Application of chitin and carbomer and other pharmaceutical excipients

The application of new medicinal excipients has a significant effect on the improvement of the performance of pharmaceutical preparations, the improvement of bioavailability and the slow and controlled release of drugs. Therefore, the replacement of medicinal excipients has become more and more concerned by pharmacy workers. focus. With the increase of research in related fields, various new types of pharmaceutical excipients have been continuously introduced and widely used in practice. The author below introduces the application of several new types of pharmaceutical excipients.

Chitin (chitin)

It is a kind of natural high molecular substance containing aminopolysaccharide, which is widely found in marine organisms such as shrimp, crab and other carapace, and is rich in resources. Chitin is chemically modified to produce a variety of derivatives, such as partial deacetylation to obtain chitosan, which is also an important pharmaceutical excipient. Chitin is completely deacetylated to obtain chitosan, which is also a valuable pharmaceutical excipient.

Tablets: Chitosan can be used as an auxiliary material for direct compression of powder, and has excellent properties, and can be used in drug-controlled, sustained-release drug delivery systems. If chitosan is added to common excipients (mannitol, lactose or starch), the angle of repose can be lowered to improve the fluidity of the mixed powder. The chitosan was directly mixed with lactose and propranol hydrochloride, and the dissolution test showed that it was a zero-order release. Gaso-chromatography was used to study the random biopsy of 10 male healthy volunteers with a single dose of oral and commercially available nifedipine-based nifedipine tablets. The bioavailability of the latter was 151.8% compared with the former. Significantly improved the bioavailability of nifedipine and significantly improved drug absorption.

The tablet formed by the direct powder unpressed tablet is coated with a foamed chitosan film on the outside to prepare a sustained release gastric floating sheet. The drug (Centreol Hydrochloride) can also be directly compressed by mixing with chitosan, lactose or the like to prepare a sustained release tablet. The aspirin granules prepared by using the aqueous solution of chitosan in acetic acid as a binding agent, the tablets formed by the wet tableting showed sustained release in the artificial stomach and intestinal juice. In addition, the theophylline controlled release tablets prepared by the hydrated colloidal skeleton system of chitosan, carbomer-934P and citric acid can form a non-erodible matrix sheet when the amount of chitosan exceeds 50% of the tablet weight; At 33%, a rapid matrix sheet can be formed; when it is used in an amount of less than 10%, it can be used as a disintegrating agent.

Microspheres and microcapsules: Chitosan microspheres can be prepared by emulsion crosslinking, spray drying, precipitation/coacervation, etc., which have the characteristics of controlled release and increased drug targeting. If the prepared insulin microspheres release insulin at a constant rate, the release can be up to 80 hours. Intravenous microspheres, all of which have a particle size of less than 1.4 μm, all pass through the pulmonary circulation. The 7 to 4 micron microspheres mainly stop the amine microspheres, and the drug encapsulation efficiency increases significantly with the increase of chitosan content. Similarly, using chitosan, sodium tripolyphosphate and other auxiliary materials, pharmaceutical microcapsules can be prepared. For example, in 20 g of theophylline and 6 g of sodium tripolyphosphate, 200 ml of ethyl acetate and 22 to 28 ml of water are slowly added. The microparticles which can pass through the No. 3 sieve are prepared, and 3 g of the microparticles which are added to the shell concentrate are prepared, and the microparticles are encapsulated to form a microcapsule, which has a sustained release effect.

In addition, chitosan and its derivatives can also be used as gels, bioadhesives, wound healing agents, etc., and their colloidal and film-forming properties can be used to achieve different formulation effects. In addition, it also promotes the dissolution of poorly soluble drugs and promotes absorption. For example, phenytoin sodium can be added to the shell to improve the dissolution of the drug by 7 to 8 times. After the griseofulvin and chitosan (or chitosan) are mixed at a ratio of 1:2, they are pulverized in a ball mill for 24 hours, and the drug elution property is increased by 2 to 3 times than that without treatment.

Carbomer

It is a family of acrylic polymers crosslinked with acrylic acid and alkyl sucrose. They are easily soluble in water and form an acidic colloid. At a pH of 6 to 10, the viscosity of the carbomer gel is large. The addition of an inorganic or organic base such as triethanolamine neutralizes a clear and thick gel which is non-toxic, non-irritating and has good coupling to the skin. They can be divided into different types of low, medium and high viscosity. China has medicinal standards, which can be used as a binder for tablets and thickeners for ointments, creams and other pharmaceutical preparations. It should be noted that the viscosity type and the word "P" can be used as an auxiliary preparation for internal use.


The carbomer solution can be gelled to a stable hydrogel at a pH of 6-12, which is selected as the main matrix for the preparation of semi-solid preparations, and satisfactory results are obtained. The utility model has the characteristics of quick release, no greasy property, easy spreading, no irritation to skin and mucous membrane, mixing with aqueous solution, absorbing tissue exudate, and facilitating secretion discharge, and is particularly suitable for treating seborrheicity. skin disease. For example, methotrexate gel has a good therapeutic effect for the treatment of psoriasis and rheumatoid arthritis, and carbomer matrix sulphur ointment can also significantly improve the therapeutic effect of sulphur.

Because carbomer is a light-weight, hygroscopic powder, it has strong ductility and good coupling with the skin after swelling in ethanol, and can be a good film-forming material for coating agents. Such as salicylic acid, ketoconazole, dexamethasone coating agent, each formulation is stable in nature, and does not contain visible solid components, sealed storage at room temperature, easy to spread, fast drying after coating, film has Good adhesion, uniformity, easy to elute, no pollution to clothing.

In addition, carbomer can also be used as a binder for tablets and as a sustained release material for coating materials and pharmaceuticals, and as a preparation base for emulsifiers, suspending agents, gels and suppositories.

Azone

Azone has received extensive attention and application as a transdermal enhancer that accelerates the transdermal absorption rate of drugs without causing severe irritation and damage to the skin. Modern pharmacy research believes. Transdermal administration not only has a local therapeutic effect, but also requires systemic treatment through skin administration. The development and utilization of Azone makes this idea a reality. For example, if aminophylline is 80%-90% orally inactivated by liver metabolism, its intramuscular injection can be rarely used because it can cause local redness and pain. The intravenous drip is too fast or the concentration is too high (blood concentration >5 μg/ml) Can strongly excite the heart, causing heart palpitations, arrhythmia and so on. The use of Azone to prepare aminophylline transdermal emulsion (O / W), topical topical application can effectively treat bronchitis. It was observed that the effects of different concentrations of Azone on the permeation of isolated skin of aminophylline mice showed that aminophylline creams of different concentrations of Azone can increase the skin penetration of the drug. Azone was measured (mouth + ca) in promethazine, and the results showed that there was a significant difference in transdermal absorption between 0.5% and 3.0% of Azone and Azone-free promethazine wipes (P<0.05). It is determined to be 0.5% Azonezui.

In addition, Azone's transdermal absorption and corneal permeability to tinidazole and fluconazole also demonstrated significant osmotic effect. Some people have verified the Azone penetration-enhancing effect of 81 different kinds of chemicals and natural drugs. It is proved that: 1Azone has different effects on transdermal absorption of different drugs, and has different degrees of osmotic effect on water-soluble drugs, but some fat-soluble drugs. Strong drug effects are not obvious and may even have a negative effect. The usual amount of 2Azone is <10%. It is not the higher the concentration, the promotion of transdermal absorption is too strong, and the excessive amount will have the opposite effect.

Source: Search for medicine online

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