CN112791093A - Transdermal drug delivery composition for treating acne and preparation method thereof - Google Patents
Transdermal drug delivery composition for treating acne and preparation method thereof Download PDFInfo
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- 208000002874 Acne Vulgaris Diseases 0.000 title claims abstract description 55
- 239000000203 mixture Substances 0.000 title claims abstract description 55
- 238000013271 transdermal drug delivery Methods 0.000 title claims abstract description 23
- 238000002360 preparation method Methods 0.000 title abstract description 8
- 239000007924 injection Substances 0.000 claims abstract description 30
- 238000002347 injection Methods 0.000 claims abstract description 30
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 claims abstract description 30
- 229920001661 Chitosan Polymers 0.000 claims abstract description 15
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000011726 vitamin B6 Substances 0.000 claims abstract description 15
- 235000019158 vitamin B6 Nutrition 0.000 claims abstract description 15
- 229940011671 vitamin b6 Drugs 0.000 claims abstract description 15
- UFUVLHLTWXBHGZ-MGZQPHGTSA-N [(2r,3r,4s,5r,6r)-6-[(1s,2s)-2-chloro-1-[[(2s,4r)-1-methyl-4-propylpyrrolidine-2-carbonyl]amino]propyl]-4,5-dihydroxy-2-methylsulfanyloxan-3-yl] dihydrogen phosphate Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@H](C)Cl)[C@@H]1[C@H](O)[C@H](O)[C@@H](OP(O)(O)=O)[C@@H](SC)O1 UFUVLHLTWXBHGZ-MGZQPHGTSA-N 0.000 claims abstract description 14
- 229960002291 clindamycin phosphate Drugs 0.000 claims abstract description 14
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- PLCQGRYPOISRTQ-FCJDYXGNSA-L dexamethasone sodium phosphate Chemical compound [Na+].[Na+].C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COP([O-])([O-])=O)(O)[C@@]1(C)C[C@@H]2O PLCQGRYPOISRTQ-FCJDYXGNSA-L 0.000 claims abstract description 13
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Images
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4415—Pyridoxine, i.e. Vitamin B6
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/716—Glucans
- A61K31/722—Chitin, chitosan
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61P17/10—Anti-acne agents
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Abstract
The invention relates to the technical field of medicaments for treating acne, in particular to a transdermal drug delivery composition for treating acne and a preparation method thereof. The transdermal drug delivery composition for treating acne is composed of the following raw materials in parts by volume: 10 parts of normal saline, 2-3 parts of clindamycin phosphate injection, 1-2 parts of dexamethasone sodium phosphate injection, 2-3 parts of vitamin B6 injection and 1-3 parts of chitosan wound fluid dressing. The transdermal drug delivery composition for treating acne has the advantages of small dosage, quick response, bacteriostasis, anti-inflammation, promotion of wound healing, prevention or reduction of scar formation, small damage to skin, no thinning of stratum corneum and no adverse effect on the whole body; the invention also provides a preparation method of the composition.
Description
Technical Field
The invention relates to the technical field of medicaments for treating acne, in particular to a transdermal drug delivery composition for treating acne and a preparation method thereof.
Background
Acne is a chronic inflammatory skin disease of hair follicles and sebaceous glands, and is also one of the most common diseases in the cosmetology dermatology department. Usually, the acne is better in face and neck, chest and back, shoulders and upper arm, and clinically, the acne is mainly manifested by leucocephalin, comedones, inflammatory papules, pustules, nodules, cysts and the like. The disease is common in adolescence, but is not completely limited by age stage, and can occur in almost all ages from children to adults.
Acne occurs mainly and closely related to factors such as excessive sebum secretion, follicular sebaceous gland duct keratosis, blockage, propionibacterium acnes infection and inflammatory reaction. The pathogenesis of acne is that the body develops to cause the secretion of androgen in the body to be vigorous, the androgen controls sebaceous glands to produce more sebum, and the sebum is mixed with exfoliated epidermal tissues to block pores to cause acne. The onset of some patients is also influenced by genetic, immunological, endocrine, emotional, and dietary factors.
The currently commonly used oral medicines comprise oral antibiotics, oral isotretinoin, antiandrogen, oral glucocorticoid and the like, and the oral medicines generally have large side effects on the body. The topical medicine comprises tretinoin, benzoyl peroxide, antibiotic, azelaic acid, etc. Wherein the retinoic acid can cause local irritation reactions such as erythema, desquamation, tightness and burning feeling in the initial use; the benzoyl peroxide can slowly release nascent oxygen and benzoic acid after being externally used, has the effects of killing propionibacterium acnes, dissolving comedo and astringing, and causes mild irritation to the skin of a few patients; azelaic acid has therapeutic effect on inflammation and acne, and can relieve pigmentation after inflammation, and its adverse reaction is local mild erythema and stabbing pain. The long-term use of the medicine can easily cause the thinning of the cuticle and the sensitivity of the skin, and the effect is not obvious.
Patent CN202010590341.4 discloses a gel composition for treating inflammatory acne and a preparation method thereof, wherein the gel composition comprises: clindamycin or clindamycin hydrochloride or clindamycin phosphate, hyaluronic acid or salt thereof with molecular weight of 100kDa-1200kDa, and ergothioneine; dissolving clindamycin or clindamycin hydrochloride or clindamycin phosphate, hyaluronic acid or salt thereof and ergothioneine in water; adding humectant and antiseptic, and stirring to dissolve; adding the thickening agent, and stirring to uniformly disperse the thickening agent; adding a pH regulator, and regulating the pH to 6-7.5; the rest is filled with water, and the gel composition is obtained after even stirring. The gel composition has antibacterial, anti-inflammatory, antioxidant, ultraviolet injury relieving, wound healing promoting, and scar formation preventing or reducing effects.
Patent CN201811426391.8 discloses a composition for treating acne and application thereof, which comprises the following components by weight: 10-30 parts of isotretinoin, 125 parts of erythromycin 110-. The medicine for treating acne has the advantages of small dosage, long treatment course and less adverse reaction.
Disclosure of Invention
The technical problem to be solved by the invention is to provide a transdermal drug delivery composition for treating acne, which has the advantages of small dosage, quick response, bacteriostasis, anti-inflammation, promotion of wound healing, prevention or reduction of scar formation, small damage to skin, no cuticle thinning and no adverse effect on the whole body; the invention also provides a preparation method of the composition.
The transdermal drug delivery composition for treating acne provided by the invention comprises the following raw materials in parts by volume:
preferably, the transdermal drug delivery composition for treating acne is composed of the following raw materials in parts by volume:
the specification of the normal saline is 90mg/10mL by the content of sodium chloride.
The specification of the clindamycin phosphate injection is 0.3g/2mL based on the content of clindamycin phosphate. Clindamycin can effectively inhibit propionibacterium acnes, and excessive consumption of clindamycin can cause skin sensitivity and skin irritation, and easily generate drug resistance, and the effect is not obvious when the consumption is too small.
The specification of the dexamethasone sodium phosphate injection is 5mg/1mL based on the content of dexamethasone sodium phosphate. Dexamethasone can effectively improve the red and swollen symptom of the inflammation of the hair follicle, and excessive dosage of dexamethasone can cause skin sensitivity and damage to the skin, and insufficient dosage of dexamethasone can cause unobvious effect.
The specification of the vitamin B6 injection is 0.1g/2mL calculated by the content of the vitamin B6. The vitamin B6 injection can effectively inhibit the secretion of skin oil through clinical verification.
The chitosan wound liquid dressing contains 0.5-1.5 wt% of chitosan and the balance of water. The chitosan wound liquid dressing has the excellent performances of resisting bacteria, preventing infection, promoting the repair and regeneration of damaged tissues, inhibiting and repairing scars, stopping bleeding, relieving pain, having no antigenicity and the like.
The preparation method of the transdermal drug delivery composition for treating acne comprises the following steps:
the physiological saline, clindamycin phosphate injection, dexamethasone sodium phosphate injection, vitamin B6 injection and chitosan wound liquid with the formula amount are applied at normal temperature and uniformly mixed, and the mixture is sealed and stored at 0-4 ℃ to obtain the transdermal drug delivery composition for treating acne.
When in use, the skin of a patient suffering from acne is cleaned and disinfected, then the epidermis is punctured by adopting a disposable medical skin roller pin with the thickness of 1.0-1.5mm in a deep, thin, shallow and dense mode, the skin transdermal administration is carried out, the administration amount is 5-10mL, and the transdermal administration composition is kept on the surface of the skin for 3-5min after the administration for full absorption; after 3 days of administration, the acne was removed by needle application and transdermal administration to the skin was performed again as described above.
Repeating the above operations according to the treatment condition of acne, and 3-5 times as a treatment course.
The formula of the transdermal drug delivery composition is obtained through repeated clinical verification, and the components interact with each other to achieve the best treatment effect.
Compared with the prior art, the invention has the following beneficial effects:
(1) according to the invention, different medicines are combined, wherein clindamycin effectively inhibits propionibacterium acnes, dexamethasone improves the red and swollen symptom of the inflammation of hair follicles, vitamin B6 inhibits secretion of skin grease, and the chitosan wound liquid dressing promotes repair and regeneration of damaged tissues, inhibits and repairs scars, and adjusts the dosage of each component, so that the effective utilization rate of the medicines is improved, and the adverse reaction of the medicines is reduced;
(2) the transdermal drug delivery composition for treating acne has the advantages of small dosage, quick response, bacteriostasis, anti-inflammation, promotion of wound healing, prevention or reduction of scar formation, small damage to skin, no thinning of stratum corneum and no adverse effect on the whole body.
Drawings
FIG. 1 is a comparison of a skin surface treatment before and after a single treatment with a composition for transdermal delivery of example 1 of the present invention for acne patients;
FIG. 2 is a comparison of subcutaneous treatment of acne patients after a single treatment with the composition of example 1 of the present invention.
Detailed Description
The present invention will be further described with reference to the following examples.
The starting materials used in the examples are all commercially available conventional products, of which:
the specification of the normal saline is 90mg/10mL by the content of sodium chloride;
the specification of the clindamycin phosphate injection is 0.3g/2mL based on the content of clindamycin phosphate;
the specification of the vitamin B6 injection is 0.1g/2mL calculated by the content of the vitamin B6;
the specification of the dexamethasone sodium phosphate injection is 5mg/1mL based on the content of dexamethasone sodium phosphate;
the chitosan content in the chitosan wound liquid dressing is 1.5 wt%, and the balance is water.
Example 1
A transdermal drug delivery composition for treating acne is composed of the following raw materials by volume:
the physiological saline, clindamycin phosphate injection, dexamethasone sodium phosphate injection, vitamin B6 injection and chitosan wound liquid with the formula amount are applied at normal temperature and mixed evenly, and the mixture is sealed and stored at 0 ℃ to obtain the transdermal drug delivery composition for treating acne.
Example 2
A transdermal drug delivery composition for treating acne is composed of the following raw materials by volume:
the physiological saline, clindamycin phosphate injection, dexamethasone sodium phosphate injection, vitamin B6 injection and chitosan wound liquid with the formula amount are applied at normal temperature and mixed evenly, and the mixture is sealed and stored at 0 ℃ to obtain the transdermal drug delivery composition for treating acne.
Example 3
A transdermal drug delivery composition for treating acne is composed of the following raw materials by volume:
the physiological saline, clindamycin phosphate injection, dexamethasone sodium phosphate injection, vitamin B6 injection and chitosan wound liquid with the formula amount are applied at normal temperature and mixed evenly, and the mixture is sealed and stored at 0 ℃ to obtain the transdermal drug delivery composition for treating acne.
Comparative example 1
Compared with example 1, the comparative example is different only in that dexamethasone sodium phosphate injection is not contained.
Comparative example 2
This comparative example differs from example 1 only in that no vitamin B6 injection was contained.
Comparative example 3
This comparative example is different from example 1 only in that the wound fluid dressing containing no chitosan was used.
Comparative examples 1 to 3 are formulations of transdermal delivery compositions used in clinic before study, examples 1 to 3 are formulations of transdermal delivery compositions of the present invention, which have good therapeutic effect on acne, wherein the formulation of example 1 has the best compatibility and the best therapeutic effect, and is the formulation of transdermal delivery composition used in clinic at present.
Examples 1-3 and comparative examples 1-3 when applied to acne treatment, the procedure was as follows:
when in use, the skin of a patient suffering from acne is cleaned and disinfected, then the epidermis is punctured by adopting a disposable medical skin roller pin with the thickness of 1.0-1.5mm in a deep, thin, shallow and dense mode, the skin transdermal administration is carried out, the administration amount is 5mL, and the transdermal administration composition is kept on the surface of the skin for 5min after the administration for full absorption; after 3 days of administration, the acne was removed by needle application and transdermal administration to the skin was performed again as described above. Repeating the above operations according to the treatment condition of acne, and 3 times is a treatment course.
After one treatment with the transdermal composition of example 1, the acne patients were analyzed for skin pathology using a VISIA skin tester, and the results are shown in fig. 1-2. FIG. 1 is a comparison of a skin surface treatment before and after treatment of the skin surface of an acne patient, from which it can be seen that acne is significantly reduced and skin lesions are partially resolved on the skin surface of the patient; FIG. 2 is a comparison of subcutaneous conditions before and after treatment of acne patients, from which it can be seen that the inflammation of the skin of the patients is significantly improved without damage to the stratum corneum.
The treatment effects of examples 1 to 3 and comparative examples 1 to 3 were compared, wherein the transdermal drug delivery compositions of comparative examples 1 to 3 had poor treatment effects and few clinical cases during clinical use, 5 acne patients (aged between 16 and 30 years) were randomly selected, respectively, and 20 acne patients (aged between 16 and 30 years) were randomly selected, respectively, from the clinical cases of the transdermal drug delivery compositions of examples 1 to 3, and the treatment results after one treatment course were evaluated.
The evaluation criteria were:
and (3) healing: the skin lesion subsides;
the effect is shown: skin lesions subsided > 60%;
the method has the following advantages: the skin damage is reduced by 20-60%;
and (4) invalidation: the skin lesions subsided < 20% or worsened.
The treatment results are shown in table 1.
TABLE 1 treatment results of the transdermal delivery compositions of examples 1-3 and comparative examples 1-3
| Item | Recovery, based on | Effective, is obtained by | Effectively, is% | Ineffectiveness, according to | Wound healing conditions | Stratum corneum condition |
| Example 1 | 100 | — | — | — | Good healing without inflammation | Without damage |
| Example 2 | 100 | — | — | — | Good healing without inflammation | Without damage |
| Example 3 | 100 | — | — | — | Good healing without inflammation | Without damage |
| Comparative example 1 | 60 | 25 | 15 | — | Slow healing and obvious inflammation | With slight injury |
| Comparative example 2 | 75 | 20 | 5 | — | Slow healing without inflammation | With slight injury |
| Comparative example 3 | 80 | 20 | — | — | Good healing with slight inflammation | With slight injury |
Claims (8)
1. A transdermal drug delivery composition for treating acne, characterized by: the composite material consists of the following raw materials in parts by volume:
2. the transdermal composition for the treatment of acne according to claim 1, characterized in that: the composite material consists of the following raw materials in parts by volume:
3. a transdermal composition for the treatment of acne according to claim 1 or 2 characterized by: the specification of the normal saline is 90mg/10mL by the content of sodium chloride.
4. A transdermal composition for the treatment of acne according to claim 1 or 2 characterized by: the specification of the clindamycin phosphate injection is 0.3g/2mL based on the content of clindamycin phosphate.
5. A transdermal composition for the treatment of acne according to claim 1 or 2 characterized by: the specification of the dexamethasone sodium phosphate injection is 5mg/1mL based on the content of dexamethasone sodium phosphate.
6. A transdermal composition for the treatment of acne according to claim 1 or 2 characterized by: the specification of the vitamin B6 injection is 0.1g/2mL calculated by the content of the vitamin B6.
7. A transdermal composition for the treatment of acne according to claim 1 or 2 characterized by: the chitosan wound liquid dressing contains 0.5-1.5 wt% of chitosan and the balance of water.
8. A method of preparing a transdermal composition for the treatment of acne according to claim 1 or 2, characterized in that: the method comprises the following steps:
the physiological saline, clindamycin phosphate injection, dexamethasone sodium phosphate injection, vitamin B6 injection and chitosan wound liquid with the formula amount are applied at normal temperature and uniformly mixed, and the mixture is sealed and stored at 0-4 ℃ to obtain the transdermal drug delivery composition for treating acne.
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| CN117838686A (en) * | 2024-01-03 | 2024-04-09 | 上海宜治生物科技有限公司 | Application of sparganolide B in preparing medicament for preventing or treating acne |
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