Skinsure Plus
Skinsure Plus Uses, Dosage, Side Effects, Food Interaction and all others data.
Extracted from the dried leaves of bearberry plant in the genus Arctostaphylos and other plants commonly in the Ericaceae family, arbutin is a beta-D-glucopyranoside of Hydroquinone. It is found in foods, over-the-counter drugs, and herbal dietary supplements . Most commonly, it is an active ingredient in skincare and cosmetic products as a skin-lightening agent for the prevention of melanin formation in various skin conditions that involve cutaneous hyperpigmentation or hyperactive melanocyte function . It has also been used as an anti-infective for the urinary system as well as a diuretic . Arbutin is available in both natural and synthetic forms; it can be synthesized from acetobromglucose and Hydroquinone . Arbutin is a competitive inhibitor of tyrosinase (E.C.1.14.18.1) in melanocytes , and the inhibition of melanin synthesis at non-toxic concentrations was observed in vitro. Arbutin was shown to be less cytotoxic to melanocytes in culture compared to Hydroquinone .
At non-toxic concentrations, arbutin inhibited the activity of tyrosinase in cultured human keratinocytes, while having minimal effect on the expression of tyrosinase mRNA or the synthesis of the enzyme . α-Arbutin produced a concentration-dependent inhibition of melanin synthesis of human melanoma cells, HMV-II . No inhibitory effect on HMV-II cell growth was seen at concentrations lower than 1.0 mM. At concentrations of 0.5 mM of arbutin, tyrosinase activity was reduced to 60% of that in non-treated cells . The addition of arbutin blocked and inhibited α-MSH-stimulated melanogenesis in B16 melanoma cells, brownish guinea pig, and human skin tissue . In a pilot study of healthy male adults exposed to UV B irradiation, topical administration of arbutin inhibited UV-induced nuclear factor-kappaB activation in human keratinocytes . In mouse skin, arbutin counteracted oxidative stress induced by 12-O-tetradecanoylphorbol-13-acetate .
Gluconolactone is a naturally-occurring food additive used as a sequestrant, an acidifier, or a curing, pickling, or leavening agent. It is a cyclic ester of D-gluconic acid. Pure gluconolactone is a white odorless crystalline powder.
Vitamin E Capsule is a Vitamin E preparation. Vitamin E acts as an antioxidant in the body. Vitamin E protects polyunsaturated fatty acids (which are components of cellular membrane) and other oxygen-sensitive substances such as vitamin A & vitamin C from oxidation. Vitamin E reacts with free radicals, which is the cause of oxidative damage to cell membranes, without the formation of another free radical in the process. The main pharmacological action of vitamin E in humans is its antioxidant effect.
In premature neonates irritability, edema, thrombosis and hemolytic anemia may be caused due to vitamin E deficiency. Creatinuria, ceroid deposition, muscle weakness, decreased erythrocyte survival or increased in vitro hemolysis by oxidizing agents have been identified in adults and children with low serum tocopherol concentrations.
Vitamin E is a collective term used to describe 8 separate fat soluble antioxidants, most commonly alpha-tocopherol. Vitamin E acts to protect cells against the effects of free radicals, which are potentially damaging by-products of the body's metabolism. Vitamin E deficiency is seen in persons with abetalipoproteinemia, premature, very low birth weight infants (birth weights less than 1500 grams, or 3½ pounds), cystic fibrosis, and cholestasis and severe liver disease. Preliminary research suggests vitamin E may help prevent or delay coronary heart disease and protect against the damaging effects of free radicals, which may contribute to the development of chronic diseases such as cancer. It also protects other fat-soluble vitamins (A and B group vitamins) from destruction by oxygen. Low levels of vitamin E have been linked to increased incidence of breast and colon cancer.
| Trade Name | Skinsure Plus |
| Generic | Arbutin + Gluconolactone + Kojic Acid + Mulberry Extract + Octyl Methoxycinnamate + Vitamin E |
| Type | Gel |
| Therapeutic Class | |
| Manufacturer | East West Pharma |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Indicated for over-the-counter use for epidermal hyperpigmentation in various skin conditions, such as melasma, freckles, and senile lentigines.
Gluconolactone is a polyhydroxy acid used in the dissolution of calculi and used as an additive in various drug products to maintain consistency and other characteristics.
As a dietary supplement:
- Vitamin E deficiency resulting from impaired absorption.
- Increased requirements due to diet rich in polyunsaturated fats.
- For healthy hair & skin
- As an Antioxidant
- Hemolytic anemia due to Vitamin E deficiency
Therapeutic use
: Heavy metal poisoning, Hepatotoxin poisoning, Hemolytic anemia, Oxygen therapy and replacement therapy in nutritional deficiency states for the betterment of skin and hair.
Skinsure Plus is also used to associated treatment for these conditions: Mild Lower Urinary Tract InfectionBladder calculus, Catheter site calcification, Medical device site calcificationVitamin Deficiency, Long-chain omega-3 fatty acid supplementation, Dietary supplementation
How Skinsure Plus works
Arbutin is a hydroquinone glycoside, however the hydroquinone moiety is not solely responsible for the de-pigmentating actions of arbutin . It acts as a competitive inhibitor of tyrosinase enzyme by acting on the L-tyrosine binding site to suppress melanogenesis and mediate its de-pigmenting actions on human skin . Tyrosinase is an enzyme involved in the regulation of rate-limiting steps during the synthesis of melanin; it regulates the conversion of L-tyrosine into L-dopa, and subsequent conversion of L-dopa to L-dopaquinone . Via inhibition of tyrosinase activity in a concentration-dependent manner, arbutin attenuates the production of melanin in melanocytes. While most studies suggest that arbutin has negligible effect on the tyrosinase mRNA expression, a study assessing the effect of arbutin on melanocyte differentiation inducement system using ES cells propose that arbutin may also downregulate the expression of tyrosinase in addition to its inhibitory action on the enzyme . The contradictory findings across studies may be due to previous studies using terminally-differentiated melanocytes and melanoma cells .
The mechanism of action for most of vitamin E's effects are still unknown. Vitamin E is an antioxidant, preventing free radical reactions with cell membranes. Though in some cases vitamin E has been shown to have pro-oxidant activity.
One mechanism of vitamin E's antioxidant effect is in the termination of lipid peroxidation. Vitamin E reacts with unstable lipid radicals, producing stable lipids and a relatively stable vitamin E radical. The vitamin E radical is then reduced back to stable vitamin E by reaction with ascorbate or glutathione.
Dosage
Skinsure Plus dosage
Betterment of Cardiovascular health: 400 mg - 800 mg / day
Deficiency syndrome in adults: 200 mg - 400 mg / day
Deficiency syndrome in children: 200 mg / day
Thalassemia: 800 mg / day
Sickle-cell anemia: 400 mg / day
Betterment of Skin & Hair: 200 mg - 400 mg / day (Topical use is also established for beautification)
Chronic cold in adults: 200 mg / day
Side Effects
Overdoses (>1g) have been associated with minor side effects, including hypertension, fatigue, diarrhea and myopathy
Toxicity
In an acute oral toxicity study, the LD50-value for β-arbutin is 9804 mg/kg bw for the mouse and 8715 mg/kg bw for the rat . Dermal LD50 value in rat and mouse was reported to be greater than 928 mg/kg bw, according to an acute dermal toxicity study . Extremely high doses may cause ringing in the ears, shortness of breath, convulsions, collapse, vomiting and delirium . Nausea and vomiting were seen individuals with sensitive stomachs following oral ingestion of 15 g of dried uva ursi leaves that contain arbutin .
There is no data available for effects in pregnancy, breast feeding, hepatic impairment, or renal impairment. However, it appears that the process of vitamin E elimination is strict and self regulating enough that vitamin E toxicity is exceedingly rare. Studies showing adverse effects from excess vitamin E generally involve people consuming more than 1000mg/day for weeks to months.
Precaution
Vitamin E may enhance the anticoagulant activity of anticoagulant drugs. Caution is advised in premature infants with high dose Vitamin E supplementation, because of reported risk of necrotizing enterocilitis.
Interaction
Vitamin E may impair the absorption of Vitamin A. Vitamin K functions impairement happens at the level of prothrombin formation and potentiates the effect of Warfarin.
Volume of Distribution
No pharmacokinetic data available.
0.41L/kg in premature neonates given a 20mg/kg intramuscular injection.
Elimination Route
Arbutin was found to be extensively absorbed from the gastrointestinal tract where it is primarily converted to hydroquinone .
10-33% of deuterium labelled vitamin E is absorbed in the small intestine. Absorption of Vitamin E is dependant upon absorption of the fat in which it is dissolved. For patients with poor fat absorption, a water soluble form of vitamin E may need to be substituted such as tocopheryl polyethylene glycol-1000 succinate.
In other studies the oral bioavailability of alpha-tocopherol was 36%, gamma-tocotrienol was 9%. The time to maximum concentration was 9.7 hours for alpha-tocopherol and 2.4 hours for gamma-tocotrienol.
Half Life
No pharmacokinetic data available.
44 hours in premature neonates given a 20mg/kg intramuscular injection. 12 minutes in intravenous injection of intestinal lymph.
Clearance
No pharmacokinetic data available.
6.5mL/hr/kg in premature neonates given a 20mg/kg intramuscular injection.
Elimination Route
During the first 4 hours following ingestion of a single dose of 210 mg arbutin in healthy volunteers, 224.5 μmol/L hydroquinone glucuronide and 182 μmol/L of hydroquinone sulfate were recovered in the urine .
Alpha tocopherol is excreted in urine as well as bile in the feces mainly as a carboxyethyl-hydrochroman (CEHC) metabolite, but it can be excreted in it's natural form .
Pregnancy & Breastfeeding use
Use in pregnancy: Vitamin E may be used in pregnancy in the normally recommended dose but the safety of high dose therapy has not been established.
Use in lactation: There appears to be no contraindication to breast feeding by mothers taking the normally recommended dose.
Contraindication
No known contraindications found.
Special Warning
Use in Children: Vitamin E is safe for children
Acute Overdose
Large doses of vitamin E (more than 1 gm/day) have been reported to increase bleeding tendency in vitamin K deficient patients such as those taking oral anticoagulants.
Storage Condition
Store at a cool and dry place, Protect from light and moisture.
Innovators Monograph
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