Natural mixture composed of higher primary aliphatic...

Details Natural mixture composed of higher primary aliphatic... Natural mixture composed of higher primary aliphatic...

1994-11-07

2001-05-22

Criares, T J (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C-o-group doai

C514S787000, C514S925000

Reexamination Certificate

active

06235795

ABSTRACT:

INTRODUCTION
This invention is related with the obtention of a new natural mixture composed by higher aliphatic primary alcohols eventually in an extended range of 22 to 38 carbon atoms, specially those between 24 and 34 carbon atoms and more specially those of 24, 26, 28, 30, 32 and 34 carbon atoms. This mixture shows a relative composition of each alcohol that is highly reproducible from batch to batch.
The present invention is related, mainly, with the pharmaceutical industry and particularly with the development of pharmaceuticals formulations with specific properties, because they can be used against gastric and duodenal ulcers as well as an antiinflamatory agents.
These formulations contains, as active ingredient, a natural mixture of higher primary aliphatic alcohols of lineal chain, from 24 to 34 carbon atoms, especially those of 24, 26, 28, 30, 32 and 34 carbon atoms obtained from bee wax (M.H.A.A.B.W. in the rest of the text).
Drugs with specific pharmacological properties, based in the use, as an active ingredient of this higher primary aliphatic alcohols saturated of lineal chain from 24 to 34 carbon atoms are not reported with frequency, only the natural mixture obtained from sugar cane wax (EPA 0 488 928) has been reported previously.
The utilization of products produced by bee in empiric medicine is known since before our Era. With the development of new methods of analysis it was posbile to identify, in many cases, the active principles present in these products, that has permited to understood some biological and pharmacodynamics effects of them. Among these products, with therapeutics properties, can be signaled the royal jelly, honey, pollen and bee wax. This last one is generally used in the pharmaceutical and cosmetics industries taking into account their nutritives, cleaning and other medicinal properties as well as it possibilities to be used as false face for skin. Bee wax is mainly composed by the following type of compounds:
saturated and unsaturated long chain hydrocarbons (55-75%) from 21 to 37 carbon atoms
fatty esthers (aproximately 30%), that contains lineal alcohols of long chains (from 16 to 30 carbon atoms)
free fatty acids (aproximately 1-5%) in a range between 16 to 30 carbon atoms, also the 18:1 acid that represents 30% of the acidic fraction.
free alcohols of long chain (aproximately 1-7%), being triacontanol, octacosanol and hexacosanol the most abundant ones.
other polar constituents (aproximately 1-3%).
The procedure of the current invention is based on a homogeneous phase saponification process of the bee wax, previously melted, with concentrated solutions of alkaline and alkaline terrum hydroxides, especially those of low molecular weight and more especially with those of sodium, potassium and calcium.
The concentration of the hydroxide solutions must be such that the ratio in weight of the corresponding hydroxide with that of the bee wax to be processed must be over 5% on, specially from 8 to 25% and more specially, from 15 to 25%. The saponification process remains for a period of 30 minutes on and more specially from 2 to 5 hours.
The solid, obtained in this step, is taken to a solid-liquid extractor, where M.H.A.A.B.W. is selectively extracted with adequate organic solvents, choosen among ketones from 3 to 8 carbon atoms, hydrocarbons from 6 to 9 carbon atoms, alcohols from 1 to 5 carbon atoms, haloforms as well as aromatic compounds such as benzene and it derivatives, including mixtures of them. Some of the solvents used in the present invention are the following: acetone, methyl ethyl ketone, pentanone, hexanone, heptanone, 2 methyl-pentanone, ethanol, methanol, 2-propanol, butanol, terbutanol, pentane, hexane, heptane, octane, chloroform, 1,2 dichloroethane, dichloromethane, trichloroethane, 1,2,3 trichloropropane, benzene, toluene, phenol, p-methyl toluene and others.
The extraction is carried out in periods ranging between 5 up to 10 hours. Afterwards, the product is successively crystallized using the above mentioned solvents or their mixtures. The yield attained ranges about 30%, while the purity of the product (M.H.A.A.B.W.) is in a attained ranges from 80 to 98% and more especially between 90 and 98%.
The product (M.H.A.A.B.W.) thus obtained in the present invention is a mixture composed by higher primary aliphatic alcohols ranging between 24 to 34 carbon atoms. It shows a fusion point between 80.0 and 82.5° C. The proposed procedure for obtaining M.H.A.A.B.W. from bee wax has some advantages with regards to other previously reported. One of these advantages is related with the short obtention time. Other advantage of this invention is related with the practical yields of M.H.A.A.B.W. obtained (near 30% in weight) compared with other results previously described. Other advantage of the proposed procedure is related with the purity degree of the obtained product, the one that is significantly higher than that of other works previously reported. In Table 1 is reported the more general qualitative and quantitative composition of the M.H.A.A.B.W. and in Table 2 is reported the qualitative and quantitative composition of the M.H.A.A.B.W.
TABLE 1
General qualitative and
quantitative composition of M.H.A.A.B.W. obtained
Percent in the
Component
mixture
1-tetracosanol
 9.0-15.0%
1-hexacosanol
12.0-18.0%
1-octacosanol
13.0-20.0%
1-triacontanol
20.0-30.0%
1-dotriacontanol
13.0-21.0%
1-tetratriacontanol
1.5-3.5%
TABLE 2
Specific qualitative and quantitative composition of
M.H.A.A.B.W. obtained
Percent in the
Component
mixture
1-tetracosanol
12.5 +/− 1.0%
1-hexacosanol
14.5 +/− 1.2%
1-octacosanol
16.5 +/− 2.0%
1-triacontanol
24.6 +/− 1.6%
1-dotriacontanol
16.7 +/− 1.4%
1-tetratriacontanol
 2.3 +/− 0.5%
The daily dosage of M.H.A.A.B.W. to be used for treatment of different diseases has been established between 1 to 100 mg per day and the most adequate route of administration is oral, in form of tablets as well as granules or capsules. Although, this drug can be administered parenterally or topically, taking into account the uses that are recomended in the present invention.
The pharmaceutical formulation contains as an active ingredient from 0.5 to 25.0% wt of M.H.A.A.B.W. This dosage is obtained by mixing this M.H.A.A.B.W. with different excipients, such as agglutinants, disintegrators, lubricants, sliders or just fillers. In these excipients are included lactose, corn starch, saccharose, magnesium stearate, microcrystalline cellulose, sodium croscarmellose gelatin, cellulose acetophtalate, titanium dioxide, special talc for tablets, polyethylenglycol, polivinylpirrolidone and others.
One of the objectives of this invention is to obtain, isolate and purify the natural mixture composed by higher primary aliphatic alcohols in the range from 24 to 34 carbon atoms starting from the bee wax, specifically the one that contains the primary alcohols of 24, 26, 28, 30, 32 and 34 carbon atoms.
Other objective of this invention is to use those natural mixture, at relatively low doses, as a component of the pharmaceutical formulation in drugs used against gastric and duodenal ulcers. Proving that this new M.H.A.A.B.W. reduce significantly the gastric ulcers induced by aspirin, ethanol, indomethacine and other related drugs that are able to produced gastric ulcers in patients under treatment. Also, this M.H.A.A.B.W. reduce significantly the duodenal ulcers.
Other of the objectives of the present invention is the development of pharmaceutical formulations, that contains M.H.A.A.B.W. as active ingredient, to be used as antiinflamatory drugs, both administered by oral, topic of parenteral route.
Finally, a global valoration of this M.H.A.A.B.W. obtained in the present invention and proposed to be used as an active ingredient and drug formulations, can concluded that it is a very safety and well tolerated mixture, that represents an important advantage. This can be sustented by the results obtained in acute, subchronic and chronic toxicity assays developed in rodents and rab

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