SI7812608A8 - Process for the preparation of bioactive adsorbent - Google Patents

Description

The present invention relates to the field of pharmacy, specifically to a novel process for the preparation of a bioactive adsorbent for use in medicine, cosmetics, physical therapy and agriculture. The new bioactive adsorbent prepared according to the invention is designed to produce effective healing and soothing effects when applied in the form of dressings, as a hot or cold patch and for similar purposes.

The bioactive adsorbent prepared according to the invention is distinguished by its healing and soothing effects when applied externally to the affected skin surfaces. When used in agriculture, it protects wrapping materials against fungal and bacterial attack and is also useful for protecting certain nutrients from fungal and bacterial attack.

A technical problem

Thixotropy is crucial when embedded in all supporting materials. Likewise, the incorporation of fatty substances as well as other difficult-to-mix substances without emulsifier is possible only at such quality. Therefore, the preparation of thixotropic bioactive adsorbent is a technical problem that has not yet been satisfactorily solved by any known method.

The state of the art

Aluminum hydroxides and aluminum hydroxides are well-known compounds and have been well established in industrial use. These compounds can occur in a variety of crystalline forms, which can have a significant effect on their properties. Examples of such various forms are known as hydrargylite, bayerite, nordstranite, boehmit, diaspor, pseudoboehmit, etc.

Basic aluminum chlorides - or aluminum chlorides, as they are sometimes called - are also well-known compounds of formula Al ₂ (OH) 6_ _n Cl _n (n = 1 to 5). Such compounds are widely used in deodorizing preparations, anti-perspirants and fungicides.

In various ways, efforts have been made to prepare aluminum chloride hydrates with different structures in order to improve their properties for various uses (e.g., e.g., U.S. Patent No. 3,655,329). A common problem with such known aluminum chloride hydroxides is their water solubility. So far, the preparation of thixotropic Alhydroxy Chloride has not yet been fortunate.

Description of solution to a technical problem with implementation examples

However, we have now found that all of the above problems are solved in the preparation of a water-insoluble thixotropic bioactive adsorbent using a novel process in which aluminum hydroxy chloride of the general formula [A1 (OH) 3] _x A1 (OH) ₂ C1 in which x varies between 4 and 6, is converted by water into thixotropic aluminum hydroxide of the general formula {[A1 (OH) ₃ ] _X A1 (OH) ₂ C1}. nH ₂ O in which x has the above meaning and n means in the case that x = 4, 90 to 1110, and in the case where x = 5, then n is 108 to 1123, in the case where x = 6, however, n is 120 to 1240, at ambient temperature and pH of the reaction mixture, 3.5 to 5, then 20 to 25 wt.% alginate or 0.3 to 0.7 wt.% KC1 as well as 1 to 4 wt.% disinfectant, bacteriostatic are added as needed , a bactericidal or antifungal agent or physiologically tolerable organic acid or fat and, where appropriate, applied or applied to (v) a porous, physiologically acceptable carrier, in an amount of 10 to 35 g per 100 cm ^{2 of} material, at a moderate temperature and at or below- pressure.

Pulp or open pore polyurethane foam is used as the carrier.

The compound prepared according to the process of the invention contains a specific amount of water, which is part of its structural formula, that is, it is a true hydroxide and not a mere mixture with water, as can be seen from the fact that the product is insoluble in water. With the amount of water outside the area shown by the formula, the structure collapses and the resulting products do not have the chemical and physical characteristics that are characteristic of the products obtained according to the invention. In addition to the precisely specified amount of water, for a successful conversion process, i.e. hydrolytic polymerizations of Ap +, which also requires certain reaction parameters, namely a moderate temperature (i.e. ambient temperature) and a narrow range of medium or high temperatures. moderately acidic pH between 3.5 and 5.

Use an inert carrier, e.g. of cellulosic material (paper, cellulose, cotton, etc.) or any other suitable carrier, such as foam, fabric, mixed goods, non-woven fabric, gauze and the like. Use an appropriate amount of effective ingredient to absorb or impregnate said carrier, the amount of effective ingredient being such that it provides as much effective amount of effective material as said carrier can tolerate. Typical values for such quantities are 10 to 35 g per 100 cm ^{2 of} material, such as plastic foam or gauze.

The bioactive adsorbent of the invention exerts an astringent effect on human skin without causing inappropriate stimulation. It exerts a certain acid binding effect and is well tolerated by human skin due to its inherent pH of about 3.5 to 7. Because it is a thixotropic system, substances such as lanolin can be easily incorporated into it; later it is generally obtained as a stable system with aqueous constituents only in relation to other constituents, as surfactants and the like. Performs anti-phlogistic and soothing action.

The starting compound is in the form of microcrystalline aluminum hydroxide, in which part of the hydroxyl groups is replaced by chlorine to give the molar ratio of aluminum to chlorine defined above. The thixotropic product obtained from the metabolism of said hydroxy chloride with water forms an oxide and can be easily liquefied using mechanical forces such as shaking, lubrication or the like. The viscosity is reduced by about 100 times, from a value in the range of 10,000 cp to about 100 cp.

Bioactive adsorbents can be applied directly to the skin or mucous membranes for medical use. It can be given together with the wrappers that serve as a carrier for said effective ingredient. The water from these adsorbents comes out gradually, leaving an active coating that allows the skin to breathe and retain its effectiveness over a long period of time.

The bioactive adsorbents prepared according to the invention are used externally and thus adsorb very little of the substantially insoluble material, if any. Toxicity testing shows that administering oral doses of about 5 g / kg of thixotropic aluminum hydroxy chloride to the rat did not cause any significant toxic effects.

On the back of the wrapper may be a layer of e.g. made of aluminum foil and can be used as a hot compress for a longer useful life of the application.

When used in conjunction with a suitable carrier, impregnate said carrier with an effective pressurized ingredient: under reduced pressure by coating, coating or spraying. Thus, a substantially homogeneous product is obtained which carries a predetermined amount of effective material per surface unit.

The bioactive adsorbents prepared according to the invention can be used in agriculture to protect against damage from various pests, especially fungi. Extensive tests have shown that thixotropic material can be applied directly to various types of agricultural products, such as cereals, e.g. maize, oats and the like, and various types of fruits, etc. A thin coating is formed that adheres well to the surface of the processed agricultural product and this thin film forms a protective barrier against various injuries, especially against fungal attacks. Prevention of fungal growth prevents the formation of aflatoxins, which are now considered a serious health threat. Under the influence of rain or watering, the protective layer does not wash out and retain its effectiveness over long periods of time. Laboratory tests were carried out with a variety of fruits, such as strawberries, peaches, citrus fruits, cherries, grapes, pears and apples. Tests were also carried out with vegetables such as cucumbers, eggplants, potatoes, tomatoes. They were sprayed or coated with a colloidal suspension of a bioactive adsorbent according to the invention containing a small amount of non-toxic surfactant. The resulting non-toxic and harmless coating significantly reduces the onset of fungi, significantly reduces oxidative effects, delays the formation of spots and the evaporation of water is significantly reduced. So e.g. the citrus fruit retained its fresh appearance and lost significantly less weight than similar unprocessed fruits. Meat and meat products such as meat, sausages, smoked meats, and the like can be protected from fungal attack and weight loss by this protective coating.

The tests were performed with cereals and maize and laboratory tests showed a significant reduction in fungal involvement on the treated samples. We further found that the treated grain dries quickly, its shrinkage is reduced, and less dust is generated. This gives a mostly even film on the surface that shows good adhesion and is slightly affected by watering or rain. The effective ingredient is characterized by very low solubility, there is virtually no diffusion into the treated product. Due to its nature, effective suction is very stable.

The bioactive adsorbent prepared according to the invention exhibits an essential quality in its consistency. This is especially important and new for its type of use and efficiency.

Thixotropic aluminum hydroxide can be mechanically applied by rolling, coating or spraying as well as displacement in any quantity required on or in a suitable support.

Thixotropic aluminum hydroxide can be readily distributed in minimal or maximum quantities in the same and homogeneous manner without draining and strongly adhering to the porous, homogeneous and lipoid surfaces of materials such as textiles, synthetic and natural materials.

There is no need to use an emulsifier to add further additives to the bioactive adsorbent.

The bioactive adsorbent prepared according to the invention is stable over a long period of time. It can be translated into any required consistency by applying pressure ah mechanical forces as a vacuum. This is very important for its economic use in medicine, cosmetics and agriculture.

Adsorbent is reversible for binding large volumes of moisture ah water. It is insoluble in water and difficult to rinse. Its osmotic properties remain unchanged and are among the strongest known aluminum compounds.

Adsorbent shows prolonged activity in low doses. Furthermore, it has reversible adhesive strength and is therefore continuously effectively reactivated. Due to its insolubility, there is an increased effect, no toxicity and therefore controlled use is possible.

Fatty, germicidal, fungicidal, fungistatic ah bacteriostatic agent, citric, lactic, tartaric a propionic acid, glycerol, polyethylene glycol, collagenase or polyalkylene may be used as an optional additive.

The new process for the preparation of bioactive adsorbent will be illustrated in the following by a detailed description, which should in no way limit the scope of the invention.

EXAMPLE 1

Colloidal aluminum hydroxy chloride containing from about 5: 1 to about 6: 1 aluminum atoms per 1 chlorine atom is allowed to react at ambient temperature at a concentration of about 10 wt. % with water. The pH is about 4.0 and at rest the product viscosity is about 10,000 cp. In heavy shaking, the viscosity is reduced to about 100 cp.

EXAMPLE 2

Colloidal aluminum hydroxy chloride containing from about 6: 1 to about 7: 1 aluminum atoms per 1 chlorine atom is allowed to react at ambient temperature at a concentration of about 10 wt. % with water. The pH is about 4.0 and at rest the product viscosity is about 10,000 cp. In heavy shaking, the viscosity is reduced to about 100 cp.

EXAMPLE 3

The thixotropic substance is prepared by incorporating 10% cocoa butter into the composition of Example 1 in the presence of about 3% potassium chloride, with vigorous stirring.

EXAMPLE 4

The substance product was prepared by incorporating 10% of the amount of a non-alkaline, soap-like composition into the substance according to Example 1.

EXAMPLE 5

The thixotropic product was prepared by incorporating 5 g of lanolin into the product of Example 1. Lanolin was gradually introduced under vigorous stirring, then about 0.3 g of potassium chloride per 100 mg of thixotropic substance was added. A uniform, stable product is obtained.

EXAMPLE 6

The thixotropic product is prepared by incorporating about 1.0 g of micronized silver sulfadiazine into the product of Example 5. This gives a thixotropic product that is particularly valuable for the treatment of infected wounds.

EXAMPLE 7

The thixotropic product is prepared by incorporating 1 to 3 wt. % of iodine-polyvinylpyrrolidone in the product of Example 1. A germicidal product is obtained.

EXAMPLE 8

The thixotropic product was prepared by incorporating 1 to 5% alginate into the product of Example 1.

EXAMPLE 9

The substantive product is prepared by incorporating about 70 wt. % powdered polymer foam, as powdered polyurethane, into the liquefied product of Example 1. This gives a kneading material which hardens upon cooling or evaporation of the majority of the water contained.

EXAMPLE 10

The highly porous polymer foam (polyurethane foam) in the form of a strip is impregnated by coating with the liquefied material prepared according to Example 1. Use an amount of about 30 g of said substance per 100 cm ^{2 of} said support. By exerting pressure on a foam carrying thixotropic material to give a volume of 50 to 70 vol. %, a substantially uniform distribution of said effective ingredient throughout the carrier is achieved when the pressure after compression of said foam is released. This foam can be cooled and used for an effective application of cold over a long period of time.

EXAMPLE 11

The polyurethane tape of the type used in Example 7 is applied to a thin, nonwoven fabric and impregnated as shown in Example 10 by applying a thixotropic material on the open side of the foam. Non-woven fabric forms a suitable carrier for application to certain types of wounds.

EXAMPLE 12

The gauze is impregnated to obtain about 20 g of Example 1 product per 100 g of gauze. The impregnation is performed by impregnation or coating.

EXAMPLE 13

The non-woven cellulose cloth was soaked in the manner shown in Example 10. Use 10 g of the material of Example 1 per 100 g of cloth.

EXAMPLE 14

The face mask is prepared from the product of Example 3 and a small amount of avocado juice is embedded therein. The mask is applied to the face in the form of a kneading product according to Example 10 and left in a layer thickness of about 4 mm for 20 minutes. Most oily deposits are removed, the redness of the skin is reduced significantly and the skin tense. So the skin is cleansed and refreshed.

EXAMPLE 15

The product obtained in the sense of Example 1 is applied with the help of flakes of cotton wool over the scalp to give loose, beautiful hair, and the sebaceous glands are cleansed. The radiant appearance of the skin disappears.

EXAMPLE 16

The impregnated tape of Example 10 is applied to edema and various wounds after surgery, wounds after accidents and burns to the third stage. We experience a pronounced effect of stimulation, granulation and accelerating smooth epithelialization without stimulation. The pain is relieved and the itching is reduced. A pronounced anti-inflammatory effect is observed and the wounds heal rapidly without infection with bacteria or fungi, since bacteria and fungi cannot grow on the surface coated with the effective material of the invention. The dressing does not cling to the wound and can be easily removed as desired without damaging the underlying tissue.

The high water content causes continuous steady evaporation of the water and this results in the effective penetration of the aluminum compound into the tissues. The wound edge is maintained in a soft state, and preventing the wound edge from solidifying is one of the main effects of new compositions. When a commitment is removed, there is no harmful or unwanted ingredient left that should be eliminated.

We tested new products on a few patients. Among these was the case of a patient with an open, extensive wound over the surface of the abdomen, about 40 cm x 5 cm. This wound did not heal in 2 years. We made an appointment and replaced it from time to time (70 times, twice a day). At the end of the 35-day period, the wound was clean, the inflammation was gone, smooth epithelialization occurred, allowing skin transplants and healing of the rest of the surface. The patient was discharged from the hospital after this treatment and the wound healed completely.

A 90-year-old patient with spastic right arm and decubitus under armpit for about 2 years, without effective treatment in the usual way, was treated with a refrigerated dressing as in Case 10. This was changed daily for 1 week. After that time, we achieved full healing.

The patient with second-degree burns on both legs was treated with the application of bandages in the sense of Example 10. We changed them three times a day. After 6 days, the wound was clean and allowed a skin transplant.

EXAMPLE 17

The patient with leg fractures was treated by applying bandages in the sense of Example 10, which were cooled prior to administration. The appointments were changed every 30 minutes and after 4 hours there were no more edema on the leg and she was ready for surgery.

EXAMPLE 18

Thixotropic aluminum hydroxide prepared in the sense of Example 1 was used to impregnate non-woven fabric or special absorbent paper. The applied amount was 3 g per unit and they were packed in individual packs with 2 1/2 x 3 wraps, which were practically airtight. After the preferred embodiment, we added some fragrances to create a refreshing effect.

EXAMPLE 19

The product in the sense of Example 14 was used for intimate care. Thus, a refreshing effect and antifungal activity were obtained. The application to the mucous membranes caused a significant effect within 4 hours.

EXAMPLE 20

A product consisting of 60 wt. parts of the substance according to Example 1 with 40 wt. parts of polyurethane foam in powder form. Suppositories were formed from this product, which were used to treat hemorrhoids. These suppositories were frozen and administered in this form. Slow melting leads to an even distribution of the effective ingredient, which results in relief and improved effect.

EXAMPLE 21

The impregnated tape in the sense of Example 10 was used in frozen form for cryotherapy. It can be effectively used to treat muscle spasms, swelling and inflammation of the musculoskeletal system, treat post-operative edema, treat phlebitis and rheumatoid arthritis.

The patient with myositis in the left gastrocnemius muscle was treated with such an ice band, at 15 minutes each. After the initial analgesia, we began the mobilization exercises and continued for 10 minutes. After the commitment was removed, the process was repeated with a fresh commitment. The therapeutic results thus obtained were much faster than conventional treatments.

EXAMPLE 22

Non-woven cotton was mixed with the product in the sense of Example 1. After the initial drying, the shoe insert was cut and placed on the sole. A person with prolonged excessive sweating (hyperhidrosis) wore a sock. After one day of regular activity, the leg with the insert was without sweat, while the other leg was sweaty. The cartridge also prevented the development of fungi.

The second test was performed with a product made of polyurethane foam impregnated with the product in the sense of Example 1. It was used for an armpit application. After a day, the surface was dry. The other armpit was wet and a pungent odor could be felt.

EXAMPLE 23

We tested the product in the sense of Example 1 to evaluate its activity on fruits and vegetables. The peach was halved and treated one half by applying a thin layer of such composition. After 4 hours, the treated surface was clean and free of staining. The other, untreated surface, showed brownish colored areas. After a further 10 hours, the treated area was still bright while the untreated was covered with fungal growth. We put the two halves in contact with each other and left them overnight. The untreated sessions further deteriorated, while the treated ones remained bright.

A further test was performed with a further peach. There was no fungal infection on the treated surface after 48 hours, during which the untreated surface was severely damaged.

The peach was coated with a thin layer of the product of Example 1 and placed between slightly contaminated peaches. After one week, the untreated fruit was completely covered with fungi, while the treated fruit was completely clean.

EXAMPLE 24

Highly effective adsorbent material for medical use, especially in general surgery and dental practice, was prepared by impregnating a suitable open-pore polymer foam as a polyurethane foam with a thixotropic substance in the sense of Example 1. The excess was removed by performing pressure and used the resulting material as adsorbent. It was very effective for its intended purpose and could be used several times after the adsorbed material had been expelled. It is clear that very little colloidal aluminum hydroxy chloride is lost from the carrier foam. In addition to the adsorptive, there is a marked astringent effect.

EXAMPLE 25

The filter material was impregnated with the product in the sense of Example 1. This gave us a very effective filter material that can be conveniently used as a filter for cigarettes, for filtering industrial contaminants and for protecting the environment.

For:

BERT KUY

AMBLU

ad-oor / lir aaa

Claims (3)

A process for the preparation of a bioactive adsorbent, characterized in that aluminum hydroxy chloride of the general formula [A1 (OH) ₃ ] _X A1 (OH) ₂ C1 (I) in which x varies between 5 and 6 is reacted with water into thixotropic aluminum an hydroxide of the general formula {[A1 (OH) ₃ ] _x A1 (OH) ₂ C1}. nH ₂ O (Π) in which x has the above meaning and in the case where x = 5, n means 108 to 1123, and in case x = 6, n is 120 to 1240, at ambient temperature and at pH of the reaction mixtures 3.5 to 5, then 20 to 25 wt. % alginate or 0.3 to 0.7 wt. % KC1 as well as 1 to 4 wt. % disinfectant, bacteriostatic, bactericidal or antifungal agent, such as Ag-sulfodiazine or J-polyvinylpyrrolidone, or physiologically tolerable organic acid or fat such as lanolin or cocoa butter or avocado juice, and optionally applied to or infused into porous, physiological 10 to 35 g per 100 cm ^{2 of} material from ambient temperature to fat melting point. (Priority 12 November 1977). Method according to claim 1, characterized in that the cellulose or open-pore polyurethane foam is used as the carrier. (Priority 12 November 1977). Process according to Claims 1 and 2, characterized in that in formulas I and II x is between 4 and 5, and in formula II n is between 90 and 1110 or. 108 to 1123. (Priority 9 November 1978). For: BERT KUY ABSTRACT A process for the preparation of a bioactive adsorbent in which aluminum hydroxy chloride of the general formula [Ai (OH) ₃ ] _x Ai (OH) ₂ Cl in which x varies between 4 and 5 is converted by water into thixotropic aluminum hydroxide of the general formula