pvp pharmaceutical excipients industry application

PVP can be used as binder, excipient, coating agent, disintegrator, co-solvent, germicidal disinfectant, solubilizer, sustained-release agent, capsule shell, dispersion stabilizer, film forming agent and so on in the field of medicine and health. In some developed countries, such as the United States, Germany, Japan, etc., the application of PVP in the field of medicine and health accounts for about 40%-55% of the total consumption of PVP.
Application of PVP as drug excipients

PVP has good bonding properties and strong dissolution ability. PVP formed tablets, after taking in the digestive tract, first quickly dissolve, so that the tablet local expansion and disintegration, the release of drug fragments, into

It accelerates the dissolution and absorption of the drug and plays a role in the rapid play of the drug effect. PVP is soluble in water and most organic solvents. It is for these reasons that PVP has been widely used in pharmaceutical tablets, especially in China

In addition, examples of common drugs that use PVP for tablet bonding are as follows:

Compound sulfamethoxazole, aspirin, compound aspirin, paracetamol, vitamin C, pyridamine, dimethyltetracycline, clonidine, benzene sulfonamide, compound analgesic, chewable tablets for example

Ming, its formula is as follows:

Aluminum hydroxide dry glue 0.4g

Magnesium hydroxide fine powder 0.08g

Powdered sugar 0.02g

Mannitol fine powder 0.2g

10%PVP ethanol (50%) solution 0.03g

Magnesium stearate 0.015g

Peppermint oil 0.0005g

As a drug tablet adhesive PVP is mainly PVP-K30, its dosage depends on the requirements of the mechanical strength of the drug tablet and the nature of the drug itself, generally 0.5%-5%.

Another important use of PVP as drug excipients is co-precipitation agent, some drugs have good efficacy, but its fatal disadvantage is that the solubility in water is very small, resulting in its bioavailability is greatly reduced, the use of some water-soluble substances with these drugs co-precipitation, and then improve the solubility and dissolution rate of drugs, to reduce the dose, improve the efficacy of the effect. As a co-precipitant of insoluble drugs, PVP is being widely used.

The main reason why PVP is used as a drug coprecipitator is that carbonyl 0 in PVP molecules can be combined with active hydrogen bonds in insoluble drug molecules. On the one hand, relatively small drug molecules become amorphous and enter PVP macromolecules. On the other hand, hydrogen bonds do not change the water-soluble nature of PVP. Therefore, the result is that the insoluble drug molecules are dispersed in the PVP macromolecules by hydrogen bonds, making them change

It is easy to dissolve, and the solubility changes after some insoluble drugs form coprecipitates with PVP are as follows:

The solubility ratio of drug name to PVP coprecipitate was increased by multiple

Phenytoin 1:52.3

Morpholine 1:538

Reserpine (297-420um) 1:315

As a drug tablet adhesive PVP is mainly PVP-K30, its dosage depends on the requirements of the mechanical strength of the drug tablet and the nature of the drug itself, generally 0.5%-5%.

Another important use of PVP as a drug excipient is co-precipitation agent, some drugs have good efficacy, but its fatal disadvantage is that the solubility in water is very small, resulting in its bioavailability is greatly reduced, the use of

Some water-soluble substances co-precipitate with these drugs, thereby increasing the solubility and dissolution rate of the drugs, achieving the effect of reducing the dose and improving the curative effect. As a co-precipitant of insoluble drugs, PVP is being widely used

The application of.

The main reason that PVP is used as a drug coprecipitator is that carbonyl O in PVP molecules can be combined with active hydrogen bonds in insoluble drug molecules, on the one hand, making relatively small drug molecules unstable

On the other hand, the hydrogen bond does not change the water-soluble nature of PVP, so the result is that the insoluble drug molecules are dispersed in the PVP macromolecules through the hydrogen bond, making it change

It is easy to dissolve, and the solubility changes after some insoluble drugs form coprecipitates with PVP are as follows:

The solubility ratio of drug name to PVP coprecipitate was increased by multiple

Phenytoin 1:52.3

Morpholine 1:538

Reserpine (297-420um) 1:315

The increase of solubility of insoluble drugs in human body also correspondingly improves the bioavailability of drugs. For example, the bioavailability of drugs increased by 1.55 times after phenytoin co-precipitation with PVP, and the increase of solubility after co-precipitation of insoluble drugs was related to the molecular weight of PVP and the amount of PVP. In the case of the same amount (quality) of PVP, the increase rate of drug solubility decreases in the order of PVP-K15>PVPK30>PVPK90, because the solubification effect of PVP itself changes in the order of PVP-K15>PVPK30>PVPK90, and PVP-K15 is generally used more.

The solubility increase of insoluble drugs and PVP coprecipitates varies with the amount of PVP in a complex way. For PVP with a certain molecular weight, the number of molecules of each PVP molecule can bind to is certain, and insoluble drugs often have a certain crystal state. When the amount of PVP is not enough to bind a certain amount of drugs and make them in an amorphous and dispersed state, The drug was still mainly in crystalline state, and the solubility changed little. When PVP must reach a certain content, the drug appears as an amorphous dispersion system, and its solubility can be significantly increased to achieve the purpose of rapid dissolution and absorption. For different drugs, the amorphous dispersed PVP content is not the same as that of PVP co-precipitation, such as 70% of cyclohexamine acetate, and B-carotene, chloramphenicol, dexamethasone, hydroprednisone, streptomycin, tetracycline and testosterone can be increased in human solubility and bioavailability by PVP co-precipitation.

Similarly, the use of hydrogen bond association between PVP molecules and drug molecules can play the opposite effect of solution-increasing and quick-acting, slow release effect, control the degree of association between PVP molecules and drug molecules, and enable drug molecules to be slowly released in the human body after association, delay the dissolution rate, and prolong the effect of drug efficacy. PVP for penicillin, chloramphenicol, insulin, sodium salicylate, procaine, cortisone and so on

All drugs have the effect of prolonging their effects.

In solid drugs, PVP can be used as a binder, solubilizer, disintegrator and delay agent, as well as a drug film coating, drug capsule shell and controlled release film. Drug film coat and glue made of PVP

The capsule shell is not easy to break in a dry environment, and the appropriate amount of PVP and other insoluble polymers together to form a permeable membrane of different thickness and different pore size can adjust the rate of drug passing through the membrane, so as to achieve the effect of controlled release.

The application of PVP in liquid drugs

In addition to the many applications of PVP in solid drugs, PVP also plays an important role in injection and ophthalmic medicine. For example, PVP is used in some injections, because of the association between it and drugs, so that one side plays a role in solubility, on the other hand, for some agents that will crystallize or precipitate after too long, PVP can play a role in dispersion and stability. PVPK17 used in ophthalmology can reduce irritation to the eyes and prolong the action time of ophthalmology.