1Student-Rashtrsant Janardhan Swami College of Pharmacy Kokamthan Tal-Kopargaon.
2Assistant professor- Rashtrsant Janardhan Swami College of Pharmacy Kokamthan Tal-Kopargaon
The formulation and evaluation of herbal rectal suppositories containing flaxseed extract is an Innovative approach in the development of natural and effective therapeutic systems. Flaxseed (Linum usitatissimum) is widely known for its pharmacological properties, including anti-inflammatory, antioxidant, and laxative effects, attributed to its high content of Lignans, omega-3 fatty acids, and mucilage. This study aimed to develop a rectal delivery System utilizing flaxseed extract to address conditions such as constipation, inflammation, And local discomfort in the rectal region. In order to prevent its reported gastrointestinal Irritation and to give children a quick onset of effect, the current study set out to develop and Assess rectal suppositories containing flex seed extract as a new dosage form. Glycerol Gelation was used as the suppository basis to make suppositories in a variety of formulations. The physical characteristics of the produced suppositories, weight variation, drug content, Melting point, fracture point, and disintegration time hardness test were examined. According To the results, different concentrations of the glycerol-gelatin base were utilised with Increasing drug concentrations, and the outcomes with their standard parameters varied. Out Of the six formulas presented, F3 demonstrated the best formulation.
An oral dose form called a suppository is used to deliver pharmaceuticals by inserting it into a body Orifice, where it dissolves or melts and has local or systemic effects. [1-2]
Flax Seeds Drug Profile
Natural Source: The dried, ripe seed of the Linum usitatissimum Linn. Plant, Family: Linaceae, is Known as flax seed. Flax seed includes a variety of chemical components, including linamarin, a cyanogenetic glycoside, Fixed oil (30–40%), mucilage (6–10%), protein (linin and colinin) at 25%, and a minor amount of the Enzyme lipase. There are four different types of carbohydrates: sucrose, raffinose, cellulose, and Mucus. Phaseolunatin and linamarin are both glucose or acetone cyanohydrines. [3]
Prepration Method of Suppositories [4-5]
Generally, there are three methods of preparation of suppositories, which are as follows:
Drug + Additive
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Fine power and mixed in bases
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Apply lubricants on rolling tile
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Above mass are rolled by hand in cylinderical shape
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Then cut it and packed and store it.
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Mould should be of stainless steel, nickel, alluminium, copper, plastic, etc
Gelatine + Glycerol base are melt by using heat
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Disolve or disperse the drug (API) into base
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Remove the mixture of API and base from the heat
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Pour the mixture into lubricated mould and allow to cool down
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Freeze the mould and remove the formed suppositories from the mould.
Drug + Additive
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Make fine powder and mixed with bases (cocoa butter)
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Lubricant apply in moulds
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Placed the mass between or centre of the cylinder
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Applied the pressure and give the desired shape to mass
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Applied pressure and release the suppositories by removing stop plate
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Cooled, Packed, and Stored the suppositories
Factors Affecting from Rectal Suppostories [5]
Generally, there are two main factors which affects the rectal suppositories:
Following factors affects the rectal suppositories
Affects the absorption of drug administered in the form of suppositories
METHODS
2. Extraction method of Flax seed extract
Process of Extraction of flax seed are done by following steps: -
? Weigh 20 gram of flax seed, roast and crush it in a mortar pestle.
? Add the crushed flax seed in distilled water.
? Heat the mixture of flax seed and distilled water on magnetic stirrer for 15-20 minute.
? After heating the mixture cool the mixture and filter it with muslin cloth.
3. Preparation method of suppositories by fusion method
Basically, rectal suppositories are prepared by Fusion method, formulation of suppositories by fusion
method are prepared by following steps:
Gelatin in glycerol are melt by using heat form glycerogelatin base
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Dissolve or disperse the drug (API) into base
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Mix it uniformly
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Pour the mixture into lubricated mould and allow to cool down
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Freeze the mould and remove the formed suppositories from the mould
Suppositories are ovoid or conical medicated solids intended for insertion into one of the several orifices of the body, excluding the oral cavity. These are often used for local or systemic effects in the rectum, vagina, and, to a lesser extent, the urethra. 1 It has a rapid onset of action than the oral route since the medicine is absorbed directly into the bloodstream through the rectal mucosa (avoids the first-pass metabolism). It is a
Fig: -2-Suppositories
convenient way to administer medications that cause vomiting, irritate the GI tract, or are destroyed by the stomach’s acidic pH.2 Drugs can be administered as suppositories for both local and systemic effects. The composition of the drug, its concentration, and the rate of absorption all affect its activity. Rectal suppositories with a localised effect are usually used in the treatment of constipation or discomfort caused by haemorrhoids or other anorectal problems, as well as irritation, itching, and inflammation. Anti-hemorrhoidal suppositories commonly contain local anaesthetics, vasoconstrictors, astringents, analgesics, soothing emollients, and protective agents. Glycerin suppositories are a common laxative that produces local irritation of the mucous membranes, most likely due to the drying impact of the glycerin. Flax, often known as linseed or common flax, is a natural laxative. Linum usitatissimum, a blue flowering plant belonging to the Linaceae family, is known in Indian languages as Alsi, Jawas, and Aksebija. Mature flaxseed is rectangular and flattened, with an embryo surrounded by two cotyledons, a thin endosperm, and a smooth, usually shiny yellow to dark brown Testa (hull). It is cultivated as a food, oil, and fibre crop in regions of the world with a temperate climate. Flaxseed is well-known for its high concentration of chemical constituents with specific biological activity and functions. It contains 53% α-Linolenic Acid (ALA), 30% omega-3 fatty acid, protein, dietary fibre, lignan specifically Secoisolariciresinol diglucoside (SDG). Flaxseed dietary fibre positively affects reducing constipation, keeping better bowel movement, and being a hypocholesterolemic agent. Flaxseed contains dietary fibres and omega-3 fatty acids in the form of ALA, which can help reduce the risk of cancer, particularly breast and colon, by blocking tumour formation. The suppository contains flax as a main active ingredient, intended for use as a laxative, and treatment of haemorrhoids, constipation and bacterial infections of the anus. The flax may optionally comprise the liquid or gel form or a dry extract of the juice, or any other form of flax, all of which are collectively termed “flax extract”.
Suppositories are ovoid or conical medicated solids intended for insertion into one of the several orifices of the body, excluding the oral cavity. These are often used for local or systemic effects in the rectum, vagina, and, to a lesser extent, the urethra. 1It has a rapid onset of action than the oral route since the medicine is absorbed directly into the bloodstream through the rectal mucosa (avoids the first-pass metabolism). It is a convenient way to administer medications that cause vomiting, irritate the GI tract, or are destroyed by the stomach’s acidic pH.2Drugs can be administered as suppositories for both local and systemic effects. The composition of the drug, its concentration, and the rate of absorption all affect its activity.1Rectal suppositories with a localised effect are usually used in the treatment of constipation or discomfort caused by haemorrhoids or other anorectal problems, as well as irritation, itching, and inflammation. Anti-hemorrhoidal suppositories commonly contain local anaesthetics, vasoconstrictors, astringents, analgesics, soothing emollients, and protective agents. Glycerin suppositories are a common laxative that produces local irritation of the mucous membranes, most likely due to the drying impact of the glycerin.3Flax, often known as linseed or common flax, is a natural laxative.
Linum usitatissimum, a blue flowering plant belonging to the Linaceae family, is known in Indian languages as Alsi, Jawas, and Aksebija. Mature flaxseed is rectangular and flattened, with an embryo surrounded by two cotyledons, a thin endosperm, and a smooth, usually shiny yellow to dark brown Testa (hull). It is cultivated as a food, oil, and fibre crop in regions of the world with a temperate climate. Flaxseed is well-known for its high concentration of chemical constituents with specific biological activity and functions. It contains 53% α-Linolenic Acid (ALA), 30% omega-3 fatty acid, protein, dietary fibre, lignan specifically Secoisolariciresinol diglucoside (SDG). Flaxseed dietary fibre positively affects reducing constipation, keeping better movement, and being a hypocholesterolemic agent. Flaxseed contains dietary fibres omega-3 fatty acids in the form of ALA, which can help reduce the risk of cancer, particularly breast and colon, by blocking tumour formation.
Types of Suppositories
There are five varieties of suppositories, each with a different method of administration.
In addition to suppositories, there are 4 other types of dosage forms available.
Developing Process of Suppositories:
Fusion moulding, compression moulding, and hands moulding are the three different ways that suppositories are prepared. Generally speaking, hands moulding is only employed in pharmacies and fusion procedures can be applied to all kinds of suppositories. With this technique, the suppository matrix is first melted, the drug is then dispersed or dissolved in the melted matrix, and finally the mixture is poured into the suppository mould. Once the mixture coagulates, the suppository is then withdrawn from the mould.
Fig. Suppositories for various ano-rectal pathologies
Some Other Common Diseases Treated by Suppositories:
Though these infections are fairly uncommon, vulvovaginitis brought on by Saccharomyces cerevisiae may benefit from the use of boric acid vaginal suppositories. A report of a 30-year-old female with recurrent vaginitis that had occurred five months earlier and from which C. glabrata was isolated. Clotrimazole, terconazole, ketoconazole, intravenous amphotericin B, or oral flucytosine did not help the patient. A 600 mg daily dose of vaginal boric acid suppositories eventually led to a clinical and mycological cure.57The patient, who was still getting boric acid, was discovered to be S. cerevisiae colonized and had developed frank vulvovaginitis. This condition was treated by increasing the dosage of boric acid to 600 mg twice day. After six months of boric acid maintenance medication, the patient was still symptom-free. With the help of boric acid suppositories, relapse after stopping treatment was completely eliminated. The authors also assessed the susceptibility of 20 clinical isolates of S. cerevisiae, and they discovered that extended treatment with 600 mg/day of boric acid was linked to clinical and mycologic resolution in four episodes; however, mycologic clearance required protracted treatment.
There have been a number of examples where boric acid has been used to treat azole-refractory candidal vaginitis. After nine months of daily treatment with 100 mg of fluconazole, a 32-year-old woman with severe acquired immunodeficiency syndrome (AIDS) and a CD4 level of 10/mm3 developed vulvovaginal candidiasis and thrush. This case was described by Shinohara and Tasker. Fluconazole-resistant strains of C. krusei and C. glabrata were detected in cultures.58Itraconazole failed to control the patient’s symptoms, nystatin only marginally improved them, and the patient found the gentian violet topical solution to be disappointing in terms of appearance. Treatment with 5% boric acid in lanolin vaginal suppositories and 600 mg twice daily of boric acid relieved symptoms and was well tolerated. The serum did not contain any boric acid. Three relapses occurred five months after the patient’s initial therapy; these were treated with two- to three-day treatments of boric acid.
Opioids have historically been viewed as being replaced by alternative analgesics due to the vast range of negative effects and dependence they are associated with. NSAIDs prevent the cyclooxygenase enzyme, which catalyses the conversion of arachidonic acid to prostaglandin, from doing its job.59, 60The peripheral nervous system may experience less pain by producing fewer of these substances. Abdollahi et al. found no difference in the mean pain score between the two groups at the first eight hours, but at the second and third eight hours, the feeling of pain was statistically lower in the diclofenac group. Pethidine (0.5 mg/kg intrathecal every eight hours) and diclofenac suppository (100 mg every eight hours) were compared for pain relief after inguinal herniation surgery.59The mean pain scores in the diclofenac group were lower than those in the pethidine group at 10, 18, and 26 hours after surgery, but the reported pain severity had lessened more over time. This difference between the two groups may be brought on by diclofenac’s prolonged effects, it’s blocking of pain receptors, and its inhibition of prostaglandin release.
Anus is the portion of the gastrointestinal system that travels via the anal sphincters and muscular canal of the pelvis. The body’s last opening via which stool exits is this one. The anus is 4–5 cm long in adulthood. Sensitive nerve endings line the lower portion of the anal canal. Under the lining are blood arteries, and in the middle is a great deal of little anal glands. Suppositories could well be looked as a convenient drug delivery system in patients having ano-rectal symptoms. Some suppositories formulation is described below in the table form for the various ano-rectal pathologies.
Parkinson’s disease is a slowly developing, chronic neurodegenerative condition that primarily affects the motor system (bradykinesia, stiffness, rest tremor, and postural problems). Along with late-onset motor symptoms (such postural instability and falls, freezing of gait, speech and swallowing difficulties), it is also linked to a variety of non-motor symptoms. For the best seizure control during both the acute and long-term therapy of Parkinson’s disease, the drug’s therapeutic concentration must be maintained.79 When chronic medication delivery is necessary but oral access to the medication is restricted or the IV formulation of the medication is incompatible, alternate drug dosing routes are needed. Rectal injection of anti-Parkinson drugs is crucial since it partially avoids first pass metabolism. Since many years ago, children’s recurrent or protracted seizures have been treated with diazepam by rectal route in the form of solution and gel preparation. When injected rectally, diazepam solution absorbs completely and quickly, reaching peak plasma concentration in 5 to 15 minutes.
Parkinson’s disease is a slowly developing, chronic neurodegenerative condition that primarily affects the motor system (bradykinesia, stiffness, rest tremor, and postural problems). Along with late-onset motor symptoms (such postural instability and falls, freezing of gait, speech and swallowing difficulties), it is also linked to a variety of non-motor symptoms.For the best seizure control during both the acute and long-term therapy of Parkinson’s disease, the drug’s therapeutic concentration must be maintained.79 When chronic medication delivery is necessary but oral access to the medication is restricted or the IV formulation of the medication is incompatible, alternate drug dosing routes are needed. Rectal injection of anti-Parkinson drugs is crucial since it partially avoids first pass metabolism. Since many years ago, children’s recurrent or protracted seizures have been treated with diazepam by rectal route in the form of solution and gel preparation. When injected rectally, diazepam solution absorbs completely and quickly, reaching peak plasma concentration in 5 to 15 minutes.
Cervical cancer is one of the most common cancers, and among women, it is also the one that causes the second-highest cancer mortality rate. Patients with cancer are more likely to develop and die from fungal infections than from other illnesses. The likelihood that a patient will get a fungal infection can be decreased by prescribing antifungal drugs. Curcumin, the herbal drug that was selected for the current study, is a well-known contender with antifungal and anticancer effects. Curcumin has been used extensively in the study of cancer prevention. The newly created curcumin vaginal suppository may be a natural remedy free from side effects that helps cervical cancer patients avoid candidiasis and may also help with cancer treatment.
CONCLUSION: -
The formulated herbal rectal suppositories containing flax seed extract, using cocoa butter as a base, demonstrated satisfactory physicochemical properties including uniformity of weight, adequate hardness, smooth surface texture, and appropriate melting point. The in vitro release studies indicated a sustained and controlled release of the active constituents, suggesting potential for effective therapeutic application. Furthermore, the suppositories exhibited good stability and were well-tolerated in preliminary evaluations, highlighting flax seed extract’s promise as a bioactive agent in rectal delivery systems. These findings support the feasibility of using cocoa butter-based suppositories as a suitable carrier for flax seed extract in the management of relevant rectal or systemic conditionss.
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Rutuja Sawai*, Sonali Kote, Formulation and Evaluation of Herbal Rectal Suppositories Containing A Flax Seed Extract (Cocoa Butter Based), Int. J. of Pharm. Sci., 2025, Vol 3, Issue 5, 1488-1496. https://doi.org/10.5281/zenodo.15380102
10.5281/zenodo.15380102
