Sodium dichlorophenolate self-emulsifying ointment

A technology of diclofenac sodium and self-emulsification, which is applied in the field of medicine, can solve the problems of insignificant curative effect, short half-life, and low drug loading, and achieve the effect of simple method, easy purchase, and good curative effect of the product

Inactive Publication Date: 2012-08-01
HENAN UNIV OF CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with other non-steroidal anti-inflammatory drugs, diclofenac sodium has stronger anti-inflammatory effect and higher safety, and it has become one of the most widely used non-steroidal anti-inflammatory drugs in the world; diclofenac sodium There are many domestic raw material manufacturers with low prices, and its clinical antipyretic, analgesic and anti-inflammatory effects are definite, and its strong analgesic effect is its outstanding feature; at present, diclofenac sodium is used in the treatment of lumbar disc herniation, cervical pain, rheumatism, toothache, etc. It is widely used, but because of its short half-life, it is very inconvenient to take medicine repeatedly, and it also has a certain stimulating effect on the stomach, so it is commonly used in clinical formulations such as enteric-coated tablets, sustained-release tablets, and sustained-release capsules; currently, the drug is used externally The dosage form of diclofenac sodium gel is already on the market, but its drug loading is low, and the clinical efficacy is not obvious. In order to increase the drug loading of diclofenac sodium and improve its transdermal absorption capacity, we have developed a new dosage form—— —Diclofenac sodium self-emulsifying ointment, lightly grind with water before use to form a micro-emulsion, and directly apply it on the painful part to reduce the first-pass effect and increase the utilization of the drug, which is a technical problem that those skilled in the art hope to solve

Method used

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  • Sodium dichlorophenolate self-emulsifying ointment

Examples

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Embodiment 1

[0023] In the specific implementation of the present invention, the diclofenac sodium self-emulsifying ointment is made of diclofenac sodium as medicine, and the self-emulsifying matrix is ​​mixed uniformly as a drug carrier to make, and the content of diclofenac sodium in every 1g of diclofenac sodium self-emulsifying ointment is 20~50mg, Described self-emulsifying matrix can be made by weight: oil phase 12%, emulsifier 48% and co-emulsifier 40%, and described oil phase is refining oil, glyceryl monostearate and stearyl alcohol, and its weight Ratio is 8: 2: 1, and described emulsifier is polysorbate 80 and polyoxyethylene hydrogenated castor oil (RH40), and its weight ratio is 2: 8, or is polysorbate 80 and polyoxyethylene castor oil ( EL), its weight ratio is 6: 4, and the described co-emulsifier is glycerin (glycerin), wherein, the oil phase is first placed in an 80°C constant temperature water bath to be heated and melted, and then the emulsifier and co-emulsifier are adde...

Embodiment 2

[0026] In the specific implementation of the present invention, the diclofenac sodium self-emulsifying ointment is made of diclofenac sodium as medicine, and the self-emulsifying matrix is ​​mixed uniformly as a drug carrier to make, and the content of diclofenac sodium in every 1g of diclofenac sodium self-emulsifying ointment is 20~50mg, Described self-emulsifying base can be made by weight: oil phase 15%, emulsifier 50% and co-emulsifier 35%, and described oil phase is refining oil, glyceryl monostearate and stearyl alcohol, and its weight Ratio is 8: 2: 1, and described emulsifier is polysorbate 80 and polyoxyethylene hydrogenated castor oil (RH40), and its weight ratio is 2: 8, or is polysorbate 80 and polyoxyethylene castor oil ( EL), its weight ratio is 6: 4, and the described co-emulsifier is glycerin (glycerin), wherein, the oil phase is first placed in an 80°C constant temperature water bath to be heated and melted, and then the emulsifier and co-emulsifier are added ...

Embodiment 3

[0029] In the specific implementation of the present invention, the diclofenac sodium self-emulsifying ointment is made of diclofenac sodium as medicine, and the self-emulsifying matrix is ​​mixed uniformly as a drug carrier to make, and the content of diclofenac sodium in every 1g of diclofenac sodium self-emulsifying ointment is 20~50mg, Described self-emulsifying matrix can be made by weight: oil phase 18%, emulsifier 52% and co-emulsifier 30%, and described oil phase is refining oil, glyceryl monostearate and stearyl alcohol, and its weight Ratio is 8: 2: 1, and described emulsifier is polysorbate 80 and polyoxyethylene hydrogenated castor oil (RH40), and its weight ratio is 2: 8, or is polysorbate 80 and polyoxyethylene castor oil ( EL), its weight ratio is 6: 4, and the described co-emulsifier is glycerin (glycerin), wherein, the oil phase is first placed in an 80°C constant temperature water bath to be heated and melted, and then the emulsifier and co-emulsifier are adde...

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Abstract

The invention relates to a sodium dichlorophenolate self-emulsifying ointment, which can be used for effectively reducing first pass effect and enhancing the curative effect. According to the technical scheme of the invention, the sodium dichlorophenolate self-emulsifying ointment is prepared by uniformly mixing sodium dichlorophenolate serving as a medicament and a self-emulsifying substrate serving as a medicament carrier; every gram of sodium dichlorophenolate self-emulsifying ointment contains 20-50mg of sodium dichlorophenolate; the self-emulsifying substrate is prepared from 12-20 percent by weight of an oil phase, 40-60 percent by weight of an emulsifier and 20-40 percent by weight of an auxiliary emulsifying agent; the oil phase consists of refined oil, glycerin monostearate and octadecanol in the weight ratio of 8:2:1; the emulsifier consists of polysorbate 80 and RH40 in the weight ratio of 2:8, or consists of polysorbate 80 and EL in the weight ratio of 6:4; and the auxiliary emulsifying agent is glycerol. The sodium dichlorophenolate self-emulsifying ointment is prepared by the following steps of: putting the oil phase into a constant-temperature water bath of 80 DEG Cfor heating and melting; adding the emulsifier, the auxiliary emulsifying agent and the sodium dichlorophenolate in sequence; dissolving and stirring uniformly; standing; and cooling for curing. The sodium dichlorophenolate self-emulsifying ointment has a rich raw material source, is easy to purchase, and is an innovation of a medicament for refrigerating and relieving inflammatory pain.

Description

1. Technical field [0001] The invention relates to medicine, in particular to a diclofenac sodium self-emulsifying ointment. 2. Background technology [0002] Diclofenac sodium is a non-steroidal anti-inflammatory analgesic derived from phenylacetic acid. Its mechanism of action is to block the transformation of arachidonic acid into prostaglandins by inhibiting the activity of cyclooxygenase; Adenoic acid combines with triglyceride (triacylglycerol), reduces the concentration of free arachidonic acid in cells, and indirectly inhibits the synthesis of leukotrienes. Compared with other non-steroidal anti-inflammatory drugs, diclofenac sodium has stronger anti-inflammatory effect and higher safety, and it has become one of the most widely used non-steroidal anti-inflammatory drugs in the world; diclofenac sodium There are many domestic raw material manufacturers with low prices, and its clinical antipyretic, analgesic and anti-inflammatory effects are definite, and its strong...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/196A61K47/44A61P29/00A61P19/02
Inventor 魏玉娄玉铃刘雅敏何永超杨艳娇李振国
Owner HENAN UNIV OF CHINESE MEDICINE
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