Transnasal microemulsions containing diazepam

FIELD: pharmacology.

SUBSTANCE: invention relates to medications and concerns microemulsion for transnasal diazepam introduction, including carrier, which contains water, fatty acid ester, hydrophilic surface-active substance, polar solvent and alcohol, fatty acid and water are contained in carrier in approximately equal amounts, contained amount of alcohol exceeding amount of each of surface-active substance and polar solvent. Also described is method of transnasal diazepam introduction to patient who needs it.

EFFECT: quick beginning of active substance action and improvement of absorption.

16 cl, 1 tbl

 

The technical field

This invention relates to pharmaceutical compositions for delivery of diazepam through the mucous.

The level of technology

Status epilepticus is a neurological disease in which the mortality ranges from 3 to 35%. The main goal of treatment is the rapid regulation of pathological activity convulsions; the longer status epilepticus is not exposed to the treatment, the harder it is to control and the greater the risk of permanent brain damage.

Thus, for the patient's critical is a clear plan, including appropriate treatment effective drugs in adequate doses, with a suitable pharmaceutical composition, as well as the attention hypoventilation and hypotension. Currently, for the treatment of epileptic status employing multiple treatment regimens. For this purpose one of the most commonly used benzodiazepine is diazepam. Intravenous administration of anticonvulsants is the fastest way to suppress epileptic convulsions. However, when intravenous administration is not desirable and is deposited, for example, due to technical difficulties such as the need for sterile equipment and qualified personnel, and because of the possible development of thrombophlebitis can be very desirable other route of administration. To the ome, intravenous administration is often associated with hypotension, cardiac arrhythmia and depression of the Central nervous system. Consequently, Moolenaar et al., Int. J. Pharm., 5: 127-137 (1986) tried to introduce people diazepam several other routes, such as intramuscular injection, in the form of oral tablets and rectal solution. It turned out that only rectal introduction provides a fairly rapid absorption and therefore can be considered as alternative IV injection method injection. However, the rectal route is very inconvenient, especially in urgent cases. In U.S. patent 4863720, Burghardt described sublingual spray pharmaceutical drug in which the drug can be a benzodiazepine, optimally containing polyethylene glycol (PEG) and ethanol, di - and/or triglyceride of fatty acids and pharmaceutically acceptable propellant.

Recently it was found that the mucous membrane of the nose is a practical way of introducing many medical substances. Vnutripuzarnoe introduction has the advantage that the drugs can be introduced easily to achieve systemic or localized effect. However, the main problem with the intranasal drug administration is the fact that most of the molecules of the drug diffuses slowly and poorly through the nasal mucous membrane and therefore desirable level terapeuticas the th agent cannot be achieved simply by transnasal administration. An additional disadvantage is that the introduction is limited to a small amount, i.e. usually you cannot enter more than approximately 150 ml per nostril. Amounts exceeding specified, will flow into the throat and proglatavetsa.

Therefore, there is a need to solvents - mediums, which dissolve the desired drug, namely diazepam in a high concentration and yet do not irritate the nasal mucosa. Intranasal absorption of a drug can be increased sovmestnim the introduction of chemical adjuvant or accelerators permeability. For example, Lau and Slattery [Lau et al., Iit. J. Pharm., 54: 171-174 (1989)] was trying to enter a benzodiazepine, such as diazepam, by dissolving it in a number of solvents: triacetin, dimethyl sulfoxide, PEG 400, Cremophor EL, Lipal-9-LA, isopropylacetate and Azone. Although many of the solvents was dissolved diazepam in desirable concentrations, they irritated mucous and could not be used for transnasal administration. It was found that Cremophor EL less all irritate the nose, but nasal absorption in the case of the use of the media was very slow (Tmax≈1,4 h) and the peak concentration was lower than after IV injection.

Transnasal solution with improved properties described in the application U.S. 09/624305. The media for this solution is an aqueous medium containing aliphatic the cue alcohol C 1-C5, glycol, such as propylene glycol, and biological surfactant selected from the salts of bile acids and lecithins. These solutions preferably contain equal amounts of alcohol and glycol. It has been found that such solutions are effective for transnasal the introduction of certain drugs, particularly benzodiazepines. Recently, Li et al., Int. J. of Pharmaceuticals, vol.237, p.p.77-85, 2002, described microemulsions for fast delivery of diazepam through the nose. Microemulsions of diazepam, such as those described in Li et al., but possessing improved properties provided by the present invention.

The invention

According to this invention provides new compositions of microemulsions containing diazepam. Diazepam is injected intranasally in the form of microemulsions, which have better properties as compared with such emulsions are known from the literature. Microemulsions are composed of approximately equal amounts of ether, fatty acid and water, and the rest is hydrophilic surface-active agent, a polar solvent and an alcohol, preferably an aliphatic alcohol in the weight ratio providing alcohol in larger quantities than the amount of any of the other two components. Nasal introduction of the proposed microemulsions provides a high concentration of diazepam in plasma is e almost as fast as intravenous. These micro-emulsions are particularly suitable for rapid and timely treatment of patients in acute and/or urgent treatment of epileptic status and other seizures caused by fever.

Detailed description of the invention

According to this invention provides a microemulsion containing diazepam, which has advantages compared to microemulsions, are known from the literature. The microemulsion diazepam, described by Li et al., characterized by the content of acellerate about 15 wt.% and comparable water content. The compositions also contain an aliphatic alcohol, namely ethanol, glycol, namely propylene glycol, and Polysorbate 80, namely polyoxyethylene (20)-servicemanual. In one of the compositions described in Li et al., the concentration of ethanol is about one quarter of the concentration of each of glycol and Polysorbate 80. Another weight ratio of the three components is the same. It is argued that the composition in which the weight ratio of the alcohol, glycol and Polysorbate 80 is 1:1:1, exceed the properties of the composition with a lower alcohol content compared with quantities of glycol and Polysorbate 80.

According to this invention provides compositions with a low content of polar solvent, such as glycol, even compared with the best composition described in Li et al. Yes is it in contrast to the compounds described by Li et al., the compositions according to the invention are characterized by the alcohol content greater than the amount of the polar solvent and the hydrophilic surfactants (e.g. Polysorbate 80) separately. These compositions have the best properties regarding at least one of several criteria, such as described by Li et al., and it is the speed of the commencement of the active substance, solubilization of diazepam, particle size and in vivo absorption. The compositions of this invention contain about equal quantities of water and fatty acid ester, preferably at least 10 wt.% each, more preferably about 10-25 wt.% each and most preferably about 15 wt.% everyone else is surface-active hydrophilic substance, a polar solvent and an alcohol, and alcohol is always present in greater numbers than the other two components. Suitable fatty acid esters include, without limitation, tillaart, atelierista, Etisalat, ethyllinoleate, proprietorial, isopropylene, isopropylmyristate and combinations thereof. Particularly preferred fatty acid ester is tillaart. Suitable hydrophilic surfactants include, without limitation, TWEEN 80 (POLYSORBAT 80), TWEEN 20, 40, 60, and combinations thereof. Suitable polar solvents is clucalc, without limitation, propylene glycol, polyethylene glycols such as PEG 300, PEG 400, PEG 600, and combinations thereof. Particularly preferred alcohols include lower alkanols, such as ethanol and isopropanol. You can use any aliphatic alcohol containing from 2 to 12 and, more preferably, from 2 to 8 carbon atoms. Particularly suitable alcohol is ethanol.

According to one preferred variant compositions according to the invention contain equal amounts of water and acellerate, preferably about 15 wt.% everyone else are Polysorbate 80, polypropylenglycol and ethanol, and the ethanol content of these three components is always greater than the content of the other two.

Examples

Compositions containing tillaart, according to the invention may include Polysorbate 80: polypropylenglycol: ethanol in a weight ratio 1,0:0,86:1,15; 1,0:0,72:1,29 and 1,0:1,0:1,5. Specific examples of the compounds shown in the Table, where the content of each component is indicated in percent by weight. These examples serve to illustrate but not limit the invention.

Table
ComponentComposition (% weight/weight)Composition (% weight/weight)Composition (% weight/weight)
Tillaart15,015,015,0
Polysorbate 8023,323,320,0
Polypropylenglycol20,016,720,0
Ethanol26,730,030,0
Water15,015,015,0

These emulsions receive the usual way. First diazepam is dissolved in acellerate, which is the oil component. The emulsion obtained two-phase and have a good spatter due to a higher content of ethanol. Diazepam is dissolved in the proposed emulsions at a concentration of about 40 mg/ml Therefore, the introduction of therapeutic doses of diazepam intranasally by one or two clicks in the nostril using a suitable conventional spray containing 250-500 ál of microemulsions.

From a clinical point of view intranasal introduction often provides greater duration of anticonvulsive effect. Therefore, the microemulsion according to the invention is preferred in the treatment of epileptic status and other conditions, require fast suppression of convulsions. The high content of water in these emulsions compared to the solutions described above, leads to more rare irritation of the nasal tissues. Although this invention is described for diazepam as anticonvulsant, it is obvious that the proposed emulsion can be applied to other recognized therapeutic substitutes diazepam.

This invention is not limited to the described specific examples. Indeed, in addition to described various modifications of the invention are evident from the description. Such modifications are included in the scope of this invention defined by the claims.

1. The microemulsion for transnasal administration of diazepam, comprising a carrier containing water, a fatty acid ester, a hydrophilic surfactant, a polar solvent and alcohol, and the fatty acid and water contained in the carrier in approximately equal amounts, and the alcohol contains in excess of the amount of each surfactant and a polar solvent.

2. The microemulsion according to claim 1, characterized in that the fatty acid ester is selected from the group consisting of acellerate, atelierista, aterballetto, ethyllinoleate, profiletemplate, Isopropylamine, isopropylmyristate and the x combinations.

3. The microemulsion according to claim 1, characterized in that the hydrophilic surfactant selected from the group consisting of Polysorbate 80, Tween 20, 40, 60, and combinations thereof.

4. The microemulsion according to claim 1, wherein the polar solvent is selected from the group consisting of propylene glycol, polyethylene glycol and combinations thereof.

5. The microemulsion according to claim 4, characterized in that the polyethylene glycol is selected from the group consisting of PEG 300, PEG 400, Peg 600, and combinations thereof.

6. The microemulsion according to claim 1, wherein the alcohol is selected from the group consisting of ethanol, isopropanol and combinations thereof.

7. The microemulsion according to claim 1, characterized in that the fatty acid ester and water are individually not less than 10% by weight of the carrier.

8. The microemulsion according to claim 1, characterized in that the fatty acid ester and water are separately about 10-25% by weight of the carrier.

9. The microemulsion according to claim 1, characterized in that the fatty acid ester and water are separately about 15% by weight of the carrier.

10. The microemulsion according to claim 1, characterized in that it contains about 20 wt.% the specified hydrophilic surfactant and the weight ratio of the hydrophilic surfactant: the polar solvent: alcohol is about 1.0:1.0 to:1,5.

11. The way transnasal administration of diazepam to a patient in need of it, consisting in the introduction of diazepam in the microemulsion according to any one of claims 1 to 10.

12. The microemulsion for transnasal administration of diazepam, in which the medium contains tillaart, Polysorbate 80, propylene glycol, ethanol and water, each component of acellerate and water is 15% by weight of the carrier, and the weight ratio of Polysorbate 80: propylene glycol: ethanol is such that the number of alcohol more quantities of the other two components.

13. The microemulsion according to item 12, characterized in that it contains about 23,3% wt. Polysorbate 80 and the weight ratio of Polysorbate 80: propylene glycol: ethanol is 1.0:0,86:1,15.

14. The microemulsion according to item 12, characterized in that it contains about 23,3% wt. Polysorbate 80 and the weight ratio of Polysorbate 80: propylene glycol: ethanol is 1.0:0,72:1,29.

15. The microemulsion according to item 12, characterized in that it contains about 20 wt.% Polysorbate 80 and the weight ratio of Polysorbate 80: propylene glycol: ethanol is 1.0:1.0 to:1,5.

16. The way transnasal administration of diazepam to a patient in need of it, consisting in the introduction of diazepam in the microemulsion according to any one of p-15.



 

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