CN108703946B - A kind of transdermal absorption formulation for treating diabete peripheral herve pain - Google Patents
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Abstract
The invention belongs to chemical medicine fields, and in particular to a kind of transdermal absorption formulation for treating diabete peripheral herve pain.The transdermal absorption formulation is made of gamma-aminobutyric acid analog class antalgesic and three carbonyl nitrogen-containing compound of small molecule, and the pharmaceutic adjuvant of preparation is card pool nurse 940, glycerol, Tween 80, triethanolamine, Laurocapram and distilled water.Above-mentioned transdermal absorption formulation topical administration has significant analgesic effect to diabete peripheral herve pain.And the dosage of gamma-aminobutyric acid analog class antalgesic can be reduced.
Description
Technical field
The invention belongs to chemical medicine fields, and in particular to a kind of Transdermal absorption system for treating diabete peripheral herve pain
Agent.
Background technique
Diabetes are a kind of metabolic diseases characterized by blood glucose rise.The disease and cardiovascular and cerebrovascular disease, tumour are mesh
The preceding three big major chronic illnesses for threatening human health.In recent years, with the improvement of living standards, the accelerating rhythm of life etc.,
Apparent ascendant trend is also presented in diabetes morbidity, and disease incidence has been up to 12% at present；And prediabetes crowd is also increasingly huge
Greatly.And glycemic control needs Long-term taking medicine.
Diabete peripheral herve pain is one of major complications of diabetes, and patients account for about diabetes total number of persons
7.5~24%.Early in 19th century mid-term, American-European countries has been noted that the high phenomenon of diabetic's peripheral neuralgia disease incidence.
Diabete peripheral herve pain pathogenesis it is not immediately clear that supposition may be with metabolic disorder caused by hyperglycemia, neurotrophy
Blood vessel hypoxic-ischemic, neurotrophic factor are reduced and the collective effect of many factors such as role of autoimmune factors is related.Diabetes week
Neuralgia patient is enclosed often to show as limbs pain, feel decline, is numb, scorching hot, ice-cold etc., can also appear as spontaneous pain,
Allodynia.Abnormal sensory include it is numb, ant walks, worm climbs, generate heat, the sample that get an electric shock feeling etc., paralgesia is from distal end toe uplink
Reachable above-knee, patient wears socks and wears gloves sample feeling.The serious case of sensory disturbance may occur in which that joint of lower extremity is sick and foot is burst
Ulcer generally requires amputation when being developed to diabetic foot ulcer, seriously affects patients ' life quality.In China, Diabetic Peripheral mind
Dysmenorrhoea patient accounts for the 85% of diabetes total number of persons, and pain seriously affects the quality of life of patient, and lethality of disabling is higher.
Since its pathogenic factor and mechanism is not still fully aware of, clinical treatment can only anti symptom treatment.At present clinically to sugar
The treatment for urinating sick peripheral neuralgia is general by the way of glycemic control Combinated easing pain agent.Wherein analgesic includes opiates town
Pain medicine, tricyclic antidepressant, selective serotonin and norepinephrine reuptake inhibitors, γ-aminobutyric acid are similar
Object etc..Wherein there are tolerance, drug withdrawal syndrome and abuse risks for opium kind analgesics.Tricyclic antidepressant early in
Have been used within 1977 neuralgic treatment, mechanism is to block sodium channel, calcium channel, increases monoamine release and blocks NDMA
Receptor.But since side effect (such as drowsiness, orthostatic hypotension, anticholinergic side reaction) is strong and incidence is high, patient
It is difficult to be resistant to and limit application.Selective serotonin and norepinephrine reuptake inhibitors such as Duloxetine are to nerve
Pain is also effective, but it is also not satisfactory that effect is used alone.Gamma-aminobutyric acid analog is mainly Pregabalin, Gabapentin.
Gabapentin mitigates pain and blocking primary afferent neuron to depolarize in conjunction with voltage-gated calcium channel, tests table
It is bright its to treatment diabete peripheral herve pain it is more effective compared with other neuralgias；Pregabalin is the homologous chemical combination of Gabapentin
Object is particularly effective diabete peripheral herve pain and postherpetic neuralgia.Both the above curative effect of medication is high, side effect is low,
Potential applicability in clinical practice is wide, but expensive, cannot function as a line routine administration.Clinical diabete peripheral herve pain is controlled at present
Treatment scheme is mostly that Duloxetine exclusive use or Pregabalin, Duloxetine joint plus spray fourth use.
A small number of external preparations existing at present are approved for the treatment of diabete peripheral herve pain.The theory of local application is excellent
Gesture is to reduce side effect, and the interaction between no drug is not usually required to dose titration.As supervised by U.S.'s food and medicine
The agent of lidocaine lagging, capsaicin ointment, the isosorbide dinitrate spray etc. that management board's approval lists.
Summary of the invention
For the existing existing above problem, the object of the present invention is to provide a kind of diabete peripheral herve pains for the treatment of
Transdermal absorption formulation.Unresolved above-mentioned technical problem, The technical solution adopted by the invention is as follows:
A kind of transdermal absorption formulation for treating diabete peripheral herve pain, by gamma-aminobutyric acid analog, is shown below
Compound (I) and pharmaceutic adjuvant be made:
R is one of H, methyl, ethyl in the compound (I)；The gamma-aminobutyric acid analog is Puri bar
One of woods, Gabapentin.
Preferably, the gamma-aminobutyric acid analog is Pregabalin, and R is H in the compound (I).
Preferably, the gamma-aminobutyric acid analog is Pregabalin, and R is methyl in the compound (I).
Preferably, the gamma-aminobutyric acid analog is Pregabalin, and R is ethyl in the compound (I).
Preferably, the gamma-aminobutyric acid analog is Gabapentin, and R is H in the compound (I).
Preferably, when R is H in the compound (I), the gamma-aminobutyric acid analog and compound
(I) weight part ratio is 6~9 parts by weight of gamma-aminobutyric acid analog, 1 parts by weight of compound (I)；
It is further preferred that the weight part ratio of the gamma-aminobutyric acid analog and compound (I) are γ-aminobutyric acid
9 parts by weight of analog, 1 parts by weight of compound (I).
The scheme further preferred as another, the weight part ratio of the gamma-aminobutyric acid analog and compound (I)
For 7 parts by weight of gamma-aminobutyric acid analog, 1 parts by weight of compound (I).
For the transdermal absorption formulation of above-mentioned treatment diabete peripheral herve pain, the dosage form of the transdermal absorption formulation is preferred
For gelling agent, the pharmaceutic adjuvant includes card pool nurse 940, glycerol, Tween 80, triethanolamine and distilled water.
Further, the pharmaceutic adjuvant further includes Laurocapram.
Wherein, when in compound (I) R be H, methyl, ethyl when, the structural formula of compound (I) respectively as following formula I A, IB,
Shown in IC:
Wherein the preparation method of compound (IA) discloses in the patent documents such as CN200710036109.0；Compound
(IB), compound (IC) is respectively the dimethyl ester and diethylester of compound (IA), can on the basis of compound (IA) by with
Methanol, ethanol synthesis are formed.To those skilled in the art, esterification belongs to typical organic synthesis, can join
See that Zhang great Guo writes Chemical Industry Press's " fine organism unit reaction synthetic technology handbook " published in 2014.
In a preferred scheme, the transdermal absorption formulation of the treatment diabete peripheral herve pain is by compound
(IA), Pregabalin, card pool nurse 940, glycerol, Tween 80, triethanolamine, Laurocapram and distilled water are made, specific prescription
It is as follows: Pregabalin 70g, compound (IA) 10g, card pool 940 21g of nurse, glycerol 78g, Tween 80 21g triethanolamine 32g, the moon
Osmanthus Azone 7g and distilled water 1261g.Specifically the preparation method is as follows: recipe quantity Acritamer 940 is taken to add 1029g distilled water, stand
Make sufficiently to be swollen overnight；The grinding of recipe quantity glycerol, which is added, to be made to soak, and recipe quantity triethanolamine is added to be ground into clear gel matrix.It takes
Surplus distilled water, recipe quantity Tween 80, Laurocapram, compound (IA), Pregabalin stir, 60 in addition gel-type vehicle~
90 revs/min are stirred 5~20 minutes, and cream pipe is distributed into.
In another preferred scheme, the transdermal absorption formulation of the treatment diabete peripheral herve pain is by compound
(IA), Gabapentin, card pool nurse 940, glycerol, Tween 80, triethanolamine, Laurocapram and distilled water are made, specific prescription
It is as follows: Gabapentin 90g, compound (IA) 10g, card pool 940 21g of nurse, glycerol 78g, Tween 80 21g triethanolamine 32g, the moon
Osmanthus Azone 7g and distilled water 1241g.Specifically the preparation method is as follows: recipe quantity Acritamer 940 is taken to add 1029g distilled water, stand
Make sufficiently to be swollen overnight；The grinding of recipe quantity glycerol, which is added, to be made to soak, and recipe quantity triethanolamine is added to be ground into clear gel matrix.It takes
Surplus distilled water, recipe quantity Tween 80, Laurocapram, compound (IA), Gabapentin stir, 60 in addition gel-type vehicle~
90 revs/min are stirred 5~20 minutes, and cream pipe is distributed into.
Above-mentioned Pregabalin English entitled Pregabalin, the entitled Gabapentin of Gabapentin English.
The transdermal absorption formulation of above-mentioned treatment diabete peripheral herve pain is applied to illing skin such as forearm or shank position.
Human administration's dosage is calculated by 60kg weight, is calculated with Pregabalin or Gabapentin, and daily dosage is 100 mg~200mg.
The dosage of Pregabalin or Gabapentin can be significantly reduced, to be conducive to control drug use cost, and avoids drug oral
The adverse effect to gastrointestinal tract and liver is administered.Patient can feed protein-contng foodstuffs according to conventional in drug administration process.But it should
It avoids being administered at skin injury, to prevent drug from generating stimulation to damaged skin.Inventor pass through experimental studies have found that, chemical combination
Object (I) combines topical administration with Pregabalin or Gabapentin to the therapeutic effect of diabete peripheral herve pain better than Pregabalin
Or Gabapentin independent medication, and the safety of topical administration is better than traditional Oral administration.
Specific embodiment
Below with reference to the detailed explanation present invention of specific embodiment, following embodiment is only for technical solution of the present invention
It is explained, the present invention is not limited to following embodiments.
The gelling agent and its preparation of 1 anti-diabetic peripheral neuralgia of embodiment
Gelling agent prescription: Pregabalin 70g, compound (IA) 10g, card pool 940 21g of nurse, glycerol 78g, Tween 80 21g
Triethanolamine 32g, Laurocapram 7g and distilled water 1261g.
Preparation method: taking recipe quantity Acritamer 940 to add 1029g distilled water, and standing overnight makes sufficiently to be swollen；Recipe quantity is added
Glycerol grinding makes to soak, and recipe quantity triethanolamine is added to be ground into clear gel matrix.Remainder amount distilled water, recipe quantity Tween 80,
Laurocapram, compound (IA), Pregabalin stirring, are added in gel-type vehicle and stir 8 minutes for 90 revs/min, packing is used as medicine
With ointment tube to obtain the final product.
The gelling agent and its preparation of 2 anti-diabetic peripheral neuralgia of embodiment
Gelling agent prescription: Gabapentin 90g, compound (IA) 10g, card pool 940 21g of nurse, glycerol 78g, Tween 80 21g
Triethanolamine 32g, Laurocapram 7g and distilled water 1241g.
Preparation method: taking recipe quantity Acritamer 940 to add 1029g distilled water, and standing overnight makes sufficiently to be swollen；Recipe quantity is added
Glycerol grinding makes to soak, and recipe quantity triethanolamine is added to be ground into clear gel matrix.Remainder amount distilled water, recipe quantity Tween 80,
Laurocapram, compound (IA), Gabapentin stirring, are added in gel-type vehicle and stir 12 minutes for 60 revs/min, packing is used as medicine
With ointment tube.
The Effect tests of 3 anti-diabetic peripheral neuralgia prescription of embodiment
Healthy male SD rat, 190~200g of weight are raised in the laboratory SPF.Streptozotocin is slow using sodium citrate
Fliud flushing dissolution, matching while using.Every rats by intraperitoneal injection streptozotocin 12mg after Rat Fast 24 hours.Streptozotocin note
The 14th day after penetrating, takes diabetes rat to occur the time of reactions such as licking foot, shout, jump using hot plate method measurement rat, that is, give
Pyrocondensation foot incubation period before medicine, hot plate temperature are 51-52 DEG C.Every rat replication 3 times, twice measurement between be spaced 15 points
Clock, pyrocondensation foot incubation period before taking the mean value of 3 measurement results to represent the administration of the rat.
The 15th day after streptozotocin injection, rat is randomly divided into 6 groups, every group 6, rat back shaving, in shaving
Smear administration in region:
Model group smears physiological saline, one time a day successive administration 7 days；
Dimethyl sulfoxide is added in Pregabalin by Pregabalin group, and every rat smears give Pregabalin 2.1mg every time,
It is administered daily 1 time, successive administration 7 days；
Dimethyl sulfoxide is added in Gabapentin by Gabapentin group, and every rat smears give Gabapentin 2.7mg every time,
It is administered daily 1 time, successive administration 7 days；
Dimethyl sulfoxide is added in compound (IA) by compound (IA) group, and every rat is smeared every time gives compound (IA)
0.3mg is administered daily 1 time, and successive administration 7 days；
Pregabalin and compound (IA) are added two according to the ratio of weight ratio 7:1 by Pregabalin+compound (IA) group
Methyl sulfoxide smears administration, is administered daily 1 time, successive administration 7 days, calculates each dosage of every rat with Pregabalin
For 2.1mg.
Gabapentin and compound (IA) are added two according to the ratio of weight ratio 9:1 by Gabapentin+compound (IA) group
Methyl sulfoxide smears administration, is administered daily 1 time, successive administration 7 days, calculates each dosage of every rat with Gabapentin
For 2.7mg.
Last dose next day occurs the time of reactions such as licking foot, shout, jump, i.e., using hot plate method measurement rat again
Pyrocondensation foot incubation period after administration, hot plate temperature are 51-52 DEG C.Every rat replication 3 times, twice measurement between be spaced 15 points
Clock, pyrocondensation foot incubation period after taking the mean value of 3 measurement results to represent the administration of the rat.
Percentage is improved according to the threshold of pain that following formula calculates every rat: before percentage (%)=1-(administration is improved in the threshold of pain
Pyrocondensation sufficient incubation period after pyrocondensation foot incubation period-administration)/preceding pyrocondensation sufficient incubation period is administered.
Using statistical software to pyrocondensation sufficient incubation period and the threshold of pain are improved percentage and compared before the administration of each group rat, after administration
Compared with comparison among groups are examined using t, and P < 0.05 is considered as significant difference.
Pyrocondensation foot latency result see the table below before the administration of each group rat, after administration
In table: * is indicated: P < 0.01 compared with model group；# is indicated: Pregabalin+compound (IA) group and Pregabalin group
It compares or Gabapentin+compound (IA) group P < 0.01 compared with Gabapentin group.
By result as it can be seen that preceding each group rat pyrocondensation sufficient incubation period is administered without significant difference.Compound (IA) group is removed after administration
Outside, the pyrocondensation of other each groups sufficient incubation period and the threshold of pain improve percentage and are all remarkably higher than model group (P < 0.01).Wherein, Puri bar
Percentage point is improved in pyrocondensation sufficient incubation period and the threshold of pain after the administration of woods+compound (IA) group and Gabapentin+compound (IA) group
It is not significantly higher than Pregabalin group and Gabapentin group (P < 0.01).As it can be seen that the indices of compound (IA) group and model group
No difference of science of statistics, but compound (IA) combines topical administration with Pregabalin or Gabapentin, is remarkably improved the latter to sugar
The threshold of pain for urinating sick peripheral neuralgia rat model, improves its analgesic effect.
Above embodiments give example to effect of the invention and show.But above-described embodiment is for explaining only the invention,
Not for limiting the scope of protection of the present invention.To those skilled in the art, in the structure and activity of compound (IA)
Under the premise of disclosed, analog or its ester, salt after the variation of compound (IA) substituent group etc. are such as compound (IB), compound (IC)
Being with activity similar with compound (IA) can be with rational expectation, and can pass through limited trials confirmation.
Claims (7)
1. a kind of transdermal absorption formulation for treating diabete peripheral herve pain, which is characterized in that by gamma-aminobutyric acid analog,
The compound (I) and pharmaceutic adjuvant being shown below are made:
R is H in the compound (I)；The gamma-aminobutyric acid analog is one of Pregabalin, Gabapentin；It is described
The weight part ratio of gamma-aminobutyric acid analog and compound (I) are 6~9 parts by weight of gamma-aminobutyric acid analog, compound (I)
1 parts by weight.
2. the transdermal absorption formulation for the treatment of diabete peripheral herve pain according to claim 1, which is characterized in that described
Gamma-aminobutyric acid analog is Pregabalin.
3. the transdermal absorption formulation for the treatment of diabete peripheral herve pain according to claim 1, which is characterized in that described
Gamma-aminobutyric acid analog is Gabapentin.
4. the transdermal absorption formulation for the treatment of diabete peripheral herve pain according to claim 1, which is characterized in that described
The weight part ratio of gamma-aminobutyric acid analog and compound (I) are 9 parts by weight of gamma-aminobutyric acid analog, 1 weight of compound (I)
Measure part.
5. the transdermal absorption formulation for the treatment of diabete peripheral herve pain according to claim 1, which is characterized in that described
The weight part ratio of gamma-aminobutyric acid analog and compound (I) are 7 parts by weight of gamma-aminobutyric acid analog, 1 weight of compound (I)
Measure part.
6. according to the transdermal absorption formulation of the described in any item treatment diabete peripheral herve pains of claim 4 or 5, feature exists
In the dosage form of the transdermal absorption formulation is gelling agent, and the pharmaceutic adjuvant includes card pool nurse 940, glycerol, Tween 80, three second
Hydramine and distilled water.
7. the transdermal absorption formulation for the treatment of diabete peripheral herve pain according to claim 6, which is characterized in that the medicine
It further include Laurocapram with auxiliary material.
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| CN101401783A (en) * | 2007-09-16 | 2009-04-08 | 杨喜鸿 | Percutaneous absorption agent containing Ailamode, preparation method and medical uses thereof |
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|---|---|---|---|---|
| WO2022157526A1 (en) | 2021-01-22 | 2022-07-28 | Egis Gyógyszergyár Zrt. | Topical composition comprising pregabalin |
| WO2022157527A1 (en) | 2021-01-22 | 2022-07-28 | Egis Gyógyszergyár Zrt. | Topical formulation containing dispersed pregabalin |
| WO2022157525A1 (en) | 2021-01-22 | 2022-07-28 | Egis Gyógyszergyár Zrt. | Topical formulation containing modified phospholipid compounds |
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| CN108703946A (en) | 2018-10-26 |
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