|Title of Invention||
A PROCESS OF MAKING A BIO-ACTIVE LIPID SULFUR COMPLEX
|Abstract||A process for making a bio-active lipid sulfur complex consisting of reacting a triglyceridic oils having an Iodine value from 50 -150 with with 1.5 - 10% sulfur at 120 - 150°C, under agitation, for 30 to 120 minutes, allowing the resultant oil sulfur complex liquid to cool to 20-35°C room temperature, holding the cooled liquid at room temperature for 1 hour to one week and filtering the liquid to obtain bio active lipid sulfur complex|
THE PATENTS ACT, 1970
A PROCESS OF MAKING A BIO-ACTIVE LIPID SULFUR COMPLEX.
SAURABH BHALCHANDRA APTE, OF 29 - A/1, PARK VIEW, SION (W), MUMBAI-400 022, MAHARASHTRA, INDIA, AN INDIAN NATIONAL.
The following Specification particularly describes the nature of this invention and the
manner in which it is to be performed :-
This invention relates to a process for making a bio-active lipid sulfur complex.
The use of sulfur for medical applications is well known. In Ayurved, Gandhak Druti, or Gaindhak taila has been used to cure various conditions including inflammatory states of tissue.
Larsen et al have recently synthesized a derivative of poly¬unsaturated fatty acids, where sulfur is introduced in the 3-positicn from the carboxylic group of the fatty acid and these sulfur derivatives were found to have inhibitory action on prosta-glandin synthetase, using liver homogenates in-vitro, employing labelled n-3 sulfur containing fatty acids for example Arachidonic acid. [ L.N. Larsen et al, Biochem. Biophy Acta (1992) 1348: 346-354]
It has now been possible, in accordance with the process outlined in this invention, to obtain bio-active lipid sulfur complexes by reacting refined triglycerides from both plant as well as animal origin with 2 to 20% sulfur at temperatures above the melting point of sulfur for an adequate period such that the reaction mixture is subject to a total heat amounting to 40 to 55 kilo calories per kilogram of oil.
The process resulted in a yellow to reddish/reddish brown substance slightly more viscous than the viscosity of the oil originally used.
In accordance with a preferred embodiment of the invention the preferred oils are oils having an Iodine value above 50. Where reaction occurred, the Iodine value decreased by 30 to 60%.
The sulfur moiety may bridge the gap between two glyceride molecules as a result of inter molecular bridging [I]. It is also possible that a sulfur bridge may be formed at the double bond of the fatty acids [II] or between two fatty acid chains attached to the glyceride backbone [III] of the unreacted triglycerides. All these possibilities are shown in figure 1 of the accompanying diagram where GB represents the glycerol backbone and FA the fatty acid chain and S the sulfur moiety
The lipid - sulfur complex so formed in accordance with this invention was seen to exhibit analgesic and anti-inflammatory activities on pharmacological testing and a good antimicrobial activity especially in anaerobes. The oral toxicity of these oils is very low, so much so, that, the subacute oral toxicity was noticed only at a dose of 65 ml / Kg . It showed no Gastro Intestinal (G. I.) bleeding in any animal.
In many cases the activity exhibited was equivalent if not superior to the activity exhibited by agents used currently in clinical practice.
U. V, and, HPLC studies showed a degree of polymerization. High thermal input without agitation results into resinification,
making the product devoid of any value, as a pharmaceutical material.
1] 1 Kg of Sesame oil was heated to 120°C for 3 hours, under constant agitation, with 20g of sulfur. It was allowed to get cooled to 23-25°C, by keeping overnight in an air-conditioned room. It was filtered through sintered glass funnel of Gi porosity.The Iodine value in reacted oil reduced from 60 to 40, and, viscosity was raised from 48 millipoises to 210 millipoises at25°C.
2] 0.5 Kg of Castor oil was treated with 20g of sulfur at 135°C for 1 hour, under constant agitation. It was allowed to cool to an ambient temperature of 20°C for 48 hours. It was filtered through a sintered glass filter of a G3 porosity. The Iodine value in reacted oil reduced from 151 to 85, and, viscosity increased from 350 millipoises to 360 millipoises at 25°C.
3] 2 Kgs of Sunflower oil was re-heated for 30 minutes at 140°C with 200g of sulfur under stirring. It was cooled to 20°C, using ice-water both, for 10 hours, and, then kept at ambient temperatures for 24 hours. It was filtered through an EKS filter pad. Iodine value in the treated oil to found to be decreased from 130 to 60, and, viscosity got built up from 29.54 millipoises to 155 millipoises at 25°C.
4] 1.5 Kg of Ground-nut oil was treated with 30g of sulfur under stirring to 130°C for 1 hour, and, allowed to get cooled to the ambient temperature. After 48 hours, it was cooled to 150°C for 18 hours, and, filtered by gravity through a Decron filter cloth. The resultant oil was found to have decreased Iodine value, from 130 to 78; and, its viscosity was found to be built-up from 45 millipoises to 170 millipoises at 25°C.
5] 500 g of tri-olein was reacted with 15 g of sulfur at 125 degrees C for 30 minutes, under stirring. It was cooled to ambient temperature held at thatfor 1 week and filtered. The viscosity increased from 120 millipoises to 480 millipoises and iodine value decreased from 255 to 90. This is an example using synthetic triglycerides.
Being extremely safe, (1) a 20% w/w ointment in an absorption base was prepared, and, (2) Soft gelatin capsules of 500mg were prepared to find out if the sulfur-oil complexes (sulfurated oils), prepared as above, have any effect in joint pain, and, joint swellings.
On use as an ointment as a rub, it is found to give relief on rubbing on painful areas, and, the effect lasts for 8 - 12 hours. If the same person takes a capsule every night before retiring it decreases pain, and, swelling, satisfactory to the user, within a month. No user has expressed any gastric discomfort, which is common with most of the analgesics and anti-inflammatories.
Following are a few typical example
1. A lady of 32 years age had severe pain in the neck and left
shoulder, due to sprain.
The Gandhak oil ointment reduced the pain completely on local application for 5 days twice a day.
2. Another lady of 55 years age had severe backache, for 13 years.An ointment with Gandhak oil ointment reduced it substantially, enabling here to carry out daily routine, within 3 months.
3. A female patient of 60 years age, suffering from cervical spondilitis, was prescribed rubbing Gandhak oil ointment, thrice a day. Pain and numbness was effectively controlled.
4. A woman patient of 49 years age, had a 3 year old history of accident and surgery of both knees, complained of severe induration swelling of both knees. Both, swelling and pain of knees reduced to tolerable level in 2 months using gandhak oil.
5. A male of 25 years age, having cervical spondilysis having acute pain at neck region, got relief from pain, on use of the sulfurated oil ointment in 3 weeks.
6. A male patient of 76 years age had acute pain, and, swelling in knees. Local use of the Gandhak oil ointment made it mild within 1 month.
7. A 48 years old male , had a thigh injury, resulting in acute pain and swelling. Using Gandhak oil ointment thrice a day provided complete relief in 10 days.
8. A 72 year old male patient having history of joint pain and
restricted movement of knees and ankles was given 500 mg
of sulfurated oil to be taken orally before retiring and rubbing
in the sulfurated oil in a 20 per cent ointment base on the
painful joints twice a day. The patient reported dramatic
improvement in mobility of the joints after two months and
decrease in pain and swelling.
In all the studies opinion was taken of the attending physician and of the patient as subjective parameters. In many cases lowering of E.S.R was observed.
1. A process for making a bio-active lipid sulfur complex consisting of reacting a triglyceridic oils having an Iodine value from 50 -150 with with 1.5 - 10% sulfur at 120 - 150°C, under agitation, for 30 to 120 minutes, allowing the resultant oil sulfur complex liquid to cool to 20-35°C room temperature, holding the cooled liquid at room temperature for 1 hour to one week and filtering the liquid to obtain bio active lipid sulfur complex.
2. A process for making a bio-active lipid sulfur complex as claimed in claim 1, in which Iodine value of the triglyceride oil is made to drop by 30 - 60%.
3. A process for making a bio-active lipid sulfur complex as claimed in claim 1, in which the viscosity of the tri glyceride oil is made to increase by 2.5 to 4 times.
Of R.K. Dewan & Co., Applicant's Patent Attorneys
|Indian Patent Application Number||811/MUM/2001|
|PG Journal Number||41/2007|
|Date of Filing||21-Aug-2001|
|Name of Patentee||SAURABH BHALCHANDRA APTE|
|Applicant Address||29-A/1. PARK VIEW, SION (W), MUMBAI|
|PCT International Classification Number||N/A|
|PCT International Application Number||N/A|
|PCT International Filing date|