Application of pharmaceutical cascade crosslinked POvidone

Crosslinked POvidone, also known as insoluble polyvinylpyrrolidone (PVPP), is insoluble in water and common reagents. It is a super disintegrator in tablets and is used to disintegrate tablets and improve the release rate of active ingredients in tablets, capsules and pills. Insoluble polyvinylpyrrolidone is used as a swelling polymer in the pharmaceutical industry, which has a wide range of applications, because they have a decomposition effect on tablets, can hydrophilize various insoluble drugs, can stabilize various suspension agents, and have the ability to form complexes, as well as adsorption, etc., can be used as pharmaceutical additives.

Application of pharmaceutical cascade crosslinked POvidone

Used as a disintegrating agent

Crosslinked POvidone is one of the excellent new excipients developed in recent years. Because of its strong water absorption and expansion and excellent disintegration performance, it is called the three super disintegrators with crosslinked carboxymethyl cellulose sodium and crosslinked carboxymethyl starch sodium. The main principles of super disintegrating agents are: wicking, heat ofwetting, deforming recovery, parti-cle-particle repulsion, swelling, in practical applications, is often the result of a combination of effects. Crosslinked POvidone rapidly exhibits high capillary activity and excellent hydration ability, with little tendency to gel formation.

It is mainly used as a disintegrating agent for tablets, but also as a disintegrating agent and filler for pills, granules and hard capsules. The concentration of crosslinked POvidone used in direct tablet pressing and dry or wet pellet pressing processes is generally 2% to 5%. The disintegration time and dissolution effect of tablets prepared with this product will not change with time. The bulk density of particles decreased with the increase of the dosage of main drug, but the change of density was not obvious. The tablets obtained by using this product as disintegrator have high hardness, clean and beautiful appearance, short disintegration time and high dissolution rate. Using calcium carbonate as the model drug, the compression formability of 4 fillers and the disintegration time of 8 fillers were compared. The results showed that crosslinked POvidone, crosslinked sodium carboxymethyl cellulose, dry starch and calcium carboxymethyl cellulose with strong water absorption and swelling had better disintegration effect, and the disintegration time of different fillers were all within 2min.

The basic properties of main excipients (domestic microcrystalline cellulose, Avicel PH102 microcrystalline cellulose, lactose, crosslinked sodium carboxymethyl starch, crosslinked sodium carboxymethyl cellulose, crosslinked POvidone, low replacement hydroxypropyl cellulose) of the fast release solid preparation were studied. The test results showed that the water absorption of crosslinked POvidone was small, but its water absorption rate was fast.

For high hardness tablets, this rapid water absorption behavior of crosslinked POvidone can make water quickly enter the inside of the tablet through the “oil lamp core” effect, so that the tablet quickly disintegrates. Chinese medicine extract tablets contain a lot of extract, viscosity, hardness are large, sticky in water, not easy to disintegrate, the use of general disintegrators is often not ideal.

Except for microcrystalline cellulose, the other four kinds of disperse tablets can be used as disintegrating agents, and the combination of several disintegrating agents or the proportion of extract from disperse tablets should be considered for preparation of disperse tablets from gardenia extract.

Using fenoverine as the model drug, the effects of different concentrations of disintegrators crosslinked POvidone, crosslinked carboxymethyl cellulose sodium and carboxymethyl starch sodium on the disintegration time were studied. The results showed that when using the optimal concentration of crosslinked POvidone and other excipients, the rapid collapse of fenoverine tablets prepared by direct pressing method had low fragility, acceptable taste and short disintegration time.

2. Used as dissolution accelerator

Crosslinked POvidone is also used as a dissolution accelerator to greatly improve the dissolution of solid preparations. Using Telmisartan with poor water solubility as the model drug, Telmisartan fast release tablets were prepared by adding excipients crosslinked POvidone. The physical and chemical properties and dissolution in vitro of the particles and tablets were tested. It was found that the fast release tablets prepared with crosslinked POvidone had suitable hardness and dissolution time, and the dissolution rate was significantly increased. Compared with starch, the dissolution of paracetamol in Strong Yinqiao tablets was significantly improved by cross-linked POvidone, and did not change with storage time. In the preparation of Ganciclovir dispersible tablets with strong fat solubility, poor water solubility and low oral bioavailability, the cross-linked POvidone was selected as the disintegrating agent. It was found that the cumulative dissolution percentage of the dispersible tablets could reach more than 90% after 6 min. It was concluded that the dissolution release of Ganciclovir dispersible tablets was significantly better than that of ordinary tablets and capsules. The usage and dosage of crosslinked POvidone can be determined according to the main drug, auxiliary material and production process. The experiment shows that the best dosage range of crosslinked POvidone is 3% ~ 6%. The addition method of crosslinked POvidone has A significant effect on the dissolution of retinoic acid tablets, and internal addition or mixed addition is appropriate. In addition, the crosslinked POvidone has excellent reprocessability, which is particularly important in rework production, without adding additional disintegrators, the dissolution rate is not affected, and the production is convenient.