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CN-121971428-A - Oxybuprocaine hydrochloride composition and application thereof

CN121971428ACN 121971428 ACN121971428 ACN 121971428ACN-121971428-A

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to an oxybuprocaine hydrochloride composition and application thereof. The oxybuprocaine hydrochloride composition comprises, by weight, 10-65 parts of oxybuprocaine hydrochloride, 10-42 parts of permeation enhancer, 5-20 parts of pH regulator and 900-1000 parts of water. The oxybuprocaine hydrochloride composition can remarkably improve the percutaneous permeation efficiency of medicines, improve the efficacy of superficial anesthesia, prolong ejaculation time and play a role in preventing and treating premature ejaculation.

Inventors

  • CHEN WEIHAN
  • LIN ZHIZHONG
  • TAN JIAJIA
  • HUANG WEIJING
  • HE CAIPING

Assignees

  • 广州大光制药有限公司

Dates

Publication Date
20260505
Application Date
20260123

Claims (10)

  1. 1. The oxybuprocaine hydrochloride composition is characterized by comprising, by weight, 10-65 parts of oxybuprocaine hydrochloride, 10-42 parts of permeation enhancer, 5-20 parts of pH regulator and 900-1000 parts of water.
  2. 2. The oxybuprocaine hydrochloride composition of claim 1, wherein the permeation enhancer comprises one or more of a chemically synthesized permeation enhancer, a natural extracted permeation enhancer, and a biological permeation enhancer.
  3. 3. The oxybuprocaine hydrochloride composition of claim 2, wherein the penetration enhancer is at least one of ethanol, isopropyl myristate, laurate, menthol, sodium N-lauroyl sarcosinate, ethyl oleate, laurocapram, sodium hyaluronate, cetyltrimethylammonium bromide, isopropyl N-butyrate, palmitic acid.
  4. 4. An obucaine hydrochloride composition according to claim 3, wherein the penetration enhancer is sodium N-lauroyl sarcosinate, isopropyl myristate and sodium hyaluronate, and the mass ratio of sodium N-lauroyl sarcosinate, isopropyl myristate and sodium hyaluronate is 10-20:1-10:1-10.
  5. 5. The oxybuprocaine hydrochloride composition of any one of claims 1-4, wherein the oxybuprocaine hydrochloride composition further comprises at least one of an anti-irritant, a preservative, a fragrance.
  6. 6. The oxybuprocaine hydrochloride composition of claim 5, wherein the preservative is at least one selected from the group consisting of phenoxyethanol, ethylhexyl glycerol, p-hydroxyacetophenone, octanoyl hydroxamic acid, sodium benzoate, potassium sorbate, and/or The aromatic is at least one selected from flos Matricariae Chamomillae essential oil, lavender essential oil, bergamot essential oil, and jasmine essential oil, and/or the above-mentioned components The anti-irritant agent is at least one selected from dipotassium glycyrrhizinate and allantoin.
  7. 7. The oxybuprocaine hydrochloride composition of claim 1, wherein the oxybuprocaine hydrochloride composition comprises, by weight, 30-60 parts of oxybuprocaine hydrochloride, 12-18 parts of sodium N-lauroyl sarcosinate, 3-8 parts of isopropyl myristate, 3-8 parts of sodium hyaluronate, 5-20 parts of a pH regulator, and 900-1000 parts of water.
  8. 8. The oxybuprocaine hydrochloride composition of claim 1, wherein the pH adjuster is selected from at least one of phosphate buffer pair, citric acid/citrate buffer pair, boric acid/borate buffer pair, sodium hydroxide, potassium hydroxide, hydrochloric acid, phosphoric acid, acetic acid, citric acid, tartaric acid, lactic acid, sodium carbonate, sodium bicarbonate, triethanolamine.
  9. 9. Use of an obukine hydrochloride composition according to any one of claims 1-8 for the manufacture of a medicament for anaesthesia.
  10. 10. Use of an obucaine hydrochloride composition according to any one of claims 1-8 in the manufacture of a medicament for the prevention and treatment of premature ejaculation, or for the prolongation of penile erection time or ejaculation time.

Description

Oxybuprocaine hydrochloride composition and application thereof Technical Field The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oxybuprocaine hydrochloride composition and application thereof. Background Premature ejaculation is one of the most common male sexual dysfunction, with a much higher incidence than impotence (erectile dysfunction). At present, the special oral therapeutic drug dapoxetine is marketed at home and abroad, but the dapoxetine is required to be continuously taken without interruption, and cannot be taken once, and the gastrointestinal discomfort, the inhibition of libido and other side effects are obvious. Local anesthetics are drugs that temporarily and reversibly block the generation and conduction of nerve fiber impulses within a defined range of the body without losing consciousness of the patient. The local anesthetic has the advantages of anesthesia and pain relieving effects on some operations or pains without general exposure, and has small side effects. Common local anesthetics are divided into amides and lipid anesthetics, such as compound lidocaine cream prepared from lidocaine and prilocaine, which are widely used in local anesthesia. Furthermore, the compound lidocaine cream formed by lidocaine and prilocaine has been applied to the penis to block the conduction of somatosensory afferent neurons, thereby achieving the application of treating premature ejaculation and prolonging ejaculation time. Oxcarbazepine hydrochloride is an amide local anesthetic, and is mainly used for clinical anesthesia and analgesia, and the generation and conduction of nerve impulse are inhibited by reversibly blocking a voltage-gated sodium ion channel on a nerve cell membrane, so that a local anesthetic effect is generated. The oxepin hydrochloride can be widely used for local infiltration anesthesia in small-sized surgical operations, wound suturing and dental operations. In regional nerve block (e.g., brachial plexus block), reliable intra-and post-operative analgesia is provided. Therefore, how to improve the epidermis permeation and the drug effect of the oxforine hydrochloride by the mutual collocation and the action of the main drugs and the auxiliary materials, and play a role in delaying ejaculation time and improving the function of preventing and treating premature ejaculation becomes a further research direction. Disclosure of Invention In view of the above-mentioned problems of the prior art, it is a primary object of the present invention to provide an oxybuprocaine hydrochloride composition. The second object of the invention is to provide an application of the oxybuprocaine hydrochloride composition in preparing medicines for anesthesia. The third object of the invention is to provide an application of the oxybuprocaine hydrochloride composition in preparing medicines for preventing and treating premature ejaculation or prolonging penile erection time or ejaculation time. In order to achieve the above purpose, the present invention is realized by the following technical scheme: the invention discloses an obucaine hydrochloride composition, which comprises, by weight, 10-65 parts of obucaine hydrochloride, 10-42 parts of permeation enhancer, 5-20 parts of pH regulator and 900-1000 parts of water. The oxybuprocaine hydrochloride and the penetration enhancer are matched to form the external solution for the genital organs, and the external solution has good stability and uniformity and good skin feel when being used. The oxybuprocaine hydrochloride composition can better improve the percutaneous permeation efficiency of the medicine, improve the drug effect of superficial anesthesia, reduce the sensitivity of reproductive organs, prolong ejaculation time and play a role in treating premature ejaculation. Preferably, the penetration enhancer comprises one or more of a chemical synthesis type penetration enhancer, a natural extraction type penetration enhancer and a biological type penetration enhancer. In particular, the chemical synthesis type penetration enhancers include, but are not limited to, sulfoxides, alcohols, fatty acids, fatty acid esters, polyols, amides, surfactants, alkanones, organic acids, and mixtures of these. In particular, suitable sulfoxides include dimethyl sulfoxide, decyl methyl sulfoxide, and mixtures thereof. Suitable alcohols include ethanol, propanol, butanol, pentanol, hexanol, octanol, nonanol, n-decanol, 2-butanol, 2-pentanol, benzyl alcohol, octanol, decyl alcohol, lauryl alcohol, 2-lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, oleyl alcohol, linoleyl alcohol, linolenyl alcohol, 1, 3-propanediol, polyethylene glycol, ethylene glycol, diethylene glycol, triethylene glycol, dipropylene glycol, glycerol, 1, 2-propanediol, sorbitol, dextran, butylene glycol, pentylene glycol, hexanetriol, and mixtures of these. In particular, suitable fatty acids include valeric acid, heptano