Diclofenac Diethylammonium Gel with Menthol, Methyl Salicylate and Oleum Lini.
COMPOSITION :
| Diclofenac Diethylammonium | B.P. | 1.16% w/w |
| (equivalent to Diclofenac Sodium 1% w/w) |
| Tretinoin | USP | 0.05% w/w |
| Menthol | I.P. | 5.0% w/w |
| Methyl Salicylate | I.P. | 10.0% w/w |
| Oleum Lini | | 3.0% w/w |
| (containing predominantly Linolenic Acid) |
| Gel base | | q.s. |
PHARMACOLOGIC PROPERTIES:
Pharmacodynamic properties
Sprintex Gel is an analgesic, anti-inflammatory preparation for topical application. Its active substances include diclofenac diethylammonium, oleum lini (containing predominantly Linolenic Acid), methyl salicylate and menthol, in a white creamy gel base.
Sprintex Gel containing diclofenac diethylammonium relieves pain, reduces oedema, and shorten the time to return to normal functions, in inflammation of traumatic or rheumatic origin.
Diclofenac has been shown to inhibit prostaglandin biosynthesis; and this is regarded as an important factor in its mechanism of action.
Alpha linolenic acid in Oleum lini is known for its anti-inflammatory action and has been used as topical analgesic in painful conditions.
Methyl salicylate is a salicylic acid derivative that is used topically as a counter-irritant in rubefacient preparations for the relief of pain in musculoskeletal, joint nad soft tissue disorders. Like other salicylates, methyl salicylate may be absorbed through intact skin. methyl salicylate is extensively metabolized to salicylic acid in the dermal and subcutaneous tissues following topical administration.
Menthol is a common counter-irritant in various topical analgesic preparations. When applied to the skin, menthol dilates the blood vessels, causing a sensation of coldness followed by an analgesic effect.
Pharmacokinetic properties:
Absorption
The amount of diclofenac absorbed through skin is proportional to the contact time and skin area covered with Sprintex Gel, and depends on the total topical dose and on skin hydration. About 6% of the active substance is absorbed after topical application of 2.5 gm per 500 cm2. Absorption of diclofenac increases threefold if an occlusive dressing is applied for 10 hours.
Methyl salicylate is speedily absorbed when applied cutaneously. Percutaneous absorption of methyl salicylate is enhanced by exercise, heat occlusion, or disruption of integrity of the skin. Both the rate and extent of absorption increase after repeated application.
Menthol is known to be well absorbed after topical application.
Distribution
Diclofenac can be detected in the plasma, synovial tissue and synovial fluid after topical application. The peak plasma concentrations of diclofenac are about 100 times lower after topical application than after oral administration. 99.7% of diclofenac binds to serum proteins, mainly to albumin.
50-80% of salicylic acid binds to serum proteins.
The distribution of menthol after topical application is unknown.
Metabolism:
Biotransformation of diclofenac takes place partly by glucuronidation of the intact molecule, but mainly by single or multiple hydroxylations resulting in several phenolic metabolites, most of which are converted to glucuronide conjugates. Two of these phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.
Methyl salicylate is extensively metabolized (first pass metabolism) to salicylic acid in the dermal and subcutaneous tissues following topical administration.
The metabolism of menthol after topical application is unknown.
Elimination
Total systemic clearance of diclofenac from the plasma is 263 + 56 ml/min. the terminal half-life is 1-2 hours. Diclofenac and its metabolites are excreted mainly in the urine.
Salicylic acid and its principal metabolites are excreted in the urine.
After absorption, menthol is excreted in the urine and bile as a glucuronide.
INDICATIONS:
Treatment of :
- Localized forms of soft-tissue rheumatism, like Bursitis especially of elbow and knees, etc.
- Localized rheumatic diseases, e.g., osteoarthritis of the peripheral joints and vertebral column
- Post-traumatic inflammation of the tendons, ligaments, muscles and joints, e.g., due to sprains, strains or bruises.
DOSAGE / ADMINISTRATION:
Sprintex Gel is to be applied locally 3-4 times daily to the skin and rubbed gently. Depending on the size of the painful area to be treated, 2-4 gm Sprintex Gel can be used. An occlusive dressing should not be used. The hands should be washed after application of the gel, unless the hands are the treated areas, in which case, they should be washed 30 minutes after application. The duration of treatment should not be more than 7 days, without review by the treating physician.
Children:
Safety is not established in children, hence should be avaoided in children.
Restrictions:
Contraindications
Hypersensitivity to diclofenac, oleum lini, methyl salicylate, menthol, or any of the inactive ingredients used in here. Sprintex Gel is contraindicated in patients in whom attacks of asthma, urticaria, or acute arthritis are precipitated by salicylic acid or other non-steroidal anti-inflammatory drugs.
Precautions
Sprintex Gel should be applied only to intact skin, and not to broken or irritated skin or open wounds. The preparation should not come into contact with the eyes or mucous membranes.
It should be used with care on the extremities of patients with impaired peripheral circulation or diabetes.
The gel should not be used before phototherapy or phototesting procedures.
Pregnancy and lactation
Sprintex Gel should not be used during pregnancy unless clearly necessary.
Measurable quantities of the active substance are not reportedly found in breast milk. Can be used when benefits are expected to outweigh risks associated.
Undesirable effects:
Contact dermatitis with erythema at the site of application, or generalized rash, and hypersensitivity reactions or photosensitivity reactions.
Interactions:
No interactions have been reported to date with topical treatment with diclofenac diethylammonium. Potentiation of warfarin anticoagulation has been reported with topical application of methyl salicylate preparations.
Overdosage:
Significant systemic reactions resulting from improper use or accidental overdosage (e.g., in children) should be treated with the usual measures employed to manage poisoning with non-steroidal anti-inflammatory drugs.
Pharmaceutical particulars:
This medicinal product must not be mixed with any other medicinal product.
Special precautions for storage:
Medicines should be kept out of the reach of children.
Store in a cool, dry place. Do not allow to freeze. Protect from light.
The preparation should not be used after the date marked 'Exp. Date' on the pack
Packages:
Tubes of 30 gm
