Povidone CAS 9003-39-8 Product application

This product is an aqueous synthetic polymer, a linear homopolymer of n-vinylpyrrolidone, whose molecular formula is (C6H9NO)n, where n represents the average number of N-vinylpyrrolidone chains; Povidone K30, with an average molecular weight of 38000, is the most commonly used excipient. Povidone K15, K25 and K90 were followed by POvidone K15, K25 and K90 with average molecular weight of 7700, 25000 and 630000, respectively.
Chemical structure and naming
Molecular formula (C6H9NO)n
Molecular weight: Mw=(111.1)n
Chemical name: Polyvidone; Polyvidonum; Polyvinylpyrrolidone
CTFA/INCI: PVP
CAS Number: [9003-39-8]

Product characteristics
This product is white to milky amorphous powder, its bulk density is 0.4~0.6; Odorless or slightly odorless; Tasteless; Hygroscopicity, when the relative temperature is 75%, the saturated water absorption rate is about 40%; Soluble in water, ethanol, isopropyl alcohol, glycerol or chloroform, insoluble in acetone, ether and hydrocarbon solvents.
This product can be complexed with many substances, especially compounds containing active hydrogen atoms or metal carbonyl compounds, to form solid complexes, so that the properties of the complex such as solubility, volatility, stability, toxicity and irritation have significant but reversible changes. In the application of excipients, many dosage forms with new functions can be developed or the performance of the original dosage forms can be improved.
The product is stable under normal conditions and has a strong tolerance to heat, acid and alkali; Prolonged heat can lead to discoloration or cross-chain, resulting in insolubility in water; Long time grinding will lead to degradation, molecular weight reduction; Long-term storage will also have a certain degradation, especially high molecular weight (such as PVPK90) PVP; Pure PVP aqueous solutions are also stable under normal conditions, but will discolor or hydrolyze under prolonged heating, storage, or acidic conditions.
Product application
◆ Scope of application
Soluble PVP has the properties of adhesion, thickening, dispersion, film formation and complexation, so it can be used as a binder for granules and tablets, as a thickener and suspension aid for liquid preparations. Co-solvent and stabilizer of injection, film forming agent and pigment dispersing agent of coating, co-precipitation agent of insoluble drug, delay agent and lubricant of ophthalmic medicine and sustained release agent of controlled release dosage form, etc.
◆ Use method
PVP is a multi-functional synthetic polymer excipients, its function in the preparation and its molecular weight, dosage, solvent, solution concentration, temperature, processing technology and so on are closely related, so to obtain better preparation performance should first be familiar with the physical and chemical properties of PVP, starting from the target function of the prescription to achieve, select the best molecular weight, dosage, solvent, compatibility and process. For example, for injection injections, considering the deposition of PVP in the body, PVP with low molecular weight (K value less than 17) should generally be selected; For thickening liquid preparations, considering the amount and effect, PVP with higher molecular weight can be selected, such as K90; When used in tablets. If the prescription contains more hydrophobic drugs. Suitable for the use of dry powder mixed direct tablet or PVP aqueous solution as the adhesive granulation tablet; Ethanol solution of PVP can be used as binder for water-sensitive and heat-sensitive drugs. In spray granulation, PVP dry powder can be mixed with other dry components, and then sprayed into other liquid components to save time, can also be made into PVP and other components of the water dispersion, and then spray drying to obtain direct tablet raw materials; When used as an adhesive, the amount of PVP is generally 2 ~ 5%; However, the amount of PVP can reach several times of the bulk drug when it is used as a co-precipitant of insoluble drugs to improve the dissolution and bioavailability of drugs. PVP combined with silica gel and talc powder can improve the anti-viscosity of the tablet. PVP combined with cellulose ether can improve the crushing strength of the film. PVP is combined with cellulose ether, shellac and glycerol monoacetate to solve the surface bonding phenomenon, and polyethylene glycol to increase the softness of the film. Let’s wait.
In short, multi-functional and multi-specification PVP makes the formulation and process of the preparation have broad application space and operational flexibility.
◆ Experimental analysis
Nitroglycerin is a volatile drug. If water is used as solvent, the drying temperature of granulation is higher. Easy to cause drug loss, tablet weight difference; The alcohol solution of PVP is used as binder, which reduces the drying temperature, the loss of the drug in production and the non-uniformity of the product. The disintegration rate was improved by using PVP as binder.
The outer layer of the double-layer tablet is a quick-acting component, which can dissolve quickly and have pharmacological effects. PVP was used as binder in the nuclear tablets of the double-layer tablets. Due to its complexation with pseudoephedrine and the semi-permeable properties of the nuclear tablets, the drug played a slow release and long acting role.
Other powder or liquid preparations such as doxycycline, penicillin, chloramphenicol, insulin, rifampicin, sulfamide/trimethoprim, testosterone, progesterone, Mauritiin, defatted soybean lecithin can be used as dispersant and co-solvent.
When insoluble drugs and PVP exist in the form of co-precipitation, their solubility, dissolution rate and bioavailability are doubled and increased tenfold, which is due to the combination of PVP molecules and drug molecules through hydrogen bonding, so that drugs enter and exit completely water-soluble PVP macromolecules in molecular form. Thus inhibiting the formation and growth of crystals of insoluble drug molecules, becoming susaturated, thus greatly improving their solubility and dissolution rate, in addition to the examples provided in the above table, other such as beta-carotene, gramicitracin, nystatin, testosterone and many alkaloids and anticancer drugs extracted from plants, The solubility and bioavailability of PVP can be greatly improved by forming coprecipitant with PVP.
Adding PVP to the coating can increase the adhesion of the coating to the drug base material, and because of its excellent dispersion, the stability of the coating suspension is increased, the reunion and migration of pigments are avoided, and the fine cracks on the coating surface are prevented during drying.
◆ Precautions
1, this product has strong hygroscopicity, should be stored in a cool, dry environment, after use should be sealed; For accurate measurement, moisture measurement should be carried out before use.
2. If the aqueous solution of this product is not sterilized, it may be contaminated by microorganisms. If you want to store it for a long time, it is appropriate to add bacteriostatic agents such as sodium benzoate, potassium sorbate and sodium propionate.
3, for PVP used after the shelf life, the K value should be re-determined before use. In order to choose correctly.
4. This product can form molecular complexes with drugs with active hydrogen atoms, such as sulfathiazole, salicylic acid, phenobarbital, tannin, chloramphenicol, etc., which can change the physical and chemical properties of the original drug, and should be considered when formulation.