Unorganized Drugs Lecture 10 PDF

 Unorganized drugs. Definition: Nature: mixtures of chemical substances or decomposition products of substances present in the biological source of the drug. -Source: derived from parts of plants or animals, normally or pathologically, by some process of extraction: incision, dec...

 Unorganized drugs. Definition: Nature: mixtures of chemical substances or decomposition products of substances present in the biological source of the drug. -Source: derived from parts of plants or animals, normally or pathologically, by some process of extraction: incision, decoction, and expression. Forms: Solid to semisolid, but some, such as oils and balsams, are fluids. Description: No cellular or definite structures No Morphological terms so we use physical characters of form, color, fracture; solubility and chemical tests..  Classification 1- Resins & Resin combination (large organic aids, for protection: a – Resin → Colophony, Guiacum. b – Oleoresin → Mastic, Copaiba, Canada Turpentine. c –Oleogumresin → Myrrh, Asafoetida d- Balsams → Benzoin, Balsam Peru 2- Gums (polysaccharide ,pathological) → Acacia, Tragacanth, Guar 3- Dried Extracts → Agar, Gelatin 4- Dried Juice → Aloes 5- Dried latex (milky exudate, emulsion or suspension)→ Opium 6- Oils and Fats 7- Saccharine Substances → Honey.  Resin Gum Mixture of organic compounds, Heteropolysaccharide Nature mainly acids which are solid or polymers highly viscous substances Pathological produced Production Natural or pathological, in both only after incision of in plant cases collected by incision the plant Soluble in hot water. Soluble in alcohol, organic Solubility Totally insoluble in solvents. Totally insoluble in water alcohol varieties: resin only, oleoresin or oleo gum resin For protection to Function For protection, as mostly have prevent exudation of for plant antimicrobial activity plant constituents from injured parts RESINS AND RESIN COMBINATIONS General Characters: -Hard, solid or semisolid, amorphous organic substance of complex nature. -Insoluble in water, mostly insoluble in petroleum ether, but soluble in alcohol, chloroform, ether and in many of the organic solvents as well as in fixed and volatile oils and in chloral hydrate. -Form solutions, on evaporation, deposit as a varnish like film. -Upon heating, soften and melt. They burn with a smoky flame. (incense) Occurance 1. Alone , pure resin 2. Resin+ volatile oils → oleo-resins 3. Resin+ gums → gum-resins 4. Resin+ oil + gum → oleo-gum-resins 5. Resin+ sugar→ glycosidal resin How can we obtain resin? 1. Extraction with ethanol and precipitating the resin in water. 2. Plant punctures 3. Heating. 4. Distillation to separate volatile oil from oleoresin. ***On injuring the plant, other ducts produce a large amount of resins to protect the injured part, this resin is called Secondary Flow while Primary Flow is the one produced without injury BOX METHOD: (For reading only) It is very old method, which was previously used in many countries. A large box was cut in the trunk and blaze cut about it. The length of which was increased from time to time. The oleoresin, which was collected in the box, was removed at intervals with a dipper and sent in barrels to the distillery. This method is often baseful causing destruction of most areas. CUP AND GUTTER METHOD: This method with different modifications is used in different countries. A series of ‘V’ shaped incisions are made in the trunk of the tree of a distance of about one-foot. The bark and young wood being removed so that a blaze or a groove is formed in the trunk. This is usually done early in the year. At the base of incision and aluminium earthen ware cup is fixed in the trunk and two strips of galvanized iron or aluminium are inserted about to deflect the flow of oleoresin into the cup. The length of the blaze is increased and the cups are moved higher up the trees and now grooves are started with the older ones. As the cups become filled, their contents are emptied into the barrels, which are delivered to the distillery where the turpentine oil is removed by steam distillation, and the resin become rosin. Box Method Cup and Gutter  Boswellia ‫لبان الدكر‬ Names: frankincense. Botanical Origin: oleogum resin from Boswellia serrata (Fam. Burseraceae). Active constituents Boswellic acid isomers (β-boswellic acid, acetyl-β-boswellic acid, 11-keto-β-boswellic acid and acetyl-11-keto-β-boswellic acid) + volatile oil (p-cymene and thujene) Uses: Currently, boswellic is investigated as anti- inflammatory in osteoarthritis. As it reduces inflammation and cartilage degradation. It has anticancer activity. In Ayruveda, it is used as antiasthmatic drug. Dosage: for inflammatory or asthmatic conditions, 300-400 mg of a standardized extract (containing 60% boswellic acids) three times daily is suggested boswellic acid  Oleogum resin: Myrrh ‫المر‬ Names: MyrrhGum Myrrh Botanical Origin: Myrrh is an oleo- gum-resin, obtained from the stems and branches of Commiphora molmol Engler, (Fam. Burseraceae). Commiphora molmol  Active constituents:(Oleo-Gum-Resin) Myrrh contains 7 to 17 %, thick volatile oil having the characteristic odor of myrrh. The volatile oil contains terpenes, sesquiterpenes i.e, cuminaldehyde and eugenol. resin which contains: β and γ-commiphoric acids. gum of acacia type containing galactose, arabinose, xylose  Uses Mainly have antimicrobial and antiulcer activities. **Sore throats and gingivitis (gum infections). Externally used in treating hemorrhoids, bed sores, and wounds. Treatment for acne and boils, for mild inflammatory skin problems (It exhibits anti-inflammatory and anti-ulcer effects) Sesquiterpenes have antibacterial, antifungal and analgesic effect and for irregular and painful menstruation. **It is not soluble in water and so normally taken in the form of a powder or a tincture, rather than as an infusion. Benzoin (Balsam) is a balsamic resin obtained from the bark of several species of trees in the genus Styrax. Balsam: is a resin but additionally contain benzoic or cinnamic acids. It is used in 1. Perfumes, some kinds of incense, as a flavoring and medicine 2. Laryngitis, bronchitis by inhalation. 3. Promote wound healing because of its hemostatic and antiseptic actions, so used in bed sores, skin fissures. Gums Gum acacia Gum tragacanth Guar gum  GUMMI ARABICUM Gum acacia ‫الصمغ العربى‬ Name: Gum Arabic Botanical Origin: Gum arabic is the dried gummy exudation from the stem and branches of Acacia senegal (L) (Fam. Leguminosae) Gum acacia Gum exudate Gum is a polysaccharide exudate obtained after injury (pathological product).  Active constituents Arabin: a mixture of Ca, Mg and K salts of arabic acid (polysaccharide containing uronic aids). and an oxidase enzyme 1- Oxidase enzyme test: aqueous solution of gum arabic + few drops of solution of hydrogen peroxide + few drops of benzidine tincture, shake, and allow to stand, a deep blue or a greenish- blue color is slowly formed It is used in medicine as a demulcent. suspending agent & emulsifying agent It is used in the food (chewing gum), drinks and other industries. Misuse: there is no report about safety of long term administration of gum arabic as antidiabetic. In this aspect, oats or psyllium are safe alternatives.  GUAR GUM ‫صمغ الجوار‬ Hydrocolloidal polysaccharide composed of galactan and.. mannan units linked through glycosidic linkages. (so it is neutral) oral hypoglycemic; it produces changes in gastric emptying and in the gastrointestinal transition time, which can delay absorption of sugars in the gut. Guar also lowers cholesterol levels, possibly by binding bile salts in the gut. The gum , 5-6 times the thickening power of starch, is used in food industry. Nature & preparation Dried extract Dried juice Dried latex The plant material is The plant Latex is a milky fluid extracted with water, parts are present in special then water is expressed to laticiferous ducts, it evaporated to expel the presents naturally and dryness. Hence, the juice from it, obtained from plant left residue is called then the juice by incision. Then it is (dried extract) is dried. dried. Example Extraction of polysaccharides from red algae (Agar), Extraction of Extraction of opium extraction of protein aloe gel latex (rich in narcotics) from animal tissues (Gelatin)  DRIED EXTRACTS 1.Agar-Agar 2. Gelatin 3. Gambir or catechu These are official in Egyptian Pharmacopoeia 1972.  AGAR- AGAR ‫أجار‬ Names: Agar, Japanese Isinglass. Botanical Origin: the dried mucilaginous substance prepared from Gelidium corneum Red algae (Ruds.) F.Gelidiaceae) Agar is insoluble in cold water but soluble in hot water. ⚫ Ca salt of polysaccharide. It yields on hydrolysis D-and L- galactose and sulphate ions, the two principal constituents of which are agarose and agaropectin. ⚫ Agarose is a neutral galactose polymer, free from sulphate ion. It is responsible for the gel strength of agar.). ⚫ Agaropectin, responsible for the viscosity of agar solutions, it is sulphonated Action and Uses Chemical test -**Agar is used in the ⚫ 1. Boil pd. agar for 10´ with 100 ml water preparation of culture → a stiff jelly on cooling. media, as an emulsifying ⚫ 2. Dissolve pd.by boiling for 5´ in 10 ml of water, add 1 ml of hydrochloric acid & suspending agent, for and heat on a w.b, then add 1 ml of suppositories and surgical barium chloride; a white precipitate is lubricants. formed (BaSO4) -OUTDATED: It is used ⚫ 3. Mix a little of powdered agar with a drop of iodine T.S.; some particles are in treatment of colored reddish but not blue (c.f. Starch constipation: it swells in and Gum Tragacanth). water and increases the moisture of stool thus producing the laxative effect.  GELATIN ‫جيالتين‬ ⚫ Sheet gelatin may be cut into strips or made into a granular powder. Gelatin is colorless or pale yellow, translucent and has little odor or taste. ⚫ Solubility: ⚫ Gelatin is insoluble in cold water but absorbs a volume of liquid; it dissolves on heating and a 2% solution forms a jelly on cooling. ⚫ The gelatinizing power of gelatin is reduced by long boiling. Constituents and uses Extracted from bone and skin of animals by boiling in water. Gelatin consists of the protein glutin and gives the usual tests for proteins Zinc Gelatin and for capsules, emulsions, and suppositories. Gelatin is a nutrient and used for the preparation of commercial food products (as suspending agent) and for bacteriologic culture media.  Chemical tests: general for any protein 1.Solution of gelatin+ picric acid solution a canary yellow precipitate is formed. 2. To another solution of gelatin, add drops of 5% Cu SO4, shake and add excess N/10 NaOH, a violet colour is produced (Biurette test)  DRIED JUICES Juices are fluid plant saps containing dissolved substances and usually present in plant special structures  ALOES ‫صبر‬ Names: Aloes; aloe Botanical Origin: solid residue obtained by evaporation of the liquid which drains from transversely cut leaves of several species of Aloes (F. Liliaceae). Aloe juice: comes spontaneous by incision of the leaves (pericycle). Aloe-gel: found deep inside the leaf tissues (pith)  Constituents Aloetic Juice Aloe- gel (mucilage) Aloin the major cathartic It is a saccharide material formed constituent. It is a C- glycosides of glycoproteins, (anthracene type) namely mucopolysaccharides or barbaloin and isobarbaloin. polysaccharide consisting of *resin (Alosin) which have a glucomannan. purgative action. -***Other constituents which -Small quantity of aloe-emodin. facilitate wound healing include, vitamins C and E and Zn metal. **Immunostimulant activity It presents in the pericycle. It presents in the pith.  Action and uses -**Aloe gel has no laxative effect but is used in cosmetic, and topical products. -The gel is used as moisturizing& emollient. Antimicrobial and antifungal (fungus→ tinea),inhibits growth of Streptococcus and Shigella species -Treatment of psoriasis in the form of hydrophilic cream -Aloe-gel used in treatment ,peptic ulcers, hair loss, as a spermicide and as a cancer chemo- preventive agent. Stimulant purgative: Aloe juice -Anthrones are more active than anthraquinones as purgative. N.B: A carminative or antispasmodic drug is recommended to be used with aloes to prevent its griping effect (e.g., fennel, mentha). - It also has antimicrobial activity so used as antiseptic Herpes simplex viruses. -eye inflammation and syphilis.  Mode of action on skin Tightens and balances skin through astringent pH properties. Holds moisture and adds flexibility to retard aging. Increases fibroblast production in skin tissue. The fibroblasts stimulate new collagen, thus accelerating wound healing. (hinders formation of thromboxane → promotes wound healing) Recent researches →the use of Aloe vera for the healing of first to second degree burns. Used with natural anti-inflammatory agents reduces pain -Repairs damaged skin by carrying added emollients into the skin up to seven layers.  Chemical tests Modified Borntrager's test: (for C-glycosides). the filtrate + benzene and allow to separate….. 10 ml of the benzene layer +drops of ferric chloride (to oxidize anthrone to anthraquinone) + dil. HCl (to break glycosides). Render the medium alkaline by ammonium hydroxide T. S. and notice the formation of a cherry-red color in the benzene layer.  Poppy Flower Dried Latex OPIUM ‫األفيون‬ Names: (Gum Opium- Raw Opium) ‫أفيون‬ Opium = milky juice Papaver = Poppy Somniferum = Induces sleep Botanical Origin: Raw opium is the dried milky exudation obtained by incising the unripe but fully-grown capsules of Papaver somniferum L (Fa. Papaveraceae) The quality of opium is judged by its morphine contents. **The USP requires that opium should contain not less than 9.5 % anhydrous morphine.  Preparation and collection The unripe capsule is incised with a knife to cut it where the milky latex is oozed out the capsule in the early morning. The latex is scrapped off and collected, kneaded into balls and wrapped in leaves for drying in the shade. On standing the color changes from milky white to chocolate brown. Opium latex Collection of Opium latex Action and Uses: (Mostly attributed to morphine) (remedy for pain) for emergency cases where pain is intolerable e.g. post-operative, severe traumatic conditions such as bone fracture, skin burns. Relieves intense pain of cancer patients &in angina pectoris. Morphine is preceding the use of anesthetics to increase their efficacy, allow lesser dosage and to prevent shock. *Opium is preferable to morphine in excessive diarrheas e.g. persistent summer diarrhea to restrain further abnormal used. Opium is also useful in polyuria especially that of true diabetes, in which the drug restrains both the quantity of urine and the output of sugar. `  Addiction Opium is highly addictive. Tolerance (the need for higher and higher doses to maintain the same effect) and physical and psychological dependence develop quickly. Withdrawal from opium causes nausea, tearing, yawning, chills, and sweating. Opium contains more than 19 alkaloids, some of which are combined with meconic acid forming meconates, some with sulfuric acid and some free as narcotine which is a weak base. **The presence of meconic acid even in a small quantity indicates the presence of opium or a preparation of poppy capsule. The presence of morphine alone in a vegetable extract does not prove that the extract contains opium. It must also give the tests for meconic acid. Accordingly, meconic acid can serve as a chemotaxonomic marker in members of papaveraceae. Chemical test Test for meconic acid: To an aqueous solution add neutral solution of Ferric chloride. It gives blood-red coloration