The role of methyl silicone oil and drugs
The role of methyl silicone oil and drugs
Methyl silicone oil is widely used in the field of medicine. As a pharmaceutical excipient and active ingredient, it not only has excellent performance but is also very safe.
1. The best application of hydrophobic agent
1. Preparation of acid-resistant capsules
Glycerin 22.02kg, distilled water 34.13kg, dimethyl silicone oil 10kg, add gelatin 43.85kg, dissolved under reduced pressure at 70 ~ 80 ℃, usually made into capsules. The mixed solution of formaldehyde / acetone (1/60) is sprayed on the capsules to prepare. Due to the hydrophobic effect of dimethyl silicone oil, the prepared capsules do not disintegrate in acid gastric juice for 2 hours, dissolve in alkaline intestinal solution for 200 to 620 seconds, are stable to enzymes and temperatures, and have good mechanical strength.
2. Polishing of sugar-coated tablets (glazing agent)
During the polishing operation, the Sichuan wax fine powder with 2% dimethyl silicone oil is added to the color-coated tablets for polishing. The sugar-coated tablets are brighter and more beautiful than the dimethyl silicone oil, and the color surface is bright and beautiful. Moisture-proof effect, to ensure that the sugar-coated tablets do not discolor or mold during the storage period.
3. Film coating materials
It is used as a plasticizer for film coating materials. It uses the hydrophobicity and oxygen resistance of dimethyl silicone oil to isolate the core from the outside, is not affected by moisture and oxygen in the air, does not absorb moisture and deteriorate, and the coat is firm and smooth.
2. The best condensing agent for water-soluble dropping pills
The behavior of dripping pills in the condensate includes spreading, droplet formation and mixing. Generally, when a liquid with a small surface tension is placed in a liquid with a high surface tension, the surface will spread, otherwise it is easy to form droplets. Dimethicone is the most water-soluble dripping pill condensate with the smallest surface energy (liquid paraffin 0.035N / m, vegetable oil 0.035N / m, dimethicone 0.021N / m).
There are many types and specifications of dimethicone. You can adjust the temperature and select different types of dimethicone to adjust the formation and precipitation speed of droplets in the condensate to achieve the best process and quality conditions. There are hidden dangers of toxic substances in contaminated petrochemical products and discoloration and mildew of water-based dripping pills, which cannot be guaranteed by liquid paraffin and vegetable oil.
Especially the dripping pills using S-40 (polyoxyethylene monostearate) and poloxamer as the matrix must use dimethyl silicone oil as the condensate, and cannot use liquid paraffin as the condensate. Silicone oil can increase the solubility of water-insoluble active drugs, which is conducive to the absorption of drugs; poloxamer (poloxamer) can not use liquid paraffin as a condensate because of its hygroscopicity. (Simethicone is regularly processed in the production of dripping pills; due to the high price of dimethicone, it should be recycled as much as possible in production. Dimethicone that has been used will be mixed with foreign objects. The broken pellets can be removed by filtration, static precipitation or centrifugation; in addition, the common foreign body is water. When using dimethicone mixed with oil and water as the condensing agent, the dropping pills may be dissolved, deformed or even unable to condense Hard, the method of removing the water in the dimethicone is: freeze the water-containing dimethicone at -4 ℃, take it out after the water condenses into ice, and filter it quickly to remove it.
3. The only effective antistatic agent in the production of micropowders and pellets
Pills or pellets establish fluidization in the fluidized bed. When the material passes through the spray area, the mist particles of the clothing material are sprayed on the surface, and they are attached after bonding, spreading, and drying to form a small piece of coating film. After repeated spraying, the film gradually expanded, and finally formed a continuous overall layer to achieve the purpose of coating. In order to ensure safe operation and complete dispersion of the materials, so that the powder will not stick and form agglomerates, antistatic agents should be added when the powder is sprayed.
Dimethicone is currently the only medicinal adjuvant with antistatic effect. The amount of antistatic agent used is 0.1% of the weight of the powder.
4. Used as lubricant in solid preparations
Lubricant refers to the general name of the auxiliary materials added to the material to be compressed before tableting to make it have or increase fluidity, anti-adhesion and lubricity, so as to facilitate the tableting process. Lubricants are classified into three types according to their mechanism of action; lubricants are auxiliary materials that reduce the friction between granules or tablets and the die.
After cleaning the tablet die, smearing a layer of dimethicone can also solve the sticking problem of some varieties.
1. Slow-release aspirin tablets
Take aspirin powder 1000g (crystal diameter 0.1770mm), ethoxyethyl cellulose (containing 12% ethoxy group) 70g, dissolved in 300ml (1: 1) toluene-dichloromethane solution and 30g containing dimethicone Toluene solution, starch 400g, glycerol palmitic acid fatty acid ester 300g, talc powder 50g, microcrystalline cellulose 100g, usually made into tablets.
2. Compound Paracetamol Capsules
Take the aspirin granules to 50 ℃, coat with 1: 1 copolymer of methacrylic acid and methacrylic acid ester and 0.045% AF emulsion (defoamer), and dry at 37.8 ℃ for 24h in a boiling drying bed, then Weigh 52.144g, add 0.203g of sodium lauryl sulfate, 41.45g of paracetamol, 0.363g of dimethicone, and 0.145g of polyoxyethylene dehydrated monooleate. The capsule weighs 700 mg, and each capsule contains 325 mg of aspirin and paracetamol.
3. Ibuprofen sustained-release tablets
Take ibuprofen 58.25%, lactose 14.50%, dicalcium phosphate 12.60%, glyceryl behenate 11.65%, magnesium stearate 1.0%, talc + silicone oil (4: 1) 2.0% to make tablets.
5. Used as a release agent in the production of suppositories and other preparations
The preparation of suppositories refers to a preparation for cavities prepared by melting the drug and the matrix, pouring it into the suppository mold while hot, and cooling and molding.
The release agent of water-soluble suppository products is commonly used simethicone, liquid paraffin; simethicone non-petrochemical products, reduce the possible risk of allergies, irritation and other reactions.
Suppositories based on poloxamer 188 (poloxamer) must use dimethicone as a mold release agent, because poloxamer 188 (poloxamer) is hygroscopic.
6. Safe defoamer in the process of extraction and reflux of Chinese medicine and biological fermentation
A large amount of air bubbles are often generated during the extraction and reflux of Chinese medicine and in the process of biological fermentation, which leads to overflow or bursting. The common method is to add a small amount of anti-foaming agent. The surface tension of the anti-foaming agent is small, which can change the surface tension of the air bubble to make it Cracked, can eliminate the gas stored in the foam during the extraction and biological fermentation of traditional Chinese medicine. Common antifoaming agents are diethyl ether, simethicone or others; the components of diethyl ether and some composite defoaming liquids are physiologically active and safe. Sex is not recognized.
Dimethicone is the only defoamer approved by the drug regulatory authority.
The amount of simethicone is about 10 ml per cubic extract (fermentation broth), which has a significant defoaming effect.
7. Main raw materials of medical defoaming emulsion
Silicone No. 1 prescription;
Dimethyl silicone oil (type 500) 20ml, differential silica gel 10g, flatly add 2ml of A20, 5% ethyl hydroxyphenyl ethyl alcohol solution, the amount of purified water, made 1000ml.
It is used for defoaming during gastrointestinal X-ray gastrointestinal examination, which can improve the diagnosis effect; it can also be used to eliminate abdominal distension caused by various reasons.
Eight, the matrix composition of high-end cream products-dimethicone
Used as an ointment base, it can increase the penetration of drugs into the skin and improve the efficacy; improve patient comfort and increase the speed of drug dispersion.
It is a fine, smooth and pearl-like bright, high-end cream base composed of cosmetic-like sensory intuition and obvious advantages in drug release speed.
Common formula
1. Oil-in-water (O / W) cream base;
Active ingredient, oil phase; cetyl alcohol, dimethicone, azone, stearic acid, Span-60; water phase; glycerin, purified water, etc., the proportion of dimethicone is generally 6-10%. Such as ketoconazole cream.
2. Water-in-oil (W / O) cream base;
Active ingredient, oil phase; simethicone, white petrolatum, glyceryl monostearate, Pingping A20, water phase; glycerin, purified water, etc., the proportion of simethicone is generally 1-5%.
Such as compound ketoconazole cream.
3. Sunscreen
Liquid paraffin 5 parts, white beeswax 10 parts, microcrystalline paraffin 5 parts, dimethicone 5 parts, white petrolatum 5 parts, polyoxyethylene sorbitan monolaurate 1 part, sorbitan half oleate 5 parts, proper amount of essence, 1 part isopropyl alcohol myristate, 2 parts titanium dioxide, 21 parts purified water, usually made into cream. Because there are ten different types of dimethicone, but products with the same properties, their density and viscosity become a physical and chemical property that can be flexibly adjusted. There is always a product or combination of the most suitable specifications that can adjust the best preparation product status. This is unmatched by any other similar pharmaceutical excipients.
It can be seen that simethicone, as a pharmaceutical excipient and / or pharmaceutical active ingredient, not only has excellent performance but is also very safe.
9. Application Technology of Dimethicone in Medical Devices and Medicine Packaging Materials
Silicification; refers to the process of spraying dimethicone (or dimethicone diluent) evenly on the surface of utensils or materials, and then drying to coat a thin layer of dimethicone on the surfaces of utensils or materials. The silicification degree is generally 0.012-0.02mg / c㎡. After the product is siliconized, the related performance has been significantly improved.
1. After the dental material is siliconized, the compatibility will be significantly improved.
2. After the surface of the surgical instrument and the injection needle are siliconized, the damage to the tissue can be reduced and it is easy to puncture;
3. Due to the anticoagulant properties of simethicone, the surface of the vacuum blood collection tube, blood reservoir, and hemodialysis equipment can be prolonged after the siliconized treatment of this product can prolong the storage time of blood samples and defoam the blood of the blood circulation device.
4. The friction coefficient of the surface of the butyl rubber plug is very high. It is necessary to treat the surface of the rubber plug. Siliconization is a traditional method to overcome the problems of operation and mechanical aspects of the rubber plug.
5. After the surface of the disposable dressing is siliconized, such as gauze, cotton wool, etc., it can make it not stick to the wound;
6. Lubricating oil for medical appliances, such as the lubrication of disposable injection syringes, is the safest lubricant;
7. Dimethicone is the best non-benzene lubricant for condoms;
8. Dimethicone can be used directly as a first aid for mild burns and scalds (used by the family) and to prevent scars;
9. Dimethicone is a lubricant that can be used in the sex life of middle-aged and elderly people without hidden safety hazards.
Due to the huge differences in raw materials, production process, production environment, quality control and quality standards, and impurity components in industrial dimethicone and dimethicone medicinal raw and auxiliary materials, the product quality difference is obvious. Industrial dimethicone contains a variety of chemical substances that are complex and harmful to the human body, and there are no related detection methods in conventional standards. Therefore, it is recommended that manufacturers of pharmaceuticals, medical devices, food and cosmetics use dimethicone medicinal grade raw and auxiliary materials To ensure the safety of such products directly related to the lives and health of the people.
Methyl silicone oil is widely used in the field of medicine. As a pharmaceutical excipient and active ingredient, it not only has excellent performance but is also very safe.
1. The best application of hydrophobic agent
1. Preparation of acid-resistant capsules
Glycerin 22.02kg, distilled water 34.13kg, dimethyl silicone oil 10kg, add gelatin 43.85kg, dissolved under reduced pressure at 70 ~ 80 ℃, usually made into capsules. The mixed solution of formaldehyde / acetone (1/60) is sprayed on the capsules to prepare. Due to the hydrophobic effect of dimethyl silicone oil, the prepared capsules do not disintegrate in acid gastric juice for 2 hours, dissolve in alkaline intestinal solution for 200 to 620 seconds, are stable to enzymes and temperatures, and have good mechanical strength.
2. Polishing of sugar-coated tablets (glazing agent)
During the polishing operation, the Sichuan wax fine powder with 2% dimethyl silicone oil is added to the color-coated tablets for polishing. The sugar-coated tablets are brighter and more beautiful than the dimethyl silicone oil, and the color surface is bright and beautiful. Moisture-proof effect, to ensure that the sugar-coated tablets do not discolor or mold during the storage period.
3. Film coating materials
It is used as a plasticizer for film coating materials. It uses the hydrophobicity and oxygen resistance of dimethyl silicone oil to isolate the core from the outside, is not affected by moisture and oxygen in the air, does not absorb moisture and deteriorate, and the coat is firm and smooth.
2. The best condensing agent for water-soluble dropping pills
The behavior of dripping pills in the condensate includes spreading, droplet formation and mixing. Generally, when a liquid with a small surface tension is placed in a liquid with a high surface tension, the surface will spread, otherwise it is easy to form droplets. Dimethicone is the most water-soluble dripping pill condensate with the smallest surface energy (liquid paraffin 0.035N / m, vegetable oil 0.035N / m, dimethicone 0.021N / m).
There are many types and specifications of dimethicone. You can adjust the temperature and select different types of dimethicone to adjust the formation and precipitation speed of droplets in the condensate to achieve the best process and quality conditions. There are hidden dangers of toxic substances in contaminated petrochemical products and discoloration and mildew of water-based dripping pills, which cannot be guaranteed by liquid paraffin and vegetable oil.
Especially the dripping pills using S-40 (polyoxyethylene monostearate) and poloxamer as the matrix must use dimethyl silicone oil as the condensate, and cannot use liquid paraffin as the condensate. Silicone oil can increase the solubility of water-insoluble active drugs, which is conducive to the absorption of drugs; poloxamer (poloxamer) can not use liquid paraffin as a condensate because of its hygroscopicity. (Simethicone is regularly processed in the production of dripping pills; due to the high price of dimethicone, it should be recycled as much as possible in production. Dimethicone that has been used will be mixed with foreign objects. The broken pellets can be removed by filtration, static precipitation or centrifugation; in addition, the common foreign body is water. When using dimethicone mixed with oil and water as the condensing agent, the dropping pills may be dissolved, deformed or even unable to condense Hard, the method of removing the water in the dimethicone is: freeze the water-containing dimethicone at -4 ℃, take it out after the water condenses into ice, and filter it quickly to remove it.
3. The only effective antistatic agent in the production of micropowders and pellets
Pills or pellets establish fluidization in the fluidized bed. When the material passes through the spray area, the mist particles of the clothing material are sprayed on the surface, and they are attached after bonding, spreading, and drying to form a small piece of coating film. After repeated spraying, the film gradually expanded, and finally formed a continuous overall layer to achieve the purpose of coating. In order to ensure safe operation and complete dispersion of the materials, so that the powder will not stick and form agglomerates, antistatic agents should be added when the powder is sprayed.
Dimethicone is currently the only medicinal adjuvant with antistatic effect. The amount of antistatic agent used is 0.1% of the weight of the powder.
4. Used as lubricant in solid preparations
Lubricant refers to the general name of the auxiliary materials added to the material to be compressed before tableting to make it have or increase fluidity, anti-adhesion and lubricity, so as to facilitate the tableting process. Lubricants are classified into three types according to their mechanism of action; lubricants are auxiliary materials that reduce the friction between granules or tablets and the die.
After cleaning the tablet die, smearing a layer of dimethicone can also solve the sticking problem of some varieties.
1. Slow-release aspirin tablets
Take aspirin powder 1000g (crystal diameter 0.1770mm), ethoxyethyl cellulose (containing 12% ethoxy group) 70g, dissolved in 300ml (1: 1) toluene-dichloromethane solution and 30g containing dimethicone Toluene solution, starch 400g, glycerol palmitic acid fatty acid ester 300g, talc powder 50g, microcrystalline cellulose 100g, usually made into tablets.
2. Compound Paracetamol Capsules
Take the aspirin granules to 50 ℃, coat with 1: 1 copolymer of methacrylic acid and methacrylic acid ester and 0.045% AF emulsion (defoamer), and dry at 37.8 ℃ for 24h in a boiling drying bed, then Weigh 52.144g, add 0.203g of sodium lauryl sulfate, 41.45g of paracetamol, 0.363g of dimethicone, and 0.145g of polyoxyethylene dehydrated monooleate. The capsule weighs 700 mg, and each capsule contains 325 mg of aspirin and paracetamol.
3. Ibuprofen sustained-release tablets
Take ibuprofen 58.25%, lactose 14.50%, dicalcium phosphate 12.60%, glyceryl behenate 11.65%, magnesium stearate 1.0%, talc + silicone oil (4: 1) 2.0% to make tablets.
5. Used as a release agent in the production of suppositories and other preparations
The preparation of suppositories refers to a preparation for cavities prepared by melting the drug and the matrix, pouring it into the suppository mold while hot, and cooling and molding.
The release agent of water-soluble suppository products is commonly used simethicone, liquid paraffin; simethicone non-petrochemical products, reduce the possible risk of allergies, irritation and other reactions.
Suppositories based on poloxamer 188 (poloxamer) must use dimethicone as a mold release agent, because poloxamer 188 (poloxamer) is hygroscopic.
6. Safe defoamer in the process of extraction and reflux of Chinese medicine and biological fermentation
A large amount of air bubbles are often generated during the extraction and reflux of Chinese medicine and in the process of biological fermentation, which leads to overflow or bursting. The common method is to add a small amount of anti-foaming agent. The surface tension of the anti-foaming agent is small, which can change the surface tension of the air bubble to make it Cracked, can eliminate the gas stored in the foam during the extraction and biological fermentation of traditional Chinese medicine. Common antifoaming agents are diethyl ether, simethicone or others; the components of diethyl ether and some composite defoaming liquids are physiologically active and safe. Sex is not recognized.
Dimethicone is the only defoamer approved by the drug regulatory authority.
The amount of simethicone is about 10 ml per cubic extract (fermentation broth), which has a significant defoaming effect.
7. Main raw materials of medical defoaming emulsion
Silicone No. 1 prescription;
Dimethyl silicone oil (type 500) 20ml, differential silica gel 10g, flatly add 2ml of A20, 5% ethyl hydroxyphenyl ethyl alcohol solution, the amount of purified water, made 1000ml.
It is used for defoaming during gastrointestinal X-ray gastrointestinal examination, which can improve the diagnosis effect; it can also be used to eliminate abdominal distension caused by various reasons.
Eight, the matrix composition of high-end cream products-dimethicone
Used as an ointment base, it can increase the penetration of drugs into the skin and improve the efficacy; improve patient comfort and increase the speed of drug dispersion.
It is a fine, smooth and pearl-like bright, high-end cream base composed of cosmetic-like sensory intuition and obvious advantages in drug release speed.
Common formula
1. Oil-in-water (O / W) cream base;
Active ingredient, oil phase; cetyl alcohol, dimethicone, azone, stearic acid, Span-60; water phase; glycerin, purified water, etc., the proportion of dimethicone is generally 6-10%. Such as ketoconazole cream.
2. Water-in-oil (W / O) cream base;
Active ingredient, oil phase; simethicone, white petrolatum, glyceryl monostearate, Pingping A20, water phase; glycerin, purified water, etc., the proportion of simethicone is generally 1-5%.
Such as compound ketoconazole cream.
3. Sunscreen
Liquid paraffin 5 parts, white beeswax 10 parts, microcrystalline paraffin 5 parts, dimethicone 5 parts, white petrolatum 5 parts, polyoxyethylene sorbitan monolaurate 1 part, sorbitan half oleate 5 parts, proper amount of essence, 1 part isopropyl alcohol myristate, 2 parts titanium dioxide, 21 parts purified water, usually made into cream. Because there are ten different types of dimethicone, but products with the same properties, their density and viscosity become a physical and chemical property that can be flexibly adjusted. There is always a product or combination of the most suitable specifications that can adjust the best preparation product status. This is unmatched by any other similar pharmaceutical excipients.
It can be seen that simethicone, as a pharmaceutical excipient and / or pharmaceutical active ingredient, not only has excellent performance but is also very safe.
9. Application Technology of Dimethicone in Medical Devices and Medicine Packaging Materials
Silicification; refers to the process of spraying dimethicone (or dimethicone diluent) evenly on the surface of utensils or materials, and then drying to coat a thin layer of dimethicone on the surfaces of utensils or materials. The silicification degree is generally 0.012-0.02mg / c㎡. After the product is siliconized, the related performance has been significantly improved.
1. After the dental material is siliconized, the compatibility will be significantly improved.
2. After the surface of the surgical instrument and the injection needle are siliconized, the damage to the tissue can be reduced and it is easy to puncture;
3. Due to the anticoagulant properties of simethicone, the surface of the vacuum blood collection tube, blood reservoir, and hemodialysis equipment can be prolonged after the siliconized treatment of this product can prolong the storage time of blood samples and defoam the blood of the blood circulation device.
4. The friction coefficient of the surface of the butyl rubber plug is very high. It is necessary to treat the surface of the rubber plug. Siliconization is a traditional method to overcome the problems of operation and mechanical aspects of the rubber plug.
5. After the surface of the disposable dressing is siliconized, such as gauze, cotton wool, etc., it can make it not stick to the wound;
6. Lubricating oil for medical appliances, such as the lubrication of disposable injection syringes, is the safest lubricant;
7. Dimethicone is the best non-benzene lubricant for condoms;
8. Dimethicone can be used directly as a first aid for mild burns and scalds (used by the family) and to prevent scars;
9. Dimethicone is a lubricant that can be used in the sex life of middle-aged and elderly people without hidden safety hazards.
Due to the huge differences in raw materials, production process, production environment, quality control and quality standards, and impurity components in industrial dimethicone and dimethicone medicinal raw and auxiliary materials, the product quality difference is obvious. Industrial dimethicone contains a variety of chemical substances that are complex and harmful to the human body, and there are no related detection methods in conventional standards. Therefore, it is recommended that manufacturers of pharmaceuticals, medical devices, food and cosmetics use dimethicone medicinal grade raw and auxiliary materials To ensure the safety of such products directly related to the lives and health of the people.
