consists of a variable mixture of calcium phosphates having the approximate composition of 10 CaO.3P2O5.H2O [corresponding to a molecular formula of Ca5(OH)(PO4)3 or Ca10(OH)2(PO4)6] containing between 34 and 40% of calcium. It occurs as a white, odorless, tasteless powder that is stable in air. It is practically insoluble in water, insoluble in alcohol, and readily soluble in 3 N hydrochloric acid and 2 N nitric acid. It is used as an anticaking agent, glidant and tablet/capsule diluent. Calcium salts are incompatible with tetracycline antibiotics. Tribasic calcium phosphate is also incompatible with tocopheryl acetate (but not tocopheryl succinate). It can influence the absorption of vitamin D and may form sparingly soluble phosphates with hormones.

Calcium Sulfate, NF
Properties: Calcium sulfate is either anhydrous (CaSO4, MW 136.14, anhydrous gypsum, anhydrous sulfate of lime) or contains two molecules of water of hydration (CaSO4.2H2O, MW 172.17, alabaster, gypsum, light spar, mineral white, native calcium sulfate, precipitated calcium sulfate, satinite, satin spar, selenite, terra alba). It occurs as a fine, white to slightly yellow-white, odorless powder. It is slightly soluble in water (1 in 375) and soluble in 3 N hydrochloric acid. It should be labeled to indicate whether it is anhydrous or dihydrate. It also occurs as a hemihydrate form used in the preparation of plaster of paris bandages; this form should NOT be used in the preparation of tablets or capsules. Calcium sulfate anhydrous is hygroscopic and the uptake of water can result; it is not recommended for the formulation of tablets, capsules or powders for oral administration. The dihydrate form is used in oral preparations.

Properties: Calcium salts may be incompatible, in the presence of moisture, with amines, amino acids, peptides and proteins, which may form complexes. Calcium salts will interfere with tetracycline antibiotics. Calcium sulfate would be incompatible with indomethacin, aspirin, aspartame, ampicillin, cephalexin and erythromycin. Calcium sulfate, at high temperatures, may react violently with phosphorus and aluminum powder.

Microcrystalline Cellulose, NF
Properties: Microcrystalline cellulose [(C6H10O5)n where n ~~ 220, MW ~~36,000] is purified, partially depolymerized cellulose prepared by treating alpha cellulose, obtained as a pulp from fibrous plant material, with mineral acids. It occurs as a fine, white or almost white powder consisting of free-flowing, nonfibrous particles. It is insoluble in water, dilute acids and most organic solvents. It is practically insoluble in sodium hydroxide solution (1 g in 20 mL). It should be labeled to indicate it's nominal loss on drying, bulk density and degree of polymerization values. It is used as an adsorbent, suspending agent, tablet disintegrant and tablet/capsule diluent. It is incompatible with strong oxidizing agents.

Powdered Cellulose, NF
Properties: Powdered cellulose [(C6H10O5)n where n = 500, MW ~~243,000] is derived from a natural polymer, hence it has a variable chain length and variable molecular weight. It is purified, mechanically disintegrated cellulose prepared by processing alpha cellulose obtained as a pulp from fibrous plant materials. It occurs as a white or almost white powder that exhibits degrees of fineness ranging from a free-flowing dense powder to a coarse, fluffy, nonflowing material. It is insoluble in water, dilute acids and in nearly all organic solvents. It is slightly soluble in sodium hydroxide solution (1 g in 20 mL). It is used as an adsorbent, glidant, suspending agent, tablet disintegrant and tablet/capsule diluent. It has also been used in oily suspension filled capsules to reduce the sedimentation rate of the incorporated powders. It is incompatible with strong oxidizing agents. It should be labeled to indicate the nominal degree of polymerization.

Dextrates, NF
Properties: Dextrates is a purified mixture of saccharides resulting from the controlled enzymatic hydrolysis of starch. It is either anhydrous or hydrated and contains between 93 and 99% of dextrose equivalent, calculated on the dried basis. It is free-flowing, porous, white, odorless, spherical granules consisting of aggregates of microcrystals. It has a sweet taste and produces a cooling sensation in the mouth. It may be directly compressed into self-binding tablets; it is used in the preparation of chewable, nonchewable, soluble, dispersible and effervescent tablets. Dextrates is freely soluble in water (1 g in 1 mL), insoluble in ethanol, and soluble in dilute acids and alkalies. It should be labeled to state whether it is anhydrous or hydrated. Dextrates are incompatible with oxidizing agents and also may react with substances containing a primary amino group at high temperatures and humidities; the Maillard reaction.

Dextrin, NF
Properties: Dextrin (British gum, canary dextrin, crystal gum, starch gum, yellow dextrin, white dextrin, [(C6H10O5)n.xH20, MW 162.14--the molecular weight is typically 4,500-85,000 depending upon the number of monomer units] is starch, or partially hydrolyzed starch, modified by heating in a dry state, with or without acids, alkalies or pH control agents. Its source is primarily from corn or potatoes; it has different characteristics depending upon its source and method of preparation. It occurs as a free-flowing, white, yellow or brown powder. It is also defined as a dextrose polymer. Its solubility in water varies but it is usually very soluble; it may contain an insoluble portion. It is incompatible with strong oxidizing agents.

Dextrose Excipient, NF
Properties: Dextrose excipient is a sugar usually obtained by hydrolysis of starch, containing one molecule of water of hydration. It occurs as colorless crystals or as a white, crystalline or granular powder. It is odorless and sweet-tasting. It is freely soluble in water and very soluble in boiling water. It is slightly soluble in alcohol. It should be labeled to indicate that it is not intended for parenteral use. It may cause browning in tablets containing amines.

Fructose, USP
Properties: Fructose (fruit sugar, levulose, C6H12O6, MW 180.16) occurs as colorless crystals or as a white, crystalline odorless powder with a sweet taste. It is freely soluble in water (1g in 0.3 mL) and soluble in alcohol (1 g in 15 mL). Fructose is incompatible with strong acids or alkalis forming a brown coloration. When in aldehyde form, it can react with amines, amino acids, peptides, and proteins; it may cause browning of tablets containing amines.

Kaolin, USP
Properties: Kaolin (argilla, bolus alba, china clay, porcelain clay, white bole, hydrated aluminum silicate, Al2O3.2SiO2.2H20) occurs as a soft, white or yellowish white powder or as lumps. It is a naturally occurring mineral, has an earthy or clay-like taste and, when moistened with water, assumes a darker color and develops a marked clay-like odor. It is insoluble in water, cold dilute acids and in solutions of alkali hydroxides. Kaolin is an adsorbent and may alter the absorption of orally administered drugs such as amoxicillin, ampicillin, cimetidine, digoxin, lincomycin, phenytoin, and tetracycline.

Lactitol, NF
Properties: Lactitol (C12H24O11, MW 344.31, lactil, lactite, lactobiosit, lactosit) occurs as the anhydrous, monohydrate (MW 362.34) or the dihydrate (MW 380.35) forms. It is produced by the catalytic hydrogenation of lactose. It is odorless and has a sweet taste (about one-third that of sucrose) imparting a cooling sensation in the mouth; it does not promote dental caries. It is soluble in water (1 g in1.75 mL). It should be labeled to indicate whether it is the monohydrate, the dihydrate or the anhydrous form.

Lactose Anhydrous, NF
Properties: Lactose anhydrous (C12H22O11, MW 342.3, milk sugar, saccharum lactis) is primarily beta lactose or a mixture of alpha and beta lactose. It occurs as a white or almost white powder that is freely soluble in water (1 g in 5 mL) and practically insoluble in alcohol.

Lactose Monohydrate, NF
Properties: Lactose monohydrate (C12H22O11.H2O, MW 360.31) is a natural disaccharide, obtained from milk, which consists of one glucose and one galactose moiety. Lactose monohydrate is widely used as a filler or diluent in tablets, capsules, infant formulas and lyophilized products. It is available in different grades with varying physical properties such as particle size distribution and flow characteristics. The dosage form being prepared dictates the type of lactose to be used. Lactose occurs as a white, free-flowing powder that is freely but slowly soluble in water (1 g in 4.63 mL) and practically insoluble in alcohol; it is odorless and slightly sweet-tasting. It should be labeled to state the particle size distribution and if modified, it should indicate the method of modification. Lactose may undergo a Maillard-type condensation reaction with compounds containing a primary amine group to form brownish colored products; this is accelerated in alkaline environments. Lactose is listed as incompatible with amino acids, aminophylline and amphetamines.

Mannitol, USP
Properties: Mannitol (C6H14O6, MW 182.17, manna sugar, mannite) occurs as a white, crystalline powder or as free-flowing granules. It is odorless and has a sweet taste. It is freely soluble in water (1 g in 5.5 mL), soluble in alkaline solutions and very slightly soluble in alcohol (1 g in 83 mL). It is commonly used in direct-compression tablets and as an excipient in the manufacture of chewable tablets due to its negative heat of solution and the resulting cooling effect. There are no listed incompatibilities of mannitol when in the dry state.

Sorbitol, NF
Properties: Sorbitol (C6H14O6, MW 182.17, d-Glucitol) occurs as white, hygroscopic powder, granules or flakes, with a sweet taste. It is very soluble in water (1 g in 0.45 mL) and slightly soluble in alcohol (1:25). It is used as a humectant, plasticizer, sweetening agent, and tablet and capsule diluent. There are no listed incompatibilities of sorbitol in the dry state.

Starch, NF
Properties: Starch [(C6H10O5)n where n = 300-1000] consists of the granules separated from the mature grain of corn, wheat, tubers or tapioca. Starches obtained from different botanical sources may not have identical properties with respect to their use for specific pharmaceutical purposes, therefore, types of starch should not be interchanged unless performance equivalency has been demonstrated. As an example, corn starch contains about 27% amylose, potato starch about 22% and tapioca starch about 17%; these differences provide for different physical properties. Starch generally occurs as irregular, angular, white masses or as a fine powder. It is odorless and has a slight, characteristic taste. It is insoluble in cold water and in alcohol. It should be labeled to indicate the botanical source from which it was derived. Corn starch is also known as maize starch and tapioca starch is also known as cassava starch. Starch has no listed incompatibilities.

Pregelatinized Starch, NF
Properties: Pregelatinized starch [(C6H10O5)n, where n = 300-1000)] is starch that has been chemically and/or mechanically processed to rupture all or part of the granules in the presence of water and subsequently dried. Pregelatinized starch occurs as a moderately coarse to fine, white to off-white powder. It is odorless and has a slight, characteristic taste. It is slightly soluble to soluble in cold water and is insoluble in alcohol. It has no listed incompatibilities.

Sucrose, NF
Properties: Sucrose (C12H22O11, MW 342.30, beet sugar, cane sugar, refined sugar, saccharose, sugar) is obtained from various sources. It occurs as a white crystalline powder or as lustrous, dry, colorless or white crystals. It is very soluble in water (1 g in 0.5 mL), slightly soluble in alcohol (1 in 170) and practically insoluble in dehydrated alcohol. Sucrose may be contaminated with traces of heavy metals that can lead to an incompatibility with active ingredients as ascorbic acid. It also may contain sulfite from the refining process

Compressible Sugar, NF
Properties: Compressible sugar may contain starch, malto-dextrin or invert sugar and may contain a suitable lubricant; it contains between 95 and 98% sucrose. It is used in the preparation of direct compression chewable tablets. It occurs as a practically white, crystalline, odorless powder with a sweet taste; it is stable in air. The sucrose portion of compressible sugar is very soluble in water. It is incompatible with dilute acids and can react with alkaline earth hydroxides to form sucrates.

Confectioner's Sugar, NF
Properties: Confectioner's sugar is sucrose ground with corn starch to a fine powder; it contains not less than 95% sucrose. It has been used in pharmaceutical formulations when a rapidly dissolving form of sugar is needed for flavoring or sweetening. It occurs as a fine, white, odorless powder with a sweet taste; it is stable in air. The sucrose portion of confectioner's sugar is soluble in cold water. Confectioner's sugar is freely soluble in boiling water. It is incompatible with dilute acids and can react with alkaline earth hydroxides to form sucrates.

Polyethylene Glycol
Properties: Sol in many organic solvents. Readily sol in water & in alcohol.

Povidone
Properties: White, hygroscopic powder. Sol in water, alcohol, chloroform, formic acid, acetic acid, N-methylpyrrolidone, methylcyclohexanone, dichloromethane, ethylenediamine, glycerol, diethyleneglycol, PEG 400. Insol in xylene, toluene, diethylether, ethylacetate, acetone, cyclohexanone, chlorobenzene, dioxane, carbon tetrachloride, mineral oil.

Polysorbate 80(Emulsifier)

PROPERTIES: non-ionic emulsifier (enables water & oil to mix), dispersing agent, solubilizer, antistat, solubilizer & stabilizer of essential oils. Soluble in water & alcohols, insoluble in oils.

Gum Arabic/Acacia gum.(Emulsifier & Stabilizer)
PROPERTIES: Water soluble, insoluble in alcohol. o/w-emulsifier (good dispersing agent), foam & emulsion stabilizer, thickener, adhesive & film-forming properties.

Stearic acid (C18H36O2, MW 284.47, octadecanoic acid) is a mixture of stearic acid
C18H36O2) and palmitic acid (C16H32O2); the content of stearic acid is not less than 40.0% and the sum
of the two acids is not less than 90.0%. It is used as an emulsifying agent, solubilizing agent and as a
tablet/capsule lubricant. It is described as a hard, white or faintly yellow colored, somewhat glossy,
crystalline solid or as a white, or yellowish white, powder. It has a slight odor and taste suggesting
tallow. It is listed as incompatible with most metal hydroxides and may be incompatible with oxidizing
agents. It will form insoluble stearates with many metals and ointment bases made with it may show
evidence of drying out or lumpiness due to such a reaction when compounded with zinc or calcium salts.
is freely soluble in benzene, carbon tetrachloride, chloroform and ether; it is soluble in ethanol, hexane
and propylene glycol and practically insoluble in water.9
Purified stearic acid (C18H36O2, MW 284.47) is manufactured from fats and oils derived from
edible sources and is a mixture of stearic acid (C18H36O2) and palmitic acid (C16H32O2) which together
constitute not less than 96.0% of the total content. The content of the stearic acid portion is not less than
90.0%. It is used solely for external use and is exempt from the requirement that it be prepared from
edible sources. It is soluble one part in five parts benzene, six parts carbon tetrachloride, two parts
chloroform, 15 parts ethanol, three parts ether and is practically insoluble in water.9

java · Consumer

Good find........thank you for sharing the info, as we all benefit.......saludos, y gracias por compartir la informacion, camara............java